Erdman Paul,Xu Shuichan,Narla Rama K.,Calabrese Andrew Antony,Jeffy Brandon,Robinson Dale,Zhu Dan,Huang Dehua,Elsner Jan,Boylan John,Tehrani Lida,Nagy Mark A.,Raheja Raj Kumar,Harris Roy L.,Tran Tam M
申请号：
NZ63046714
公开号：
NZ630467A
申请日:
2014.01.15
申请国别(地区):
NZ
年份:
2017
代理人:
摘要：
Disclosed are heterocyclically substituted pyrrolo[2,3-d]pyrimidine derivatives as represented by general formula (I) and pharmaceutically acceptable salts, tautomers, stereoisomers, enantiomers, and isotopologues thereof, wherein: R1 is substituted or unsubstituted saturated, partially saturated, or unsaturated alkyl, substituted or unsubstituted saturated, or partially saturated cycloalkyl, or substituted or unsubstituted non-aromatic heterocyclyl； and R2 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl； R3 is substituted or unsubstituted heterocyclyl or substituted or unsubstituted aryl； L is O； and wherein the remaining substituents are as defined herein； provided R3 is not pyridyl when R2 is pyrazolyl； and the compound is not N-methyl-N-[trans-3-[[5-(1-methyl-1H-pyrazol-4-yl)-2-[(1-methyl-1H-pyrazol-4-yI)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]cyclobutyl]-2-propenamide； or N-methyl-N-[trans-3-[[5-(1-methyl-1H-pyrazol-3-yl)-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]cyclobutyl]-2-propenamide. Representative compounds include N-methyl-4-(4-(cyclopentyloxy)-5-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)benzamide, 4-(2-(1H-indazol-5-ylamino)-4-(cyclohexyloxy)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenol, 4-(4-(cyclopentyloxy)-5-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-3-methoxy-N-methylbenzamide, 4-(4-(cyclopentyloxy)-5-(pyridin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-3-methoxy-N-methylbenzamide, (4-(5-(4-(4H-1,2,4-triazol-3-yl)phenyl)-4-methoxy-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-3-chlorophenyl)(morpholino)-methanone and 4-(cyclopentyloxy)-2-(2-methoxyphenylamino)-5-(2-methylbenzo[d]oxazol-6-yl)-7H-pyrrolo[2,3-d]pyrimidine. Also disclosed is a pharmaceutical composition which comprises an effective amount of a compound of as defined above, or a pharmaceutically acceptable salt, tautomer, stereoisomer, enantiomer, or isotopologue thereof, and a pharmaceutically acceptable carri
