发明名称 Isoxazolo-quinazolines as modulators of protein kinase activity
摘要 The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. 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 US9333205(B2) 申请公布日期 2016.05.10
申请号 US201113813200 申请日期 2011.07.20
申请人 NERVIANO MEDICAL SCIENCES S.R.L. 发明人 Caldarelli Marina;Beria Italo;Colombo Nicoletta;Piutti Claudia;Salsa Matteo;Traquandi Gabriella
分类号 C07D498/04;A61K31/519;C07D498/02;A61K45/06;A61N5/10 主分类号 C07D498/04
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: Y is O and Z is N, or Y is N and Z is O; X is NH; R1 is a phenyl that is optionally substituted with a first 1 to 6 groups, independently selected from: C1-C6 alkyl, polyfluorinated alkyl, polyfluorinated alkoxy, hydroxyalkyl, heterocyclyl, C3-C7 cycloalkyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, arylamino, diarylamino, heterocyclylamino, formylamino, alkylcarbonylamino, arylcarbonylamino, heterocyclylcarbonylamino, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, heterocyclylaminocarbonyl, alkylcarbonyl, cycloalkylcarbonyl, and heterocyclylcarbonyl, wherein heterocyclyl is a 3 to 7 membered saturated carbocyclic ring wherein 1 to 3 carbon atoms are replaced with nitrogen, wherein the first 1 to 6 groups is further optionally substituted with a second 1 to 6 groups independently selected from C1-C6 alkyl, polyfluorinated alkyl, polyfluorinated alkoxy, hydroxyalkyl, heterocyclyl, C3-C7 cycloalkyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, arylamino, diarylamino, heterocyclylamino, formylamino, alkylcarbonylamino, arylcarbonylamino, heterocyclylcarbonylamino, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, heterocyclylaminocarbonyl, alkylcarbonyl, cycloalkylcarbonyl, and heterocyclylcarbonyl, wherein heterocyclyl is a 3 to 7 membered saturated carbocyclic ring wherein 1 to 3 carbon atoms are replaced with nitrogen; R2 is —NR′R″, wherein R′ is hydrogen and R″ is hydrogen or a group, selected from straight or branched C1-C6 alkyl and phenyl, that is optionally substituted with 1 to 6 groups, independently selected from: C1-C6 alkyl, phenyl, amino, alkylamino and dialkylamino; A is a divalent group selected from —(CH2)2—, —CH2—C(CH3)2—, and —C(CH3)2—CH2—; and the pharmaceutically acceptable salts thereof.
地址 Nerviano (MI) IT