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13 条记录 (耗时 0.033 秒)

    2-aminocarbonyl-9H-purine derivatives
    2.
    发明授权
    2-aminocarbonyl-9H-purine derivatives 失效
    2-氨基羰基-9H-嘌呤衍生物

    公开(公告)号：US06753322B2

    公开(公告)日：2004-06-22

    申请号：US09874007

    申请日：2001-06-05

    申请人： Simon John Mantell ,  Peter Thomas Stephenson

    发明人： Simon John Mantell ,  Peter Thomas Stephenson

    IPC分类号： A61K3170

    CPC分类号： C07H19/16

    摘要： The present invention relates to compounds of the formula: and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.

    摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐和溶剂合物，以及制备用于制备含这些化合物的组合物和用途的中间体的方法。

    Tropane derivatives useful in therapy
    4.
    发明授权
    Tropane derivatives useful in therapy 有权
    托烷衍生物可用于治疗

    公开(公告)号：US07217721B2

    公开(公告)日：2007-05-15

    申请号：US11013634

    申请日：2004-12-15

    申请人： Patricia Ann Basford ,  Peter Thomas Stephenson ,  Stefan Colin John Taylor ,  Anthony Wood

    发明人： Patricia Ann Basford ,  Peter Thomas Stephenson ,  Stefan Colin John Taylor ,  Anthony Wood

    IPC分类号： A61K31/44

    CPC分类号： C07D519/00 ,  C07D401/04

    摘要： The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

    摘要翻译： 本发明提供式（I）化合物，其中X，Y，R 1，R 2和R 3如上所定义。 本发明的化合物是趋化因子CCR5受体活性的调节剂，特别是拮抗剂。 CCR5受体的调节剂可用于治疗各种炎性疾病和病症，以及用于治疗HIV和遗传相关逆转录病毒的感染。

    Triazole antifungal agents
    6.
    发明授权
    Triazole antifungal agents 失效
    三唑抗真菌剂

    公开(公告)号：US06376526B1

    公开(公告)日：2002-04-23

    申请号：US09452492

    申请日：1999-12-01

    申请人： Andrew Simon Bell ,  Peter Thomas Stephenson

    发明人： Andrew Simon Bell ,  Peter Thomas Stephenson

    IPC分类号： A61K314196

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： An antifungal compound of formula (I): or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R1 is phenyl subsituted with 1 to 3 substituents each independently selected from halo and CF3; R2 is (hydroxy)C1-C4 alkyl, CONH2, S(O)m(C1-C4 alkyl), Ar or Het; m is 1 or 2; Ar is phenyl optionally monosubstituted with halo or CF3; and Het is a C-linked 6-membered nitrogen-containing aromatic heterocyclic group containing 1 or 2 nitrogen atoms, or a C- or N-linked 5-membered nitrogen-containing aromatic heterocyclic group containing from 2 to 4 nitrogen atoms, wherein either of said heterocyclic groups is optionally substituted with C1-C4 alkyl or (C1-C4 alkoxy)methyl.

    摘要翻译： 式（I）的抗真菌化合物：或其药学上可接受的盐，或任一实体的药学上可接受的溶剂合物，其中X为CH或N; R1是被1至3个取代基取代的苯基，各自独立地选自卤素和CF 3; R2是（羟基）C1-C4烷基，CONH2，S（O）m（C1-C4烷基），Ar或Het; m为1或2; Ar是任选被卤素或CF 3单取代的苯基; Het是含有1或2个氮原子的C连接的6元含氮芳族杂环基或含有2至4个氮原子的C或N-连接的5元含氮芳族杂环基，其中任一 的所述杂环基任选被C 1 -C 4烷基或（C 1 -C 4烷氧基）甲基取代。

    Tropane derivatives useful in therapy
    7.
    发明授权
    Tropane derivatives useful in therapy 有权
    托烷衍生物可用于治疗

    公开(公告)号：US07579471B2

    公开(公告)日：2009-08-25

    申请号：US11696642

    申请日：2007-04-04

    申请人： Patricia Ann Basford ,  Peter Thomas Stephenson ,  Stefan Colin John Taylor ,  Anthony Wood

    发明人： Patricia Ann Basford ,  Peter Thomas Stephenson ,  Stefan Colin John Taylor ,  Anthony Wood

    IPC分类号： C07D451/04

    CPC分类号： C07D519/00 ,  C07D401/04

    摘要： The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

    摘要翻译： 本发明提供式（I）化合物，其中X，Y，R 1，R 2和R 3如上所定义。 本发明的化合物是趋化因子CCR5受体活性的调节剂，特别是拮抗剂。 CCR5受体的调节剂可用于治疗各种炎性疾病和病症，以及用于治疗HIV和遗传相关逆转录病毒的感染。

    Purine derivatives
    8.
    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。