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    • 9. 发明授权
    • Purine derivatives
    • 嘌呤衍生物
    • US06525032B2
    • 2003-02-25
    • US09789236
    • 2001-02-20
    • Simon John MantellSandra Marina MonaghanPeter Thomas Stephenson
    • Simon John MantellSandra Marina MonaghanPeter Thomas Stephenson
    • A61K3170
    • C07D473/00C07H13/08C07H15/04C07H19/16
    • The present invention relates to compounds of the class of purin-2-ylcarboxamides, useful as anti-inflammatory agents, having the formula: and pharmaceutically acceptable salts and solvates thereof; wherein R1 is H, C1-C 6 alkyl or C3-C7 cycloalkyl, each optionally substituted by 1 or 2 of hydroxyl, fluorenyl, or optionally substituted phenyl or naphthyl ; A is a bond or C1-C6 alkylene; R2 is (i) H, C1-C6 alkyl, or optionally substituted C3-C7 cycloalkyl, phenyl, or naphthyl; or (ii) when A is C2-C6 alkylene, —NR3R3, —OR3, —COOR3, —OCOR4, —SO2R4, —CN, —SO2NR3R4, —NR3SO2R4, —NR3COR4 or —CONR3R3; or (iii) a C-linked, 4 to 11 membered, mono or bicyclic heterocycle having either from 1 to 4 ring nitrogen atom(s) or 1 or 2 nitrogen and 1 oxygen or 1 sulphur ring atoms, said heterocycle being optionally C-substituted or N-substituted; or (iv) when A is C2-C6 alkylene, optionally substituted N-linked azetidinyl, pyrrolidinyl, morpholinyl, tetrahydroisoquinolinyl, piperidinyl or piperazinyl; R7 is H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl, naphthyl, azetidin-3-yl, pyrrolidin-3-yl, piperidin-3-yl, piperidin-4-yl, or het; and R8 is H or C1-C6 alkyl; and to intermediates used in processes for the preparation of, compositions containing, and uses as adenosine A2a receptor agonists of, compounds of formula (I).
    • 本发明涉及可用作抗炎剂的具有下式的嘌呤-2-基甲酰胺类化合物及其药学上可接受的盐和溶剂合物: 其中R 1是H,C 1 -C 6烷基或C 3 -C 7环烷基,各自任选被1或2个羟基,芴基或任选取代的苯基或萘基取代; A是键或C1-C6亚烷基; R 2是(i)H,C 1 -C 6烷基或任选取代的C 3 -C 7环烷基,苯基或萘基; 或(ii)当A是C 2 -C 6亚烷基,-NR 3 R 3,-OR 3,-COOR 3,-OCOR 4,-SO 2 R 4,-CN,-SO 2 NR 3 R 4,-NR 3 SO 2 R 4,-NR 3 COR 4或-CONR 3 R 3时; 或(iii)具有1至4个环氮原子或1或2个氮和1个氧或1个硫环原子的C连接的4至11元单环或双环杂环,所述杂环任选为C- 取代或N-取代的; 或(iv)当A为C 2 -C 6亚烷基时,任选取代的N-连接的氮杂环丁烷基,吡咯烷基,吗啉基,四氢异喹啉基,哌啶基或哌嗪基; R 7是H,C 1 -C 6烷基,C 3 -C 7环烷基,苯基,萘基,氮杂环丁烷-3-基,吡咯烷-3-基,哌啶-3-基,哌啶-4-基或咔唑; 且R 8为H或C 1 -C 6烷基; 以及用于制备含有和用作式(I)化合物的腺苷A2a受体激动剂的组合物的方法中使用的中间体。