发明名称 Substituted dihydropyrazoles as sphingosine receptor modulators
摘要 The present invention relates to substituted dihydropyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
申请公布号 US8987471(B2) 申请公布日期 2015.03.24
申请号 US201414179713 申请日期 2014.02.13
申请人 Allergan, Inc. 发明人 Takeuchi Janet A.;Li Ling;Im Wha Bin;Chow Ken
分类号 C07D231/06;A61K31/415;C07F9/6503 主分类号 C07D231/06
代理机构 代理人 Potts Barbara C.
主权项 1. A compound represented by Formula I, its enantiomers, diastereoisomers, tautomers, or a pharmaceutically acceptable salt thereof,wherein: R1 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14; R2 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14; R3 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14; R4 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14; R5 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14; R6 is H, optionally substituted C6-10 aryl, optionally substituted heterocycle or optionally substituted C1-6 alkyl; R7 is H, OH, OC1-6 alkyl or optionally substituted C1-6 alkyl; R8 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14,R9 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14;R10 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14;R11 is H, halogen or optionally substituted C1-6 alkyl, CN, NO2, C(O)R7, NR12R13 or OR14;R12 is H or optionally substituted C1-6 alkyl;R13 is H or optionally substituted C1-6 alkyl;R14 is H or optionally substituted C1-6 alkyl;X is O, CH2, NR12 or S;a is 0, 1, 2 or 3;b is 0, 1, 2 or 3;Z is OPO3H2, carboxylic acid, PO3H2, —P(O)MeOH, —P(O)(H)OH or OR15; andR15 is H, C(O)R7 or optionally substituted C1-6 alkyl.
地址 Irvine CA US