首页> 外国专利> DI- OR TRIAZA-SPIRO4,5DECANE DERIVATIVES AS AGONIST AND/OR ANTAGONIST OF THE ORPHANIN FQ(OFQ) RECEPTOR, PREPARATION AND USE THEREOF

DI- OR TRIAZA-SPIRO4,5DECANE DERIVATIVES AS AGONIST AND/OR ANTAGONIST OF THE ORPHANIN FQ(OFQ) RECEPTOR, PREPARATION AND USE THEREOF

机译:DI-或TRIAZA-SPIRO [4,5]癸烷衍生物作为邻苯二甲酸FQ(OFQ)受体的激动剂和/或拮抗剂,其制备和用途

摘要

The present invention relates to compounds of the general formula CHEM 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; bicycloÄ6.2.0Üdec-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; A &cir& 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 and/or antagonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
机译:本发明涉及通式的化合物,其中R 1是C6-10-环烷基,任选地被低级烷基或-C(O)O-低级烷基取代;十氢萘-1-基;十氢萘-2-基;茚满-1-基或茚满-2-基,任选地被低级烷基取代;十氢azulen-2-基; bicycloÄ6.2.0Üdec-9-yl; acenaphthen-1-yl; 2,3-二氢-1H-苯-1-基; 2,3,3a,4,5,6-六氢-1H-苯-1-基或八氢-茚-2-基; R 2为氢;低级烷基; = O或苯基,任选地被低级烷基,卤素或烷氧基取代; A cir是环己基或苯基,任选地被低级烷基,卤素或烷氧基取代; X为-CH(OH)-; -C(O)-; -CHR 3- -CR <3> =; -O- ;; -S-; -CH(COOR <4>)-或-C(COOR <4>)=; Y为-CH 2-; -CH =; -CH(COOR <4>)-,-C(COOR <4>)=;或-C(CN)-; R 3为氢或低级烷氧基; R 4是低级烷基,环烷基,苯基或苄基,并且a或b任选地是另外的键,及其药学上可接受的酸加成盐。该化合物是孤儿蛋白FQ(QFQ)受体的激动剂和/或拮抗剂,因此可用于治疗与该受体有关的疾病。

著录项

  • 公开/公告号HU9901910A3

    专利类型

  • 公开/公告日2001-11-28

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG. BAZEL;

    申请/专利号HU19990001910

  • 发明设计人

    申请日1999-06-09

  • 分类号C07D471/10;A61K31/44;C07D498/10;C07D513/10;

  • 国家 HU

  • 入库时间 2022-08-22 00:45:06

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