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    Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them
    1.
    发明申请
    Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them 审中-公开
    氨基嘧啶化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US20050043315A1

    公开(公告)日：2005-02-24

    申请号：US10498016

    申请日：2002-12-27

    申请人： Hideo Tsutsumi ,  Satoshi Yonishi ,  Atsushi Akahane

    发明人： Hideo Tsutsumi ,  Satoshi Yonishi ,  Atsushi Akahane

    IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D43/02 ,  A61K31/501

    CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D409/14

    摘要： An aminopyrimidine compound of the following formula (I) wherein Q is (a) or (b) in which R and R′ are each optionally substituted aryl or heterocyclic group,R5 is hydrogen, halogen, lower alkyl,optionally substituted hydroxy, optionally substituted amino which may form N-containing heterocyclic group, optionally substituted mercapto, lower alkylsulfinyl or lower alkylsulfonyl, and X is oxygen or sulfur; R1 is hydrogen, optionally substituted lower alkyl or cyclo(lower) alkyl which may be interrupted by an oxygen atom; R2 and R3 are each independently hydrogen, lower alkyl, acyl, aryl or heterocyclic(lower)alkyl, R2 and R3 may be combined together with N atom to which they are attached to form N-containing heterocyclic group; or a salt thereof. The aminopyrimidine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.

    摘要翻译： 其中Q为（a）或（b）的下式（I）的氨基嘧啶化合物，其中R和R'各自为任选取代的芳基或杂环基，R 5为氢，卤素，低级烷基，任选取代的羟基 ，可以形成含氮杂环基的任选取代的氨基，任选取代的巯基，低级烷基亚磺酰基或低级烷基磺酰基，X是氧或硫; R 1是氢，任选取代的可被氧原子间隔的低级烷基或环（低级）烷基; R 2和R 3各自独立地为氢，低级烷基，酰基，芳基或杂环（低级）烷基，R 2和R 3可以与它们所连接的N原子一起形成 含氮杂环基; 或其盐。 本发明的氨基嘧啶化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病， 焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

    Hetero compound
    7.
    发明授权
    Hetero compound 有权
    杂环化合物

    公开(公告)号：US07951825B2

    公开(公告)日：2011-05-31

    申请号：US12696327

    申请日：2010-01-29

    申请人： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    发明人： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    IPC分类号： C07D413/02 ,  C07D413/14 ,  C07D401/02 ,  C07D401/14 ,  A61K31/443

    CPC分类号： C07D413/04 ,  C07D417/04 ,  C07D471/04

    摘要： To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.

    摘要翻译： 为了提供具有优异的S1P1激动剂活性的器官，骨髓或组织，自身免疫疾病等的移植中的预防和/或治疗剂的有效成分的有用化合物。 由于本发明的化合物具有S1P1激动剂活性，因此可用作治疗或预防由不利淋巴细胞浸润引起的疾病的活性成分，例如自体免疫疾病例如器官移植中的移植排斥反应 骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化症，系统性红斑狼疮，肾病综合征，脑炎，重症肌无力，胰腺炎，肝炎，肾炎，糖尿病，肺病，哮喘，特应性皮炎 炎症性肠病，动脉粥样硬化，缺血再灌注损伤或炎性疾病，以及由细胞如癌症和白血病的异常生长或积累引起的疾病。

    Hetero compound
    9.
    发明授权
    Hetero compound 有权
    杂环化合物

    公开(公告)号：US07678820B2

    公开(公告)日：2010-03-16

    申请号：US12244102

    申请日：2008-10-02

    申请人： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    发明人： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

    IPC分类号： A61K31/4245 ,  C07D271/06

    CPC分类号： C07D413/04 ,  C07D417/04 ,  C07D471/04

    摘要： To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity. Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.

    摘要翻译： 为了提供具有优异的S1P1激动剂活性的器官，骨髓或组织，自身免疫疾病等的移植中的预防和/或治疗剂的有效成分的有用化合物。 由于本发明的化合物具有S1P1激动剂活性，因此可用作治疗或预防由不利淋巴细胞浸润引起的疾病的活性成分，例如自体免疫疾病例如器官移植中的移植排斥反应 骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化症，系统性红斑狼疮，肾病综合征，脑炎，重症肌无力，胰腺炎，肝炎，肾炎，糖尿病，肺病，哮喘，特应性皮炎 炎症性肠病，动脉粥样硬化，缺血再灌注损伤或炎性疾病，以及由细胞如癌症和白血病的异常生长或积累引起的疾病。