Agonist compounds

US5886001A · kind A · utility

Assignee

• Astra AB · SE

Inventor

• Helmut Schmidhammer · Innsbruck, AT

Key dates

• Filing date: Aug 22, 1995
• Grant date: Mar 23, 1999
• Expiry date: Aug 22, 2015

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

New morphinane derivatives of the formula (I) ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in therapy. The variables in the above structure are as follows: R.sub.1 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl and hydrogen; PA1 R.sub.2 is selected from the group consisting of hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; C.sub.7 -C.sub.16 arylalkyloxy, wherein the aryl is C.sub.6 -C.sub.10 aryl and the alkyloxy is C.sub.1 -C.sub.6 alkyloxy; PA1 R.sub.3 is a C.sub.1 -C.sub.6 alkyl; PA1 R.sub.4 is a hydrogen; hydroxy; or a C.sub.1 -C.sub.6 alkoxy; PA1 R.sub.5 and R.sub.6 each and independently are selected from the group consisting of hydrogen; and C.sub.1 -C.sub.6 alkyl; PA1 X is NR.sub.9, wherein R.sub.9 is selected from the group consisting of hydrogen; and C.sub.1 -C.sub.6 alkyl; PA1 and wherein any aryl group in the compound may be unsubstituted or mono-, di-, or tri-substituted independently with hydroxy; halo; nitro; cyano; thiocyanato; trifluoromethyl; C.sub.1 -C.sub.3 alkyl; C.sub.1 -C.sub.3 alkoxy; CO.sub.2 H; CONH.sub.2 ; CO.sub.2 (C.sub.1 -C.sub.3 alkyl); CONH(C.sub.1 -C.sub.3 alkyl); CON(C.sub.1 -C.sub.3 …