PMID

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Article Title

Organization

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

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

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

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

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

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

2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.

Wyeth Research

Non-peptide gonadotropin-releasing hormone receptor antagonists.

Neurocrine Biosciences

Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.

Astrazeneca

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 a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.

Pfizer

Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.

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

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

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

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

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

Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists.

Agouron Pharmaceuticals

The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists.

Agouron Pharmaceuticals

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

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

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

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

Betidamino acid scan of the GnRH antagonist acyline.

Salk Institute

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

Design of potent cyclic gonadotropin releasing hormone antagonists.

Salk Institute

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