发明名称 BROMODOMAIN INHIBITOR
摘要 The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
申请公布号 US2017050968(A1) 申请公布日期 2017.02.23
申请号 US201615130503 申请日期 2016.04.15
申请人 Celgene Quanticel Research, Inc. 发明人 Bennett Michael John;Betancort Juan Manuel;Boloor Amogh;Kaldor Stephen W.;Stafford Jeffrey Alan;Veal James Marvin
分类号 C07D473/34;C07D471/04;C07D405/04;C07D413/04;C07D417/04;C07D401/04 主分类号 C07D473/34
代理机构 代理人
主权项 1. A compound of Formula I, or a pharmaceutically acceptable salt thereof,wherein, Ring A is an optionally substituted 5- or 6-membered heteroaryl ring containing at least one S or N atom, or an optionally substituted 5- or 6-membered heterocyclyl ring containing at least one S or N atom; X2 is N or C—R12, in which R12 is hydrogen, halogen, alkyl, or alkoxy; X5 is N or C—R15, in which R15 is hydrogen, halogen, —CN, alkyl or alkoxy; X6 is N or C—R16, in which R16 is hydrogen, halogen, or —W—X, wherein W is a bond, —O—, —S—, or —NH—, and X is alkyl, alkynyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkynyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl; and G is: wherein, R22 is alkyl;R23 is hydrogen, halogen, or alkyl; or optionally, when R23 is alkyl, R22 and R23 join to form an optionally substituted ring;R25 is hydrogen, halogen, alkyl, alkoxy, or alkenyl;R26 is hydrogen, halogen, alkyl, alkoxy, aminoalkyl, or alkenyl; or optionally, when R23 is hydrogen, R25 is not hydrogen and R26 is not hydrogen or halogen, R25 and R26 join to form an optionally substituted ring;provided that the compound of Formula I is not: 4-(3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-2-methylisoquinolin-1(2H)-one; 2-methyl-4-(2-oxoindolin-6-yl)isoquinolin-1(2H)-one; 4-methyl-6-(2-methyl-1-oxo-1,2-dihydroisoquinolin-4-yl)-2H-benzo[b][1,4]oxazin-3 (4H)-one; nor 4-(1′-cyclobutyl-4H-spiro[benzo[d][1,3]dioxine-2,4′-piperidine]-6-yl)-2-methylisoquinolin-1(2H)-one.
地址 San Diego CA US