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
    • 64. 发明申请
    • PYRROLOPYRIDINE OR PYRAZOLOPYRIDINE DERIVATIVES
    • 吡咯并吡啶或吡唑并吡啶衍生物
    • WO2015028483A1
    • 2015-03-05
    • PCT/EP2014/068114
    • 2014-08-27
    • F. HOFFMANN-LA ROCHE AGHOFFMANN-LA ROCHE INC.
    • BALLARD, Theresa MariaFLOHR, AlexanderGROEBKE ZBINDEN, KatrinPINARD, EmmanuelRYCKMANS, ThomasSCHAFFHAUSER, Hervé
    • C07D471/04A61K31/437A61P25/00A61P25/18A61P25/28
    • C07D471/04
    • The present invention relates to compounds of formula I wherein R 1 halogen, lower alkyl, lower alkoxy, cyano, phenyl, C(O)NHCH 3 , C(O)NH 2 , lower alkyl substituted by halogen or is a five-membered heteroaryl group, optionally substituted by lower alkyl; Y 1 is N or CH; Y 2 is CH; and if Y 1 is CH, Y 1 and Y 2 may form together with the C-atoms to which they are attached a ring, containing −CH=N-N(CH 3 )-, -CH=N-N(H)-; X is CH or N; R is (CH 2 ) m -cycloalkyl, optionally substituted by hydroxy, lower alkoxy or lower alkyl, or is tetrahydropyran, optionally substituted by hydroxy, or is lower alkoxy, substituted by hydroxy, or is lower alkyl substituted by one or two hydroxy, or is (CH 2 ) m -pyridinyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, or is L-phenyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, and L is a bond, -CH(CH 2 OH)- or −CH 2 CH(OH)-; n is 0, 1 or 2; m is 0 or 1; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds of the present invention are muscarinic M1 receptor positive allosteric modulators (PAM) and hence are useful in the treatment of diseases, mediated by the muscarinic M1 receptor, such as Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
    • 本发明涉及式I化合物,其中R 1卤素,低级烷基,低级烷氧基,氰基,苯基,C(O)NHCH 3,C(O)NH 2,被卤素取代的低级烷基或是五元杂芳基, 被低级烷基取代; Y1是N或CH; Y2是CH; 并且如果Y 1是CH,则Y 1和Y 2可以与它们所连接的含有-CH = N-N(CH 3) - , - CH = N-N(H) - 的环的C原子一起形成。 X是CH或N; R是任选被羟基,低级烷氧基或低级烷基取代的(CH 2)m - 环烷基,或任选被羟基取代的四氢吡喃,或被羟基取代的低级烷氧基,或被一个或两个羟基取代的低级烷基,或 是任选被羟基取代的(CH 2)m - 吡啶基,或被羟基取代的低级烷基或低级烷基,或者是被羟基,被羟基取代的低级烷基或低级烷基取代的L-苯基,L是一个键,-CH (CH 2 OH) - 或-CH 2 CH(OH) - ; n为0,1或2; m为0或1; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应。 本发明的化合物是毒蕈碱M1受体阳性变构调节剂(PAM),因此可用于治疗由毒蕈碱M1受体介导的疾病,如阿尔茨海默病,认知障碍,精神分裂症,疼痛或睡眠障碍。