BEARSS, David J.,WARNER, Steve L.,SHARMA, Sunil,STEPHENS, Bret,Venkataswamy SORNA,Hariprasad VANKAYALAPATI
申请号:
MX2015018032
公开号:
MX2015018032A
申请日:
2014.06.19
申请国别(地区):
MX
年份:
2016
代理人:
摘要:
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.En un aspecto, la invención se refiere a análogos sustituidos de (E)-N´-(1-feniletiliden)benzohidrazida, derivados de los mismos, y compuestos relacionados, que son útiles como inhibidores de histona desmetilasa especifica de lisina, incluyendo LSD1 métodos de síntesis para fabricar los compuestos composiciones farmacéuticas que comprenden los compuestos y métodos de uso de los compuestos y composiciones para tratar trastornos asociados con la disfunción de la LSD1 este resumen es ideado como una herramienta de exploración para propósitos de búsqueda en la técnica particular no pretende ser limitativo de la presente invención.