Document Type

Patent

Abstract

Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula ##STR1## wherein n is 4 or 5; X is (D- or L-)Tyr(R), D-Phe, D-Val, D-Leu, D-Ile, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, Ile, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; Z is (D- or L-) Arg, Orn or Lys; Q is Arg(NH2), Ser(NH2), (D- or L-)Ala(NH2), Gly, OH or NH2 and R is methyl, ethyl, propyl or butyl; provided that, when Y is Gln or Val, R may also be H. Further compounds are those wherein Q is NH(CH2)3-6 NH2, NH(CH2)2-6 OH, NHalk or NHbzl, provided that when Y is Val, Q is other than NHalk or NHbzl. Other compounds are those wherein Q is M-P, wherein M is Gly, (D- or L-)beta-Ala, (D- or L-)Ala, Sar, Orn, Val, Phe, Ile, Thr, Pro, Tyr, Arg or Ser and P is NHalk, NHbzl, NH(CH2)2-6 OH, NH(CH2)2-6 NH2 or OH, provided that when M is Gly, P is other than OH, and that when M is (D-or L-)beta-Ala, P is also NH2. Further compounds include decapeptides wherein Q is M-A-P', wherein M and A are selected independently from Gly, (D- or L-)beta-Ala, (D-or L-)Ala, Sar, Orn, Val, Phe, Ile, Thr, Pro, Tyr, Arg or Ser and P' is OH, NH2, NHalk, NH(CH2)2-6 NH2, NHbzl or NH(CH2)2-6 OH. Additional compounds include those wherein X is D-Tyr.

Patent Country

US

Patent Number

US4772586

Publication Date

9-20-1988

Assignee(s)

Medical College of Ohio; The Trustees of Columbia University

Application Number

06/947725

Filing Date

December 1986

Primary Class

514/10.9

Secondary Class

514/15.4; 514/21.1; 514/807; 530/315; 930/20; 930/21; 930/150; 930/DIG.565; 930/DIG.566; 930/DIG.567

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.

Institution

The University of Toledo

Repository

University of Toledo Libraries

Digital Publisher

Digital Initiatives

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