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Therapeutically Active compounds and Methods of use
专利权人:
AGIOS PHARMACEUTICALS; INC.
发明人:
JANETA POPOVICI-MULLER,DING ZHOU,RENE M. LEMIEUX
申请号:
ARP130100177
公开号:
AR089768A1
申请日:
2013.01.21
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Methods are provided for treating a cancer characterized by the presence of a mutant allele of IDH1 / 2 comprising administering to a person in need thereof a compound described herein. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt, isotopologist or hydrate thereof, wherein: R¹ is optionally substituted C₄₋₆ carbocyclyl; each R² and R³ is independently selected from optionally substituted aryl or optionally substituted heteroaryl; R⁴ is alkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl or optionally substituted heteroaralkyl;a. Ring a is a 4-6 member aromatic free ring with 0-1 extra heteroatoms selected from n or s, in which the ring a can be replaced by one or two r83099 groups;a. Each r83099 independent halo; - cf832323;-CN; -OR⁶;-N (R) -C (O) C₁₋₄ alkyl;a. Halogenated tar c83218d31832424;C₁₋₄ alkyl optionally substituted by -OR⁶ or -N (R⁶) ₂;-O-or8310o-n (r8310a) 832224, the substitute is halo;-SO N (R)-So832222 (lease No. c833213183);-No. 8310; No. so8322; No. 8310;C₃₋₅ carbocyclyl optionally substituted by one or two R⁶ groups;-O - (carbocciillo c8332-833318326 was selectively replaced by one or two r8310 groups);5-6 membered heteroaryl; -C₁₋₄-C (O) alkyl O-C₁₋₄ alkyl or -C (O) O-C₁₋₄ alkyl;or each R⁶ is independently H or C₁₋₃ alkyl.Se proporcionan métodos para tratar un cáncer caracterizado por la presencia de un alelo mutante de IDH1/2 que comprenden administrar a un individuo que lo necesita un compuesto descrito en la presente. Reivindicación 1: Un compuesto de fórmula (1) o una sal, tautómero isotopólogo o hidrato farmacéuticamente aceptable del mismo, en donde: R¹ es carbociclilo C₄₋₆ opcionalmente sustituido; cada R² y R³ se selecciona independientemente de arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R⁴ es alquilo, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, aralquilo opcionalmente sustituido o heteroaralquilo opcionalment
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