发明名称 Androgen receptor modulators and uses thereof
摘要 Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.
申请公布号 US9108944(B2) 申请公布日期 2015.08.18
申请号 US201113579009 申请日期 2011.02.16
申请人 ARAGON PHARMACEUTICALS, INC. 发明人 Smith Nicholas D.;Bonnefous Celine;Julien Jackaline D.
分类号 C07D401/04;A61K31/4439;C07D487/04;C07D471/04;C07D401/14;C07D405/14 主分类号 C07D401/04
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A compound of Formula (Ia), or a pharmaceutically acceptable salt, or N-oxide thereof: wherein, ring A is pyridinyl; m is 1, 2, 3 or 4; each RA is independently halogen, —CN, —NO2, —OH, —OR9, —SR9, —S(═O)R10, —S(═O)2R10, —N(R11)S(═O)2R10, —S(═O)2N(R9)2, —C(═O)R10, —OC(═O)R10, —CO2R9, —N(R9)2, —C(═O)N(R9)2, C1-C6alkyl, C1-C6fluoroalkyl, C1-C6fluoroalkoxy, C1-C6alkoxy, or C1-C6heteroalkyl; both R1 are taken together with the carbon atom to which they are attached to form a C3-C6cycloalkyl; X is S or O; ring B is phenyl; n is 1, or 2; each R4 is independently hydrogen, halogen, —CN, —NO2, —OH, —OR9, —SR9, —S(═O)R10, —S(═O)2R10, —N(R11)S(═O)2R10, —S(═O)2N(R9)2, —C(═O)R10, —OC(═O)R10, —CO2R9, —OCO2R10, —N(R9)2, —C(═O)N(R9)2, —OC(═O)N(R9)2, —NR11C(═O)N(R9)2, —NR11C(═O)R10, —NR11C(═O)OR10, C1-C6alkyl, C1-C6fluoroalkyl, C1-C6fluoroalkoxy, or C1-C6alkoxy; R5 is -L1-L2-R6; and (i) L1 is —O—, —S—, —S(═O)—, —S(═O)2—, —NH—, —N(CH3)—; —C(═O)—, —C(═O)NH—, —NHC(═O)—, —NHC(═O)O—, —NHC(═O)NH—, —C(═O)O—, —OC(═O)—OC(═O)O—, —OC(═O)NH—, —NHS(═O)2—, or —S(═O)2NH—; and (ii) L2 is C1-C6alkylene, C1-C6fluoroalkylene or C1-C6heteroalkylene; or R5 is L1-R7; and L1 is —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)NH—, —NHC(═O)—, —NHC(═O)O—, —NHC(═O)NH—, —C(═O)O—, —OC(═O)—, —OC(═O)O—, —OC(═O)NH—, —NHS(═O)2—, or —S(═O)2NH—; R6 and R7 are independently optionally substituted piperidinyl; said optional substituents including at least one of alkyl, fluoroalkyl, —CN, halo, —C(O)—O—(C1-6 alkyl), —CH2—C(O)—O—(C1-6 alkyl), —NH2, —NH(CH3), —N(CH3)2, —OH, —CO2H, —C(O)NH2, —C(O)NH(alkyl), —C(O)N(alkyl)2, alkoxy, fluoroalkoxy, -(alkyl)sulfonyl, -(alkylene)-OH, or —C(O)-(alkyl); each R9 is independently H, C1-C6alkyl, or C1-C6fluoroalkyl; R10 is C1-C6alkyl; and R11 is independently H or C1-C4alkyl.
地址 San Diego CA US