发明名称 IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS
摘要 The invention provides compounds of Formula (I);;and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.
申请公布号 US2014179674(A1) 申请公布日期 2014.06.26
申请号 US201414191861 申请日期 2014.02.27
申请人 Bristol-Myers Squibb Company 发明人 Fink Brian E.;Chen Libing;Gavai Ashvinikumar V.;He Liqi;Kim Soong-Hoon;Nation Andrew James;Zhao Yufen;Zhang Litai H.
分类号 C07D487/04;C07D498/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to Formula (I):or a pharmaceutically acceptable salt thereof, wherein R1 is selected from H, F, Cl, Br, CN, and C1-6alkyl; R2 is selected from aryl substituted with 0-5 R2a and heteroaryl substituted with 0-5 R2a; R2a, at each occurrence, is independently selected from H, F, Cl, Br, ═O, CN, NO2, —ORb, —S(O)pRc, —C(C═O)Rd, —NRaRa, —(CR2bR2c)rC(═O)NRaRa, —NRaC(═O)Rd, —NRaC(═O)ORb, —OC(═O)NRaRa, —NRaC(═O)NRaRa, —(CR2bR2c)rC(═O)ORb, —S(O)2NRaRa, —NRaS(O)2NRaRa, —NRaS(O)2Rc, C1-6 alkyl substituted with 0-5 Re, —(CR2bR2c)r—C3-6carbocyclyl substituted with 0-5 Re, and —(CR2bR2c)r-heterocyclyl substituted with 0-5 Re; R2b, at each occurrence, is independently selected from H and C1-6alkyl substituted with 0-5 Re; R2c, at each occurrence, is independently selected from H and C1-6alkyl substituted with 0-5 Re; R3 is selected from H, F, Cl, Br, CN, —ORb, —NRaRa, —C(C═O)NRaRa, —NRaS(O)2Rc, —NRaC(═O)Rd, —NRaC(═O)ORb, and C1-6alkyl substituted with 0-5 Re; R4 is selected from H, C1-6alkyl substituted with 0-5 Re, —(CR4bR4c)rORb, —(CR4bR4c)rS(O)pRc, —(CR4bR4c)rC(═O)Rd, —(CR4bR4c)rNRaRa, —(CR4bR4c)rC(═O)NRaRa, —(CR4bR4c)rNRaC(═O)Rd, —(CR4bR4c)rNRaC(═O)ORb, —(CR4bR4c)rOC(═O)NRaRa, —(CR4bR4c)rNRaC(═O)NRaRa, —(CR4bR4c)rC(═O)ORb, —(CR4bR4c)rS(O)2NRaRa, —(CR4bR4c)rNRaS(O)2NRaRa, —(CR4bR4c)rNRaS(O)2Rc, —(CR4bR4c)r—C3-6carbocyclyl substituted with 0-5 R4a, —(CR4bR4c)r-heterocyclyl substituted with 0-5 R4a; R4a, at each occurrence, is independently selected from F, Cl, Br, C1-6alkyl substituted with 0-5 Re, C2-6alkenyl, C2-6alkynyl, NO2, ═O, CN, —SO3H, —S(O)pRc, —S(O)2NRaRa, —NRaS(O)2Rc, —ORb, —NRaRa, —NRaC(═O)Rd, —NRaC(═O)NRaRa; —C(═O)ORb, —C(C═O)Rd, —OC(═O)Rd, —C(C═O)NRaRa, C3-6cycloalkyl, heterocyclyl, and aryl; R4b, at each occurrence, is independently selected from H and C1-6alkyl substituted with 0-5 Re; R4c, at each occurrence, is independently selected from H and C1-6alkyl substituted with 0-5 Re; R5 is selected from hydrogen and C1-6alkyl substituted with 0-5 Re; R6 is selected from hydrogen and C1-6alkyl substituted with 0-5 Re; Ra, at each occurrence, is independently selected from H, CN, C1-6 alkyl substituted with 0-5 Re, C2-6 alkenyl substituted with 0-5 Re, C2-6 alkynyl substituted with 0-5 Re, —(CH2)r—C3-10carbocyclyl substituted with 0-5 Re, and —(CH2)r-heterocyclyl substituted with 0-5 Re; or Ra and Ra together with the nitrogen atom to which they are both attached form a heterocyclic ring substituted with 0-5 Re; Rb, at each occurrence, is independently selected from H, C1-6 alkyl substituted with 0-5 Re, C2-6 alkenyl substituted with 0-5 Re, C2-6 alkynyl substituted with 0-5 Re, —(CH2)r—C3-10carbocyclyl substituted with 0-5 Re, and —(CH2)r-heterocyclyl substituted with 0-5 Re; Rc, at each occurrence, is independently selected from C1-6 alkyl substituted with 0-5 Re, C2-6alkenyl substituted with 0-5 Re, C2-6alkynyl substituted with 0-5 Re, C3-6carbocyclyl, and heterocyclyl; Rd, at each occurrence, is independently selected from H, C1-6 alkyl substituted with 0-5 Re, C2-6alkenyl substituted with 0-5 Re, C2-6alkynyl substituted with 0-5 Re, —(CH2)r—C3-10carbocyclyl substituted with 0-5 Re, and —(CH2)r-heterocyclyl substituted with 0-5 Re; Re, at each occurrence, is independently selected from C1-6 alkyl substituted with 0-5 Rf, C2-6 alkenyl, C2-6 alkynyl, —(CH2)r—C3-6 cycloalkyl, F, Cl, Br, CN, NO2, ═O, CO2H, —(CH2)rOC1-5 alkyl, —(CH2)rOH, SH, and —(CH2)rNRfRf; Rf, at each occurrence, is independently selected from H, C1-5 alkyl, C3-6 cycloalkyl, and phenyl, or Rf and Rf together with the nitrogen atom to which they are both attached form a heterocyclic ring; p, at each occurrence, is independently selected from zero, 1, and 2; and r, at each occurrence, is independently selected from zero, 1, 2, 3, and 4.
地址 Princeton NJ US