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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

    Compound containing basic group and use thereof
    2.
    发明公开
    Compound containing basic group and use thereof 审中-公开
    Verbindung mit基金会Gruppe和Verwendung davon

    公开(公告)号：EP2657235A1

    公开(公告)日：2013-10-30

    申请号：EP13170147.6

    申请日：2006-10-27

    申请人： ONO PHARMACEUTICAL CO., LTD.

    发明人： Kokubo, Masaya ,  Tanaka, Motoyuki ,  Ochiai, Hiroshi ,  Takaoka, Yoshikazu ,  Shibayama, Shiro

    IPC分类号： C07D471/10 ,  A61K31/437 ,  A61K39/21 ,  A61K39/395 ,  A61K45/00 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06

    CPC分类号： A61K31/695 ,  A61K31/4178 ,  A61K31/435 ,  A61K31/5377 ,  A61K45/06 ,  C07D233/64 ,  C07D471/10 ,  C07F7/1844

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

    wherein all symbols are as defined here, a salt thereof or a solvate thereof.
    The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.

    摘要翻译： 本发明涉及由式（I）表示的化合物：其中所有符号如本文所定义，其盐或其溶剂合物。 本发明的化合物对CXCR4具有拮抗作用，因此可用作CXCR4介导的疾病的预防和/或治疗剂，例如炎性和免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，肺纤维化 ，移植器官的排斥等），过敏性疾病，感染（例如人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心血管疾病，代谢疾病和癌性疾病（例如， 癌症，癌症转移等）或再生治疗剂。

    LPA Receptor Antagonists
    3.
    发明公开
    LPA Receptor Antagonists 审中-公开
    LPA-Rezeptorantagonisten

    公开(公告)号：EP2565178A1

    公开(公告)日：2013-03-06

    申请号：EP12007801.9

    申请日：2003-05-28

    申请人： ONO PHARMACEUTICAL CO., LTD.

    发明人： Terakado, Masahiko ,  Nakade, Shinji ,  Seko, Takuya ,  Takaoka, Yoshikazu

    IPC分类号： C07C65/40 ,  C07C235/52 ,  A61K31/192 ,  A61K31/216 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/4402 ,  A61K31/445

    CPC分类号： C07D211/96 ,  C07C217/58 ,  C07C233/22 ,  C07C233/51 ,  C07C233/63 ,  C07C233/73 ,  C07C233/87 ,  C07C235/34 ,  C07C235/48 ,  C07C235/52 ,  C07C2601/08 ,  C07D207/12 ,  C07D207/327 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D209/46 ,  C07D213/65 ,  C07D213/89 ,  C07D217/06 ,  C07D231/12 ,  C07D231/14 ,  C07D235/12 ,  C07D239/91 ,  C07D257/04 ,  C07D277/36 ,  C07D277/56 ,  C07D279/08 ,  C07D307/68 ,  C07D317/68 ,  C07D333/70

    摘要： A compound of the general formula (I):

    (wherein the symbols are as defined in the description), or a non-toxic salt thereof This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention and/or treatment of urinary system disease (symptom with prostatic hypertrophy or neurogenic bladder dysfunction disease, symptom to be caused by spinal cord neoplasm, nucleous hernia, spinal canal stenosis or diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, polyuria), carcinoma-associated disease (solid tumor, solid tumor metastasis, angiofibroma, myeloma, multiple myeloma, Kaposi's sarcoma, leucemia and carcinomatous infiltration transition), proliferative disease (disorder with aberrant angiogenesis, artery obstruction and pulmonary fibrosis), inflammation / immune system disease (psoriasis, nephropathy, hepatitis and pneumonitis symptom), disease caused by secretory dysfunction (Sjogren syndrome), brain-related disease (brain infarction, cerebral apoplexy and brain or peripheral neuropathy) or chronic disease (chronic asthma, glomerulonephritis, obesity, prostate hyperplasia, diseases caused by arteriosclerosis process, rheumatism or atopic dermatitis).

    摘要翻译： 通式（I）的化合物（其中符号如说明书中所定义）或其无毒盐。该化合物参与LPA受体结合和拮抗作用，因此可用于预防和/或治疗 泌尿系统疾病（前列腺肥大或神经源性膀胱功能障碍疾病症状，脊髓肿瘤引起的症状，核疝，椎管狭窄或糖尿病，下尿路闭塞症，下尿路炎症，多尿症），癌症 相关疾病（实体瘤，实体肿瘤转移，血管纤维瘤，骨髓瘤，多发性骨髓瘤，卡波西肉瘤，乳腺癌和癌性浸润转换），增殖性疾病（异常血管生成障碍，动脉阻塞和肺纤维化），炎症/免疫系统疾病（牛皮癣 ，肾病，肝炎和肺炎症状），由分泌功能障碍引起的疾病（干燥综合征），脑相关疾病 （脑梗塞，脑中风和脑或周围神经病变）或慢性疾病（慢性哮喘，肾小球性肾炎，肥胖症，前列腺增生，由动脉硬化过程引起的疾病，风湿病或特应性皮炎）。

    Spiro-piperidine compounds as chemokine receptor antagonists and medicinal use thereof
    4.
    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。

    Triazaspiro[5.5]undecane derivatives and pharmaceutical composition comprising the same as active ingredient
    7.
    发明公开
    Triazaspiro[5.5]undecane derivatives and pharmaceutical composition comprising the same as active ingredient 审中-公开
    Triazaspiro [5.5] undecanderivative und dieses als aktiven Bestandteil enthaltende pharmazeutische Zusammensetzung

    公开(公告)号：EP1619194A2

    公开(公告)日：2006-01-25

    申请号：EP05105154.8

    申请日：2002-03-18

    申请人： ONO PHARMACEUTICAL CO., LTD.

    发明人： Habashita, Hiromu ,  Hamano, Shin-ichi ,  Shibayama, Shiro ,  Takaoka, Yoshikazu

    IPC分类号： C07D471/10 ,  A61K31/503 ,  A61K31/5377 ,  A61P43/00 ,  A61P29/00 ,  A61P37/08 ,  A61P11/06 ,  A61P17/00 ,  A61P17/04 ,  A61P13/12 ,  A61P1/16

    CPC分类号： C07D471/10

    摘要： Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R 1 is formula (II) or formula (III); R 2 is alkyl or alkynyl etc.; R 3 , R 4 is H, (substituted) alkyl etc., or R 3 and R 4 together to form formula (IV); R 5 is H or alkyl).


    Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.

    摘要翻译： 式（I）的三氮杂螺[5.5]十一烷衍生物，其季铵盐，其N-氧化物，其无毒盐或包含它们的药物组合物作为活性成分（其中R 1为式（II）或式 III）; R 2是烷基或炔基等; R 3，R 4是H，（取代的）烷基等，或R 3和R 4一起形成式（IV）; R 5是H或烷基）。 因此，式（I）化合物调节趋化因子/趋化因子受体的作用，它们用于预防和治疗各种炎性疾病，哮喘，特应性皮炎，荨麻疹，过敏性疾病，肾炎，肾病，肝炎，关节炎或类风湿性关节炎 等等