公开(公告)号：US08476290B2

公开(公告)日：2013-07-02

申请号：US13378799

申请日：2010-06-15

申请人： Koji Yoshida ,  Hiroshi Ochiai ,  Kousuke Tani ,  Shiro Shibayama ,  Miki Kasano

发明人： Koji Yoshida ,  Hiroshi Ochiai ,  Kousuke Tani ,  Shiro Shibayama ,  Miki Kasano

IPC分类号： A61K31/438 ,  C07D471/10

CPC分类号： C07D471/10

摘要： A compound represented by formula (I): a salt thereof, an N-oxide thereof, or a solvate thereof (symbols in the formula are as described in the specification). The compounds of the present invention exhibit very low risk of side effects and also have persistent and strong antagonistic activity against CXCR4, and are therefore useful as pharmaceuticals, for example, as a preventive and/or therapeutic agent for inflammatory and immune diseases, infections (for example, HIV infection), diseases associated with HIV infection (for example, acquired immunodeficiency syndrome (AIDS)), cancer, cancer metastasis, psychoneurotic diseases and cardiovascular diseases (for example, retinopathy), metabolic diseases, cancerous diseases, or as an agent for regeneration therapy.

摘要翻译： 由式（I）表示的化合物：其盐，其N-氧化物或其溶剂化物（式中的符号如说明书中所述）。 本发明的化合物显示出非常低的副作用风险，并且对CXCR4具有持久和强烈的拮抗活性，因此可用作药物，例如作为炎症和免疫疾病，感染的预防和/或治疗剂（ 例如艾滋病毒感染），与艾滋病毒感染有关的疾病（例如，获得性免疫缺陷综合征（AIDS）），癌症，癌症转移，精神神经病和心血管疾病（例如视网膜病变），代谢疾病，癌性疾病或作为 再生治疗剂。

公开(公告)号：US20120101280A1

公开(公告)日：2012-04-26

申请号：US13378799

申请日：2010-06-15

申请人： Koji Yoshida ,  Hiroshi Ochiai ,  Kousuke Tani ,  Shiro Shibayama ,  Miki Kasano

发明人： Koji Yoshida ,  Hiroshi Ochiai ,  Kousuke Tani ,  Shiro Shibayama ,  Miki Kasano

IPC分类号： C07D471/10

CPC分类号： C07D471/10

摘要： The invention relates to a compound represented by formula (I): a salt thereof, an N-oxide thereof, or a solvate thereof (symbols in the formula are as described in the specification).The compound of the present invention exhibits very low risk of side effects and also has persistent and strong antagonistic activity against CXCR4, and is therefore useful as pharmaceuticals, for example, preventive and/or therapeutic agent for inflammatory and immune diseases, infections (for example, HIV infection), diseases associated with HIV infection (for example, acquired immunodeficiency syndrome (AIDS)), cancer, cancer metastasis, psychoneurotic diseases and cardiovascular diseases (for example, retinopathy), metabolic diseases, cancerous diseases, or an agent for regeneration therapy.

摘要翻译： 本发明涉及由式（I）表示的化合物：其盐，其N-氧化物或其溶剂化物（式中的符号如说明书中所述）。 本发明的化合物显示出非常低的副作用风险，并且对CXCR4具有持久和强烈的拮抗活性，因此可用作药物，例如用于炎症和免疫疾病，感染的预防和/或治疗剂（例如 ，艾滋病毒感染），与艾滋病毒感染有关的疾病（例如，获得性免疫缺陷综合征（AIDS）），癌症，癌症转移，精神神经病和心血管疾病（例如视网膜病变），代谢疾病，癌性疾病或再生药剂 治疗。

公开(公告)号：US20070270429A1

公开(公告)日：2007-11-22

申请号：US10555611

申请日：2004-04-28

申请人： Shiro Shibayama ,  Tetsuya Sugiyama ,  Kenji Sagawa ,  Miki Kasano

发明人： Shiro Shibayama ,  Tetsuya Sugiyama ,  Kenji Sagawa ,  Miki Kasano

IPC分类号： A61K31/498

CPC分类号： C07D471/10 ,  A61K31/499 ,  A61K45/06

摘要： The present invention relates to a function inhibitor of an effector cell comprising a CCR5 antagonist. Since the function inhibitor of an effector cell comprising a CCR5 antagonist inhibits the function of effector cells which play an important role in formation of diseases and the like, it is effective for the prevention and/or treatment of, for example, a transplant rejection (e.g., rejection of a solid organ graft, rejection of islet cell transplantation in diabetes mellitus, graft-versus-host disease (GVHD), etc.), an autoimmune disease (e.g., arthritis, rheumatoid arthritis, multiple sclerosis, ulcerative colitis, etc.), an allergic disease (e.g., asthma, etc.), an ischemic disease (e.g., ischemia-reperfusion injury, etc.), cancer or a metastatic disease or the like.

摘要翻译： 本发明涉及包含CCR5拮抗剂的效应细胞的功能抑制剂。 由于包含CCR5拮抗剂的效应细胞的功能抑制剂抑制在疾病形成等中起重要作用的效应细胞的功能，所以有效预防和/或治疗例如移植排斥反应（ 例如，实体器官移植排斥反应，糖尿病胰岛细胞移植排斥反应，移植物抗宿主病（GVHD）等），自身免疫性疾病（例如关节炎，类风湿性关节炎，多发性硬化症，溃疡性结肠炎等） ），过敏性疾病（例如哮喘等），缺血性疾病（例如缺血再灌注损伤等），癌症或转移性疾病等。