发明名称 2,4-Diaminoquinazolines for spinal muscular atrophy
摘要 2,4-Diaminoquinazolines of formulae I-IV and VI; are useful for treating spinal muscular atrophy (SMA).
申请公布号 US9067897(B2) 申请公布日期 2015.06.30
申请号 US201113010556 申请日期 2011.01.20
申请人 Families of Spinal Muscular Atrophy 发明人 Singh Jasbir;Gurney Mark E.
分类号 A61K31/517;C07D239/84;A61P21/00;C07D239/95;C07D401/12;C07D405/12;C07D409/12;C07D413/12;C07D417/12 主分类号 A61K31/517
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A 2,4-diaminoquinazoline compound selected from: (A) 2,4-diaminoquinazoline compounds selected from the group consisting of formula II: wherein G is selected from the group consisting of —NR6—, —CH2—, and —CH2O—; R2 is selected from the group consisting of cycloalkyl, fused cycloalkylaryl, heterocyclyl, heteroaryl; substituted cycloalkyl, substituted aryl, substituted fused cycloalkylaryl, substituted heterocyclyl, and substituted heteroaryl with the proviso that when G is —CH2— then R2 is other than phenyl or substituted phenyl, wherein said aryl is selected from phenyl, naphthalenyl, indanyl, tetralinyl, and fluorenyl and said heterocyclyl or heteroaryl is selected from imidazolyl, pyridinyl, indolyl, thiophenyl, benzopyranonyl, thiazolyl, furanyl, benzimidazolyl, quinolinyl, isoquinolinyl, quinoxalinyl, pyrimidinyl, pyrazinyl, tetrazolyl, and pyrazolyl, and wherein substituents are selected from alkyl, aryl, halogen, hydroxy, lower alkoxy, carboxy, carboxamido, cyano, nitro, amino, dialkylamino, and alkylthio; and, (B) 2,4-diaminoquinazoline compounds of formula IV: wherein G2 is selected from the group consisting of —O—, —S—, and NH—; and R12 is selected from the group consisting of C7-C10 polycyclic hydrocarbon, substituted C7-C10 polycyclic hydrocarbon, and wherein the wavy line indicates the point of attachment; and wherein one or more carbon atoms in the cyclopentyl ring is optionally replaced by a heteroatom independently selected from the group consisting of N, O, and S; and R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, haloalkyl, hydroxy, carboxy, C1-C6 alkoxycarbonyl, carboxamido, cyano, formyl, nitro, amino, C1-C6 alkylamino, C1-C6 dialkylamino, mercapto, C1-C6 alkylthio, C1-C6 alkylsulfoxide, C1-C6 alkylsulfone, C1-C6 acylamino, amidino, phenyl, benzyl, phenoxy and benzyloxy, with the proviso that at least one of R3, R4 and R5 must be other than hydrogen or a pharmaceutically acceptable salt of such a compound, in any stereoisomeric or tautomeric form, or a mixture of any such compounds in any ratio.
地址 Elk Grove Village IL US