发明名称 ANDROGEN RECEPTOR ANTAGONISTS
摘要 Disclosed herein are compositions and methods for modulating the androgen receptor.
申请公布号 US2017101384(A1) 申请公布日期 2017.04.13
申请号 US201615382942 申请日期 2016.12.19
申请人 THE REGENTS OF THE UNIVERSITY OF CALIFORNIA 发明人 ENGLAND Pamela M.;Fletterick Robert J.;Kuchenbecker Kristopher;Cortez Felipe de Jesus
分类号 C07D257/08;C07D213/84;C07D253/07;C07D213/74;C07D241/26;C07D237/24;C07K14/72;C07D239/42 主分类号 C07D257/08
代理机构 代理人
主权项 1. A compound having the formula: wherein Ring A is a heteroaryl; Ring B is a phenyl or heteroaryl; R1 is independently a halogen, —CXa3, —CN, —SO2Cl, —SOn1R10, —SOv1NR7R8, —NHNH2, —ONR7R8, —NHC═(O)NHNH2, —NHC═(O)NR7R8, —N(O)m1, —NR7R8, —C(O)R9, —C(O)—OR9, —C(O)NR7R8, —OR10, —NR7SO2R10, —NR7C═(O)R9, —NR7C(O)—OR9, —NR7OR9, —OCXa3, —OCHXa2, E, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; two adjacent R1 substituents may optionally be joined to form a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; E is an electrophilic moiety; R2 is independently a halogen, —CXb3, —CN, —SO2Cl, —SOn2R14, —SOv2NR11R12, —NHNH2, —ONR11R12, —NHC═(O)NHNH2, —NHC═(O)NR11R12, —N(O)m2, —NR11R12, —C(O)R13, —C(O)—OR13, —C(O)NR11R12, —OR14, —NR11SO2R14, —NR11C═(O)R13, —NR11C(O)—OR13, —NR11OR13, —OCXb3, —OCHXb2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; two adjacent R2 substituents may optionally be joined to form a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R7, R8, R9, R10, R11, R12, R13, and R14 are independently hydrogen, halogen, —CXc3, —CN, —OH, —NH2, —COOH, —CONH2, —NO2, —SH, —SO2Cl, —SO3H, —SO4H, —SO2NH2, —NHNH2, —ONH2, —NHC═(O)NHNH2, —NHC═(O) NH2, —NHSO2H, —NHC═(O)H, —NHC(O)—OH, —NHOH, —OCXc3, —OCHX2, —CF3, —OCF3, —OCHF2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R7 and R8 substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl; R11 and R12 substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl; a1 is independently an integer from 0 to 4; b1 is independently an integer from 0 to 5; m1, m2, v1, and v2 are independently 1 or 2; n1 and n2 are independently an integer from 0 to 4; Xa, Xb, and Xc are independently —Cl, —Br, —I, or —F.
地址 Oakland CA US