发明名称 Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process
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: wherein: n is an integer of 1 to 6; X, Y, Z1 and Z2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C1-C6) alkoxy, N-alkyl, (C2-C6) acyloxy, N-alkylene, —SH, —SR, wherein R is from the same group as R1 and R2 and can be the same or different than R1 and R2, amino, nitro, cyano, hydroxy, C(═O)OR6, —C(═O)NR5R4, NR3R2, or S(═O)kR1 wherein k is 1 or 2, and R1 to R6 are independently hydrogen or (C1-C6) alkyl; R1, and R2 can be the same or different and are hydrogen, (C1-C6) alkyl, hydroxyalkyl or mercaptoalkyl, —C(═O)OR1, cyano, (C1-C6) alkenyl, (C2-C6) alkynyl, or 1,2,4-oxadiazol-5-yl optionally substituted at the 3-position by Z4 wherein any (C1-C6) alky, (C1-C6) alkanoyl, (C2-C6) alkenyl or (C2-C6) alkynyl can optionally be substituted by 1, 2 or 3 Z; R7 can be hydrogen, O or phenyl R8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl Z4 is (C1-C6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z1 W is O or S T is amino or C1-C6 aminoalkyl A is N or C T is C1-C6 alklyl or sulfonyl and V is alkyl (C0-C6), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R1 or R2 as indicated above and &phgr; is phenyl, naphthyl, thienyl or pyridinyl.
申请公布号 US8114379(B2) 申请公布日期 2012.02.14
申请号 US20080100067 申请日期 2008.04.09
申请人 ELMALEH DAVID R.;SUNGWOON CHOI;FISCHMAN ALAN J.;THE GENERAL HOSPITAL CORPORATION 发明人 ELMALEH DAVID R.;SUNGWOON CHOI;FISCHMAN ALAN J.
分类号 A61K51/04;A61K31/445;A61K31/495;A61K31/496;A61K31/4965;A61K31/497;A61K49/22 主分类号 A61K51/04
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