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    • 9. 发明公开
    • SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE) BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIBITORS
    • 替代物(E)-N' - (1-苯基乙基) - 苯甲酰基 - 阿诺考酸二甲基乙酰化酶
    • EP3010915A4
    • 2016-12-28
    • EP14813387
    • 2014-06-19
    • UNIV UTAH RES FOUND
    • VANKAYALAPATI HARIPRASADSORNA VENKATASWAMYWARNER STEVE LBEARSS DAVID JSHARMA SUNILSTEPHENS BRET
    • A61K31/506A61P35/00C07D211/96C07D213/87C07D231/50C07D295/26
    • C07D295/26C07D211/96C07D213/87C07D231/12
    • Substituted (E)-N'-(1-phenylethylidene)benzohydrazide analogs or (3-(5-chloro-2-hydroxyphenyl)-4-METHYL-1 H-pyrazol-1-YL)(3- (morpholinosulfonyl)phenyl)methanone, derivatives thereof, and related compounds are useful as inhibitors of lysine-specific histone demethylase, including LSD1. Synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1 (lysine-specific demethylase). A pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof, and one or more of: (a) at least one agent known to increase histone demethylase activity; (b) at least one agent known to decrease histone demethylase activity; (c) at least one agent known to treat a disorder of uncontrolled cellular proliferation; (d) at least one agent known to treat a neurodegenerative disorder; (e) instructions for treating a neurodegenerative disorder; or (f) instructions for treating a disorder associated with uncontrolled cellular proliferation.
    • 取代的(E)-N' - (1-苯基亚乙基)苯甲酰肼类似物或(3-(5-氯-2-羟基苯基)-4-甲基-1H-吡唑-1-基)(3-(吗啉代磺酰基)苯基) 甲酮,其衍生物和相关化合物可用作赖氨酸特异性组蛋白脱甲基酶(包括LSD1)的抑制剂。 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用该化合物和组合物来治疗与LSD1(赖氨酸特异性脱甲基酶)的功能障碍相关的疾病的方法。 其药学上可接受的盐,水合物,溶剂化物或多晶型物,以及一种或多种:(a)已知增加组蛋白脱甲基酶活性的至少一种试剂; (b)至少一种已知降低组蛋白脱甲基酶活性的药剂; (c)至少一种已知治疗不受控制的细胞增殖病症的药剂; (d)至少一种已知治疗神经变性疾病的药物; (e)治疗神经变性疾病的说明书; 或(f)治疗与不受控制的细胞增殖相关的病症的说明书。