会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 10. 发明申请
    • TRIAZOLYL DERIVATIVES OF AZABICYCLO [3.1.0] HEXANE AS DOPAMINE D3 RECEPTOR MODULATORS
    • AZABICYCLO的三唑衍生物[3.1.0] HEXANE作为DOPAMINE D3受体调节剂
    • WO2007022936A1
    • 2007-03-01
    • PCT/EP2006/008203
    • 2006-08-18
    • GLAXO GROUP LIMITEDCAPELLI, Anna MariaFAZZOLARI, ElettraMICHELI, FabrizioTEDESCO, GiovannaTERRENI, Silvia
    • CAPELLI, Anna MariaFAZZOLARI, ElettraMICHELI, FabrizioTEDESCO, GiovannaTERRENI, Silvia
    • C07D413/14A61K31/422A61P25/18
    • C07D413/14
    • The present invention relates to novel compounds of formula (IC) or a salt thereof, wherein p is an integer ranging from 0 to 4; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1 - 4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl or SF 5 ; or corresponds to a group R 5 ; m 1 , m 2 , m 3 , and m 4 are 0; m 5 , m 6 and m 7 are each independently 0, 1 or 2 wherein the sum of m 5 , m 6 and m 7 is 1 or 2; R 6 is C 1-6 alkyl; R 7 is halogen, C 1-6 alkyl or haloC 1-6 alkyl; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is S or -CH 2 -; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1 , 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; R 5 is isoxazolyl, -CH 2 -N-pyrrolyl, 1 ,1 -dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; with the proviso that when m 5 =m 6 =1 , R 7 is not chlorine; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.
    • 本发明涉及式(IC)的新化合物或其盐,其中p为0至4的整数; R 1独立地选自:卤素,羟基,氰基,C 1 -C 4 - 烷基,卤代C 1 - C 1-4烷基,C 1-4烷氧基,卤代C 1-4烷氧基,C 1-4烷酰基或C 1-4烷氧基, 5 ; 或对应于基团R 5; m 1,m 2,m 3和m 4是0; m 5,m 6和m 7各自独立地为0,1或2,其中m为5〜 m 6和m 7是1或2; R 6是C 1-6烷基; R 7是卤素,C 1-6烷基或卤代C 1-6烷基; R 2是氢或C 1-4烷基; n为2或3; X是S或-CH 2 - ; R 3是C 1-4烷基; R 4是氢或苯基,杂环基,5或6元杂芳族基团或8至11元双环基团,其中任何基团任选被 1,2,3或4个选自以下的取代基:卤素,氰基,C 1-4烷基,卤代C 1-4烷基,C 1 -4个烷氧基和C 1-4烷酰基; R 5是异恶唑基,-CH 2 - N-吡咯基,1,1-二氧代-2-异噻唑烷基,噻吩基,噻唑基,吡啶基或2-吡咯烷基,其中各基团 任选地被一个或两个选自以下的取代基取代:卤素,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4 - 烷氧基和C 1-4烷酰基; 条件是当m 5 = m 6 = 1时,R 7不是氯; 其制备方法,这些方法中使用的中间体,含有它们的药物组合物及其在治疗中的用途,作为多巴胺D 3受体的调节剂,例如。 治疗与物质相关的疾病,作为抗精神病药,早泄或认知障碍。