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    Fused azole-pyrimidine derivatives
    33.
    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。

    PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES MEDIATED BY CRTH2
    34.
    发明申请
    PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES MEDIATED BY CRTH2 有权
    用于治疗由CRTH2介导的疾病的吡咯烷衍生物

    公开(公告)号：US20100322980A1

    公开(公告)日：2010-12-23

    申请号：US12868663

    申请日：2010-08-25

    申请人： Tai-wei Ly ,  Yuji Koriyama ,  Takashi Yoshino ,  Hiroki Sato ,  Kazuho Tanaka ,  Hiromi Sugimoto ,  Yoshihisa Manabe ,  Kevin Bacon ,  Klaus Urbahns ,  Masanori Seki ,  Takuya Shintani

    发明人： Tai-wei Ly ,  Yuji Koriyama ,  Takashi Yoshino ,  Hiroki Sato ,  Kazuho Tanaka ,  Hiromi Sugimoto ,  Yoshihisa Manabe ,  Kevin Bacon ,  Klaus Urbahns ,  Masanori Seki ,  Takuya Shintani

    IPC分类号： A61K9/00 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/506

    CPC分类号： C07D239/42 ,  C07D239/30 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12

    摘要： The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.

    摘要翻译： 本发明涉及式（I）的嘧啶衍生物及其盐，其可用作药物制剂的活性成分。 本发明的嘧啶衍生物具有优异的CRTH2（G蛋白偶联化学引诱物受体，在Th2细胞上表达）拮抗活性，可用于预防和治疗与CRTH2活性相关的疾病，特别是用于治疗过敏性疾病 ，如哮喘，过敏性鼻炎，特应性皮炎和过敏性结膜炎; 嗜酸性粒细胞相关疾病，如中华综合征和鼻窦炎; 嗜碱性粒细胞相关疾病，如嗜碱性白血病，慢性荨麻疹和人类和其他哺乳动物的嗜碱性白细胞增多症; 以T淋巴细胞为特征的炎性疾病和白血球浸润如银屑病，湿疹，炎性肠病，溃疡性结肠炎，克罗恩病，COPD（慢性阻塞性肺病）和关节炎等。

    FUSED AZOLE-PYRIMIDINE DERIVATIVES
    35.
    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。

    Carboxamides derivatives
    39.
    发明申请
    Carboxamides derivatives 审中-公开
    甲酰胺衍生物

    公开(公告)号：US20060135613A1

    公开(公告)日：2006-06-22

    申请号：US10517646

    申请日：2003-06-12

    申请人： Makoto Shimazaki ,  Osamu Sakurai ,  Kanako Hirai ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Satoru Yoshikawa ,  Masaomi Umeda ,  Masaomi Tajimi

    发明人： Makoto Shimazaki ,  Osamu Sakurai ,  Kanako Hirai ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Satoru Yoshikawa ,  Masaomi Umeda ,  Masaomi Tajimi

    IPC分类号： A61K31/198 ,  A61K31/195 ,  C07C237/38

    CPC分类号： C07C235/34

    摘要： The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the diseases are alleviated by treatment with an IP receptor antagonist.

    摘要翻译： 本发明涉及可用作药物制剂活性成分的羧酰胺。 本发明的甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗活性相关的疾病。 这些疾病包括泌尿系统疾病或紊乱，如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱反应过度，前列腺肥大 ），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。 本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压 血友病和出血; 和炎症，因为通过用IP受体拮抗剂治疗来减轻疾病。