发明名称 Substituted Quinazolin-4-one Derivatives
摘要 Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R1, R2, R3, R5, R6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases.;
申请公布号 US2016168131(A1) 申请公布日期 2016.06.16
申请号 US201414907225 申请日期 2014.07.24
申请人 NOVARTIS AG 发明人 DU Zhenxing;HINTERMANN Samuel;HURTH Konstanze;JACQUIER Sébastien;LEHMANN Hansjoerg;MOEBITZ Henrik;SOLDERMANN Nicolas;STOJANOVIC Aleksandar
分类号 C07D403/14;A61K31/52;C07D473/16;A61K31/517;C07D417/14 主分类号 C07D403/14
代理机构 代理人
主权项 1. A compound of formula (I)or a pharmaceutically acceptable salt thereof wherein R1 is selected from phenyl, which is unsubstituted or substituted by 1, 2 or 3 substituents independently selected from methyl, ethyl, difluoromethyl, methoxy, difluoromethoxy, cyclopropyl, chloro or fluoro; pyridyl, which is unsubstituted or substituted by 1, 2 or 3 substituents independently selected from methyl, ethyl, difluoromethyl, methoxy, difluoromethoxy, cyclopropyl, chloro or fluoro; 1-methylpyrazol-5-yl; 2-methylthiophen-5-yl; C3-C6-cycloalkyl, which is unsubstituted or substituted in the 1 position by methyl; tetrahydropyran-4-yl; piperidin-1-yl; morpholin-4-yl; pyrolidin-3-yl, which is unsubstituted or substituted in the 1 position by a substituent which is selected from methoxycarbonyl, methylsulfonyl, methyl or methylcarbonyl; or dimethylamine; R2 is selected from C4-C7-heteroaryl, containing one nitrogen atom and additional 0, 1, 2 or 3 heteroatoms independently selected from N, O or S, wherein C4-C7-heteroaryl is unsubstituted or substituted by 1-3 substituents independently selected from C1-C4-alkyl,C1-C4-fluoroalkyl,hydroxy-C1-C4-alkyl,hydroxy-C1-C4-fluoroalkyl,C1-C4-alkoxy,C1-C4-fluoroalkoxy,C3-C6-cycloalkyl, which is unsubstituted or substituted by 1-3 substituents independently selected from methyl, or fluoro,C3-C6-heterocycloalkyl, which is unsubstituted or substituted by 1-3 substituents independently selected from methyl, or fluoro,cyano,fluoro,amino,C1-C4-alkylamino, orC1-C4-dialkylamino; or C2-C5-alkynyl, which is unsubstituted or substituted by 1-2 substituents independently selected from C1-C4-fluoroalkyl,C3-C6-cycloalkyl, which is unsubstituted or substituted by 1-3 substituents independently selected from methyl, or fluoro,C3-C6-heterocycloalkyl, which is unsubstituted or substituted by 1-3 substituents independently selected from methyl, or fluoro,C1-C4-alkoxy,C1-C4-fluoroalkoxy,hydroxyl,cyano,fluoro,amino,C1-C4-alkylamino, orC1-C4-dialkylamino; R5 and R6 are independently selected from hydrogen, deuterium or fluoro; -L-R3 is selected from wherein R7 is selected from methoxy, difluoromethoxy, trifluoromethoxy, hydroxy, fluoro or methylsulfonylamine; and R3 is selected from wherein R4 is selected from hydrogen or amino, R8 is selected from hydrogen, methyl, fluoromethyl, difluoromethyl, trideuteromethyl or amino, and X is selected from NH, NMe or S.
地址 Basel CH