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1. 发明授权

US06642247B2 Di-or triaza-spiro [4,5] decane derivatives 失效
标题翻译：二 - 或三氮杂螺[4,5]癸烷衍生物
公开(公告)号：US06642247B2
公开(公告)日：2003-11-04
申请号：US09330724
申请日：1999-06-11
申请人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , Jürgen Wichmann
发明人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , Jürgen Wichmann
IPC分类号： A61K31438
CPC分类号： C07D471/10 , C07D513/10
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; 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.
摘要翻译：本发明涉及通式化合物R 1的化合物是任选被低级烷基或-C（O）O-低级烷基取代的C 6-10 - 环烷基; 十氢萘-1-基; 十氢萘-2-基; 茚满-1-基或茚满-2-基，任选被低级烷基取代; 十氢 - 薁-2-基; 双环[6.2.0]癸-9-基; 苊-1-基; 2,3-二氢-1H-苯并芬-1-基; 2,3,3a，4,5,6-六氢-1H-吩酚-1-基或八氢 - 茚-2-基; R 2是氢; 低级烷基任选被低级烷基，卤素或烷氧基取代的O或苯基;是任选被低级烷基，卤素或烷氧基取代的环己基或苯基; X是-CH（OH） - ; -C（O） - ; -CHR 3 - ; -CR 3 = -O-; -S-; -CH（COOR 4） - 或C（COOR 4）=; Y是-CH 2 - ; -CH =; -CH（COOR 4） - ， - C（COOR 4）=; 或-C（CN） - ; R 3是氢或低级烷氧基; R 4是低级烷基，环烷基，苯基或苄基，a或b任选是另外的键，以及其药学上可接受的酸加成盐该化合物是孤儿素FQ（QFQ）受体的激动剂，因此可用于治疗与该受体有关的疾病。

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