Novel derivatives of arginine vasopressin antagonists

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-lle, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, lle, 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 Orn(NH2), NHCH2 CH2 NH2, Val(NH2), Phe(NH2), lle(NH2), Thr(NH2), Pro(NH2) or Tyr(NH2).
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Abstract/Description: 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-lle, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, lle, 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 Orn(NH2), NHCH2 CH2 NH2, Val(NH2), Phe(NH2), lle(NH2), Thr(NH2), Pro(NH2) or Tyr(NH2).
Subject(s): 514/10.9
514/15.4
514/21.1
514/807
530/315
930/20
930/21
930/150
Date Issued: 1987-03-10
Title: Novel derivatives of arginine vasopressin antagonists.
Name(s): Medical College of Ohio; The Trustees of Columbia University, assignee
Manning, Maurice, inventor
Sawyer, Wilbur H., inventor
Type of Resource: text
Genre: patent
Publisher: United States Patent and Trademark Office
Other Date: Date Filed: 1985-01-23
Date Issued: 1987-03-10
Physical Form: application/pdf
Extent: 9 p.
Abstract/Description: 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-lle, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, lle, 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 Orn(NH2), NHCH2 CH2 NH2, Val(NH2), Phe(NH2), lle(NH2), Thr(NH2), Pro(NH2) or Tyr(NH2).
Identifier(s): utpatents-US4649130 (IID)
Patent No.: US4649130 (patno)
Appl. No.: 06/693870 (appno)
Subject(s): 514/10.9
514/15.4
514/21.1
514/807
530/315
930/20
930/21
930/150
Held by: United States Patent and Trademark Office (USPTO) Public Search Facility
Location: University of Toledo Digital Repository
Rights Statement: No Copyright - United States
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