发明名称 S1P3 ANTAGONISTS
摘要 The present invention relates to antagonists of the S1P3 receptor formula (A) as herein described and pharmaceutical compositions thereof. The compounds of formula (A) are useful in the preparation of a medicament, in particular for the treatment of Alzheimer's disease.
申请公布号 US2016297762(A1) 申请公布日期 2016.10.13
申请号 US201415100326 申请日期 2014.11.28
申请人 SIENA BIOTECH S.P.A. 发明人 Caramelli Chiara;Federico Cesare;Gabellieri Emanuele;Magnani Matteo;Micco Iolanda;Terstappen Georg C.
分类号 C07D213/75;C07D417/12;C07D405/14;C07D277/32;C07D417/14;C07D401/14;C07D241/16;C07D401/12;C07D413/12 主分类号 C07D213/75
代理机构 代理人
主权项 1. A compound of formula (A), wherein —R1 is X1, X6, X7, X9 and X10 are halogen, C1-C4 linear branched or cyclic alkyl optionally substituted with one or more fluorine atoms; X2, X3, X4, X5 and X8, are hydrogen, halogen, C1-C4 linear branched or cyclic alkyl optionally substituted with one or more fluorine atoms; with the proviso that at least one of X2, X3, X4, and X5 is not hydrogen R2 is a C3-C6 linear branched or cyclic alkyl optionally substituted with phenyl, with one or more fluorine atoms or with trifluoromethyl-furanyl; R2′ is hydrogen, F, C1-C3 linear or branched alkyl optionally substituted with one or more fluorine atoms; or R2 and R2′ together with the carbon atom they are attached to form a C3-C6 cycloalkyl ring; —R3 is Y1 is halogen; Y1′ is C1-C3 linear branched or cyclic alkyl optionally substituted with one or more fluorine atoms; Y2 is cyano or methoxyphenyl, C1-C3 linear branched or cyclic alkyl optionally substituted with one or more fluorine atoms; Y3 is hydrogen, halogen or methoxyphenyl; Y4 is hydrogen, halogen, N-methylpyrazolyl or a C1-C3 linear branched or cyclic alkoxy optionally substituted with one or more fluorine atoms, Y5 is hydrogen halogen, cyano, or a C1-C3 linear branched or cyclic alkyl optionally substituted with one or more fluorine atoms; with the proviso that at least one of Y4 and Y5 is not hydrogen; Y6 is halogen, C1-C3 linear branched or cyclic alkyl optionally substituted with one or more fluorine atoms, or a C1-C3 linear branched or cyclic alkoxy optionally substituted with one or more fluorine atoms; enantiomers, enantiomerically enriched mixtures, and pharmaceutically acceptable salts thereof.
地址 Siena IT