发明名称 NOVEL CYTOCHROME P450 INHIBITORS AND THEIR METHOD OF USE
摘要 Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the overproduction of cortisol that include metabolic syndrome, and any involving the overproduction of cortisol.
申请公布号 US2015210641(A1) 申请公布日期 2015.07.30
申请号 US201514595344 申请日期 2015.01.13
申请人 CORTENDO AB (PUBL) 发明人 Blass Benjamin Eric;Abou-Gharbia Magid A.;Childers Wayne E.;Ramanjulu Mercy M.;Morton George Charles
分类号 C07D213/30;C07D401/06;C07D405/04 主分类号 C07D213/30
代理机构 代理人
主权项 1. A compound having formula (I): including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein: A1 is selected from the group consisting of nitrogen and CH; A2 is selected from the group consisting of nitrogen and CH; At least one of A1 and A2 is nitrogen; R1 is selected from the group consisting of hydrogen, fluorine, OR4, NR5aR5b, R2 is selected from the group consisting of hydrogen, fluorine, OR7, NR5aR5b, At least one of R1 and R2 is not hydrogen; R3a, R3b, R3c, R3d, and R3e are each independently selected from the group consisting of hydrogen, halogen, OH, optionally substituted C1-6 linear alkyl, optionally substituted C1-6 branched alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C1-6haloalkyl, C1-6, optionally substituted alkoxy, —NR8aR8b, —NR9COR10, —CO2R10, —CONR8aR8b, —NHSO2R11, —SH, —SR11, SO2R11 and —SO2NHR10; R4 is an optionally branched C1-6 alkyl; R5a is an optionally branched C1-6 alkyl; R5b is an optionally branched C1-6 alkyl; R5a and R5b are taken together with the atoms to which they are bound to form an optionally substituted 5 membered ring; R5a and R5b are taken together with the atoms to which they are bound to form an optionally substituted 6 membered ring; R6 is selected from the group consisting of hydrogen, optionally branched C1-6 alkyl, optionally branched C3-6 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, and COR11; R7 is an optionally branched C1-6 alkyl; R4 and R7 are taken together with the atoms to which they are bound to form an optionally substituted 5 membered ring; R4 and R7 are taken together with the atoms to which they are bound to form an optionally substituted 6 membered ring; R8a and R8b are each independently selected from the group consisting of hydrogen, optionally substituted C1-6 linear alkyl, optionally substituted C1-6 branched alkyl, and optionally substituted C3-7 cycloalkyl; R9 is selected from the group consisting of hydrogen, optionally substituted C1-6 linear alkyl, optionally substituted C1-6branched alkyl, and optionally substituted C3-7 cycloalkyl; R10 is selected from the group consisting of hydrogen, optionally substituted C1-6 linear alkyl, optionally substituted C1-6branched alkyl, and optionally substituted C3-7 cycloalkyl; R11 is selected from the group consisting of optionally substituted C1-6 linear alkyl, optionally substituted C1-6branched alkyl, and optionally substituted C3-7 cycloalkyl.
地址 Radnor PA US