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1. 发明申请

US20110166343A1 THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY 审中-公开
标题翻译：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）]。

2. 发明授权

US07268128B2 1,3,5-trisubstituted-5-phenyl and 5-pyridyl pyrazolopyrimidinone derivatives having PDE7 inhibiting action 有权
标题翻译：具有PDE7抑制作用的1,3,5-三取代-5-苯基和5-吡啶基吡唑并嘧啶酮衍生物
公开(公告)号：US07268128B2
公开(公告)日：2007-09-11
申请号：US10866198
申请日：2004-06-14
申请人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
发明人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
IPC分类号： A61K31/551 , A61K31/519 , A61K31/541 , A61K31/5355 , C07D243/08 , C07D487/04 , C07D417/12 , C07D413/12
CPC分类号： C07D487/04
摘要： Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, these compounds are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.
摘要翻译：由以下通式（IA）或（IB）表示的吡唑并嘧啶酮衍生物：其中符号如说明书中所公开的，作为所需化合物提供。这些化合物选择性地抑制PDE7，从而增加细胞内cAMP水平并抑制T细胞的活化。因此，这些化合物可用于预防和治疗各种过敏性疾病和炎性或免疫性疾病。

3. 发明申请

US20070270419A1 PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS 失效
标题翻译：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。

4. 发明申请

US20060128728A1 Pyridinylpyrazolopyrimidinone derivatives as pde 7 inhibitors 审中-公开
标题翻译：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。

5. 发明授权

US07943624B2 Pyridinylpyrazolopyrimidinone derivatives as PDE 7 inhibitors 失效
标题翻译：吡啶基吡唑并嘧啶酮衍生物作为PDE 7抑制剂
公开(公告)号：US07943624B2
公开(公告)日：2011-05-17
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： C07D487/04 , A61K31/519 , A61P37/02 , A61P29/00
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。该化合物是下式（IA）或（IB）表示的吡啶基吡唑并嘧啶酮化合物：特别是R 1是环己基或环庚基，R 2是甲基; R3是基团：-NR5R6或-S（O）0-2R8;氢原子; 硝基; 氰基; 卤素原子; 杂芳基; R4为甲氧基或乙氧基。

6. 发明授权

US07932250B2 Thienopyrazole derivative having PDE7 inhibitory activity 有权
标题翻译：具有PDE7抑制活性的噻吩衍生物
公开(公告)号：US07932250B2
公开(公告)日：2011-04-26
申请号：US11630757
申请日：2005-07-01
申请人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
发明人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
IPC分类号： A61K31/5355 , A61K31/496 , A61K31/4436 , A61K31/4162 , C07D413/12 , C07D413/14 , C07D403/12 , C07D491/113 , C07D401/12 , C07D487/04
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）]。

7. 发明授权

US07713972B2 Imidazotriazinone derivatives as PDE 7 (phosphodiesterase 7) inhibitors 失效
标题翻译：咪唑并三嗪酮衍生物作为PDE 7（磷酸二酯酶7）抑制剂
公开(公告)号：US07713972B2
公开(公告)日：2010-05-11
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 , A01N43/64 , A01N43/66 , C07D253/08 , C07D487/00
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 imidazotriazinone 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）表示的咪唑并三氮酮化合物：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。

8. 发明申请

US20090131413A1 Thienopyrazole Derivative Having PDE7 Inhibitory Activity 有权
标题翻译：具有PDE7抑制活性的噻吩衍生物
公开(公告)号：US20090131413A1
公开(公告)日：2009-05-21
申请号：US11630757
申请日：2005-07-01
申请人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
发明人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
IPC分类号： A61K31/4162 , C07D495/04 , A61K31/551 , A61K31/496 , A61K31/454 , C07D231/14 , C07D231/18 , A61K31/4188 , A61K31/4439 , A61K31/5377 , A61K31/438
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）]。

9. 发明申请

US20060128707A1 Imidazotriazinone derivatives as pde 7 (phosphodiesterase 7) inhibitors 失效
标题翻译：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。

10. 发明申请

US20050148604A1 Pyrazolopyrimidinone derivatives having PDE7 inhibiting action 有权
标题翻译：具有PDE7抑制作用的吡唑并嘧啶酮衍生物
公开(公告)号：US20050148604A1
公开(公告)日：2005-07-07
申请号：US10866198
申请日：2004-06-14
申请人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
发明人： Hidekazu Inoue , Hidenobu Murafuji , Yasuhiro Hayashi
IPC分类号： A61P1/04 , A61P1/16 , A61P1/18 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D487/04 , A61K31/519 , C07D487/02
CPC分类号： C07D487/04
摘要： Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): and the following general formula (IA′) or (IB′): where the symbols are as disclosed in the specification, are provided as desired compounds. These compounds have the action of selectively inhibiting PDE7, thereby increasing the intracellular cAMP level and inhibiting the activation of T cells. Thus, they are useful for prevention and treatment of various allergic diseases and inflammatory or immunological diseases.
摘要翻译：由以下通式（IA）或（IB）表示的吡唑并嘧啶酮衍生物：和以下通式（IA'）或（IB'）：符号如说明书中所公开的，作为所需化合物提供。这些化合物具有选择性抑制PDE7的作用，从而增加细胞内cAMP水平并抑制T细胞的活化。因此，它们可用于预防和治疗各种过敏性疾病和炎性或免疫性疾病。

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