V1-vasopressin antagonists

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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530315, C07K 716, A61K 3734

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active

045993246

ABSTRACT:
Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.

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patent: 4491577 (1985-01-01), Manning et al.
J. Lowbridge et al., J. Med. Chem. 22 565 (1979).
M. Manning et al., J. Med. Chem. 20 1228 (1977).
K. Bankowski et al., J. Med. Chem. 21 350 (1978).
H. Schulz et al., J. Med. Chem. 9 647 (1966).
Derwent Abstract of European Patent No. 112,809-A.
M. Manning et al., J. Med. Chem. 25 408-414 (1982).
Peptides: Chemistry, Structure and Biology (Ann Arbor Sciences) 737 (1975).
Rittel et al., Experientia, 32(2), 246-248 (1976).
March, Advanced Organic Chemistry, 2nd Ed., McGraw-Hill Book Company, N.Y. 1977, pp. 251-256.

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