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    PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
    4.
    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

    申请人： Sonali Rudra ,  Nidhi Gupta ,  Lalit Kumar Baregama ,  Ritu Agarwal ,  Mandadapu Raghuramaiah ,  Vinayak Vasantrao Khairnar ,  Venkata P. Palle ,  Sarala Balachandran ,  Abhijit Ray ,  Sunada G. Dastidar ,  Lalitha Vijaykrishnan

    发明人： Sonali Rudra ,  Nidhi Gupta ,  Lalit Kumar Baregama ,  Ritu Agarwal ,  Mandadapu Raghuramaiah ,  Vinayak Vasantrao Khairnar ,  Venkata P. Palle ,  Sarala Balachandran ,  Abhijit Ray ,  Sunada G. Dastidar ,  Lalitha Vijaykrishnan

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61P29/00 ,  A61P37/06 ,  A61P25/00

    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。

    Pyrazolo (3, 4-B) pyridine derivatives as phosphodiesterase inhibitors
    5.
    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

    申请人： Sonali Rudra ,  Nidhi Gupta ,  Lalit Kumar Baregama ,  Ritu Agarwal ,  Vinayak Vasantrao Khairnar ,  Mandadapu Raghu Ramaiah ,  Venkata P. Palle ,  Sarala Balachandran ,  Atul Kondaskar ,  Manohar Salla ,  Abhijit Ray ,  Sunanda G. Dastidar ,  Lalitha Vijaykrishnan

    发明人： Sonali Rudra ,  Nidhi Gupta ,  Lalit Kumar Baregama ,  Ritu Agarwal ,  Vinayak Vasantrao Khairnar ,  Mandadapu Raghu Ramaiah ,  Venkata P. Palle ,  Sarala Balachandran ,  Atul Kondaskar ,  Manohar Salla ,  Abhijit Ray ,  Sunanda G. Dastidar ,  Lalitha Vijaykrishnan

    IPC分类号： C07D513/02 ,  C07D515/02 ,  A01N43/42 ,  A61K31/44

    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。

    Inhibitors of phosphodiesterase type-IV
    10.
    发明授权
    Inhibitors of phosphodiesterase type-IV 失效
    磷酸二酯酶IV型抑制剂

    公开(公告)号：US07825147B2

    公开(公告)日：2010-11-02

    申请号：US10930569

    申请日：2004-08-30

    申请人： Venkata P. Palle ,  Sarala Balachandran ,  Mohammad Salman ,  Gagan Kukreja ,  Nidhi Gupta ,  Abhijit Ray ,  Sunanda G. Dastidar

    发明人： Venkata P. Palle ,  Sarala Balachandran ,  Mohammad Salman ,  Gagan Kukreja ,  Nidhi Gupta ,  Abhijit Ray ,  Sunanda G. Dastidar

    IPC分类号： A61K31/422 ,  A61K31/341 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/496 ,  C07D261/04 ,  C07D493/10 ,  C07D413/02

    CPC分类号： C07D261/04 ,  C07D498/10

    摘要： The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

    摘要翻译： 本发明涉及异恶唑啉衍生物，其可用作IV型磷酸二酯酶（PDE）的选择性抑制剂。 特别地，本文公开的化合物可用于治疗AIDS，哮喘，关节炎，支气管炎，慢性阻塞性肺病（COPD），牛皮癣，过敏性鼻炎，休克，特应性皮炎，克罗恩病，成人呼吸窘迫综合征（ARDS） 嗜酸粒细胞肉芽肿，过敏性结膜炎，骨关节炎，溃疡性结肠炎和其他炎性疾病，特别是在人类中。 本发明还涉及制备所公开的化合物及其药物组合物及其作为磷酸二酯酶（PDE）IV型抑制剂的用途的方法。