Pyrazolo (3, 4-B) pyridine derivatives as phosphodiesterase inhibitors
    1.
    发明授权
    Pyrazolo (3, 4-B) pyridine derivatives as phosphodiesterase inhibitors 有权
    吡唑并(3,4-B)吡啶衍生物作为磷酸二酯酶抑制剂

    公开(公告)号:US08420666B2

    公开(公告)日:2013-04-16

    申请号:US12531043

    申请日:2008-03-14

    CPC分类号: C07D471/04 C07D519/00

    摘要: The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4/PDE type 7 inhibitors are provided.

    摘要翻译: 本发明涉及磷酸二酯酶(PDE)4型,磷酸二酯酶(PDE)7型和双重PDE型4 / PDE型7型抑制剂。 本文公开的具有式1结构的化合物可用于治疗,预防,抑制或抑制CNS疾病,例如多发性硬化; 各种病理状况如影响免疫系统的疾病,包括艾滋病,移植排斥反应,自身免疫性疾病如T细胞相关疾病,例如类风湿性关节炎; 炎性疾病如呼吸道炎症疾病,包括慢性阻塞性肺疾病(COPD),哮喘,支气管炎,过敏性鼻炎,成人呼吸窘迫综合征(ARDS)和其他炎性疾病,包括但不限于银屑病,休克,特应性皮炎,嗜酸性肉芽肿,过敏性 结膜炎,骨关节炎; 胃肠道炎症性疾病如克罗恩病,结肠炎,胰腺炎以及不同类型的癌症,包括白血病; 特别是在人类。 提供了制备所公开的化合物的方法,含有所公开的化合物的药物组合物及其作为PDE 4型,PDE型7和双重PDE型4 / PDE 7型抑制剂的用途。

    PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
    5.
    发明申请
    PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS 审中-公开
    吡咯并[3,4-B]吡啶衍生物作为磷酸二酯酶抑制剂

    公开(公告)号:US20110130403A1

    公开(公告)日:2011-06-02

    申请号:US12531045

    申请日:2008-03-13

    CPC分类号: C07D471/04

    摘要: The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed hereinf having the structure of Formula I: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE t e 4/PDE t e 7 inhibitors are rovided.

    摘要翻译: 本发明涉及磷酸二酯酶(PDE)4型,磷酸二酯酶(PDE)7型和双重PDE型4 / PDE型7型抑制剂。 本文公开的具有式I结构的化合物可用于治疗,预防,抑制或抑制CNS疾病,例如多发性硬化; 各种病理状况如影响免疫系统的疾病,包括艾滋病,移植排斥反应,自身免疫性疾病如T细胞相关疾病,例如类风湿性关节炎; 炎性疾病如呼吸道炎症疾病,包括慢性阻塞性肺疾病(COPD),哮喘,支气管炎,过敏性鼻炎,成人呼吸窘迫综合征(ARDS)和其他炎性疾病,包括但不限于银屑病,休克,特应性皮炎,嗜酸性肉芽肿,过敏性 结膜炎,骨关节炎; 胃肠道炎症性疾病如克罗恩病,结肠炎,胰腺炎以及不同类型的癌症,包括白血病; 特别是在人类。 制备所公开的化合物的方法,包含所公开的化合物的药物组合物及其作为PDE 4型,PDE型7和双重PDE 4 / PDE 7抑制剂的用途是有争议的。

    PHOSPHODIESTARASE INHIBITORS
    6.
    发明申请
    PHOSPHODIESTARASE INHIBITORS 审中-公开
    磷酸酶抑制剂

    公开(公告)号:US20120004201A1

    公开(公告)日:2012-01-05

    申请号:US13060832

    申请日:2009-09-19

    CPC分类号: C07D471/04 C07D519/00

    摘要: The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4/PDE type 7 inhibitors are provided.

    摘要翻译: 本发明涉及磷酸二酯酶(PDE)4型,磷酸二酯酶(PDE)7型和双重PDE型4 / PDE型7型抑制剂。 本文公开的化合物可用于治疗,预防,抑制或抑制CNS疾病,例如多发性硬化; 各种病理状况如影响免疫系统的疾病,包括艾滋病,移植排斥反应,自身免疫性疾病如T细胞相关疾病,例如类风湿性关节炎; 炎性疾病如呼吸道炎症疾病,包括慢性阻塞性肺疾病(COPD),哮喘,支气管炎,过敏性鼻炎,成人呼吸窘迫综合征(ARDS)和其他炎性疾病,包括但不限于银屑病,休克,特应性皮炎,嗜酸性肉芽肿,过敏性 结膜炎,骨关节炎; 胃肠道炎症性疾病如克罗恩病,结肠炎,胰腺炎以及不同类型的癌症,包括白血病; 特别是在人类。 提供了制备所公开的化合物的方法,含有所公开的化合物的药物组合物及其作为PDE 4型,PDE型7和双重PDE型4 / PDE 7型抑制剂的用途。

    Oxazolidinone piperazinyl derivatives as potential antimicrobials
    7.
    发明授权
    Oxazolidinone piperazinyl derivatives as potential antimicrobials 失效
    恶唑烷酮哌嗪衍生物作为潜在的抗菌药物

    公开(公告)号:US06956040B2

    公开(公告)日:2005-10-18

    申请号:US10051784

    申请日:2002-01-17

    CPC分类号: C07D413/12

    摘要: The present invention relates to certain substituted phenyl piperazinyl oxazolidinones, for example, to those having the structure of Formula I with the variables as defined within, and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

    摘要翻译: 本发明涉及某些取代的苯基哌嗪基恶唑烷酮,例如具有式I结构的具有变量的定义的那些,以及其合成方法。 本发明还涉及含有作为抗微生物剂的本发明化合物的药物组合物。 这些化合物是有用的抗微生物剂,对许多人类和兽医病原体有效,包括革兰氏阳性好氧细菌如多重耐药性葡萄球菌,链球菌和肠球菌以及厌氧生物如细菌属。 和梭菌属(Clostridia spp。) 物种和酸性快速生物如结核分枝杆菌,鸟分枝杆菌和分枝杆菌属。

    Oxazolidinone derivatives as antimicrobials
    8.
    发明申请
    Oxazolidinone derivatives as antimicrobials 审中-公开
    恶唑烷酮衍生物作为抗微生物剂

    公开(公告)号:US20060293307A1

    公开(公告)日:2006-12-28

    申请号:US10523207

    申请日:2002-07-29

    CPC分类号: C07D413/12 C07D413/14

    摘要: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

    摘要翻译: 本发明涉及某些取代的苯基恶唑烷酮及其合成方法。 本发明还涉及含有作为抗微生物剂的本发明化合物的药物组合物。 这些化合物是有用的抗微生物剂,对许多人和兽医病原体有效,包括革兰氏阳性好氧细菌如多重耐药性葡萄球菌,链球菌和肠球菌以及厌氧生物如细菌属。 和梭菌属(Clostridia spp。) 物种和酸性快速生物如结核分枝杆菌,鸟分枝杆菌和分枝杆菌属。

    Oxazolidinone derivatives as antimicrobials
    10.
    发明授权
    Oxazolidinone derivatives as antimicrobials 失效
    恶唑烷酮衍生物作为抗微生物剂

    公开(公告)号:US07592335B2

    公开(公告)日:2009-09-22

    申请号:US11911576

    申请日:2006-04-12

    IPC分类号: C07D498/04 A61K31/5383

    CPC分类号: Y02A50/478 Y02P20/55

    摘要: Provided herein are novel substituted phenyl oxazolidinones and to processes for the synthesis thereof. Also provided are pharmaceutical compositions comprising one or more compounds described herein The compounds described can be useful antimicrobial agents, which can be effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci, as well as, anaerobic organisms, such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms, such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

    摘要翻译: 本文提供了新的取代的苯基恶唑烷酮,以及其合成方法。 还提供了包含本文所述的一种或多种化合物的药物组合物。所述化合物可以是有用的抗微生物剂,其可以对许多人和兽医病原体有效,包括革兰氏阳性好氧细菌如多重耐药性葡萄球菌,链球菌和肠球菌 ,以及厌氧生物,如细菌属。 和梭菌属(Clostridia spp。) 物种和酸性快速生物,如结核分枝杆菌,鸟分枝杆菌和分枝杆菌。