发明名称 Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
摘要 The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
申请公布号 US9309253(B2) 申请公布日期 2016.04.12
申请号 US201514609534 申请日期 2015.01.30
申请人 NERVIANO MEDICAL SCIENCES S.R.L. 发明人 Caldarelli Marina;Angiolini Mauro;Beria Italo;Brasca Maria Gabriella;Casuscelli Francesco;D'Alessio Roberto;Lombardi Borgia Andrea
分类号 A61K31/55;A61K45/06;C07D487/04;A61K31/519;C07C67/00;C07D207/34;C07D209/42;C07D401/04;C12N9/99 主分类号 A61K31/55
代理机构 Scully, Scott, Murphy & Presser, P.C. 代理人 Scully, Scott, Murphy & Presser, P.C.
主权项 1. A compound of formula (I): wherein R1 is hydrogen, halogen or an optionally substituted group selected from amino, straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl; R2 is a group selected from —NR″R′″, —N(OR′″)R″ and OR″, wherein R″ and R′″ are, each independently, hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl or, together with the nitrogen atom to which they are bonded, R″ and R′″ may form a 5 to 6 membered heteroaryl or heterocyclyl group, optionally containing one additional heteroatom selected among N, O and S; R3 is hydrogen or optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl; R4 is hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl; X is a single bond or a divalent radical selected from —NR′—, —CONR′—, —NH—CO—NH—, —O—, —S—, —SO2— and —OSO2—, wherein R′ is hydrogen or an optionally substituted group selected from straight or branched C1-C6 alkyl, C3-C7 cycloalkyl, cycloalkyl-alkyl, aryl, arylalkyl, heterocyclyl and heterocyclylalkyl or, together with the nitrogen atom to which they are bound, R1 and R′ may form a 5 to 6 membered heteroaryl or heterocyclyl group optionally containing one additional heteroatom selected from N, O and S; A is —(CH2)3—; or a pharmaceutically acceptable salt thereof.
地址 Nerviano (MI) IT