Heptapeptide oxytocin analogues

US6143722A · kind A · utility

Assignee

• Ferring B.V. · NL

Inventors

• Per Melin · Malmö, SE
• Anders Nilsson · Västerås, SE
• Jerzy Trojnar · Vintrie, SE
• Carl-Johan Aurell · Timrå, SE
• Pierre Riviere · San Diego, US
• Robert Haigh · Ormskirk, GB

Key dates

• Filing date: Aug 2, 1999
• Grant date: Nov 7, 2000
• Expiry date: Aug 2, 2019

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal .beta.-aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the .beta.-aminoalcohol Z is --NR--CH(Q)--CH.sub.2 OH, Q is (CH.sub.2).sub.n --NH--A is H or --C(.dbd.NH)NH.sub.2, and R is CH.sub.3 or C.sub.2 H.sub.5, and the moiety S wherein H is a D-aromatic .alpha.-aminoacid and Y is an aliphatic .alpha.-aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.