916 articles for thisTarget
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Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Merck Research Laboratories
p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.
Merck Research Laboratories
Synthesis and activity of 2-(sulfonamido)methyl-carbapenems: discovery of a novel, anti-MRSA 1,8-naphthosultam pharmacophore.
Merck Research Laboratories
Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.
Merck Research Laboratories
Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension.
Merck Research Laboratories
Substituted 4-morpholine N-arylsulfonamides as¿-secretase inhibitors.
Merck Research Laboratories
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Merck Research Laboratories
Design and synthesis of water solubleß-aminosulfone analogues of SCH 900229 as¿-secretase inhibitors.
Merck Research Laboratories
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.
Merck Research Laboratories
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.
Merck Research Laboratories
Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.
Merck Research Laboratories
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Merck Research Laboratories
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.
Merck Research Laboratories
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
Merck Research Laboratories
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Merck Research Laboratories
Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.
Merck Research Laboratories
Potent, selective and orally bioavailable leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Merck Research Laboratories
Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.
Merck Research Laboratories
Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates.
Merck Research Laboratories
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.
Merck Research Laboratories
SAR exploration at the C-3 position of tetrahydro-ß-carboline sstr3 antagonists.
Merck Research Laboratories
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.
Merck Research Laboratories
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
Merck Research Laboratories
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Merck Research Laboratories
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Merck Research Laboratories
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Merck Research Laboratories
Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists.
Merck Research Laboratories
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Merck Research Laboratories
Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.
Merck Research Laboratories
Discovery of a Novel, Potent Spirocyclic Series of¿-Secretase Inhibitors.
Merck Research Laboratories
Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Merck Research Laboratories
Development of a novel tricyclic class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.
Merck Research Laboratories
Development of a novel class of potent and selective FIXa inhibitors.
Merck Research Laboratories
Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.
Merck Research Laboratories
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
Merck Research Laboratories
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Merck Research Laboratories
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.
Merck Research Laboratories
A novel series of indazole-/indole-based glucagon receptor antagonists.
Merck Research Laboratories
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
Merck Research Laboratories
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.
Merck Research Laboratories
Potent benzoazepinone¿-secretase modulators with improved bioavailability.
Merck Research Laboratories
Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5).
Merck Research Laboratories
Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6).
Merck Research Laboratories
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.
Merck Research Laboratories
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.
Merck Research Laboratories
Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.
Merck Research Laboratories
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.
Merck Research Laboratories
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
Synthesis and Evaluation of Heterocyclic Catechol Mimics as Inhibitors of Catechol-O-methyltransferase (COMT).
Merck Research Laboratories
Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.
Merck Research Laboratories
Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).
Merck Research Laboratories
Rapid development of two factor IXa inhibitors from hit to lead.
Merck Research Laboratories
Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4).
Merck Research Laboratories
Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4.
Merck Research Laboratories
Discovery of novel spiro 1,3,4-thiadiazolines as potent, orally bioavailable and brain penetrant KSP inhibitors.
Merck Research Laboratories
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Merck Research Laboratories
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
Merck Research Laboratories
Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors.
Merck Research Laboratories
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Merck Research Laboratories
Investigation of Cardiovascular Effects of Tetrahydro-ß-carboline sstr3 antagonists.
Merck Research Laboratories
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
Merck Research Laboratories
Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.
Merck Research Laboratories
Biased ligand modulation of seven transmembrane receptors (7TMRs): functional implications for drug discovery.
Merck Research Laboratories
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.
Merck Research Laboratories
Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.
Merck Research Laboratories
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Merck Research Laboratories
Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.
Merck Research Laboratories
Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Merck Research Laboratories
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
Merck Research Laboratories
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.
Merck Research Laboratories
Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
Merck Research Laboratories
Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar.
Merck Research Laboratories
Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
Merck Research Laboratories
Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase.
Merck Research Laboratories
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.
Merck Research Laboratories
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.
Merck Research Laboratories
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.
Merck Research Laboratories
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
Merck Research Laboratories
Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
Merck Research Laboratories
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.
Merck Research Laboratories
Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.
Merck Research Laboratories
Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.
Merck Research Laboratories
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
Merck Research Laboratories
Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar.
Merck Research Laboratories
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.
Merck Research Laboratories
Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).
Merck Research Laboratories
Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.
Merck Research Laboratories
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Merck Research Laboratories
Identification of 2-aminooxazole amides as acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy.
Merck Research Laboratories
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.
Merck Research Laboratories
Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl)ethyl)isobenzofuran-1(3H)-one.
Merck Research Laboratories
Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.
Merck Research Laboratories
Bicyclic and tricyclic heterocycle derivatives as histamine H3 receptor antagonists for the treatment of obesity.
Merck Research Laboratories
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine (23).
Merck Research Laboratories
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.
Merck Research Laboratories
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Merck Research Laboratories
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Merck Research Laboratories
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Merck Research Laboratories
Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.
Merck Research Laboratories
Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.
Merck Research Laboratories
Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.
Merck Research Laboratories
Discovery of liver-targeted inhibitors of stearoyl-CoA desaturase (SCD1).
Merck Research Laboratories
Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.
Merck Research Laboratories
Influence of acid surrogates toward potency of VLA-4 antagonist.
Merck Research Laboratories
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.
Merck Research Laboratories
N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists.
Merck Research Laboratories
Identification of unique VLA-4 antagonists from a combinatorial library.
Merck Research Laboratories
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.
Merck Research Laboratories
Synthesis and biological activity of pyridopyridazin-6-one p38a MAP kinase inhibitors. Part 2.
Merck Research Laboratories
Discovery and optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives as a novel class of selective cannabinoid CB2 receptor agonists.
Merck Research Laboratories
Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.
Merck Research Laboratories
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Merck Research Laboratories
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Merck Research Laboratories
Structure based evolution of a novel series of positive modulators of the AMPA receptor.
Merck Research Laboratories
A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Merck Research Laboratories
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Merck Research Laboratories
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Merck Research Laboratories
Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.
Merck Research Laboratories
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist.
Merck Research Laboratories
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Merck Research Laboratories
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Merck Research Laboratories
Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.
Merck Research Laboratories
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.
Merck Research Laboratories
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Merck Research Laboratories
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes.
Merck Research Laboratories
Discovery of selective glucocorticoid receptor modulator MK-5932.
Merck Research Laboratories
Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.
Merck Research Laboratories
Discovery of inhibitors of soluble epoxide hydrolase: a target with multiple potential therapeutic indications.
Merck Research Laboratories
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Merck Research Laboratories
Inhibition of cap (m7GpppXm)-dependent endonuclease of influenza virus by 4-substituted 2,4-dioxobutanoic acid compounds.
Merck Research Laboratories
Synthesis of natural flutimide and analogous fully substituted pyrazine-2,6-diones, endonuclease inhibitors of influenza virus.
Merck Research Laboratories
Anti-influenza virus activities of 4-substituted 2,4-dioxobutanoic acid inhibitors.
Merck Research Laboratories
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Merck Research Laboratories
Evaluation of endo- and exo-aryl-substitutions and central scaffold modifications on diphenyl substituted alkanes as 5-lipoxygenase activating protein inhibitors.
Merck Research Laboratories
Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.
Merck Research Laboratories
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.
Merck Research Laboratories
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
Merck Research Laboratories
The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization.
Merck Research Laboratories
Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).
Merck Research Laboratories
Triazoloamides as potent¿-secretase modulators with reduced hERG liability.
Merck Research Laboratories
Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain.
Merck Research Laboratories
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
Discovery of oxazole-based PDE4 inhibitors with picomolar potency.
Merck Research Laboratories
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.
Merck Research Laboratories
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Merck Research Laboratories
Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.
Merck Research Laboratories
Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.
Merck Research Laboratories
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Merck Research Laboratories
Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.
Merck Research Laboratories
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.
Merck Research Laboratories
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Merck Research Laboratories
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.
Merck Research Laboratories
Multiple strategies for the preparation of a sulfur-35 labeled NPC1L1 radioligand.
Merck Research Laboratories
Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.
Merck Research Laboratories
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Merck Research Laboratories
GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.
Merck Research Laboratories
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.
Merck Research Laboratories
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Merck Research Laboratories
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.
Merck Research Laboratories
N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents.
Merck Research Laboratories
Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists.
Merck Research Laboratories
Proline bis-amides as potent dual orexin receptor antagonists.
Merck Research Laboratories
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Merck Research Laboratories
Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.
Merck Research Laboratories
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Merck Research Laboratories
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
Merck Research Laboratories
Noreupenifeldin, a tropolone from an unidentified ascomycete.
Merck Research Laboratories
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
Merck Research Laboratories
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).
Merck Research Laboratories
Rapid assembly of diverse and potent allosteric Akt inhibitors.
Merck Research Laboratories
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.
Merck Research Laboratories
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.
Merck Research Laboratories
Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.
Merck Research Laboratories
A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.
Merck Research Laboratories
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.
Merck Research Laboratories
Imidazopyridines: a novel class of hNav1.7 channel blockers.
Merck Research Laboratories
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.
Merck Research Laboratories
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Merck Research Laboratories
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
Merck Research Laboratories
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Merck Research Laboratories
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
Merck Research Laboratories
P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.
Merck Research Laboratories
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Merck Research Laboratories
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.
Merck Research Laboratories
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
Merck Research Laboratories
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
Merck Research Laboratories
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
Merck Research Laboratories
Benzodiazepines as potent and selective bradykinin B1 antagonists.
Merck Research Laboratories
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
Merck Research Laboratories
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.
Merck Research Laboratories
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Merck Research Laboratories
Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.
Merck Research Laboratories
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
Merck Research Laboratories
Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.
Merck Research Laboratories
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.
Merck Research Laboratories
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.
Merck Research Laboratories
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.
Merck Research Laboratories
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
Merck Research Laboratories
4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency.
Merck Research Laboratories
Pseudopeptide inhibitors of Ras farnesyl-protein transferase.
Merck Research Laboratories
4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase.
Merck Research Laboratories
3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors.
Merck Research Laboratories
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Merck Research Laboratories
4-Oxospiro[benzopyran-2,4'-piperidines] as class III antiarrhythmic agents. Pharmacological studies on 3,4-dihydro-1'-[2-(benzofurazan-5-yl)- ethyl]-6-methanesulfonamidospiro[(2H)-1-benzopyran-2,4'-piperidin]-4-on e (L-691,121).
Merck Research Laboratories
Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.
Merck Research Laboratories
4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Merck Research Laboratories
Highly potent, orally active diester macrocyclic human renin inhibitors.
Merck Research Laboratories
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
Merck Research Laboratories
Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Merck Research Laboratories
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Merck Research Laboratories
Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel.
Merck Research Laboratories
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.
Merck Research Laboratories
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype.
Merck Research Laboratories
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.
Merck Research Laboratories
Design and synthesis of potent and selective macrocyclic thrombin inhibitors.
Merck Research Laboratories
2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.
Merck Research Laboratories
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.
Merck Research Laboratories
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1.
Merck Research Laboratories
Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements.
Merck Research Laboratories
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.
Merck Research Laboratories
Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.
Merck Research Laboratories
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.
Merck Research Laboratories
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.
Merck Research Laboratories
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.
Merck Research Laboratories
Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.
Merck Research Laboratories
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators.
Merck Research Laboratories
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.
Merck Research Laboratories
Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).
Merck Research Laboratories
Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.
Merck Research Laboratories
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Merck Research Laboratories
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
Merck Research Laboratories
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Merck Research Laboratories
Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Merck Research Laboratories
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 2.
Merck Research Laboratories
Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.
Merck Research Laboratories
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.
Merck Research Laboratories
Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.
Merck Research Laboratories
Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.
Merck Research Laboratories
Identification of a novel RAMP-independent CGRP receptor antagonist.
Merck Research Laboratories
Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.
Merck Research Laboratories
Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.
Merck Research Laboratories
N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.
Merck Research Laboratories
Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.
Merck Research Laboratories
Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.
Merck Research Laboratories
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Merck Research Laboratories
Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.
Merck Research Laboratories
Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold.
Merck Research Laboratories
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.
Merck Research Laboratories
Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).
Merck Research Laboratories
Indazole derivatives as novel bradykinin B1 receptor antagonists.
Merck Research Laboratories
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Merck Research Laboratories
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.
Merck Research Laboratories
Structure-based lead identification of ATP-competitive MK2 inhibitors.
Merck Research Laboratories
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Merck Research Laboratories
Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes.
Merck Research Laboratories
3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.
Merck Research Laboratories
Structure and activity relationships of tartrate-based TACE inhibitors.
Merck Research Laboratories
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Merck Research Laboratories
2-(4-Carbonylphenyl)benzoxazole inhibitors of CETP: attenuation of hERG binding and improved HDLc-raising efficacy.
Merck Research Laboratories
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Merck Research Laboratories
Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.
Merck Research Laboratories
The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.
Merck Research Laboratories
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Merck Research Laboratories
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Merck Research Laboratories
Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists.
Merck Research Laboratories
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Merck Research Laboratories
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.
Merck Research Laboratories
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.
Merck Research Laboratories
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.
Merck Research Laboratories
Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones.
Merck Research Laboratories
Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective humanß3 adrenergic receptor agonists.
Merck Research Laboratories
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.
Merck Research Laboratories
Pyridyl amides as potent inhibitors of T-type calcium channels.
Merck Research Laboratories
Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
Merck Research Laboratories
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.
Merck Research Laboratories
P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.
Merck Research Laboratories
2-(4-carbonylphenyl)benzoxazole inhibitors of CETP: scaffold design and advancement in HDLc-raising efficacy.
Merck Research Laboratories
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Merck Research Laboratories
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.
Merck Research Laboratories
Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.
Merck Research Laboratories
2-Arylbenzoxazoles as CETP inhibitors: raising HDL-C in cynoCETP transgenic mice.
Merck Research Laboratories
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Merck Research Laboratories
A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.
Merck Research Laboratories
Discovery of a series of potent arylthiadiazole H(3) antagonists.
Merck Research Laboratories
ApoA-I mimetic peptides promote pre-ß HDL formation in vivo causing remodeling of HDL and triglyceride accumulation at higher dose.
Merck Research Laboratories
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Merck Research Laboratories
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
Merck Research Laboratories
Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists.
Merck Research Laboratories
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors.
Merck Research Laboratories
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.
Merck Research Laboratories
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Merck Research Laboratories
Positive allosteric modulators of thea-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
Merck Research Laboratories
Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.
Merck Research Laboratories
Discovery of a vorapaxar analog with increased aqueous solubility.
Merck Research Laboratories
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Merck Research Laboratories
Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands.
Merck Research Laboratories
Discovery of a series of potent, orally activea,a-disubstituted piperidine NK(1) antagonists.
Merck Research Laboratories
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Merck Research Laboratories
Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.
Merck Research Laboratories
Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.
Merck Research Laboratories
Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.
Merck Research Laboratories
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Merck Research Laboratories
Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.
Merck Research Laboratories
The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.
Merck Research Laboratories
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Merck Research Laboratories
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
Merck Research Laboratories
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
Merck Research Laboratories
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Merck Research Laboratories
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
Merck Research Laboratories
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Merck Research Laboratories
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.
Merck Research Laboratories
Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Merck Research Laboratories
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Merck Research Laboratories
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.
Merck Research Laboratories
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Merck Research Laboratories
Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.
Merck Research Laboratories
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Merck Research Laboratories
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Merck Research Laboratories
A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties.
Merck Research Laboratories
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Merck Research Laboratories
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Merck Research Laboratories
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Merck Research Laboratories
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
Merck Research Laboratories
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Merck Research Laboratories
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
Merck Research Laboratories
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Merck Research Laboratories
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Merck Research Laboratories
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Merck Research Laboratories
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
Merck Research Laboratories
Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.
Merck Research Laboratories
Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.
Merck Research Laboratories
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.
Merck Research Laboratories
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Merck Research Laboratories
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.
Merck Research Laboratories
Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists.
Merck Research Laboratories
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Merck Research Laboratories
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.
Merck Research Laboratories
Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.
Merck Research Laboratories
Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
Merck Research Laboratories
A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain.
Merck Research Laboratories
Discovery of a novel class of isoxazoline voltage gated sodium channel blockers.
Merck Research Laboratories
Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.
Merck Research Laboratories
A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.
Merck Research Laboratories
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Merck Research Laboratories
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Merck Research Laboratories
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Merck Research Laboratories
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
Merck Research Laboratories
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma a
Merck Research Laboratories
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
Merck Research Laboratories
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Merck Research Laboratories
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Merck Research Laboratories
Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding.
Merck Research Laboratories
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Merck Research Laboratories
Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Merck Research Laboratories
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
Merck Research Laboratories
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Merck Research Laboratories
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Merck Research Laboratories
Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2).
Merck Research Laboratories
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
Merck Research Laboratories
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Merck Research Laboratories
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
Merck Research Laboratories
SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).
Merck Research Laboratories
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Merck Research Laboratories
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.
Merck Research Laboratories
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
Merck Research Laboratories
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat.
Merck Research Laboratories
Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
Merck Research Laboratories
The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.
Merck Research Laboratories
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Merck Research Laboratories
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.
Merck Research Laboratories
Discovery of potent, orally active benzimidazole glucagon receptor antagonists.
Merck Research Laboratories
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Merck Research Laboratories
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Merck Research Laboratories
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Merck Research Laboratories
Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.
Merck Research Laboratories
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
Merck Research Laboratories
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
Merck Research Laboratories
Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.
Merck Research Laboratories
Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity.
Merck Research Laboratories
Isolation and structure of antagonists of chemokine receptor (CCR5).
Merck Research Laboratories
Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.
Merck Research Laboratories
3-Amino-1,5-benzodiazepinones: potent, state-dependent sodium channel blockers with anti-epileptic activity.
Merck Research Laboratories
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.
Merck Research Laboratories
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
Merck Research Laboratories
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Merck Research Laboratories
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).
Merck Research Laboratories
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Merck Research Laboratories
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Merck Research Laboratories
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.
Merck Research Laboratories
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.
Merck Research Laboratories
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Merck Research Laboratories
Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.
Merck Research Laboratories
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
Merck Research Laboratories
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Aminosuberoyl hydroxamic acids (ASHAs): a potent new class of HDAC inhibitors.
Merck Research Laboratories
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.
Merck Research Laboratories
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.
Merck Research Laboratories
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2.
Merck Research Laboratories
Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.
Merck Research Laboratories
Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.
Merck Research Laboratories
Potent and selective agonists of human melanocortin receptor 5: cyclic analogues of alpha-melanocyte-stimulating hormone.
Merck Research Laboratories
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).
Merck Research Laboratories
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Merck Research Laboratories
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Merck Research Laboratories
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Merck Research Laboratories
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.
Merck Research Laboratories
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Merck Research Laboratories
Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.
Merck Research Laboratories
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.
Merck Research Laboratories
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Merck Research Laboratories
Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.
Merck Research Laboratories
Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.
Merck Research Laboratories
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Merck Research Laboratories
Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents.
Merck Research Laboratories
Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors.
Merck Research Laboratories
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Merck Research Laboratories
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
Merck Research Laboratories
4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Merck Research Laboratories
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.
Merck Research Laboratories
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Merck Research Laboratories
4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties.
Merck Research Laboratories
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Merck Research Laboratories
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Merck Research Laboratories
Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands.
Merck Research Laboratories
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
Merck Research Laboratories
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.
Merck Research Laboratories
Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.
Merck Research Laboratories
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Merck Research Laboratories
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Merck Research Laboratories
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
Merck Research Laboratories
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Merck Research Laboratories
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Merck Research Laboratories
5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.
Merck Research Laboratories
Synthesis and SAR studies of diarylpyrrole anticoccidial agents.
Merck Research Laboratories
Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents.
Merck Research Laboratories
The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Merck Research Laboratories
6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.
Merck Research Laboratories
Design and synthesis of potent and subtype-selective PPARalpha agonists.
Merck Research Laboratories
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Merck Research Laboratories
Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.
Merck Research Laboratories
Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.
Merck Research Laboratories
Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
Merck Research Laboratories
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Merck Research Laboratories
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles.
Merck Research Laboratories
Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.
Merck Research Laboratories
3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists.
Merck Research Laboratories
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Merck Research Laboratories
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.
Merck Research Laboratories
Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis.
Merck Research Laboratories
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Merck Research Laboratories
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
Merck Research Laboratories
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.
Merck Research Laboratories
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Merck Research Laboratories
Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents.
Merck Research Laboratories
Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists.
Merck Research Laboratories
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif.
Merck Research Laboratories
Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.
Merck Research Laboratories
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
Merck Research Laboratories
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Merck Research Laboratories
Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
Merck Research Laboratories
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Merck Research Laboratories
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.
Merck Research Laboratories
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.
Merck Research Laboratories
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.
Merck Research Laboratories
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity.
Merck Research Laboratories
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Merck Research Laboratories
Selective PPARgamma modulators with improved pharmacological profiles.
Merck Research Laboratories
2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.
Merck Research Laboratories
Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor.
Merck Research Laboratories
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Merck Research Laboratories
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.
Merck Research Laboratories
Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
Merck Research Laboratories
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Merck Research Laboratories
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.
Merck Research Laboratories
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Merck Research Laboratories
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.
Merck Research Laboratories
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.
Merck Research Laboratories
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Merck Research Laboratories
Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.
Merck Research Laboratories
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.
Merck Research Laboratories
Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
Merck Research Laboratories
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.
Merck Research Laboratories
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Merck Research Laboratories
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Merck Research Laboratories
Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Merck Research Laboratories
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
Merck Research Laboratories
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Merck Research Laboratories
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.
Merck Research Laboratories
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.
Merck Research Laboratories
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
Merck Research Laboratories
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.
Merck Research Laboratories
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity.
Merck Research Laboratories
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Merck Research Laboratories
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Merck Research Laboratories
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.
Merck Research Laboratories
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Merck Research Laboratories
Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability.
Merck Research Laboratories
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Merck Research Laboratories
Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.
Merck Research Laboratories
Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.
Merck Research Laboratories
Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.
Merck Research Laboratories
Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.
Merck Research Laboratories
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Merck Research Laboratories
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Merck Research Laboratories
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Merck Research Laboratories
(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
Merck Research Laboratories
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Merck Research Laboratories
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Merck Research Laboratories
Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.
Merck Research Laboratories
Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.
Merck Research Laboratories
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.
Merck Research Laboratories
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
Merck Research Laboratories
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Merck Research Laboratories
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Merck Research Laboratories
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.
Merck Research Laboratories
Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!
Merck Research Laboratories
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives: high-affinity ligands to the alpha 2 delta subunit of voltage gated calcium channels.
Merck Research Laboratories
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
Rational design and synthesis of selective BACE-1 inhibitors.
Merck Research Laboratories
Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.
Merck Research Laboratories
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
Merck Research Laboratories
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
Merck Research Laboratories
Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.
Merck Research Laboratories
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.
Merck Research Laboratories
Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.
Merck Research Laboratories
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Merck Research Laboratories
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.
Merck Research Laboratories
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.
Merck Research Laboratories
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.
Merck Research Laboratories
5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
Merck Research Laboratories
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.
Merck Research Laboratories
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Merck Research Laboratories
Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase.
Merck Research Laboratories
Orally efficacious NR2B-selective NMDA receptor antagonists.
Merck Research Laboratories
Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
Merck Research Laboratories
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists.
Merck Research Laboratories
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.
Merck Research Laboratories
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.
Merck Research Laboratories
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Merck Research Laboratories
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).
Merck Research Laboratories
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Merck Research Laboratories
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.
Merck Research Laboratories
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.
Merck Research Laboratories
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Merck Research Laboratories
Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.
Merck Research Laboratories
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
Merck Research Laboratories
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.
Merck Research Laboratories
Discovery and development of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists for the treatment of diabetes.
Merck Research Laboratories
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.
Merck Research Laboratories
Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.
Merck Research Laboratories
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.
Merck Research Laboratories
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Merck Research Laboratories
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.
Merck Research Laboratories
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Merck Research Laboratories
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Merck Research Laboratories
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.
Merck Research Laboratories
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Merck Research Laboratories
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.
Merck Research Laboratories
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Merck Research Laboratories
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Merck Research Laboratories
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Merck Research Laboratories
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Merck Research Laboratories
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).
Merck Research Laboratories
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Merck Research Laboratories
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.
Merck Research Laboratories
Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure-activity relationships of 2-methoxystypandrone and its analogues.
Merck Research Laboratories
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.
Merck Research Laboratories
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
Merck Research Laboratories
Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro.
Merck Research Laboratories
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Merck Research Laboratories
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Merck Research Laboratories
Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.
Merck Research Laboratories
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted)piperidin-1-yl]butanes.
Merck Research Laboratories
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Merck Research Laboratories
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus.
Merck Research Laboratories
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.
Merck Research Laboratories
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Merck Research Laboratories
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.
Merck Research Laboratories
2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.
Merck Research Laboratories
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.
Merck Research Laboratories
Perspectives in animal health: old targets and new opportunities.
Merck Research Laboratories
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Merck Research Laboratories
SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists.
Merck Research Laboratories
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles.
Merck Research Laboratories
Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Merck Research Laboratories
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Merck Research Laboratories
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Merck Research Laboratories
Structure-function studies on the new growth hormone-releasing peptide, ghrelin: minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a.
Merck Research Laboratories
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
Merck Research Laboratories
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
Merck Research Laboratories
Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor.
Merck Research Laboratories
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
Merck Research Laboratories
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.
Merck Research Laboratories
Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.
Merck Research Laboratories
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
Merck Research Laboratories
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.
Merck Research Laboratories
Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.
Merck Research Laboratories
Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.
Merck Research Laboratories
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
Merck Research Laboratories
Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors.
Merck Research Laboratories
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.
Merck Research Laboratories
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Merck Research Laboratories
Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.
Merck Research Laboratories
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Merck Research Laboratories
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.
Merck Research Laboratories
Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.
Merck Research Laboratories
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
Merck Research Laboratories
Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.
Merck Research Laboratories
Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.
Merck Research Laboratories
N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.
Merck Research Laboratories
Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists.
Merck Research Laboratories
Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.
Merck Research Laboratories
Tetrapeptide derived inhibitors of complexation of a class II MHC: fully unnatural ligands.
Merck Research Laboratories
Tetrapeptide derived inhibitors of complexation of a class II MHC: the peptide backbone is not inviolate.
Merck Research Laboratories
Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity.
Merck Research Laboratories
C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study.
Merck Research Laboratories
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.
Merck Research Laboratories
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.
Merck Research Laboratories
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Merck Research Laboratories
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.
Merck Research Laboratories
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.
Merck Research Laboratories
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Merck Research Laboratories
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.
Merck Research Laboratories
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
Merck Research Laboratories
Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.
Merck Research Laboratories
Carbohydroxamido-oxazolidines: antibacterial agents that target lipid A biosynthesis.
Merck Research Laboratories
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
Merck Research Laboratories
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.
Merck Research Laboratories
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.
Merck Research Laboratories
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Merck Research Laboratories
Kampanols: novel Ras farnesyl-protein transferase inhibitors from Stachybotrys kampalensis.
Merck Research Laboratories
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.
Merck Research Laboratories
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.
Merck Research Laboratories
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.
Merck Research Laboratories
Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.
Merck Research Laboratories
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.
Merck Research Laboratories
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
Merck Research Laboratories
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.
Merck Research Laboratories
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Merck Research Laboratories
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.
Merck Research Laboratories
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.
Merck Research Laboratories
Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.
Merck Research Laboratories
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Merck Research Laboratories
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.
Merck Research Laboratories
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.
Merck Research Laboratories
Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.
Merck Research Laboratories
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Merck Research Laboratories
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
Development of a high specific activity sulfur-35-labeled sulfonamide radioligand that allowed the identification of a new growth hormone secretagogue receptor.
Merck Research Laboratories
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Merck Research Laboratories
Novel orally active inhibitors of β-1,3-glucan synthesis derived from enfumafungin.
Merck Research Laboratories
Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
Merck Research Laboratories
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
Merck Research Laboratories
Selective protection and relative importance of the carboxylic acid groups of zaragozic acid A for squalene synthase inhibition.
Merck Research Laboratories
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides.
Merck Research Laboratories
Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.
Merck Research Laboratories
Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.
Merck Research Laboratories
Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors.
Merck Research Laboratories
New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.
Merck Research Laboratories
Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Merck Research Laboratories
(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.
Merck Research Laboratories
Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.
Merck Research Laboratories
A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.
Merck Research Laboratories
Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.
Merck Research Laboratories
1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor.
Merck Research Laboratories
Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity.
Merck Research Laboratories
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp.
Merck Research Laboratories
Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran.
Merck Research Laboratories
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
Merck Research Laboratories
Structure-activity relationships of C1 and C6 side chains of zaragozic acid A derivatives.
Merck Research Laboratories
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.
Merck Research Laboratories
A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain.
Merck Research Laboratories
Synthesis and antifungal evaluation of pentyloxyl-diphenylisoxazoloyl pneumocandins and echinocandins.
Merck Research Laboratories
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Merck Research Laboratories
Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes.
Merck Research Laboratories
A-ring modification of SCH 900229 and related chromene sulfone γ-secretase inhibitors.
Merck Research Laboratories
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.
Merck Research Laboratories
Orally active beta-lactam inhibitors of human leukocyte elastase. 3. Stereospecific synthesis and structure-activity relationships for 3,3-dialkylazetidin-2-ones.
Merck Research Laboratories
Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.
Merck Research Laboratories
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
Merck Research Laboratories
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Merck Research Laboratories
Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Merck Research Laboratories
Synthesis and Evaluation of 5-Fluoro-2-aryloxazolo[5,4-b]pyridines as β-Amyloid PET Ligands and Identification of MK-3328.
Merck Research Laboratories
Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
Merck Research Laboratories
The optimization of pyridazinone series of glucan synthase inhibitors.
Merck Research Laboratories
Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors.
Merck Research Laboratories
Platensimycin and platencin congeners from Streptomyces platensis.
Merck Research Laboratories
SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors.
Merck Research Laboratories
The synthesis and structure-activity relationship of pyridazinones as glucan synthase inhibitors.
Merck Research Laboratories
Design and synthesis of potent Gram-negative specific LpxC inhibitors.
Merck Research Laboratories
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
Merck Research Laboratories
Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.
Merck Research Laboratories
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors.
Merck Research Laboratories
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
Merck Research Laboratories
Fluorinated piperidine acetic acids as gamma-secretase modulators.
Merck Research Laboratories
2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety.
Merck Research Laboratories
Synthesis and biological evaluation of platensimycin analogs.
Merck Research Laboratories
Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.
Merck Research Laboratories
Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Merck Research Laboratories
Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.
Merck Research Laboratories
Barceloneic acid A, a new farnesyl-protein transferase inhibitor from a Phoma species.
Merck Research Laboratories
Microbial transformation of L-696,474, a novel cytochalasin as an inhibitor of HIV-1 protease.
Merck Research Laboratories
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
Merck Research Laboratories
The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I.
Merck Research Laboratories
Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
Merck Research Laboratories
The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.
Merck Research Laboratories
Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.
Merck Research Laboratories
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Merck Research Laboratories
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Merck Research Laboratories
p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.
Merck Research Laboratories
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Merck Research Laboratories
Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.
Merck Research Laboratories
Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators.
Merck Research Laboratories
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.
Merck Research Laboratories
Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.
Merck Research Laboratories
Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Merck Research Laboratories
Inhibitors of human renin with C-termini derived from amides and esters of alpha-mercaptoalkanoic acids.
Merck Research Laboratories
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.
Merck Research Laboratories
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.
Merck Research Laboratories
Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
Hanmi Pharm.
Pyrrolidine-2, 5-dione derivatives, pharmaceutical compositions and methods for use as IDO1 inhibitors
Iteos Therapeutics
1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
Astrazeneca
Sulfonyl piperidine derivatives and their use for treating prokineticin mediated diseases
Takeda Pharmaceutical
Pyrazolyl-substituted heteroaryls and their use as medicaments
Boehringer Ingelheim International
N2-(2-methoxyphenyl)pyrimidine derivative, method for preparing same, and pharmaceutical composition for cancer prevention or treatment containing same as active ingredient
Korea Research Institute of Chemical Technology
1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
Novartis
Piperidine derivative and preparation method and pharmaceutical use thereof
Jiangsu Hengrui Medicine
Fused bicylic pyridine compounds and their use as AMPA receptor modulators
Janssen Pharmaceutica
Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof
Jiangsu Hengrui Medicine
Ethyl N-boc piperidinyl pyrazolo pyridones as Janus kinase inhibitors
Merck Sharp & Dohme
Pyrrole six-membered heteroaryl ring derivative, preparation method thereof, and medicinal uses thereof
Jiangsu Hengrui Medicine
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Boehringer Ingelheim International
5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
Bayer Pharma Aktiengesellschaft
Substituted naphthyridine and quinoline compounds as MAO inhibitors
Dart Neuroscience (Cayman)
G protein-coupled receptor kinase 2 inhibitors and methods for use of the same
The Regents of The University of Michigan
Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy.
University of Illinois
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).
Astrazeneca
Design, synthesis, and pharmacological evaluation of N-bicyclo-5-chloro-1H-indole-2-carboxamide derivatives as potent glycogen phosphorylase inhibitors.
Astellas Pharma
Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
University Hospital Basel
Phthalazinone compounds and methods for the treatment of cystic fibrosis
Flatley Discovery Lab
Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL.
Yale University
Substituted 7-azabicycles and their use as orexin receptor modulators
Janssen Pharmaceutica
Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.
Washington University
Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity.
University of St. Andrews
Structure-activity relationships of a new family of steroidal aromatase inhibitors. 1. Synthesis and evaluation of a series of analogs related to 19-[(methylthio)methyl]androstenedione (RU54115).
Centre De Recherche De Roussel Uclaf
1,2,5,6-tetra-O-benzyl-D-mannitol derivatives as novel HIV protease inhibitors.
Pharmacor
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.
Abbott Bioresearch Center
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.
Wyeth-Ayerst Research
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.
Glaxosmithkline
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
Glaxosmithkline
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
Merck Research Laboratories
Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.
Merck Research Laboratories
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.
Merck Research Laboratories
Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives.
Biocryst Pharmaceuticals
Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor.
University of Auckland
Tyrosine kinase inhibitors. 5. Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth factor receptor.
University of Auckland
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
Boehringer Ingelheim Pharmaceuticals
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
Boehringer Ingelheim Pharmaceuticals
Energetics of heme binding to native and denatured states of cytochrome b562.
University of Illinois
Equilibrium thermodynamics of a physiologically-relevant heme-protein complex.
University of North Carolina At Chapel Hill
Distinct Ca2+ binding properties of novel C2 domains of plant phospholipase dalpha and beta.
Kansas State University
Calorimetric investigation of ethidium and netropsin binding to chicken erythrocyte chromatin.
Universite De Liege
Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor.
Indian Institute of Science
Thermodynamic and structural analysis of phosphotyrosine polypeptide binding to Grb2-SH2.
Schering-Plough Research Institute
Bound water molecules and conformational stabilization help mediate an antigen-antibody association.
Institut Pasteur
Role of salt bridge formation in antigen-antibody interaction. Entropic contribution to the complex between hen egg white lysozyme and its monoclonal antibody HyHEL10.
Tohoku University