Linear derivatives of arginine vasopressin antagonists

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.
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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 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.
Subject(s): 514/10.9
514/15.4
514/807
530/315
530/317
530/328
530/329
Date Issued: 1991-10-08
Title: Linear 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: 1987-06-25
Date Issued: 1991-10-08
Physical Form: application/pdf
Extent: 11 p.
Abstract/Description: 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.
Identifier(s): utpatents-US5055448 (IID)
Patent No.: US5055448 (patno)
Appl. No.: 07/066949 (appno)
Subject(s): 514/10.9
514/15.4
514/807
530/315
530/317
530/328
530/329
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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