442 articles for thisTarget
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Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics.
Abbott Laboratories
Synthesis and activity of nonhydrolyzable pseudomonic acid analogues.
Abbott Laboratories
Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.
Abbott Laboratories
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
Abbott Laboratories
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
Abbott Laboratories
Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC).
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.
Abbott Laboratories
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
Abbott Laboratories
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
Abbott Laboratories
Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.
Abbott Laboratories
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Abbott Laboratories
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
Abbott Laboratories
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Abbott Laboratories
Large-scale application of high-throughput molecular mechanics with Poisson-Boltzmann surface area for routine physics-based scoring of protein-ligand complexes.
Abbott Laboratories
Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.
Abbott Laboratories
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Abbott Laboratories
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Abbott Laboratories
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.
Abbott Laboratories
Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.
Abbott Laboratories
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
Abbott Laboratories
Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.
Abbott Laboratories
Active reduced-size hexapeptide analogues of luteinizing hormone-releasing hormone.
Abbott Laboratories
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.
Abbott Laboratories
Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.
Abbott Laboratories
Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.
Abbott Laboratories
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Abbott Laboratories
Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.
Abbott Laboratories
Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.
Abbott Laboratories
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²¿ channel blockers with analgesic activity.
Abbott Laboratories
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Abbott Laboratories
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management.
Abbott Laboratories
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.
Abbott Laboratories
Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
Abbott Laboratories
Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors.
Abbott Laboratories
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.
Abbott Laboratories
Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.
Abbott Laboratories
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
Abbott Laboratories
Allosteric modulators of the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R).
Abbott Laboratories
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Abbott Laboratories
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.
Abbott Laboratories
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Abbott Laboratories
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Abbott Laboratories
Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.
Abbott Laboratories
Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
Abbott Laboratories
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Abbott Laboratories
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.
Abbott Laboratories
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
Abbott Laboratories
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Abbott Laboratories
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.
Abbott Laboratories
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.
Abbott Laboratories
Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.
Abbott Laboratories
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.
Abbott Laboratories
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
Abbott Laboratories
Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.
Abbott Laboratories
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
Abbott Laboratories
Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase.
Abbott Laboratories
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
Abbott Laboratories
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
Abbott Laboratories
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.
Abbott Laboratories
(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor.
Abbott Laboratories
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).
Abbott Laboratories
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Abbott Laboratories
Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity.
Abbott Laboratories
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
Abbott Laboratories
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
Abbott Laboratories
CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.
Abbott Laboratories
Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes.
Abbott Laboratories
Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung.
Abbott Laboratories
2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists.
Abbott Laboratories
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.
Abbott Laboratories
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.
Abbott Laboratories
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
Abbott Laboratories
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.
Abbott Laboratories
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
Abbott Laboratories
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.
Abbott Laboratories
Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue.
Abbott Laboratories
Optimization and in vivo evaluations of a series of small, potent, and specific renin inhibitors containing a novel Leu-Val replacement.
Abbott Laboratories
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Abbott Laboratories
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.
Abbott Laboratories
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
Abbott Laboratories
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Abbott Laboratories
SAR ofa7 nicotinic receptor agonists derived from tilorone: exploration of a novel nicotinic pharmacophore.
Abbott Laboratories
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
Abbott Laboratories
Cracking the molecular weight barrier: fragment screening of an aminotransferase using an NMR-based functional assay.
Abbott Laboratories
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.
Abbott Laboratories
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.
Abbott Laboratories
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.
Abbott Laboratories
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Abbott Laboratories
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
Abbott Laboratories
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Abbott Laboratories
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Abbott Laboratories
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
Abbott Laboratories
Biochemical and biophysical characterization of unique switch pocket inhibitors of p38a.
Abbott Laboratories
Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
Abbott Laboratories
In vitro studies on a class of quinoline containing histamine H3 antagonists.
Abbott Laboratories
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Abbott Laboratories
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Abbott Laboratories
Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs.
Abbott Laboratories
Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Abbott Laboratories
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
Abbott Laboratories
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Abbott Laboratories
Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Abbott Laboratories
Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.
Abbott Laboratories
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
Abbott Laboratories
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
Abbott Laboratories
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.
Abbott Laboratories
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Abbott Laboratories
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Abbott Laboratories
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Abbott Laboratories
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Abbott Laboratories
7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Abbott Laboratories
Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase.
Abbott Laboratories
Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.
Abbott Laboratories
Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor.
Abbott Laboratories
Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies.
Abbott Laboratories
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.
Abbott Laboratories
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors.
Abbott Laboratories
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
Abbott Laboratories
Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.
Abbott Laboratories
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
Abbott Laboratories
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.
Abbott Laboratories
Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.
Abbott Laboratories
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Abbott Laboratories
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Abbott Laboratories
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Abbott Laboratories
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Abbott Laboratories
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
Abbott Laboratories
N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-coA carboxylase inhibitors--improvement of cardiovascular and neurological liabilities via structural modifications.
Abbott Laboratories
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Abbott Laboratories
Phenoxy thiazole derivatives as potent and selective acetyl-CoA carboxylase 2 inhibitors: Modulation of isozyme selectivity by incorporation of phenyl ring substituents.
Abbott Laboratories
The synthesis and structure-activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: polar region modifications.
Abbott Laboratories
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Abbott Laboratories
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Abbott Laboratories
4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.
Abbott Laboratories
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Abbott Laboratories
4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.
Abbott Laboratories
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Abbott Laboratories
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Abbott Laboratories
Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
Abbott Laboratories
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
Abbott Laboratories
Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.
Abbott Laboratories
Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.
Abbott Laboratories
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Abbott Laboratories
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Abbott Laboratories
Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.
Abbott Laboratories
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Abbott Laboratories
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists.
Abbott Laboratories
1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.
Abbott Laboratories
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Abbott Laboratories
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Abbott Laboratories
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring.
Abbott Laboratories
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides.
Abbott Laboratories
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Abbott Laboratories
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Abbott Laboratories
Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.
Abbott Laboratories
Optimization of 2,4-diaminopyrimidines as GHS-R antagonists: side chain exploration.
Abbott Laboratories
Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels.
Abbott Laboratories
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists.
Abbott Laboratories
Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
Abbott Laboratories
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
Abbott Laboratories
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Abbott Laboratories
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.
Abbott Laboratories
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Abbott Laboratories
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Abbott Laboratories
Synthesis and biological evaluation of 6,7-disubstituted 4-aminopyrido[2,3-d]pyrimidines as adenosine kinase inhibitors.
Abbott Laboratories
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Abbott Laboratories
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.
Abbott Laboratories
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Abbott Laboratories
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Abbott Laboratories
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
Abbott Laboratories
Amino-substituted heterocycles as isosteres of trans-cinnamides: design and synthesis of heterocyclic biaryl sulfides as potent antagonists of LFA-1/ICAM-1 binding.
Abbott Laboratories
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Abbott Laboratories
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.
Abbott Laboratories
Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.
Abbott Laboratories
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.
Abbott Laboratories
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Abbott Laboratories
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
Abbott Laboratories
Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand.
Abbott Laboratories
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Abbott Laboratories
Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors.
Abbott Laboratories
Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
Abbott Laboratories
Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors.
Abbott Laboratories
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
Abbott Laboratories
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.
Abbott Laboratories
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
Abbott Laboratories
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
Abbott Laboratories
A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.
Abbott Laboratories
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Abbott Laboratories
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.
Abbott Laboratories
5,6,7-trisubstituted 4-aminopyrido[2,3-d]pyrimidines as novel inhibitors of adenosine kinase.
Abbott Laboratories
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Abbott Laboratories
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
Abbott Laboratories
Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor.
Abbott Laboratories
Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors.
Abbott Laboratories
Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.
Abbott Laboratories
Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.
Abbott Laboratories
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.
Abbott Laboratories
The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure-activity relationships of 2-amino-4-azaindoles.
Abbott Laboratories
Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
Abbott Laboratories
Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Abbott Laboratories
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.
Abbott Laboratories
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Abbott Laboratories
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor.
Abbott Laboratories
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Abbott Laboratories
NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.
Abbott Laboratories
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
Abbott Laboratories
Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors.
Abbott Laboratories
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
Abbott Laboratories
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
Abbott Laboratories
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Abbott Laboratories
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Abbott Laboratories
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.
Abbott Laboratories
Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.
Abbott Laboratories
Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides.
Abbott Laboratories
Synthesis and biological evaluation of clitocine analogues as adenosine kinase inhibitors.
Abbott Laboratories
Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.
Abbott Laboratories
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Abbott Laboratories
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.
Abbott Laboratories
Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.
Abbott Laboratories
Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor..
Abbott Laboratories
Thiazole analogues of the NSAID indomethacin as selective COX-2 inhibitors.
Abbott Laboratories
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
Abbott Laboratories
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Abbott Laboratories
Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists.
Abbott Laboratories
Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.
Abbott Laboratories
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.
Abbott Laboratories
Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression.
Abbott Laboratories
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
Abbott Laboratories
Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.
Abbott Laboratories
Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.
Abbott Laboratories
Design of adenosine kinase inhibitors from the NMR-based screening of fragments.
Abbott Laboratories
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.
Abbott Laboratories
Identification of novel inhibitors of urokinase via NMR-based screening.
Abbott Laboratories
Antifungal rapamycin analogues with reduced immunosuppressive activity.
Abbott Laboratories
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Abbott Laboratories
Discovery of a series of cyclohexylethylamine-containing protein farnesyltransferase inhibitors exhibiting potent cellular activity.
Abbott Laboratories
Retention of immunosuppressant activity in an ascomycin analogue lacking a hydrogen-bonding interaction with FKBP12.
Abbott Laboratories
Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework.
Abbott Laboratories
Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
Abbott Laboratories
Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.
Abbott Laboratories
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.
Abbott Laboratories
NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.
Abbott Laboratories
Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.
Abbott Laboratories
trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.
Abbott Laboratories
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.
Abbott Laboratories
Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.
Abbott Laboratories
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.
Abbott Laboratories
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Abbott Laboratories
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.
Abbott Laboratories
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.
Abbott Laboratories
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Abbott Laboratories
Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.
Abbott Laboratories
Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).
Abbott Laboratories
Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase.
Abbott Laboratories
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency.
Abbott Laboratories
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.
Abbott Laboratories
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.
Abbott Laboratories
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.
Abbott Laboratories
NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.
Abbott Laboratories
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign pr
Abbott Laboratories
(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.
Abbott Laboratories
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.
Abbott Laboratories
Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.
Abbott Laboratories
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
Abbott Laboratories
Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.
Abbott Laboratories
Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.
Abbott Laboratories
5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.
Abbott Laboratories
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Abbott Laboratories
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
Abbott Laboratories
Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.
Abbott Laboratories
Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-725
Abbott Laboratories
Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides.
Abbott Laboratories
Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol.
Abbott Laboratories
Novel Asp32-replacement tetrapeptide analogues as potent and selective CCK-A agonists.
Abbott Laboratories
Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog.
Abbott Laboratories
Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores.
Abbott Laboratories
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.
Abbott Laboratories
Structure-activity studies of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
Abbott Laboratories
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
Abbott Laboratories
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Abbott Laboratories
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
Abbott Laboratories
The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists.
Abbott Laboratories
In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase.
Abbott Laboratories
Renin inhibitors based on novel dipeptide analogues. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond.
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.
Abbott Laboratories
New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site.
Abbott Laboratories
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.
Abbott Laboratories
Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.
Abbott Laboratories
Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists.
Abbott Laboratories
LH-RH antagonists: design and synthesis of a novel series of peptidomimetics.
Abbott Laboratories
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.
Abbott Laboratories
Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships.
Abbott Laboratories
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.
Abbott Laboratories
New inhibitors of renin that contain novel phosphostatine Leu-Val replacements.
Abbott Laboratories
Identification and synthesis of a receptor binding site of human anaphylatoxin C5a.
Abbott Laboratories
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Abbott Laboratories
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
Abbott Laboratories
Improvements in the minimum binding sequence of C5a: examination of His-67.
Abbott Laboratories
Structure-function studies in a series of carboxyl-terminal octapeptide analogues of anaphylatoxin C5a.
Abbott Laboratories
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
Abbott Laboratories
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.
Abbott Laboratories
C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties.
Abbott Laboratories
Nonpeptide renin inhibitors employing a novel 3-aza(or oxa)-2,4-dialkyl glutaric acid moiety as a P2/P3 amide bond replacement.
Abbott Laboratories
Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
Abbott Laboratories
Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.
Abbott Laboratories
Discovery of a novel class of orally active, non-peptide angiotensin II antagonists.
Abbott Laboratories
Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists.
Abbott Laboratories
Oxepan-2-yl-pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
Genentech
Antibacterial cyclopental[C]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones
Janssen Ireland
Substituted 4,5,6,7-tetrahydropyrazolo[1,5-A]pyrazine derivatives as casein kinase 1 D/E inhibitors
Bristol-Myers Squibb
Heterocyclylalkyne derivatives and their use as modulators of mGluR5 receptors
Recordati Ireland
Substituted pyrrolidines as factor XIa inhibitors for the treatment thromboembolic diseases
Ono Pharmaceutical
Heterocyclic GSK-3 allosteric modulators
Consejo Superior de Investigaciones Cientificas (CSIC)
Preparation method for benzoxazoleoxazine ketone compound and intermediate and crystal form thereof
North China Pharmaceutical New Drug R&D
Therapeutic thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6h)-ones
Dart Neuroscience (Cayman)
2-oxo-6,7-dihydrobenzo[a]quinolizine-3-carboxylic acid derivatives for the treatment and prophylaxis of hepatitis B virus infection
Hoffmann-La Roche
Substituted [1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists
Ogeda
Quinazoline scaffold based compounds, pharmaceutical compositions and methods of use thereof
Technion Research & Development Foundation
Dihydropyridinone MGAT2 inhibitors for use in the treatment of metabolic disorders
Bristol-Myers Squibb
Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.
University of California San Francisco
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.
Merck Research Laboratories
Ethylene biosynthesis: processing of a substrate analog supports a radical mechanism for the ethylene-forming enzyme.
Duke University
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
University of California San Francisco
Thermodynamics of molecular recognition by cyclodextrins. 1. Calorimetric titration of inclusion complexation of naphthalenesulfonates with .alpha.-, .beta.-, and .gamma.-cyclodextrins: enthalpy-entropy compensation
Himeji Institute of Technology
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.
Boehringer Ingelheim Pharmaceuticals
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School
Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR).
Exelixis
Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct.
Universita Degli Studi Di Firenze
Discovery of novel nitrobenzothiazole inhibitors for Mycobacterium tuberculosis ATP phosphoribosyl transferase (HisG) through virtual screening.
Yale University
BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.
University of Dundee
Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).
Paradigm Pharmaceuticals
5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
National Institutes of Health
Methylxanthine drugs are chitinase inhibitors: investigation of inhibition and binding modes.
University of Dundee
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
University of North Carolina at Chapel Hill
6-aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
Glaxosmithkline
Hydroxyethylene sulfones as a new scaffold to address aspartic proteases: design, synthesis, and structural characterization.
Philipps-Universitat Marburg
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes.
Uppsala University
Pyrazolo[3,4-c]pyridazines as novel and selective inhibitors of cyclin-dependent kinases.
Universidad San Pablo Ceu
A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.
Banyu Tsukuba Research Institute
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.
Bristol-Myers Squibb
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.
Bristol-Myers Squibb
The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.
Merck Research Laboratories
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Merck Research Laboratories
Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.
Merck Research Laboratories
Structure-activity relationships of carbocyclic influenza neuraminidase inhibitors
Gilead Sciences
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.
Yamanouchi Pharmaceutical
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70.
Ariad Pharmaceuticals
Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Sugen
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src).
University of Auckland
Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor
Parke-Davis Pharmaceutical Research