公开(公告)号：US06172075B2

公开(公告)日：2001-01-09

申请号：US09330724

申请日：1999-06-11

申请人： Geo Adam ,  Andrea Cesura ,  François Jenck ,  Sabine Kolczewski ,  Stephan Röver ,  J{umlaut over (u)}rgen Wichmann

发明人： Geo Adam ,  Andrea Cesura ,  François Jenck ,  Sabine Kolczewski ,  Stephan Röver ,  J{umlaut over (u)}rgen Wichmann

IPC分类号： A61K31438

摘要： The present invention relates to compounds of the general formula wherein R1 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; {circumflex over (A)} 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 and either 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 diseases, related to this receptor.