发明名称 Therapeutically Active Fused Pyrimidine Derivatives
摘要 A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
申请公布号 US2014309222(A1) 申请公布日期 2014.10.16
申请号 US201214239406 申请日期 2012.08.15
申请人 Brookings Daniel Christopher;Ford Daniel James;Ghawalkar Anant Ramrao;Herman Jean;Huang Qiuya;Kulisa Claire Louise;Louat Thierry;Neuss Judi Charlotte;Reuberson James Thomas;Vanderhoydonck Bart 发明人 Brookings Daniel Christopher;Ford Daniel James;Ghawalkar Anant Ramrao;Herman Jean;Huang Qiuya;Kulisa Claire Louise;Louat Thierry;Neuss Judi Charlotte;Reuberson James Thomas;Vanderhoydonck Bart
分类号 C07D495/04;C07D513/04 主分类号 C07D495/04
代理机构 代理人
主权项 1. A compound of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof:wherein Q represents a group of formula (Qa) or (Qb):in which the asterisk (*) represents the point of attachment to the remainder of the molecule; V represents —CH2—, —CH2CH2— or —CH2CH2CH2—; X represents C—R3 or N; Y represents a covalent bond, or a linker group selected from —C(O)—, —S(O)—, —S(O)2—, —C(O)O—, —C(O)N(R4)— and —S(O)2N(R4)—; Z represents hydrogen; or C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents; A represents hydrogen or trifluoromethyl; or C1-6 alkyl, optionally substituted by one or more substituents independently selected from —ORa and —NRbRc; R1 and R2 independently represent hydrogen, halogen, cyano, nitro, hydroxy, trifluoromethyl, trifluoromethoxy, —ORa, —SRa, —SORa, —SO2Ra, —NRbRc, —CH2NRbRc, —NRcCORd, —CH2NRcCORd, —NRcCO2Rd, —NHCONRbRc, —NRcSO2Re, —N(SO2Re)2, —NHSO2NRbRc, —CORd, —CO2Rd, —CONRbRc, —CON(ORa)Rb or —SO2NRbRc; or C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents; R3 and R4 independently represent hydrogen; or C1-6 alkyl, optionally substituted by one or more substituents independently selected from —ORa and —NRbRc; Ra represents hydrogen; or Ra represents C1-6 alkyl, aryl, aryl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents; Rb and Rc independently represent hydrogen or trifluoromethyl; or C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents; or Rb and Rc, when taken together with the nitrogen atom to which they are both attached, represent azetidin-1-yl, pyrrolidin-1-yl, oxazolidin-3-yl, isoxazolidin-2-yl, thiazolidin-3-yl, isothiazolidin-2-yl, piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, piperazin-1-yl, homopiperidin-1-yl, homomorpholin-4-yl or homopiperazin-1-yl, any of which groups may be optionally substituted by one or more substituents; Rd represents hydrogen; or C1-6 alkyl, C3-7 cycloalkyl, aryl, C3-7 heterocycloalkyl or heteroaryl, any of which groups may be optionally substituted by one or more substituents; and Re represents C1-6 alkyl, aryl or heteroaryl, any of which groups may be optionally substituted by one or more substituents.
地址 Slough, Berkshire GB