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    Nitrogeneous heterocyclic derivative and medicine containing the same as an active ingredient
    1.
    发明公开
    Nitrogeneous heterocyclic derivative and medicine containing the same as an active ingredient 审中-公开
    Stickstoffhaltige hybridlische Derivate und Medizin damit als ein Wirkstoff

    公开(公告)号：EP2546234A1

    公开(公告)日：2013-01-16

    申请号：EP12186689.1

    申请日：2005-09-12

    申请人： ONO PHARMACEUTICAL CO., LTD.

    发明人： Takaoka, Yoshikazu ,  Shibayama, Shiro ,  Nishizawa, Rena

    IPC分类号： C07D211/58 ,  A61K31/444 ,  A61K31/4468 ,  A61K45/00 ,  A61P11/06 ,  A61P29/00 ,  A61P31/04 ,  A61P31/18 ,  A61P37/00 ,  A61P37/06 ,  A61P43/00

    CPC分类号： C07D413/12 ,  A61K31/00 ,  C07D211/58 ,  C07D231/12 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14

    摘要： Compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof:

    (wherein the characters are as defined in the description). The compounds of the general formula (I) have a CCR5 antagonistic activity, so that they are useful in the prevention and/or therapy for CCR5 mediated diseases, for example, various inflammatory diseases (asthma, gastritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis and other inflammatory intestinal failure, etc.), immunologic diseases (autoimmune disease, rejection of transplanted organ (rejection of solid organ transplant graft, rejection of pancreatic islet cell transplant in diabetes, graft-versus-host disease, etc.), immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (human immunodeficiency virus infection, acquired immunodeficiency syndrome, RSV infection, etc.) allergoses (atopic dermatitis, hives, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), cardiovascular risks (arteriosclerosis suppression of ischemic reperfusion injury, etc.), acute respiratory distress syndrome, shock caused by bacterial infection, diabetes, cancer metastasis, etc.

    摘要翻译： 通式（I）的化合物，其盐和N-氧化物及其溶剂合物和前药：（其中字符如说明书中所定义）。 通式（I）的化合物具有CCR5拮抗活性，因此它们可用于预防和/或治疗CCR5介导的疾病，例如各种炎性疾病（哮喘，胃炎，肾病，肝炎，关节炎，类风湿病 关节炎，鼻炎，结膜炎，溃疡性结肠炎和其他炎性肠衰竭等），免疫疾病（自身免疫性疾病，移植器官的排斥反应（实体器官移植移植排斥反应，糖尿病胰岛细胞移植排斥反应，移植物抗宿主 疾病等），感染性疾病（人类免疫缺陷病毒感染，获得性免疫缺陷综合征，RSV感染等）变态反应（特应性皮炎，荨麻疹，过敏性支气管肺曲霉病，过敏嗜酸性肠胃炎， 等等），心血管风险（动脉硬化抑制缺血再灌注损伤等），急性呼吸道分泌物 ess综合征，细菌感染引起的休克，糖尿病，癌转移等

    Spiro-piperidine compounds as chemokine receptor antagonists and medicinal use thereof
    2.
    发明公开
    Spiro-piperidine compounds as chemokine receptor antagonists and medicinal use thereof 审中-公开
    Spiropiperidinderivate als Chemokin Rezeptor Antagonisten und deren medizinische Verwendung

    公开(公告)号：EP2364982A1

    公开(公告)日：2011-09-14

    申请号：EP10013312.3

    申请日：2004-04-16

    申请人： ONO Pharmaceutical Co., Ltd.

    发明人： Nishizawa, Rena ,  Takaoka, Yoshikazu ,  Habashita, Hiromu ,  Kokubo, Masaya ,  Shibayama, Shiro

    IPC分类号： C07D471/10 ,  A61K31/438 ,  A61K31/527 ,  A61K31/5513 ,  A61K45/06 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P9/10 ,  A61P11/00 ,  A61P11/02

    CPC分类号： C07D471/10 ,  A61K31/438

    摘要： The present invention relates to a spiro-piperidine compound represented by formula (I):

    wherein R 1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.

    摘要翻译： 本发明涉及由式（I）表示的螺哌啶化合物：其中R 1表示氢，可具有取代基的脂族烃基或可具有取代基的环状基团; 环A表示可以具有取代基的5-至8-元环基，其盐，其N-氧化物，其季铵盐或其溶剂合物或其前药。 由式（I）表示的化合物具有趋化因子拮抗作用，因此它们可用于预防和/或治疗各种炎性疾病，免疫疾病如自身免疫性疾病或过敏性疾病或HIV感染。