104 articles for thisTarget
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Article Title
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Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.
Abbott Laboratories
GnRH antagonists: the promise of treating sex-hormone-related diseases.
Therachem Research Medilab (India)
Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression.
Norwegian Medical Cyclotron Centre
Influences of hydrocarbon linkers on the receptor binding affinities of gonadotropin-releasing hormone peptides.
University of New Mexico
Enhanced cellular uptake and in vitro antitumor activity of short-chain fatty acid acylated daunorubicin-GnRH-III bioconjugates.
TBA
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
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Neurocrine Biosciences
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.
Leiden University
The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies.
Neurocrine Biosciences
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.
Takeda Pharmaceutical
Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.
Salk Institute
Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.
Salk Institute
Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.
Neurocrine Biosciences
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
Takeda Chemical Industries
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.
Ferring Research Institute
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
Takeda Chemical Industries
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Takeda Pharmaceutical
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Merck Research Laboratories
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.
Wyeth Research
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Wyeth Research
Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.
Wyeth Research
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
Neurocrine Biosciences
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Neurocrine Biosciences
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Wyeth Research
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Neurocrine Biosciences
Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.
Astrazeneca
Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists.
Neurocrine Biosciences
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.
Neurocrine Biosciences
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.
Salk Institute
Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist.
Yantai University
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.
Neurocrine Biosciences
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
Neurocrine Biosciences
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.
Neurocrine Biosciences
Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.
Salk Institute
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.
Neurocrine Biosciences
Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives.
Kyoto 619-0216
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
Neurocrine Biosciences
Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.
Neurocrine Biosciences
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides.
Kyoto 619-0216
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.
Kyoto 619-0216
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.
Neurocrine Biosciences
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
Merck Research Laboratories
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.
Neurocrine Biosciences
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.
Neurocrine Biosciences
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
Neurocrine Biosciences
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.
Merck
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.
Neurocrine Biosciences
Development of programmable gemcitabine-GnRH pro-drugs bearing linker controllable "click" oxime bond tethers and preclinical evaluation against prostate cancer.
University of Ioannina
Receptor-mediated targeting of a photosensitizer by its conjugation to gonadotropin-releasing hormone analogues.
Institute of Science
Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.
Neurocrine Biosciences
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.
Neurocrine Biosciences
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.
Neurocrine Biosciences
Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Neurocrine Biosciences
Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists.
Agouron Pharmaceuticals
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.
Neurocrine Biosciences
The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists.
Agouron Pharmaceuticals
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.
Merck Research Laboratories
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Neurocrine Biosciences
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Neurocrine Biosciences
A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones.
Takeda Chemical Industries
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.
Merck Research Laboratories
A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.
Neurocrine Biosciences
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.
Neurocrine Biosciences
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Bayer
Design, synthesis, and evaluation of a long-acting, potent analogue of gonadotropin-releasing hormone.
Institute of Science
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
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
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
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
Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.
Institute of Science
Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.
Institute of Science
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.
Merck Research Laboratories
Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.
Sk Chemicals
Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.
Merck Research Laboratories
Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling.
Salk Institute
Design of potent dicyclic (1-5/4-10) gonadotropin releasing hormone (GnRH) antagonists.
Salk Institute
Design of monocyclic (1-3) and dicyclic (1-3/4-10) gonadotropin releasing hormone (GnRH) antagonists.
Salk Institute
Design of potent dicyclic (4-10/5-8) gonadotropin releasing hormone (GnRH) antagonists.
Salk Institute
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
In vitro and in vivo activities of reduced-size antagonists of luteinizing hormone-releasing hormone.
Tap Pharmaceuticals
The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists.
Abbott Laboratories
LH-RH antagonists: design and synthesis of a novel series of peptidomimetics.
Abbott Laboratories
Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
Tiumbio
Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N omega-cyanoguanidino moieties.
Salk Institute
Gonadotropin-releasing hormone antagonists with N omega-triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6.
Salk Institute
FUSED BICYCLIC SUBSTITUTED N-(1H-INDOL-7-YL)BENZENESULFONAMIDES AND USES THEREOF
Triana Biomedicines
Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)
Indiana University Research and Technology
Identification of Inhibitors of PvdQ, an Enzyme Involved in the Synthesis of the Siderophore Pyoverdine.
The Broad Institute , Cambridge, Massachusetts 02142, United States