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    • 1. 发明申请
    • Antagonist and agonist which bind to a strong binding site of chemokine receptor
    • 拮抗剂和激动剂,其结合趋化因子受体的强结合位点
    • US20060251651A1
    • 2006-11-09
    • US10538364
    • 2003-12-12
    • Shiro ShibayamaKenji SagawaNoriki WatanabeKazuhiko TakedaHideaki TadaDaikichi Fukushima
    • Shiro ShibayamaKenji SagawaNoriki WatanabeKazuhiko TakedaHideaki TadaDaikichi Fukushima
    • A61K39/395G01N33/567C07K16/28
    • A61K31/49A61K31/00A61K31/503A61K31/5377G01N2333/715G01N2500/04
    • An antagonist or an agonist which binds to a strong binding site of CCR5; a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the same; a method for screening a compound which binds to a strong binding site of CCR5; a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the antagonist or the agonist selected by the screening method; an antagonist or an agonist which binds to a strong binding site of a chemokine receptor; a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the same; a method for screening a compound which binds to a strong binding site of a chemokine receptor; and a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer which comprises the antagonist or the agonist selected by the screening method. The antagonist or the agonist of the present invention is useful as a preventive and/or therapeutic agent for an allergic disease, an inflammatory disease, an immune disease and/or a cancer.
    • 结合CCR5的强结合位点的拮抗剂或激动剂; 用于过敏性疾病,炎性疾病,免疫疾病和/或包含该疾病的癌症的预防和/或治疗剂; 用于筛选结合CCR5的强结合位点的化合物的方法; 包含通过筛选方法选择的拮抗剂或激动剂的过敏性疾病,炎性疾病,免疫疾病和/或癌症的预防和/或治疗剂; 结合趋化因子受体的强结合位点的拮抗剂或激动剂; 用于过敏性疾病,炎性疾病,免疫疾病和/或包含该疾病的癌症的预防和/或治疗剂; 用于筛选结合趋化因子受体的强结合位点的化合物的方法; 以及包含通过筛选方法选择的拮抗剂或激动剂的过敏性疾病,炎性疾病,免疫疾病和/或癌症的预防和/或治疗剂。 本发明的拮抗剂或激动剂可用作过敏性疾病,炎性疾病,免疫疾病和/或癌症的预防和/或治疗剂。
    • 3. 发明授权
    • Chemokine receptor antagonist and medical use thereof
    • 趋化因子受体拮抗剂及其医疗用途
    • US07732442B2
    • 2010-06-08
    • US10570813
    • 2004-09-03
    • Hiromu HabashitaHiroshi OchiaiNatsuko TokudaShiro ShibayamaNoriki WatanabeTakaki KomiyaKazuhiko Takeda
    • Hiromu HabashitaHiroshi OchiaiNatsuko TokudaShiro ShibayamaNoriki WatanabeTakaki KomiyaKazuhiko Takeda
    • A61K31/538
    • C07D213/82C07D213/76C07D241/22C07D241/44C07D401/12C07D403/12C07D417/12
    • The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.
    • 本发明涉及由式(I)表示的化合物,其盐,其N-氧化物,其溶剂合物或前体药物及其医疗用途(式中的符号如说明书中所述)。 由式(I)表示的化合物具有趋化因子受体(特别是CCR4和/或CCR5)拮抗活性。 因此,可用于预防和/或治疗趋化因子受体介导的疾病如炎性和/或过敏性疾病[全身炎症反应综合征(SIRS),过敏反应,过敏反应,过敏性血管炎,移植排斥反应,肝炎,肾炎, 肾病,胰腺炎,鼻炎,关节炎,炎症性眼病,炎性肠病,脑脊液和/或循环系统疾病,呼吸系统疾病,皮肤病,自身免疫性疾病等),感染[病毒性疾病(人类免疫缺陷病毒感染,获得性免疫缺陷 综合征,SARS等)等]等。