发明名称 BISPHENOL COMPOUNDS AND METHODS FOR THEIR USE
摘要 Compounds having a structure of Formula I: wherein G, a, Q, L2, R1, R2, R3, R4, R5 and R6 are as defined herein are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.;
申请公布号 US2014248263(A1) 申请公布日期 2014.09.04
申请号 US201214110615 申请日期 2012.04.06
申请人 Andersen Raymond John;Fernandez Javier Garcia;Sadar Marianne Dorothy;Mawji Nasrin;Banuelos Carmen Adriana;Wang Jun 发明人 Andersen Raymond John;Fernandez Javier Garcia;Sadar Marianne Dorothy;Mawji Nasrin;Banuelos Carmen Adriana;Wang Jun
分类号 A61K31/336;A61K45/06;A61K31/09;C07C43/215;C07D303/14;C07C43/23 主分类号 A61K31/336
代理机构 代理人
主权项 1. A compound having a structure of Formula I: or a pharmaceutically acceptable salt thereof, wherein:G is a linear, branched or non-aromatic cyclic, substituted or unsubstituted, saturated or unsaturated C1-C20 alkyl, wherein one or more carbon atoms of the C1-C20 alkyl may optionally be replaced with an oxygen atom; a is 0 or 1; R1 and R2 are each independently H or linear or branched, substituted or unsubstituted, saturated or unsaturated C1-C10 alkyl, or R1 and R2 together may form a substituted or unsubstituted, saturated or unsaturated cyclic C3-C10 alkyl; R3, R4, R5 and R6 are each independently H, halo or linear or branched, substituted or unsubstituted, saturated or unsaturated C1-C10 alkyl; Q is J is G1, O, CH2, CHG1, CG12, S, NH, NG1, SO, SO2, or NR; M is H, OH, F, Cl, Br, CH2OH, CH2F, CH2Cl, CHCl2, CCl3, CH2Br, CHBr2 or CBr3; L is H, A-D or —CH2-A-D; A is O, S, NH, NG1, N+H2, or N+HG1; D is H, G1, R, or a moiety from TABLE 1; R is C1-C10 acyl; n is 0, 1, 2, 3, 4, 5, 6, 7 or 8; L2 is H or A2-D2; A2 is O, S, SO, SO2, NH, NG1, N+H2 or N+HG1; D2 is H, G1, R7, or a moiety from TABLE 1; G1 is a linear or branched, aromatic or non-aromatic cyclic, substituted or unsubstituted, saturated or unsaturated C2-C10 alkyl, and wherein the optional substituents for any of the C1-C20 alkyl, C1-C10 alkyl and cyclic C3-C10 alkyl moieties are each independently oxo, OR8, COOH, R9, OH, OR9, F, Cl, Br, I, NH2, NHR9, N(R9)2, CN, SH, SR9, SO3H, SO3R9, SO2R9, OSO3R9, OR, CO2R9, CONH2, CONHR9, CONHR, CON(R9)2, NHR, OPO3H3, CONR9R, NR9R or NO2, wherein R8 is a moiety from TABLE 1 and each R9 is independently unsubstituted C1-C10 alkyl, wherein the use is for modulating androgen receptor (AR) activity; provided that M is not CH2Cl when G is isopropyl and L is not H when G is a saturated C1-C20 alkyl, wherein one or more carbon atoms of the saturated C1-C20 alkyl have been replaced with an oxygen atom.
地址 Vancouver CA