Piperazine compounds as fibrinogen inhibitors

US5908843A · kind A · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Joachim Gante · Darmstadt, DE
• Peter Raddatz · Darmstadt, DE
• Horst Juraszyk · Seeheim-Jugenheim, DE
• Sabine Bernotat-Danielowski · Bad Nauheim, DE
• Guido Melzer · Hofheim, DE

Key dates

• Filing date: Jan 31, 1994
• Grant date: Jun 1, 1999
• Expiry date: Jan 31, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D295/215
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel piperazine derivatives of formula I: EQU Y--(C.sub.m H.sub.2m --CHR.sup.1).sub.n --CO--(NH--CHR.sup.2 --CO).sub.r -- Z wherein ##STR1## R.sup.1, R.sup.2 and R.sup.7 are each, independently, --C.sub.t H.sub.2t --R.sup.9, benzyl, hydroxybenzyl, imidazolylmethyl or indolylmethyl; PA1 R.sup.3 is H or H.sub.2 N--C(.dbd.NH)--; PA1 R.sup.4 and R.sup.6 are each, independently, (H,H) or .dbd.O; PA1 R.sup.5 is H, H.sub.2 N--C(.dbd.NH)-- or H.sub.2 N--C(.dbd.NH)--NH; PA1 R.sup.8 is OH, OA or NHOH; PA1 R.sup.9 is H, OH, NH.sub.2, SH, SA, COOH, CONH.sub.2 or NH--C(.dbd.NH)--NH.sub.2 ; PA1 A is in each case, independently, alkyl having 1-4 C atoms; PA1 m and t are each, independently, 0, 1, 2, 3 or 4; PA1 n and r are each, independently, 0 or 1; and PA1 p is 0, 1 or 2, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for the treatment of thrombosis, apoplexy, cardiac infarctus, inflammation, arteriosclerosis and tumors.