Back to results
US 4,724,229 AGranted
Arg-arg-arg-vasopressin antagonists
AssigneeSmithKline Beckman Corporation
InventorFadia E. Ali
Life of this patent
Estimating the term…
Abstract
Vasopressin antagonists which have a tripeptide side chain comprised of three basic amino acids, such as arginine, lysine or ornithine, demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-arginine]-va sopression.
Claims30
A compound having the formula:
- ##STR14## in which:
- P is a D or L isomer of Arg, Lys, Orn, HArg, MeArg, MeLys or MeHArg;
- A is a D or L isomer of Arg, Lys, Orn, HArg, MeArg, MeLys or MeHArg;
- E is a D or L isomer of Arg, Lys, Orn, HArg, MeArg, MeLys or MeHArg;
- B is OH, NH.sub.2 or NHAlk;
- Z is Phe, 4'-Alk Phe, O-Alk Tyr, Ile or Tyr;
- X is a D or L isomer of Phe, 4'-Alk Phe, Val, Nva, Leu, Ile, Pba, Nle, Cha, Abu, Met, Chg, Tyr or O-Alk Tyr;
- Y is Val, Ile, Abu, Ala, Chg, Gln, Lys, Cha, Nle, Thr, Phe, Leu or Gly;
- and
- R.sub.1 and R.sub.2 are, each, hydrogen, methyl, ethyl or, when taken together and with the .beta.-carbon to which they are attached, a cycloalkylene ring of 4 to 6 members;
- and wherein Alk is an alkyl of 1 to 4 carbons;
- or a pharmaceutically acceptable salt or prodrug thereof.
9 more elements
Dependencies are inferred from the claim text.