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    • 1. 发明申请
    • Novel compounds
    • 新型化合物
    • US20060052380A1
    • 2006-03-09
    • US10542194
    • 2004-01-15
    • Martin CooperSimon GuileAnthony IngallRukhsana Rasul
    • Martin CooperSimon GuileAnthony IngallRukhsana Rasul
    • A61K31/503C07D498/02
    • C07D495/04
    • The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.
    • 本发明涉及式(I)的噻吩并哒嗪酮:其中:R 1是C 1-6烷基,C 2-6链烯基或C 任选被C 1-6烷基取代的,任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G,其中G是含有氮原子的5-或6-元环,和选自氧和/ 硫邻近氮,并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5,其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮,氧和硫的杂原子的5至10元单环或双环芳族环系统,所述环系统如上所述被任选地取代 在本说明书及其药学上可接受的盐和溶剂化物中。 还描述了其制备方法,含有它们的药物组合物及其在治疗中的用途,特别是在调节自身免疫疾病中
    • 2. 发明申请
    • Novel compounds
    • 新型化合物
    • US20060223809A1
    • 2006-10-05
    • US11447343
    • 2006-06-06
    • Martin CooperSimon GuileAnthony IngallRukhsana Rasul
    • Martin CooperSimon GuileAnthony IngallRukhsana Rasul
    • A61K31/503C07D498/02
    • C07D495/04
    • The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.
    • 本发明涉及式(I)的噻吩并哒嗪酮:其中:R 1是C 1-6烷基,C 2-6链烯基或C 任选被C 1-6烷基取代的,任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G,其中G是含有氮原子的5-或6-元环,和选自氧和/ 硫邻近氮,并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5,其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮,氧和硫的杂原子的5至10元单环或双环芳族环系统,所述环系统如上所述被任选地取代 在本说明书及其药学上可接受的盐和溶剂化物中。 还描述了其制备方法,含有它们的药物组合物及其在治疗中的用途,特别是在调节自身免疫疾病中。