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    • 1. 发明申请
    • USE OF PIPERAZINE PHENOTHIAZINE DERIVATIVES, OR A PHARMACEUTICALLY ACCEPTABLE SALT OR ESTER THEREOF, IN THE MANUFACTURE OF A MEDICAMENT WITH NEUROPROTECTOR AND/OR NEUROTROPHIC EFFECTS ON CNS AND/OR PNS
    • 在具有神经元和/或神经营养因子对CNS和/或PNS的药物的制造中使用哌嗪类苯并恶嗪衍生物或其药学上可接受的盐或其衍生物
    • WO2004096231A2
    • 2004-11-11
    • PCT/EP2004005183
    • 2004-04-23
    • NEURO 3DCALLIZOT NOELLEAPPERT COLLIN ALINE
    • CALLIZOT NOELLEAPPERT COLLIN ALINE
    • A61K31/5415A61P25/02A61P25/16A61P25/28A61P27/16
    • A61K31/5415
    • This invention relates to a new use of piperazinephenothiazine derivatives and their pharmaceutically acceptable salts or esters in the manufacture of a medicament with neuroprotector and/or neurotrophic effects on CNS and/or PNS. The piperazine phenothiazine derivatives are selected from compounds of formula (I) wherein A represents a straight or branched alkylene chain of from 2 to 6 carbon atoms separating the nitrogen atoms linked thereto by at least two carbon atoms ; R1 represents hydrogen, halogen, lower alkyl, lower alkoxy, lower alkanoyl, lower alkyl-mercapto, trifluoromethylmercapto, lower alkyl-sulfonyl (preferably methylsulfonyl), perfluoroalkyl of 1 to 3 carbon atoms; R2, R3, R4 and R5 each represent methyl, ethyl or hydrogen, R6 represents hydrogen, lower alkyl, hydroxy-lower-alkyl or aliphatic acyloxy-lower-alkyl having 1 to 4 carbon atoms in the acyloxy portion and 1 to 6 carbon atoms in the alkyl portion, CH2-CH2-O-R7 where R7 represents hydrogen, COR8 where R8 is a branched or straight chain alkyl radical of from seven to fourteen carbon atoms.
    • 本发明涉及哌嗪并噻嗪衍生物及其药学上可接受的盐或酯在制备对CNS和/或PNS具有神经保护素和/或神经营养作用的药物中的新用途。 哌嗪吩噻嗪衍生物选自式(I)的化合物,其中A表示2至6个碳原子的直链或支链亚烷基链,其与其连接的氮原子分开至少两个碳原子; R 1表示氢,卤素,低级烷基,低级烷氧基,低级烷酰基,低级烷基 - 巯基,三氟甲基巯基,低级烷基 - 磺酰基(优选甲基磺酰基),1〜3个碳原子的全氟烷基; R2,R3,R4和R5各自表示甲基,乙基或氢,R6表示氢,低级烷基,羟基 - 低级烷基或酰氧基中具有1至4个碳原子的脂族酰氧基 - 低级烷基和1至6个碳原子 在烷基部分,其中R 7表示氢的CH 2 -CH 2 -O-R 7,COR 8,其中R 8是具有7至14个碳原子的支链或直链烷基。