PMID

Data

Article Title

Organization

Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.

Msd

The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists.

Msd

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

Medical College of Ohio

Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.

Schering-Plough Research Institute

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

Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.

Wyeth Research

Design of benzophenone-containing photoactivatable linear vasopressin antagonists: pharmacological and photoreactive properties.

University of Montpellier

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

Merck Research Laboratories

Preparation and biological activities of potential vasopressin photoaffinity labels.

University of Sherbrooke

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

New, potent, selective, and short-acting peptidic V1a receptor agonists.

Ferring Research Institute

Oral oxytocin antagonists.

Drugmoldesign

Khusimol, a Non-Peptide Ligand for Vasopressin V_1a Receptors

TBA

 

Vasopressin trisulphide: synthesis, NMR study and affinity studies with V₁ and V₂ subtypes receptors

TBA

 

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

TBA

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 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

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