The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Sep. 20, 1988
Filed:
Dec. 30, 1986
Maurice Manning, Toledo, OH (US);
Wilbur H Sawyer, Scarsdale, NY (US);
Medical College of Ohio, Toledo, OH (US);
Trustees of Columbia University, New York, NY (US);
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(NH.sub.2), Ser(NH.sub.2), (D- or L-)Ala(NH.sub.2), Gly, OH or NH.sub.2 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(CH.sub.2).sub.3-6 NH.sub.2, NH(CH.sub.2).sub.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(CH.sub.2).sub.2-6 OH, NH(CH.sub.2).sub.2-6 NH.sub.2 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 NH.sub.2. 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, NH.sub.2, NHalk, NH(CH.sub.2).sub.2-6 NH.sub.2, NHbzl or NH(CH.sub.2).sub.2-6 OH. Additional compounds include those wherein X is D-Tyr.