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3 - pyrimidin-4-yl - oxazolidin - 2 - onas as inhibitors of IDH Mutant
专利权人:
NOVARTIS AG
发明人:
YOUNG SHIN CHO,MICHAEL DAVID SHULTZ,QIAN ZHAO,ZHUOLIANG CHEN,THOMAS RAYMOND CAFERRO,JAMES SUTTON,YAPING WANG,ABRAN Q. COSTALES,JULIAN ROY LEVELL,GANG LIU,JAMES R. MANNING,MARTIN SENDZIK,CYNTHIA SHAFER
申请号:
ARP140101012
公开号:
AR095311A1
申请日:
2014.03.14
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Compound of the formula (1) in the treatment of diseases or disorders associated with such mutant HDI proteins including but not limited to, cell proliferation disorders such as cancer. Claim 1: A compound according to formula (1) wherein R¹ is hydrogen, methyl or ethyl; R²ᵃ is hydrogen, methyl or C₁₋₃ haloalkyl;Rs7495es Oh, halogen, alcoxyl c83215331;Halogenated tar c83218323;NH.8322;NH (ch832323) or n (ch832323) 8322;R³ and R⁴ are each independently hydrogen, methyl or ethyl or R³ and R⁴ are joined to form cyclopropyl, cyclobutyl or oxetanyl; R⁵ and R⁶ are each independently hydrogen, deuterium, halogen, -C (O) OCH₃,C₁₋₃ alkyl or C₁₋₃ haloalkyl;R⁷ is a compound of the group of formulas (2) in which: ring A is a 6-membered heteroaryl ring having one to three nitrogen atoms; Ring B is a 5-membered heteroaryl ring having one to four heteroatoms each independently selected from the group consisting of N, O and S; X is N or CH; each R⁸ is independently hydrogen, halogen, C₁₋₃ alkyl,Halogenated tar c83218323;C₁₋₃ alkoxy or Co haloalkoxy;n is 1 or 2; R⁹ is hydrogen, halogen, haloalkyl C₁₋₃,optionally substituted C₁₋₆ alkyl, optionally substituted C₁₋₆ cycloalkyl, optionally substituted aryl, optionally substituted 5 or 6 membered heterocyclic, optionally substituted heteroaryl, -OR⁹ᵃ,-SO RC (O) NHRCh8322; r8313; 7495 or ch8323; r8313; 74955;as long as X is N, R⁹ is hydrogen, haloalkyl C₁₋₃,optionally substituted C₁₋₆ alkyl, optionally substituted C₁₋₆ cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, -SO₂R⁹ᵃ or C (O) NHR⁹ᵃ,wherein: said C₁₋₆ alkyl is optionally substituted by one to three substituents independently selected from the group consisting of OH, phenyl and phenoxy, and said C₃₋₆ cycloalkyl,5- or 6-membered heterocyclic, aryl and heteroaryl are each optionally substituted by one to three substituents independently selected from the group consisting of: halogen, hydroxyl, cyano, -NRR, C₁₋₆ alkyl,C₁₋₆ haloalkyl,C₁₋₃ alkoxy,e. Halogenated
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