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    1-aryl-1,8-naphthylidin-4-one derivative as type IV phosphodiesterase inhibitor
    1.
    发明授权
    1-aryl-1,8-naphthylidin-4-one derivative as type IV phosphodiesterase inhibitor 失效
    1-芳基-1,8-二氮杂萘-4-酮衍生物作为IV型磷酸二酯酶抑制剂

    公开(公告)号：US06297248B1

    公开(公告)日：2001-10-02

    申请号：US09284019

    申请日：1999-04-06

    申请人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

    发明人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

    IPC分类号： A61K314375

    CPC分类号： C07D471/04

    摘要： A 1-aryl-1,8-naphthylidin-4-one derivative having the formula (I): wherein R1 indicates a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group, R2, R3, and R4 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a halogen atom, X indicates a group NR5R6 or a group OR7, wherein R5 and R6 independently indicate a hydrogen a atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, and R7 indicates a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group or a salt or solvate thereof and a type IV phosphodiesterase inhibitor containing the same as an effective component.

    摘要翻译： 具有式（I）的1-芳基-1,8-二氮杂萘-4-酮衍生物：其中R 1表示取代或未取代的芳基或取代或未取代的杂芳基，R 2，R 3和R 4独立地表示氢原子 取代或未取代的低级烷基或卤素原子，X表示基团NR5R6或基团OR7，其中R5和R6独立地表示氢原子，取代或未取代的低级烷基，取代或未取代的环烷基， 取代或未取代的芳基或取代或未取代的杂芳基，R7表示氢原子，取代或未取代的低级烷基或取代或未取代的环烷基或其盐或溶剂化物，以及含有 与有效成分相同。

    1-aryl-1,8-naphthylidin-4-one derivative as type IV phosphodiesterase inhibitor
    2.
    发明授权
    1-aryl-1,8-naphthylidin-4-one derivative as type IV phosphodiesterase inhibitor 失效
    1-芳基-1,8-二氮杂萘-4-酮衍生物作为IV型磷酸二酯酶抑制剂

    公开(公告)号：US06541480B2

    公开(公告)日：2003-04-01

    申请号：US09907741

    申请日：2001-07-19

    申请人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

    发明人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

    IPC分类号： A61K314375

    CPC分类号： C07D471/04

    摘要： A 1-aryl-1,8-naphthylidin-4-one derivative having the formula (I): wherein R1 indicates a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group, R2, R3, and R4 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a halogen atom, X indicates a group NR5R6 or a group OR7, wherein R5 and R6 independently indicate a hydrogen a atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, and R7 indicates a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group or a salt or solvate thereof and a type IV phosphodiesterase inhibitor containing the same as an effective component.

    摘要翻译： 具有式（I）的1-芳基-1,8-二氮杂萘-4-酮衍生物：其中R 1表示取代或未取代的芳基或取代或未取代的杂芳基，R 2，R 3和R 4独立地表示氢原子 取代或未取代的低级烷基或卤素原子，X表示基团NR5R6或基团OR7，其中R5和R6独立地表示氢原子，取代或未取代的低级烷基，取代或未取代的环烷基， 取代或未取代的芳基或取代或未取代的杂芳基，R7表示氢原子，取代或未取代的低级烷基或取代或未取代的环烷基或其盐或溶剂化物，以及含有 与有效成分相同。

    1-cycloalkyl-1,8-naphthyridin-4-one derivative as type IV phosphodiesterase inhibitor
    3.
    发明授权
    1-cycloalkyl-1,8-naphthyridin-4-one derivative as type IV phosphodiesterase inhibitor 失效
    1-环烷基-1,8-萘啶-4-酮衍生物作为IV型磷酸二酯酶抑制剂

    公开(公告)号：US06331548B1

    公开(公告)日：2001-12-18

    申请号：US09402142

    申请日：1999-09-29

    申请人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

    发明人： Tetsuo Shimamoto ,  Hidekazu Inoue ,  Yasuhiro Hayashi

    IPC分类号： A61K31435

    CPC分类号： C07D471/04

    摘要： A 1-cycloalkyl-1,8-naphthylidin-4-one derivative having the formula (I): wherein R1 indicates a substituted or unsubstituted cycloalkyl group or a substituted or unsubstituted heterocycloalkyl group, R2, R3, and R4 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a halogen atom, X indicates a group NR5R6 or a group OR7, wherein R5 and R6 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, and R7 indicates a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group or a pharmaceutically acceptable salt or solvate thereof and a type IV phosphodiesterase inhibitor containing the same as an effective component.

    摘要翻译： 具有式（I）的1-环烷基-1,8-二氮杂萘-4-酮衍生物：其中R1表示取代或未取代的环烷基或取代或未取代的杂环烷基，R2，R3和R4独立地表示氢原子 取代或未取代的低级烷基或卤素原子，X表示基团NR5R6或基团OR7，其中R5和R6独立地表示氢原子，取代或未取代的低级烷基，取代或未取代的环烷基， 取代或未取代的芳基或取代或未取代的杂芳基，R7表示氢原子，取代或未取代的低级烷基或取代或未取代的环烷基或其药学上可接受的盐或溶剂合物和IV型磷酸二酯酶抑制剂 含有相同的有效成分。

    PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS
    4.
    发明申请
    PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS 失效
    作为PDE 7抑制剂的吡啶基二吡咯并吡啶酮衍生物

    公开(公告)号：US20070270419A1

    公开(公告)日：2007-11-22

    申请号：US11748421

    申请日：2007-05-14

    申请人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    发明人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    IPC分类号： A61K31/519 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/00 ,  A61P11/00 ,  A61P9/00 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolo-pyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl or cycloheptyl group, R2 is methyl; R3 is a group: —NR5R6 or —S(O)0-2R8;hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R4 is methoxy or ethoxy group.

    摘要翻译： 选择性地提供抑制PDE 7的化合物，从而提高细胞cAMP水平。 因此，该化合物可用于治疗各种疾病如过敏性疾病，炎性疾病或免疫疾病。 该化合物是由下式（IA）或（IB）表示的吡啶基吡唑并嘧啶酮化合物：特别地，R 1是环己基或环庚基，R 2是甲基; R 3是一个基团：-NR 5 R 6或-S（O）0-2 R 10， SUP> 8;氢原子; 硝基; 氰基; 卤素原子; 杂芳基; R 4是甲氧基或乙氧基。

    Pyridinylpyrazolopyrimidinone derivatives as pde 7 inhibitors
    5.
    发明申请
    Pyridinylpyrazolopyrimidinone derivatives as pde 7 inhibitors 审中-公开
    吡啶基吡唑并嘧啶酮衍生物作为pde 7抑制剂

    公开(公告)号：US20060128728A1

    公开(公告)日：2006-06-15

    申请号：US10560386

    申请日：2004-06-11

    申请人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    发明人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolopyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl or cycloheptyl group, R2 is methyl; R3 is a group: —NR5R6 or —S(O)0-2R8; hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R4 is methoxy or ethoxy group.

    摘要翻译： 选择性地提供抑制PDE 7的化合物，从而提高细胞cAMP水平。 因此，该化合物可用于治疗各种疾病如过敏性疾病，炎性疾病或免疫疾病。 化合物是由下式（IA）或（IB）表示的吡啶基吡唑并嘧啶酮化合物：特别地，R 1是环己基或环庚基，R 2是甲基; R 3是一个基团：-NR 5 R 6或-S（O）0-2 R 10， SUP> 8 氢原子; 硝基; 氰基; 卤素原子; 杂芳基; R 4是甲氧基或乙氧基。

    THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY
    6.
    发明申请
    THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY 审中-公开
    具有PDE7抑制活性的噻吩衍生物

    公开(公告)号：US20110166343A1

    公开(公告)日：2011-07-07

    申请号：US13047660

    申请日：2011-03-14

    申请人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    发明人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    IPC分类号： C07D403/14 ,  C07D231/20 ,  C07D231/16 ,  C07D231/18 ,  C07D487/04 ,  C07D413/14 ,  C07D401/14 ,  C07D471/10

    CPC分类号： C07D231/18 ,  C07D495/04

    摘要： To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].

    摘要翻译： 提供抑制PDE 7的噻吩并吡唑衍生物，从而提高细胞cAMP水平。 因此，该化合物可用于治疗各种疾病如过敏性疾病，炎性疾病或免疫疾病。 该化合物是由下式（I）表示的噻吩并吡唑化合物：[其中，特别是R 1是环己基，环庚基或四氢吡喃基; R2是甲基; R3是氢原子; 和R 4是基团-CONR 5 R 6（其中R 5和R 6中的任一个是氢原子）]。

    Imidazotriazinone derivatives as pde 7 (phosphodiesterase 7) inhibitors
    9.
    发明申请
    Imidazotriazinone derivatives as pde 7 (phosphodiesterase 7) inhibitors 失效
    咪唑三嗪酮衍生物作为pde 7（磷酸二酯酶7）抑制剂

    公开(公告)号：US20060128707A1

    公开(公告)日：2006-06-15

    申请号：US10560503

    申请日：2004-06-11

    申请人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    发明人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    IPC分类号： A61K31/53 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotirazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.

    摘要翻译： 本发明提供了选择性抑制PDE7的化合物，因此增强细胞cAMP水平。 因此，该化合物可用于治疗各种疾病如过敏性疾病，炎性疾病或免疫疾病。 该化合物是由下式（IA）或（IB）表示的咪唑并嗪酮化合物：特别是R 1是环己基，R 2是甲基; R3是氢原子; 硝基; 氰基; 卤素原子; 杂芳基; 取代或未取代的C 1 -C 6烷基; 取代或未取代的C 2 -C 6烯基; 取代或未取代的饱和或不饱和杂环烷基; 基团：-NR5R6，-C（O）R7，-SO2R7，-OR8，-NR8COR7，-NR8S02R7; A是CR4; 而B是CH。