发明名称 Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
摘要 The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
申请公布号 US9273047(B2) 申请公布日期 2016.03.01
申请号 US201414487347 申请日期 2014.09.16
申请人 Corcept Therapeutics, Inc. 发明人 Hunt Hazel;Johnson Tony;Ray Nicholas;Walters Iain
分类号 A01N43/42;C07D471/04;A61K31/4745;A61K31/506;A61K31/5377;A61K31/497;C07D498/04;A61K31/5383;A61K31/56;C07D519/00;A61K45/06 主分类号 A01N43/42
代理机构 Kilpatrick Townsend Stockton LLP 代理人 Kilpatrick Townsend Stockton LLP
主权项 1. A method of modulating a glucocorticoid receptor, comprising contacting a glucocorticoid receptor with a compound of Formula I, thereby modulating the glucocorticoid receptor, wherein the compound of Formula I has the formula:wherein R1 is a heteroaryl ring having from 5 to 6 ring members and from 1 to 4 heteroatoms each independently selected from the group consisting of N, O and S, optionally substituted with 1-4 groups each independently selected from R1a; each R1a is independently selected from the group consisting of hydrogen, C1-6 alkyl, halogen, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, —CN, N-oxide, C3-8 cycloalkyl, and C3-8 heterocycloalkyl; ring J is selected from the group consisting of a cycloalkyl ring, a heterocycloalkyl ring, an aryl ring and a heteroaryl ring, wherein the heterocycloalkyl and heteroaryl rings have from 5 to 6 ring members and from 1 to 4 heteroatoms each independently selected from the group consisting of N, O and S; each R2 is independently selected from the group consisting of hydrogen, C1-6 alkyl, halogen, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkyl-C1-6 alkoxy, —CN, —OH, —NR2aR2b, —C(O)R2a, —C(O)OR2a, —C(O)NR2aR2b, —SR2a, —S(O) R2a, —S(O)2R2a, C3-8 cycloalkyl, and C3-8 heterocycloalkyl, wherein the heterocycloalkyl groups are optionally substituted with 1-4 R2c groups; alternatively, two R2 groups linked to the same carbon are combined to form an oxo group (═O); alternatively, two R2 groups are combined to form a heterocycloalkyl ring having from 5 to 6 ring members and from 1 to 3 heteroatoms each independently selected from the group consisting of N, O and S, wherein the heterocycloalkyl ring is optionally substituted with from 1 to 3 R2d groups; R2a and R2b are each independently selected from the group consisting of hydrogen and C1-6 alkyl; each R2c is independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, —CN, and —NR2aR2b; each R2d is independently selected from the group consisting of hydrogen and C1-6 alkyl, or two R2d groups attached to the same ring atom are combined to form (═O); R3 is selected from the group consisting of phenyl and pyridyl, each optionally substituted with 1-4 R3a groups; each R3a is independently selected from the group consisting of hydrogen, halogen, and C1haloalkyl; subscript n is an integer from 0 to 3; or salts thereof.
地址 Menlo Park CA US
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