发明名称 PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS
摘要 The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
申请公布号 US2014162361(A1) 申请公布日期 2014.06.12
申请号 US201414179960 申请日期 2014.02.13
申请人 Corcept Therapeutics, Inc. 发明人 Clark Robin;Hynd George;Ray Nicholas;Sajad Mohammad
分类号 C07D239/56;C07D417/06;C07D401/06;C07D403/06;C07D239/553;C07D239/545 主分类号 C07D239/56
代理机构 代理人
主权项 1. A method of modulating a glucocorticoid receptor, comprising contacting a glucocorticoid receptor with an effective amount of a compound of Formula I and detecting a change in the activity of the glucocorticoid receptor, wherein the compound of Formula I has the structure:wherein the dashed line is absent or a bond; X is selected from the group consisting of O and S; R1 is selected from the group consisting of cycloalkyl, heterocycloalkyl, aryl and heteroaryl, optionally substituted with from 1 to 3 R1a groups; each R1a is independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkyl-OR1b, halogen, C1-6 haloalkyl, C1-6 haloaloxy, —OR1b, —NR1bR1c, —C(O)R1b, —C(O)OR1b, —OC(O)R1b, —C(O)NR1bR1c, —NR1bC(O)R1c, —SO2R1b, —SO2NR1bR1c, cycloalkyl, heterocycloalkyl, aryl and heteroaryl; R1b and R1c are each independently selected from the group consisting of H and C1-6 alkyl; R2 is selected from the group consisting of H, C1-6 alkyl, C1-6 alkyl-OR1b, C1-6 alkyl-NR1bR1c and C1-6 alkylene-heterocycloalkyl; R3 is selected from the group consisting of H and C1-6 alkyl; Ar is aryl, optionally substituted with 1-4 R4 groups; each R4 is independently selected from the group consisting of H, C1-6 alkyl, C1-6 alkoxy, halogen, C1-6 haloalkyl and C1-6 haloalkoxy; L1 is a bond or C1-6 alkylene; subscript n is an integer from 0 to 3, and salts and isomers thereof, thereby modulating the glucocorticoid receptor.
地址 Menlo Park CA US