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1. 发明申请

WO2004063150A2 DIAGNOSTIC AND THERAPEUTIC ALKYL PIPERIDINE/PIPERAZINE COMPOUNDS AND PROCESS 审中-公开
标题翻译：诊断和治疗碱性哌啶/哌嗪化合物和方法
公开(公告)号：WO2004063150A2
公开(公告)日：2004-07-29
申请号：PCT/US2003/041731
申请日：2003-12-31
申请人： THE GENERAL HOSPITAL CORPORATION
发明人： ELMALEH, David, R. , CHOI, Sangwoon , FISHMAN, Alan, J.
IPC分类号： C07D
CPC分类号： C07D213/75 , C07D211/26 , C07D211/58 , C07D295/215 , C07D401/12
摘要： Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: (I), (II), (III), (IV), (V) wherein: n is an integer of 1 to 6; X, Y, Z 1 and Z 2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C 1 -C 6 )alkoxy, N-alkyl, (C 2 -C 6 )acyloxy, N-alkylene, -SH, -SR, wherein R is from the same group as R 1 and R 2 and can be the same or different than R 1 and R 2 , amino, nitro, cyano, hydroxy, C(=O)OR 6 , -C(=O)NR 5 R 4 , NR 3 R 2 , or S(=O) k R 1 wherein k is 1 0r 2, and R 1 to R 6 are independently hydrogen or (C 1 -C 6 )alkyl; R 1 and R 2 can be the same or different and are hydrogen, (C 1 -C 6 )alkyl, hydroxyalkyl or mercaptoalkyl, -C(=O)OR 1 , cyano, (C 1 -C 6 )alkenyl, (C 2 -C 6 ) alkynyl, or 1, 2, 4-oxadiazol-5-yl optionally substituted at the 3-position by Z 4 wherein any (C 1 -C 6 )alky, (C 1 -C 6 )alkanoyl, (C 2 -C 6 )alkenyl or (C 2 -C 6 )alkynyl can optionally be substituted by 1, 2 or 3 Z; R 7 can be hydrogen, O or phenyl; R 8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl; Z 4 is (C 1 -C 6 )alkyl or phenyl, optionally substituted by 1, 2 or 3 Z 1 ; W is O or S; T is amino or C 1 -C 6 aminoalkyl; A is N or C; T is C 1 -C 6 alkyl or sulfonyl and V is alkyl (C 0 -C 6 ), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R 1 or R 2 as indicated above and D is phenyl, naphrhyl, thienyl or pyridinyl.
摘要翻译：提供了可用于治疗特征在于缺乏多巴胺神经元活性或成像多巴胺神经元的神经变性疾病的哌啶或哌嗪化合物。该化合物的特征为：（I），（II），（III），（IV），（V）其中：n为1至6的整数; X，Y，Z 1和Z 2可以相同或不同，为氢，卤素，卤代烷基，烷基，芳基，（C1-C6）烷氧基，N-烷基，（C2-C6）酰氧基，N-亚烷基， -SR，其中R是与R1和R2相同的基团，并且可以与R1和R2相同或不同，氨基，硝基，氰基，羟基，C（= O）OR6，-C（= O）NR5R4，NR3R2 或S（= O）kR1，其中k为10r 2，并且R 1至R 6独立地为氢或（C 1 -C 6）烷基; R 1和R 2可以相同或不同，为氢，（C 1 -C 6）烷基，羟基烷基或巯基烷基，-C（= O）OR 1，氰基，（C 1 -C 6）烯基，（C 2 -C 6）炔基或1 任选通过Z 4在3位被取代的2,4-二唑-5-基，其中任何（C 1 -C 6）烷基，（C 1 -C 6）烷酰基，（C 2 -C 6）烯基或（C 2 -C 6）由1,2或3个Z代替; R7可以是氢，O或苯基; R8可以是氢，苯基，卤代苯基，硝基苯基，吡啶基，胡椒基或磺基亚硝基苯基; Z4是（C1-C6）烷基或苯基，任选被1,2或3个Z1取代; W为O或S; T是氨基或C 1 -C 6氨基烷基; A是N或C; T是C1-C6烷基或磺酰基，V是如上所述的烷基（C 0 -C 6），烯基，炔基，卤代芳基，烷基苯酚，烷基卤代苯基和R 1或R 2，D是苯基，萘基，噻吩基或吡啶基。

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