发明名称 COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
摘要 This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
申请公布号 US2014378473(A1) 申请公布日期 2014.12.25
申请号 US201214241019 申请日期 2012.08.27
申请人 Catalano Susan M.;Rishton Gilbert;Izzo Nicholas J. 发明人 Catalano Susan M.;Rishton Gilbert;Izzo Nicholas J.
分类号 C07D491/107;C07D295/096;C07D211/22;C07C217/62;C07D209/44 主分类号 C07D491/107
代理机构 代理人
主权项 1. A compound of Formula I:wherein R1 and R2 are independently selected from H, OH, halo, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, (R16)(R17)N—C1-4 alkylene-O—, or R1 and R2 are linked together to form a —O-ethylene-O— group, wherein R16 and R17 are independently C1-4 alkyl or benzyl, or R16 and R17 together with nitrogen form a ring selected fromwherein X is N or O and R18 is H or unsubstituted phenyl; and wherein at least one of R1 and R2 is not H; R3 is selected from whereinR6, R7, R8, R9, and R10, are independently selected from H, halo, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and S(O)2—C1-6 alkyl;R20 is H; andn is 1-4 R4 is C1-6 alkyl; R4′ is H or C1-6 alkyl; and R5 is H, C1-6 alkyl, and C(O)O(C1-4 alkyl), C(O)(C1-4 alkyl), or C(O)(C1-4haloalkyl); or R3 and R5 together with nitrogen form a ring selected fromwherein R11 and R12, are independently selected from H, halo, and C1-6 haloalkyl, and Y is CH or N; R13.is H, C1-6 alkyl, C3-6 cycloalkyl, unsubstituted phenyl or phenyl substituted with C1-6 haloalkyl, or unsubstituted benzyl R14 and R15 are independently selected from H and halo;R19 is H, andpharmaceutically acceptable salts thereof,with the proviso that the following racemic mixtures of compounds are excluded
地址 Pittsburgh PA US