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    FUSED AZOLE-PYRIMIDINE DERIVATIVES
    1.
    发明申请
    FUSED AZOLE-PYRIMIDINE DERIVATIVES 有权
    熔融的偶氮吡啶衍生物

    公开(公告)号：US20090270388A1

    公开(公告)日：2009-10-29

    申请号：US12414257

    申请日：2009-03-30

    申请人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    发明人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/00 ,  A61P3/10 ,  A61P35/00

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

    摘要翻译： 本发明涉及新的稠合唑吡喃衍生物，其制备方法和含有它们的药物制剂。 本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。 更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节 疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。 本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性 学科。

    Fused azole-pyrimidine derivatives
    2.
    发明授权
    Fused azole-pyrimidine derivatives 有权
    熔融唑 - 嘧啶衍生物

    公开(公告)号：US07511041B2

    公开(公告)日：2009-03-31

    申请号：US10527376

    申请日：2003-09-18

    申请人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    发明人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Tsujishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D237/26 ,  C07D237/36 ,  C07D241/36 ,  C07D239/00 ,  C07D471/00 ,  C07D471/04 ,  C07D401/04 ,  C07D401/22 ,  C07D487/00 ,  C07D487/04 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

    摘要翻译： 本发明涉及霍夫唑唑吡啶衍生物，其制备方法和含有它们的药物制剂。 本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。 更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节 疾病，自身免疫性疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。 本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性 学科。

    Fused azole-pyrimidine derivatives
    4.
    发明授权
    Fused azole-pyrimidine derivatives 有权
    熔融唑 - 嘧啶衍生物

    公开(公告)号：US08129386B2

    公开(公告)日：2012-03-06

    申请号：US12414257

    申请日：2009-03-30

    申请人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Jishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    发明人： Mitsuyuki Shimada ,  Toshiki Murata ,  Kinji Fuchikami ,  Hideki Jishita ,  Naoki Omori ,  Issei Kato ,  Mami Miura ,  Klaus Urbahns ,  Florian Gantner ,  Kevin Bacon

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

    CPC分类号： C07D471/14 ,  C07D487/04

    摘要： The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

    摘要翻译： 本发明涉及新型稠合吡唑嘧啶衍生物，其制备方法和含有它们的药物制剂。 本发明的稠合唑类嘧啶衍生物对磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是PI3K-γ抑制作用，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。 更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节 疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。 本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性 学科。