Kappa-opiate agonists for inflammatory bowel disorders

US5776972A · kind A · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Andrew Barber · Weiterstadt, DE
• Christoph Seyfried · Seeheim-Jugenheim, DE
• Gerd Bartoszyk · Weiterstadt, DE
• Rudolf Gottschlich · Reinheim, DE

Key dates

• Filing date: Jun 27, 1996
• Grant date: Jul 7, 1998
• Expiry date: Jun 27, 2016

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms, PA1 R.sup.2 is Ar, or PA1 R.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2, PA1 R.sup.5 is OH, CH.sub.2 OH, PA1 R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring, PA1 A is alkyl having 1-7 C atoms, PA1 Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2, PA1 D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --,--CH.dbd.CH--,--CH.sub.2 --NH--,--CH.sub.2 --NA-- or a bond and PA1 Hal is F, Cl, Br or I; and/or physiologically a…