发明名称 Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases
摘要 Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.
申请公布号 US8802689(B2) 申请公布日期 2014.08.12
申请号 US201213615085 申请日期 2012.09.13
申请人 The Regents of the University of California 发明人 Jung Michael E.;Sawyers Charles L.;Ouk Samedy;Tran Chris;Wongvipat John
分类号 A61K31/44 主分类号 A61K31/44
代理机构 Kilpatrick Townsend & Stockton LLP 代理人 Kilpatrick Townsend & Stockton LLP
主权项 1. A method for treating a disease or disorder related to nuclear receptor activity in a subject, comprising administering a compound, or a pharmaceutically acceptable salt thereof, to the subject in need of such treatment, the compound having the formula: wherein Het is a heterocyclic unit of 6 atoms comprising (i) 1 or 2 heteroatoms independently selected from the group consisting of nitrogen, oxygen, or sulfur; (ii) 0 or 1 double-bonded substituent on the heterocyclic unit selected from the group consisting of oxygen and sulfur; and (iii) 3 to 4 single-bonded substituents on the heterocyclic unit independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, arylalkyl, arylalkenyl, arylalkynyl, halogenated alkyl, halogenated alkenyl, halogenated alkynyl, halogen, CN, NO2, OR11, SR11, NR11R12, NH(CO)OR11, NH(CO)NR11R12, NR12(CO)R11, O(CO)R11, O(CO)OR11, O(CS)R11, NR12(CS)R11, NH(CS)NR11R12, NR12(CS)OR11, wherein two of said single-bonded substituents may be connected together with the atoms to which they are bonded to form a cycle, which is aromatic, substituted aromatic, heterocyclic aromatic or non-aromatic, substituted heterocyclic aromatic or non-aromatic, cycloalkyl, or substituted cycloalkyl; A is sulfur and B is oxygen; R11 and R12 are independently selected from hydrogen, alkyl, substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, aryl, substituted aryl, arylalkyl, arylalkenyl, arylalkynyl, heterocyclic aromatic or non-aromatic, or substituted heterocyclic aromatic or non-aromatic, wherein R11 and R12, both on the same single bonded substituent, can be connected together with the atoms to which they are bonded to form a cycle, which can be heterocyclic aromatic or non-aromatic, or substituted heterocyclic aromatic; R1 is selected from aryl and substituted aryl; R2 and R3 are independently selected from hydrogen, aryl, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, halogenated alkyl, halogenated alkenyl, halogenated alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heterocyclic aromatic or non-aromatic, substituted heterocyclic aromatic or non-aromatic, cycloalkyl, or substituted cycloalkyl, or, together with the carbon to which they are linked, form a cycle which can be cycloalkyl or substituted cycloalkyl.
地址 Oakland CA US