Compounds which are selective antagonists of the human NK.sub.3 receptor and their use as medicinal products and diagnostic tools

US5942523A · kind A · utility

Assignee

• Sanofi · FR

Inventors

• Daniel Bichon · Montpellier, FR
• Patrick Gueule · Teyran, FR
• Didier Van Broeck · Juvignac, FR
• Xavier Emonds-Alt · Juvignac, FR
• Vincenzo Proietto · Juvignac, FR

Key dates

• Filing date: Feb 29, 1996
• Grant date: Aug 24, 1999
• Expiry date: Feb 29, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound of formula: in which: PA1 Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy; PA1 R.sub.1 represents a methyl group; PA1 R.sub.11 represents hydrogen; PA1 or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group; PA1 R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.12 group; or R.sub.2 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; PA1 or Ar and R…