发明名称 Isoxazoline hydroxamic acid derivatives as LpxC inhibitors
摘要 This invention pertains generally to compounds of Formula I and compositions containing such compounds, as well as methods of using such compounds to treat bacterial infections. In certain aspects, the invention pertains to methods and compositions for treating infections caused by Gram-negative bacteria.;
申请公布号 US9637482(B2) 申请公布日期 2017.05.02
申请号 US201515304044 申请日期 2015.04.22
申请人 Novartis AG 发明人 Fu Jiping;Jin Xianming;Karur Subramanian;Lapointe Guillaume;Lee Patrick;Sweeney Zachary Kevin
分类号 C07D417/10;C07D261/04;A61K31/421;A61K45/06;C07D413/04;A61K31/4439;C07D413/10;A61K31/422;A61K31/5377 主分类号 C07D417/10
代理机构 代理人 Smith Michael G.
主权项 1. A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein: Z is N or CR1, where 1e is selected from H, halo, C1-4 alkyl and C1-4 haloalkyl; R2 and R3 are independently selected from C1-4 alkyl and C1-4 haloalkyl, R4 is H or C1-4 alkyl; X is selected from H, halo, C1-4 alkyl, C1-4 haloalkyl, and CN; L is selected from —CR5═CR6—, —O—, —S—, and a direct bond between A and the ring containing Z; R5 and R6 are independently selected from H, halo, C1-4 alkyl, and C1-4 haloalkyl; and A is halo, CN, or an optionally substituted group selected from C1-4 alkyl, C3-6 cycloalkyl, phenyl, C2-6 alkenyl, C2-6 alkynyl, 5-6 membered heteroaryl containing up to four heteroatoms selected from N, O and S as ring members, and 4-6 membered heterocyclyl containing up to two heteroatoms selected from N, O and S as ring members, wherein the C1-4 alkyl, C3-6 cycloalkyl, phenyl, C2-6 alkenyl, C2-6 alkynyl, 5-6 membered heteroaryl containing up to four heteroatoms selected from N, O and S as ring members, and 4-6 membered heterocyclyl containing up to two heteroatoms selected from N, O and S as ring members are each optionally substituted with up to three groups selected from halo, hydroxy, CN, R10, —(CH2)0-2OR10, —SR10, —S(O)R10, —SO2R10, —S(O)(NH)R10, and —(CH2)0-2N(R10)2;where each R10 is independently H or C1-4 alkyl optionally substituted with one or two groups selected from amino, hydroxy, C1-4 alkoxy, and CN; and —N(R10)2 can represent a 5-6 membered heterocyclic ring optionally containing an additional heteroatom selected from N, O and S as a ring member, and optionally substituted with one or two groups selected from oxo, halo, hydroxy, C1-4 alkyl, C1-4 alkoxy, and amino.
地址 Basel CH
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