发明名称 Therapeutically Active Oxazoline Derivatives
摘要 Compounds of formula (I) i.e. monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives substituted by an optionally substituted oxazolin-2-yl moiety, 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 US2015274748(A1) 申请公布日期 2015.10.01
申请号 US201314432842 申请日期 2013.10.02
申请人 UCB BIOPHARMA SPRL ;KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D 发明人 Kulisa Claire Louise;Brookings Daniel Christopher;Ford Daniel James;Franklin Richard Jeremy;Reuberson James Thomas;Ghawalkar Anant Ramrao
分类号 C07D495/04 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—, —C(CH3)2—, —CH2CH2— or —CH2CH2CH2—; X represents C—R6 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(R7)— and —S(O)2N(R7)—; Z represents hydrogen; or Z represents 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 A represents C1-6 alkyl, optionally substituted by one or more substituents independently selected from halogen, —ORa, —S(O)Ra and —NRbRc; R1 represents hydrogen, halogen, cyano, nitro, hydroxy, trifluoromethyl, trifluoromethoxy, —ORa, —SRa, —SORa, —SO2Ra, —NRbRc, —CH2NRbRc, —NRcORd, —CH2NRcCORd, —NRcCO2Rd, —NHCONRbRc, —NRcSO2Re, —N(SO2Re)2, —NHSO2NRbRc, —CORd, —CO2Rd, —CONRbRc, —CON(ORa)Rb or —SO2NRbRc; or R1 represents 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; R2 represents hydrogen or C1-6 alkyl; and R3 represents hydrogen; or R3 represents C1-6 alkyl, C1-6 alkoxy, 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 R2 and R3, when taken together with the carbon atom to which they are both attached, represent C3-7 cycloalkyl or C3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; R4 represents hydrogen or C1-6 alkyl; and R5 represents hydrogen; or R5 represents C1-6 alkyl, C1-6 alkoxy, 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 R4 and R5, when taken together with the carbon atom to which they are both attached, represent C3-7 cycloalkyl or C3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents; R6 and R7 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.
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