发明名称 MULTIPLE KINASE PATHWAY INHIBITORS
摘要 Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
申请公布号 US2015266870(A1) 申请公布日期 2015.09.24
申请号 US201314431476 申请日期 2013.09.25
申请人 MANNKIND CORPORATION ;TOLERO PHARMACEUTICALS, INC. 发明人 Zeng Qingping;Faris Mary;Mollard Alexis;Warner Steven L.;Flynn Gary A.
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound having the structural formula of Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a nitrogen-containing five- or six-member heteroaryl in which at least one ring nitrogen atom is adjacent to the carbon linking R1 to the amino group, optionally substituted with 1, 2, or 3 groups independently selected from the group consisting of: hydroxyl;halogen;C1-C3 alkyl;hydroxyl (C1-C3)alkylamino, optionally linked to R1 through a carbonyl group;hydroxyl (C1-C3)dialkylamino, optionally linked to R1 through a carbonyl group;C1-C3 alkylamino, optionally linked to R1 through a carbonyl group;C1-C3 dialkylamino; optionally linked to R1 through a carbonyl group;(C1-C3)alkylamino(C1-C3)alkyl, optionally linked to R1 through a carbonyl group;(C1-C3)dialkylamino(C1-C3)alkyl, optionally linked to R1 through a carbonyl group;(C1-C3)alkylamino(C2-C3)alkoxyl, optionally linked to R1 through a carbonyl group;(C1-C3)dialkylamino(C2-C3)alkoxyl, optionally linked to R1 through a carbonyl group;(C1-C3)alkylamino(C2-C3)alkylamino, optionally linked to R1 through a carbonyl group;(C1-C3)dialkylamino(C2-C3)alkylamino, optionally linked to R1 through a carbonyl group;(C1-C3)alkylamino(C2-C3)dialkylamino, optionally linked to R1 through a carbonyl group(C1-C3)dialkylamino(C2-C3)dialkylamino, optionally linked to R1 through a carbonyl group;(C1-C3)alkoxyl(C2-C3)alkylamino, optionally linked to R1 through a carbonyl group;(C1-C3)alkoxyl(C2-C3)dialkylamino, optionally linked to R1 through a carbonyl group; anda three- to six-member heterocyclic ring containing 1 or 2 heteroatoms selected from O, N, and S; and, independently, (1) optionally is substituted with (C1-C3)alkyl, (C1-C3) hydroxylalkyl, (C1-C3)alkoxyl(C1-C3)alkyl, or (C1-C3)alkylamino(C1-C3)alkyl and(2) optionally is linked to the five- or six-member heteroaryl through a carbonyl group;R2 is: hydrogen;C1-C6 alkyl, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino, and methylsulfanyl;a three- to six-member cycloalkyl, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino, and methylsulfanyl;a three- to six-member heterocyclic ring, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, C1-C3 alkyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino, and methylsulfanyl;phenyl, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino, and methylsulfanyl; orheteroaryl, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino, and methylsulfanyl; andR3 is: halogen;C1-C6 alkyl;C1-C6 hydroxylalkyl;C1-C6 alkylcarbonyl;C1-C6 perfluoroalkyl;C3-C6 cycloalkyl;C2-C6 alkenyl, optionally substituted with 1, 2, or 3 substituents selected from the group consisting of C1-C3 alkoxyl, C1-C3 alkoxylcarbonyl, and trifluoromethyl;C2-C6 alkynyl, optionally substituted with 1, 2, or 3 substituents selected from the group consisting of C1-C3 alkoxyl, hydroxyl, C1-C6 alkyl, trifluoromethyl;phenyl, optionally substituted with 1, 2, or 3 substituents selected from the group consisting of halogen, C1-C3 alkoxyl, and trifluoromethyl; anda five- to six-member heteroaryl, optionally substituted with 1, 2, or 3 substituents selected from the group consisting of halogen, C1-C3 alkoxyl, and trifluoromethyl.
地址 Valencia CA US
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