发明名称 Pyrrolopyrimidine compounds and uses thereof
摘要 The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer.
申请公布号 US9346810(B2) 申请公布日期 2016.05.24
申请号 US201113817802 申请日期 2011.08.18
申请人 HUTCHISON MEDIPHARMA LIMITED 发明人 Su Wei-Guo;Deng Wei;Li Jinshui;Ji Jianguo
分类号 C07D487/04 主分类号 C07D487/04
代理机构 Gorman IP Law, APC 代理人 Gorman IP Law, APC
主权项 1. A compound of formula (I): wherein R1 is chosen from hydrogen, alkyl, cycloalkyl and heterocycle, each of the said alkyl, cycloalkyl, and heterocycle, in R1 is optionally substituted with one or more groups chosen from optionally substituted lower alkyl, optionally substituted aryl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, —C(O)Ra, —C(O)ORb, —CN, —C(O)NRcRd, halo, optionally substituted haloalkyl, optionally substituted heterocycle, optionally substituted heteroaryl, —NRcRd, —NReC(O)Ra, —NReC(O)ORb, —NReC(O)NRcRd, —NReS(O)nRf, —NReS(O)nNRcRd, —NO2, —ORb, —S(O)nRf, and —S(O)nNRcRd; R2 iswhich is optionally substituted with one or more groups chosen from optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted haloalkyl, —C(O)Ra, —C(O)ORb, —CN, —C(O)NRcRd, halo, optionally substituted heterocycle, optionally substituted heteroaryl, —NRcRd, —NReC(O)Ra, —NReC(O)ORb, —NReC(O)NRcRd, —NReS(O)nRf, —NReS(O)nNRcRd, —NO2, ORb, —S(O)nRf, and —S(O)nNRcRd; m is 1; n is chosen from 0, 1, and 2;for each occurrence, Ra, Rb, Rc, Rd, Re and Rf are each independently chosen from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted haloalkyl, optionally substituted heteroaryl and optionally substituted heterocycle, or Rc and Rd, with the nitrogen to which they are attached, combine to form a heterocycle ring, which is optionally substituted with one or more groups chosen from halo, lower alkyl, hydroxy, and lower alkoxy, wherein the heterocycle ring further optionally comprises one or two additional heteroatoms chosen from N, O and S,wherein each optionally substituted group above can be unsubstituted or independently substituted with at least one substituent independently chosen C1-C4 alkyl, cycloalkyl, aryl, heterocycle, heteroaryl, aryl-C1-C4 alkyl-, heteroaryl-C1-C4 alkyl-, C1-C4 haloalkyl-, —OC1-C4 alkyl, —OC1-C4 alkylphenyl, —C1-C4 alkyl-OH, —C1-C4 alkyl-O—C1-C4 alkyl, —OC1-C4 haloalkyl, halo, —OH, —NH2, —C1-C4 alkyl-NH2, —N(C1-C4 alkyl)(C1-C4 alkyl), —NH(C1-C4 alkyl), —N(C1-C4 alkyl)(C1-C4 alkylphenyl), —NH(C1-C4 alkylphenyl), cyano, nitro, oxo, —CO2H, —C(O)OC1-C4 alkyl, —CON(C1-C4 alkyl)(C1-C4 alkyl), —CONH(C1-C4 alkyl), —CONH2, —NHC(O)(C1-C4 alkyl), —NHC(O)(phenyl), —N(C1-C4 alkyl)C(O)(C1-C4 alkyl), —N(C1-C4 alkyl)C(O)(phenyl), —C(O)C1-C4 alkyl, —C(O)C1-C4 phenyl, —C(O)C1-C4 haloalkyl, —OC(O)C1-C4 alkyl, —SO2(C1-C4 alkyl), —SO2(phenyl), —SO2(C1-C4 haloalkyl), —SO2NH2, —SO2NH(C1-C4 alkyl), —SO2NH(phenyl), —NHSO2(C1-C4 alkyl), —NHSO2(phenyl), and —NHSO2(C1-C4 haloalkyl), in which each of phenyl, aryl, heterocycle, and heteroaryl is optionally substituted by one or more groups chosen from halo, cycloalkyl, heterocycle, C1-C4 alkyl, C1-C4 haloalkyl-, —OC1-C4 alkyl, C1-C4 alkyl-OH, —C1-C4 alkyl-O—C1-C4 alkyl, —OC1-C4 haloalkyl, cyano, nitro, —NH2, —CO2H, —C(O)OC1-C4 alkyl, —CON(C1-C4 alkyl)(C1-C4 alkyl), —CONH(C1-C4 alkyl), —CONH2, —NHC(O)(C1-C4 alkyl), —N(C1-C4 alkyl)C(O)(C1-C4 alkyl), —SO2(C1-C4 alkyl), —SO2(phenyl), —SO2(C1-C4 haloalkyl), —SO2NH2, —SO2NH(C1-C4 alkyl), —SO2NH(phenyl), —NHSO2(C1-C4 alkyl), —NHSO2(phenyl), and —NHSO2(C1-C4 haloalkyl);and/or at least one pharmaceutically acceptable salt thereof.
地址 Shanghai CN