PMID

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Article Title

Organization

Effects of a D-Cys6/L-Cys6 interchange in nonselective and selective vasopressin and oxytocin antagonists.

Medical College of Ohio

Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.

University of Montpellier

New analgesic drugs derived from phencyclidine.

TBA

Enhanced selectivity of oxytocin antagonists containing sarcosine in position 7.

Max-Planck-Institut F£R Biophysik

Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.

Merck Research Laboratories

Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.

Merck

Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.

Johnson and Johnson Pharmaceutical Research and Development

N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.

Yamanouchi Pharmaceutical

Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.

Albert Szent-Gy£Rgyi Medical University

Oral oxytocin antagonists.

Drugmoldesign

 

Non-peptide oxytocin antagonists: identification and synthesis of a potent camphor aminosuccinimide

TBA

New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.

Vantia

Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.

Johnson & Johnson Pharmaceutical Research & Development

Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.

Central Pharmaceutical Research Institute

Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.

Wyeth Research

Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.

Johnson & Johnson Pharmaceutical Research & Development

Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.

Otsuka Pharmaceutical

Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.

Yamanouchi Pharmaceutical

Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.

Otsuka Pharmaceutical

The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.

Wyeth-Ayerst Research

Discovery of Potent, Selective, and Short-Acting Peptidic V

Ferring Research Institute

5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.

Wyeth-Ayerst Research

4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.

Wyeth-Ayerst Research

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

Merck Research Laboratories

5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.

Wyeth-Ayerst Research

Orally active, nonpeptide vasopressin V2 receptor antagonists: a novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds.

Otsuka Pharmaceutical

Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.

Otsuka Pharmaceutical

Nanomolar-affinity, non-peptide oxytocin receptor antagonists.

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

A new series of photoactivatable and iodinatable linear vasopressin antagonists.

Upr 9023 Cnrs

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

LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.

Umr7200 Cnrs/Universit£

Arginine-vasopressin analogues with high antidiuretic/vasopressor selectivity. Synthesis, biological activity, and receptor binding affinity of arginine-vasopressin analogues with substitutions in positions 1, 2, 4, 7, and 8.

TBA

Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications.

Merck Sharp & Dohme Research Laboratories

Orally active, nonpeptide oxytocin antagonists.

Merck Research Laboratories

Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.

Columbia University

Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist.

Sanofi-Synthelabo Recherche

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.

Second Tokushima Institute of New Drug Research

Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo.

Yamanouchi Pharmaceutical

GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.

Glaxo Group Research

In vitro pharmacological profile of a novel structural class of oxytocin antagonists.

Merck Sharp & Dohme Research Laboratories

Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.

Astellas Pharma