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

US6642247B2 · kind B2 · 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: Nov 4, 2003
• Expiry date: Sep 11, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/10
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of the general formula whereinR1 is C6-10-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;R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy;is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy;X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or C(COOR4)═;Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—;R3 is hydrogen or lower alkoxy;R4 is lower alkyl, cycloalkyl, phenyl, or benzyl andeither a or b is optionally an additional bond,and to pharmaceutically acceptable acid addition salts thereof.The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of dis…