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    • 9. 发明申请
    • NEUROTROPHIN ANTAGONIST COMPOSITIONS
    • 神经营养拮抗剂组合物
    • WO1998017278A1
    • 1998-04-30
    • PCT/CA1997000779
    • 1997-10-20
    • ALLELIX BIOPHARMACEUTICALS INC.TEHIM, AshokCHEN, Xiannong
    • ALLELIX BIOPHARMACEUTICALS INC.
    • A61K31/47
    • C07D221/14A61K31/473A61K31/4738C07D401/04C07D401/06C07D405/06
    • A pharmaceutical composition comprising a compound of formula (I) wherein R is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R ), (R ) wherein one of R and R is selected from H and loweralkyl and the other is selected from carboxy, carboxy-loweralkyl and loweralkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R and R are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S-, loweralkyl, and Z(O)OR wherein Z is selected from C and S and R is selected from H, loweralkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described. The compositions are useful to inhibit undesirable neurotrophin-mediated activity such as the neurite outgrowth that occurs in some neurodegenerative disease states.
    • 一种药物组合物,其包含式(I)化合物,其中R 1特别选自烷基,芳基 - 低级烷基,杂环 - 低级烷基,低级烷基 - 碳酸酯; 任选取代的氨基; benzimidaz -2-基; 任选取代的苯基; 低级烷基 - (R 5),(R 6)其中R 5和R 6中的一个选自H和低级烷基,另一个选自羧基,羧基 - 低级烷基和低级烷氧基羰基; NHCH2CH2OX其中X表示体内可水解的酯; R 2和R 3独立地选自H,NO 2,卤素,二(低级烷基)氨基,氰基,C(O)OH,苯基-S-,低级烷基和Z(O)OR 7 其中Z选自C和S,R 7选自H,低级烷基氨基和芳基氨基; 或其药学上可接受的盐或某些体内可水解的酯或酰胺,以有效抑制神经营养因子介导的活性的量和合适的载体。 所述组合物可用于抑制不期望的神经营养因子介导的活性,例如在一些神经变性疾病状态中发生的神经突向外生长。