Di-or triaza-spiro [4,5] decane derivatives

US6172075A · kind A · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Geo Adam · Schopfheim, DE
• Andrea Cesura · Nyon, CH
• François Jenck · Riedisheim, FR
• Sabine Kolczewski · Lörrach, DE
• Stephan Rover · Weil am Rhein, DE
• Jurgen Wichmann · Steinen, DE

Key dates

• Filing date: Jun 11, 1999
• Grant date: Jan 9, 2001
• Expiry date: Jun 11, 2019

Classification

• Technology area (CPC —): General

Abstract

The present invention relates to compounds of the general formula ##STR1## wherein PA1 R.sup.1 is C.sub.6 -.sub.10 -cycloalkyl, optionally substituted by lower alkyl or --C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; PA1 R.sup.2 is hydrogen; lower alkyl; .dbd.O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; PA1 .sup.A is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; PA1 X is --CH(OH)--; --C(O)--; --CHR.sup.3 --; --CR.sup.3.dbd.; --O--; --S--; --CH(COOR.sup.4)-- or --C(COOR.sup.4)--; PA1 Y is --CH.sub.2 --; --CH.dbd.; --CH(COOR.sup.4)--, --C(COOR.sup.4).dbd.; or --C(CN)--; PA1 R.sup.3 is hydrogen or lower alkoxy; PA1 R.sup.4 is lower alkyl, cycloalkyl, phenyl, or benzyl and PA1 either a or b is optionally an additional bond, PA1 and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the t…