发明名称 Androgen receptor modulator compounds and methods
摘要 Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.;
申请公布号 US8865918(B2) 申请公布日期 2014.10.21
申请号 US201313974937 申请日期 2013.08.23
申请人 Ligand Pharmaceuticals Incorporated 发明人 Zhi Lin;Higuchi Robert I.;Van Oeveren Cornelis Arjan;Lau Thomas Lot Stevens
分类号 C07D295/04;C07D207/12;C07D209/04;C07D211/22;C07D215/04;C07D265/36;C07D295/073;C07C211/52;C07D207/09;C07D209/12;C07D207/16;C07D211/60;C07D207/26;C07D215/18;C07D207/46;C07D211/56;C07C255/58;C07D207/08;C07D209/08 主分类号 C07D295/04
代理机构 Knobbe Martens Olson & Bear LLP 代理人 Knobbe Martens Olson & Bear LLP
主权项 1. A method for modulating an activity of an androgen receptor comprising contacting an androgen receptor with a compound of Formula (II): wherein: R1 is NO2 or CN; R2 is selected from among F, Cl, Br, I, SRA, NO2, and CF3; R3and R4 are each independently selected from hydrogen, F, Cl, ORA, an optionally substituted C1-C4 alkyl, and CF3; R5 is hydrogen; R10 is hydrogen; R6a and R7a are each independently hydrogen or an optionally substituted C1-C6 alkyl; R9 is selected from an optionally substituted C1-C8 alkyl, C1-C8 heteroalkyl, CH(RD)ORA, CH(RD)NRARB, and CORA; R12 and R13 are each independently selected from hydrogen, F, Cl, ORA, and (CH2)mRC; RA is hydrogen; RB is hydrogen; RC is selected from an optionally substituted aryl and an optionally substituted heteroaryl that is optionally with a substituent selected from F, Cl, Br, I, CN, ORA, NO2, NRARB, SRA, SORA, SO2RA, an optionally substituted C1-C4 alkyl, CF3, and an optionally substituted C1-C4 heteroalkyl; RD is hydrogen or CF3; Z is CRARB; n is 0; and in is 1 or 2, or a pharmaceutically acceptable salt thereof.
地址 La Jolla CA US