公开(公告)号：US20100266539A1

公开(公告)日：2010-10-21

申请号：US12731390

申请日：2010-03-25

申请人： Hiromu HABASHITA ,  Hiroshi Ochiai ,  Natsuko Tokuda ,  Shiro Shibayama ,  Noriki Watanabe ,  Takaki Komiya ,  Kazuhiko Takeda

发明人： Hiromu HABASHITA ,  Hiroshi Ochiai ,  Natsuko Tokuda ,  Shiro Shibayama ,  Noriki Watanabe ,  Takaki Komiya ,  Kazuhiko Takeda

IPC分类号： A61K38/21 ,  C07D213/76 ,  A61K31/44 ,  C07D401/12 ,  A61K31/444 ,  C07D241/22 ,  A61K31/4965 ,  A61K31/497 ,  C07D241/44 ,  A61K31/498 ,  C07D403/12 ,  C07D417/12 ,  A61K31/56 ,  A61K38/22 ,  A61P37/06 ,  A61P37/08 ,  A61P29/00 ,  A61P17/00 ,  A61P11/06 ,  A61K31/557

CPC分类号： C07D213/82 ,  C07D213/76 ,  C07D241/22 ,  C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： 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.

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，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。

公开(公告)号：US20070254886A1

公开(公告)日：2007-11-01

申请号：US10570813

申请日：2004-09-03

申请人： Hiromu Habashita ,  Hiroshi Ochiai ,  Natsuko Tokuda ,  Shiro Shibayama ,  Noriki Watanabe ,  Takaki Komiya ,  Kazuhiko Takeda

发明人： Hiromu Habashita ,  Hiroshi Ochiai ,  Natsuko Tokuda ,  Shiro Shibayama ,  Noriki Watanabe ,  Takaki Komiya ,  Kazuhiko Takeda

IPC分类号： A61K31/4412 ,  A61K31/444 ,  A61K31/4965 ,  A61K31/498 ,  A61P11/06 ,  A61P17/00 ,  A61P31/00 ,  A61P9/00 ,  C07D213/72 ,  C07D241/22 ,  C07D241/44

CPC分类号： C07D213/82 ,  C07D213/76 ,  C07D241/22 ,  C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： 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.

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，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。

公开(公告)号：US20060251651A1

公开(公告)日：2006-11-09

申请号：US10538364

申请日：2003-12-12

申请人： Shiro Shibayama ,  Kenji Sagawa ,  Noriki Watanabe ,  Kazuhiko Takeda ,  Hideaki Tada ,  Daikichi Fukushima

发明人： Shiro Shibayama ,  Kenji Sagawa ,  Noriki Watanabe ,  Kazuhiko Takeda ,  Hideaki Tada ,  Daikichi Fukushima

IPC分类号： A61K39/395 ,  G01N33/567 ,  C07K16/28

CPC分类号： A61K31/49 ,  A61K31/00 ,  A61K31/503 ,  A61K31/5377 ,  G01N2333/715 ,  G01N2500/04

摘要： 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.

摘要翻译： 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。

公开(公告)号：US07732442B2

公开(公告)日：2010-06-08

申请号：US10570813

申请日：2004-09-03

申请人： Hiromu Habashita ,  Hiroshi Ochiai ,  Natsuko Tokuda ,  Shiro Shibayama ,  Noriki Watanabe ,  Takaki Komiya ,  Kazuhiko Takeda

发明人： Hiromu Habashita ,  Hiroshi Ochiai ,  Natsuko Tokuda ,  Shiro Shibayama ,  Noriki Watanabe ,  Takaki Komiya ,  Kazuhiko Takeda

IPC分类号： A61K31/538

CPC分类号： C07D213/82 ,  C07D213/76 ,  C07D241/22 ,  C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： 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.

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，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。