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.

主权项

1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, diluent, or excipient and a compound of Formula (I), or a pharmaceutically acceptable salt or N-oxide thereof, said composition formulated in a dosage form suitable for delivering a therapeutically effective amount of the compound when administered in a single dosage form or in a divided dosage form multiple times over the span of one day: 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.