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18 条记录 (耗时 0.037 秒)

    Purine derivatives
    3.
    发明授权
    Purine derivatives 失效
    嘌呤衍生物

    公开(公告)号：US06525032B2

    公开(公告)日：2003-02-25

    申请号：US09789236

    申请日：2001-02-20

    申请人： Simon John Mantell ,  Sandra Marina Monaghan ,  Peter Thomas Stephenson

    发明人： Simon John Mantell ,  Sandra Marina Monaghan ,  Peter Thomas Stephenson

    IPC分类号： A61K3170

    CPC分类号： C07D473/00 ,  C07H13/08 ,  C07H15/04 ,  C07H19/16

    摘要： 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).

    摘要翻译： 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。

    Quinolines and quinazolines useful in therapy
    4.
    发明授权
    Quinolines and quinazolines useful in therapy 失效
    喹啉和喹唑啉可用于治疗

    公开(公告)号：US06417194B1

    公开(公告)日：2002-07-09

    申请号：US09499623

    申请日：2000-02-07

    申请人： David Nathan Abraham Fox ,  Alan John Collis ,  Simon John Mantell

    发明人： David Nathan Abraham Fox ,  Alan John Collis ,  Simon John Mantell

    IPC分类号： A61K3147

    CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D405/14

    摘要： Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally substituted); R4 represents a 4-, 5-, 6- or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.

    摘要翻译： 式I化合物，其中R 1表示任选被一个或多个氟原子取代的C 1-4烷氧基; R 2和R 3独立地表示H或C 1-6烷氧基（其任选被取代）; R 4表示4-，5-，6-或 所述环任选地与苯环或5-或6-元杂环稠合，所述环系统作为整体任选被取代; X表示CH或N; 并且L不存在，或表示式Ia的环状基团，或表示式Ib的链及其药学上可接受的盐; 可用于治疗，特别是治疗良性前列腺增生。

    ISOCYSTENE DERIVATIVES FOR THE TREATMENT OF PAIN
    5.
    发明申请
    ISOCYSTENE DERIVATIVES FOR THE TREATMENT OF PAIN 审中-公开
    用于治疗疼痛的异体衍生物

    公开(公告)号：US20090286875A1

    公开(公告)日：2009-11-19

    申请号：US12093475

    申请日：2006-11-09

    申请人： Simon John Mantell

    发明人： Simon John Mantell

    IPC分类号： A61K31/27 ,  C07C261/00

    CPC分类号： C07C323/58 ,  C07C2601/08 ,  C07C2601/14

    摘要： The present invention relates to compounds of formula (I): wherein R1, R2, R4 and R4a are as defined herein. The invention also relates to the use of compounds of formula (I) for the treatment of pain.

    摘要翻译： 本发明涉及式（I）化合物：其中R1，R2，R4和R4a如本文所定义。 本发明还涉及式（I）化合物用于治疗疼痛的用途。

    Amino Acid Derivatives
    8.
    发明申请
    Amino Acid Derivatives 审中-公开
    氨基酸衍生物

    公开(公告)号：US20090227680A1

    公开(公告)日：2009-09-10

    申请号：US12093503

    申请日：2006-11-06

    申请人： Simon John Mantell

    发明人： Simon John Mantell

    IPC分类号： A61K31/195 ,  C07C62/00

    CPC分类号： C07C229/22

    摘要： The present invention relates to a method of treating pain using a compound of formula (I), wherein Ar, R1, R3 and R3a are as defined herein. The invention also relates to certain novel compounds of formula (I).

    摘要翻译： 本发明涉及使用式（I）化合物治疗疼痛的方法，其中Ar，R 1，R 3和R 3a如本文所定义。 本发明还涉及某些新的式（I）化合物。