3-substituted pyrido[4',3':4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and their use

US6222034A · kind A · utility

Assignee

• BASF SE

Inventors

• Gerd Steiner · Tauberbischofsheim, DE
• Wilfried Lubisch · Mannheim, DE
• Alfred Bach · Heidelberg, DE
• Franz Emling · Ludwigshafen, DE
• Karsten Wicke · Ludwigshafen, DE
• Hans-Jurgen Teschendorf · Dudenhofen, DE
• Berthold Behl · Ludwigshafen, DE
• Sharon C. Cheetham · Nottingham, GB
• Frank Kerrrigan · Nottingham, GB

Key dates

• Filing date: Mar 10, 1999
• Grant date: Apr 24, 2001
• Expiry date: Mar 10, 2019

Classification

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

Abstract

A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula I ##STR1## wherein PA1 R.sup.1 is hydrogen, C.sub.1 -C.sub.4 -alkyl, acetyl or benzoyl, optionally substituted phenyl-C.sub.1 -C.sub.4 -alkyl, naphthyl-C.sub.1 -C.sub.3 -alkyl, phenyl-C.sub.2 -C.sub.3 -alkanone or a phenylcarbamoyl-C.sub.2 -alkyl, PA1 R.sup.2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring, PA1 A is NH or oxygen, PA1 B is hydrogen or methyl, PA1 C is hydrogen, methyl or hydroxyl, PA1 X is nitrogen, PA1 Y is CH.sub.2, CH.sub.2 --C.sub.2, CH.sub.2 --C.sub.2 --CH.sub.2 or CH.sub.2 --CH, PA1 Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, and PA1 n is 2, 3 or 4, or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT.sub.1B and 5HT.sub.1A and for the treatment of depression and related disorders.