Abstract

Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula A--CH2 CO--D--Tyr(R)--Phe--Y--Asn--T--U--Z--Qwherein A is a-adamantyl, cyclohexyl, cyclopentyl, 1-mercaptocyclohexyl, 1-mercaptocyclopentyl, 1-ethyl-1-mercaptopropyl, yclohexylmethyl, cyclopentylmethyl, methyl, isopropyl, tert-butyl or phenyl; R is alkyl of 1-4 carbon atoms; Y is Val, Ile, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; T is Pen, Abu, Orn, Oys, Arg, Ala, Cha or Thr; U is Pro, Arg, Lys or Orn or a single bond; Z is (d-or L-) Arg, Orn or Lys and Q is Gly(NH2), Arg (NH2), Orn(NH2), Lys (NH2), (D- or L-)Ala(NH2), Ser(NH2), Val(NH2), Phe(NH2), Ile(NH2), Thr(NH2), Pro(NH2), Tyr(NH2), NH2, OH, NHR, NGbzl, NH(CH2)p NH2 or NH(CH2)p OH, wherein R is as above and p is an integer from 2 to 6. Compounds wherein T is Cys have similar activity.

Document Type

Patent

Primary Class

514/10.9

Secondary Class

514/15.4; 514/807; 530/315; 530/317; 530/328; 530/329

Application Number

07/066949

Filing Date

June 1987

Patent Number

US5055448

Assignee(s)

Medical College of Ohio; The Trustees of Columbia University

Publication Date

10-8-1991

Patent Country

US

Language

en_US

Institution

The University of Toledo

Repository

University of Toledo Libraries

Digital Publisher

Digital Initiatives

Rights

These materials are free of copyright restrictions and are in the public domain within the United States only. The USPTO reserves the right to assert copyright protection internationally.

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Rights Statement

No Copyright - United States. URI: http://rightsstatements.org/vocab/NoC-US/1.0/
The organization that has made the Item available believes that the Item is in the Public Domain under the laws of the United States, but a determination was not made as to its copyright status under the copyright laws of other countries. The Item may not be in the Public Domain under the laws of other countries. Please refer to the organization that has made the Item available for more information.