发明名称 PYRROLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
摘要 Disclosed herein are methods of using pyrrolo[2,3-d]pyrimidine Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, and inflammatory diseases or conditions.
申请公布号 US2016375026(A1) 申请公布日期 2016.12.29
申请号 US201615261414 申请日期 2016.09.09
申请人 Pharmacyclics LLC 发明人 Chen Wei;Loury David J.;Wang Longcheng
分类号 A61K31/519 主分类号 A61K31/519
代理机构 代理人
主权项 1. A method for treating an autoimmune disease or condition, a heteroimmune disease or condition, or an inflammatory disease or condition comprising administering to a patient in need a therapeutically effective amount of a compound of Formula (I) having the structure: wherein: R1 is halogen, —CN, —OH, —NH2, —SH, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C4alkoxy, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted heteroaryl or substituted or unsubstituted C3-C8cycloalkyl;G is substituted or unsubstituted C2-C4alkenyl, substituted or unsubstituted C2-C4alkynyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C1-C4alkoxy, substituted or unsubstituted C1-C4heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, halogen, —CN, —NO2, —OH, —OCF3, —OCH2F, —OCF2H, —CF3, —SCH3, —N(R21)S(═O)2R23, S(═O)2N(R21)(R22), —S(═O)R23, —S(═O)2R23, —C(═O)R23, —OC(═O)R23, —CO2R21, N(R21)(R22), —C(═O)N(R21)(R22), —N(R21)C(═O)R23, N(R21)C(═O)OR22, N(R21)C(═O)N(R21)(R22), or La-Ar;La is a bond, —CH2—, —CH(OH)—, —C(O)—, —CH2O—, —OCH2—, —SCH2, —CH2S—, —N(R21)—, —N(R21)C(O)—, —C(O)N(R21)—, —N(R21)C(O)N(R21)—, —O—, —S—, —S(O)2—, —N(R21)S(O)2—, or —S(O)2N(R21)—;Ar is a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted heteroaryl;each R24 is independently halogen, —CN, —NO2, —OH, —OCF3, —OCH2F, —OCF2H, —CF3, —SCH3, —N(R21)S(═O)2R23, S(═O)2N(R21)(R22), —S(═O)R23, —S(═O)2R23, —C(═O)R23, —OC(═O)R23, —CO2R21, N(R21)(R22), —C(═O)N(R21)(R22), —N(R21)C(═O)R23, N(R21)C(═O)OR22, —N(R21)C(═O)N(R21)(R22), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, or substituted or unsubstituted cycloalkyl;each R21 and R22 is independently H, substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C3-C8cycloalkyl;each R23 is each independently substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C3-C8cycloalkyl;n is 0-4;Y is an optionally substituted group selected from among C1-C6alkylene, C1-C6heteroalkylene, C6-C12arylene, C3-C12heteroarylene, C1-C6alkyleneC6-C12arylene, C1-C6alkyleneC3-C12heteroarylene, C1-C6alkyleneC3-C8cycloalkylene, C1-C6alkyleneC2-C7heterocycloalkylene, C3-C8cycloalkylene, C2-C7heterocycloalkylene, fused C3-C8cycloalkyleneC2-C7heterocycloalkylene, and spiro C3-C8cycloalkyleneC2-C7heterocycloalkylene;Z is —C(═O)—, —N(Ra)C(═O)—, or —N(Ra)S(═O)x—, where x is 1 or 2, and Ra is H, substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C3—C cycloalkyl;R6 is H or L-J-W;R7 and R8 are independently H or L-J-W; or R7 and R8 taken together form a bond;L and J are each independently a bond, substituted or unsubstituted C1-C6alkylene, substituted or unsubstituted C3-C8 cycloalkylene, substituted or unsubstituted C1-C6heteroalkylene, substituted or unsubstituted C2-C7heterocycloalkylene, substituted or unsubstituted C6-C12arylene, substituted or unsubstituted C3-C12heteroarylene, —CO—, —O—, or —S—;W is H, or NR25R26; andR25 and R26 are each independently H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C3—C cycloalkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C6-C12aryl, or substituted or unsubstituted C3-C12heteroaryl; or a pharmaceutically acceptable solvate, or a pharmaceutically acceptable salt thereof.
地址 Sunnyvale CA US