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    • 52. 发明授权
    • Diagnostic and therapeutic piperazine and piperidine compounds and process
    • 诊断和治疗哌嗪和哌啶化合物和方法
    • US06835371B1
    • 2004-12-28
    • US09633482
    • 2000-08-07
    • David R. ElmalehChoi Sung-Woon
    • David R. ElmalehChoi Sung-Woon
    • A61K4900
    • C07B59/001C07C217/48C07C233/78C07D211/26C07D211/58C07D241/08
    • Piperazine or piperidine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The piperazine or piperadine compounds are characterized by the formula:Formula I wherein: A is oxygen; n is an integer of 1 to 6; X and Y can be the same or different and are hydrogen, halogen, nitro, alkyl or halalkyl, Z is carbon or nitrogen; and &phgr; is phenyl, naphthyl, thienyl or pyridinyl. When Z is carbon, R is hydrogen, cyano, hydroxy, —COOCH3, —CH20H or —COOH; R1 is 4-fluorophenyl, 4-chlorophenyl, 4-trifluoromethyl, 3-trifluoromethyl-4 -chlorophenyl 4-bromophenyl), 4-(2-keto-1-benzimidazolinyl or 1-phenyl 1, 3, 8-triazaspiro [4,5] decan-4-one. When Z is nitrogen, R and R1 combined are wherein R3 is halo, alkyl, cyano or nitro and R2 can be hydrogen or wherein R4 is halo, alkyl, cyano, nitro, alkylnyl or alkenyl
    • 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嗪或哌啶化合物。 哌嗪或哌嗪化合物的特征在于下式:其中A为氧; n为1〜6的整数。 X和Y可以相同或不同,为氢,卤素,硝基,烷基或卤代烷基,Z为碳或氮; 并且phi是苯基,萘基,噻吩基或吡啶基。当Z是碳时,R是氢,氰基,羟基,-COOCH 3,-CH 2 OH或-COOH; R1是4-氟苯基,4-氯苯基,4-三氟甲基,3-三氟甲基-4-氯苯基4-溴苯基),4-(2-酮-1-苯并咪唑啉基或1-苯基1,3,8-三氮杂螺[ 5]癸-4-酮当Z为氮时,R和R 1组合,其中R 3为卤素,烷基,氰基或硝基,R 2可为氢,或者其中R 4为卤素,烷基,氰基,硝基,烷基或烯基
    • 55. 发明授权
    • Diagnostic and therapeutic alkylenediamine compounds and process
    • 诊断和治疗亚烷基二胺化合物和方法
    • US6001330A
    • 1999-12-14
    • US928246
    • 1997-09-12
    • David R. ElmalehRobert N. HansonChoi Sung-Woon
    • David R. ElmalehRobert N. HansonChoi Sung-Woon
    • C07B59/00C07C217/48C07C233/78C07D211/26C07D211/58C07D241/08A61K51/00A61M36/14
    • C07C217/48C07B59/001C07C233/78C07D211/26C07D211/58C07D241/08
    • Diamine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The diamine compounds or serotonin are characterized by the formula: ##STR1## wherein: l, m and n can be the same or different and are an integer of 1 to 6; X, Y and Z can be the same or different and are hydrogen, halo, haloalkyl, (C.sub.1 -C.sub.6) alkyl, aryl, (C.sub.1 -C.sub.6) alkoxy, N-alkyl, (C.sub.2 -C.sub.6) acyloxy, N-alkylene, --SH, or --SR, wherein R is from the same group as R.sub.1 and R.sub.2 and can be the same or different than R.sub.1 and R.sub.2, amino, nitro, cyano, hydroxy, --C(.dbd.O) OR.sub.6, --C(.dbd.O) NR.sub.5 R.sub.4, NR.sub.3 R.sub.2, or S(.dbd.O).sub.k R.sub.1 wherein .sub.k is 1 or 2, and R.sub.4 to R.sub.6 are independently hydrogen or (C.sub.1 -C.sub.6) alkyl;R.sub.1, and R.sub.2 can be the same or different and are hydrogen, (C.sub.1 -C.sub.6) alkyl, hydroxyalkyl or mercaptoalkyl, --C(.dbd.O) OR.sub.1, cyano, (C.sub.1 -C.sub.6) alkenyl, (C.sub.2 -C.sub.6) alkynyl, or 1, 2, 4-oxadiazol-5-yl optionally substituted at he 3-position by W wherein any (C.sub.1 -C.sub.6) alky, (C.sub.1 -C.sub.6) alkanoly, (C.sub.2 -C.sub.6) alkenyl or (C.sub.2 -C.sub.6) alkynyl (C.sub.1 -C.sub.6) alkyl, hydroxy (C.sub.1 -C.sub.6) alkyl or mercapto (C.sub.1 -C.sub.6) alkyl and optionally can be substituted by 1, 2 or 3 Z;W is (C.sub.1 -C.sub.6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z..phi. is phenyl, naphthyl, thienyl or pyridinyl.
    • 提供了可用于治疗以缺乏多巴胺神经元活性或成像多巴胺神经元为特征的神经变性疾病的二胺化合物。 二胺化合物或5-羟色胺的特征在于下式:其中:l,m和n可以相同或不同,为1〜6的整数; X,Y和Z可以相同或不同,为氢,卤素,卤代烷基,(C1-C6)烷基,芳基,(C1-C6)烷氧基,N-烷基,(C2-C6)酰氧基, -SH或-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1或2,R4至R6独立地为氢或(C1-C6)烷基; R 1和R 2可以相同或不同,为氢,(C 1 -C 6)烷基,羟烷基或巯基烷基,-C(= O)OR 1,氰基,(C 1 -C 6)烯基,(C 2 -C 6)炔基或 其中任何(C 1 -C 6)烷基,(C 1 -C 6)烷基聚,(C 2 -C 6)烯基或(C 2 -C 6)炔基(C 2 -C 6) C 1 -C 6)烷基,羟基(C 1 -C 6)烷基或巯基(C 1 -C 6)烷基,并且任选地可以被1,2或3个Z取代; W是(C1-C6)烷基或苯基,任选地被1,2或3个Z取代为苯基,萘基,噻吩基或吡啶基。