发明名称 Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
摘要 The present disclosure is generally directed to neuroactive 13,17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
申请公布号 US9512170(B2) 申请公布日期 2016.12.06
申请号 US201414191740 申请日期 2014.02.27
申请人 Washington University 发明人 Covey Douglas;Jiang Xin
分类号 A61K31/57;C07J71/00;C07J3/00;C07J7/00;C07J1/00;C07J13/00;C07J21/00 主分类号 A61K31/57
代理机构 Armstrong Teasdale LLP 代理人 Armstrong Teasdale LLP
主权项 1. A method of inducing anesthesia in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof; wherein: R1 is H, optionally substituted C1-C4 alkyl, optionally substituted C2-C4 alkenyl, or optionally substituted C2-C4 alkynyl;R2 is H, optionally substituted C1-C4 alkoxy, aryloxy, optionally substituted C2-C4 alkenoxy, optionally substituted C2-C4 alkynoxy, or —O—C(O)—Rx, where Rx is optionally substituted C1-C20 alkyl;R3 is H, optionally substituted C1-C4 alkyl, optionally substituted C2-C4 alkenyl, optionally substituted alkynyl, cyclopropyl, or C(O)Ry, where Ry is C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl;R4 is optionally substituted C2-C4 alkenyl, optionally substituted C2-C4 alkynyl, optionally substituted cyclopropyl, or C(O)Rz, where Rz is C1-C4 alkyl, C2-C4 alkenyl or C2-C4 alkynyl;R5 is H, ═O, or ORv, where Rv is H, optionally substituted C1-C4 alkyl, optionally substituted C2-C4 alkenyl, optionally substituted C2-C4 alkynyl, or optionally substituted aryl;R6 is H, optionally substituted C1-C4 alkyl, optionally substituted C2-C4 alkenyl, or optionally substituted C2-C4 alkynyl;R7 is H, optionally substituted C1-C4 alkoxy, aryloxy, morpholinyl, optionally substituted C2-C4 alkenoxy, optionally substituted C2-C4 alkynoxy, or —O—C(O)—Rw, where Rw, is optionally substituted C1-C20 alkyl;R8 is, when present, H, C1-C4 alkyl, C2-C4 alkenyl, or C2-C4 alkynyl; R9 is H or C(O)Ru, where Ru is optionally substituted C1-C20 alkyl, optionally substituted C2-C20 alkenyl, or optionally substituted C2-C20 alkynyl; wherein the C5—H is in the alpha configuration; and,- - - denotes an optional, additional C—C bond, resulting in either a C═C bond between C4-C5 or C5-C6, with the proviso that when present, the C5—H substituent is not present.
地址 St. Louis MO US