发明名称 ISOTHIAZOLE DERIVATIVES AS PIM KINASE INHIBITORS AND PREPARATION METHODS AND USE IN MEDICINAL MANUFACTURE THEREOF
摘要 PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, multi drug resistance, and inflammatory bowel disease. Also provided are methods for preparing and using the compounds represented by Formula I.;
申请公布号 US2015284378(A1) 申请公布日期 2015.10.08
申请号 US201514746720 申请日期 2015.06.22
申请人 Jikai Biosciences, Inc. 发明人 GE Yu
分类号 C07D417/12;C07D417/14 主分类号 C07D417/12
代理机构 代理人
主权项 1. A compound having a structure of Formula II: wherein R1 is a hydrogen, —NHR4, a halogen, a hydroxyl, an alkyl, a cyano, or a nitro; R2 and R3 are each independently selected from a hydrogen, —NHR5, a halogen, a hydroxyl, a substituted or unsubstituted alkyl, an alkenyl, an alkynyl, an alkoxyl, a cycloalkyl, an amino, a cyano, and a nitro; R4 is a hydrogen, —C(═O)—R5, a substituted or unsubstituted alkyl, a cycloalkyl, a heterocyclyl, an aryl, or a heteroaryl; R5 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxyl, cycloalkyl, amino, or substituted amino; R6 is a substituted or unsubstituted aryl, heteroaryl, cycloalkyl, wherein each substituted R6 group is substituted with up to four substituents that is a halogen, a cyano, an amino, a C1-4 alkyl, a C3-6 cycloalkyl, an alkoxyl, a nitro, a carboxy, a carbonyl, a carboalkoxy, or an aminocarboxy; R22 is an optionally substituted C1-C8 hydrocarbon group or a group having a formula: wherein each of R23, R24, R25 is independently selected from a H, a halogen, OR15, NR16R17, C(═O)NR18R19, or an optionally substituted C1-C8 hydrocarbon group; or R23, R24 and R25, together with atoms to which they are attached, are joined together to form a chain so that the ring to which they are attached is a substituted C6-C14 membered spiral ring, a bicyclic ring, or a fused ring group; G1 is CH or N; G2 is NR28, CHR29, or O; B1 and B2 each independently represents 0, 1, 2, or 3; B3 is 0, 1, or 2; B4 is 0 or 1; each of R16, R17, R18, R19, R26 and R27 is independently selected from a H or an optionally substituted C1-C8 hydrocarbon group; R28 is H, an optionally substituted hydrocarbon group, an optionally substituted cyclic hydrocarbon group, an optionally substituted heterocyclic hydrocarbon group, C(═O)R30, C(═O)OR30, or C(═O)NHR30; R29 is OH, NHR30, C(═O)OR30, or C(═O)NHR30; and R30 is H or an optionally substituted C1-C8 hydrocarbon group.
地址 Shanghai CN