SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF
    11.
    发明申请
    SPIROPIPERIDINE COMPOUND AND MEDICINAL USE THEREOF 审中-公开
    螺吡啶化合物及其药物用途

    公开(公告)号:US20110052612A1

    公开(公告)日:2011-03-03

    申请号:US11916040

    申请日:2006-05-30

    摘要: The present invention relates to a CXCR3 antagonist comprising a compound represented by formula (I) (wherein all the symbols have the same meaning as defined in the description),a salt thereof, a quaternary ammonium salt thereof, an N-oxide form thereof or a solvate thereof, or a prodrug thereof.This antagonist is useful as a preventive, therapeutic and/or progression-suppressing agent for a CXCR3-mediated disease such as an immune or an allergic disease [e.g., an atopic disease, an autoimmune disease (e.g., multiple sclerosis, rheumatoid arthritis, systemic lupus erythematosus, type I diabetes, glomerulonephritis, Sjogren's syndrome and the like), systemic inflammatory response syndrome (SIRS), a rejection response to transplanted organ, tissue and/or cell or the like], a gastrointestinal disease [e.g., an inflammatory bowel disease or the like], or a respiratory disease [e.g., asthma, a chronic obstructive pulmonary disease or the like].

    摘要翻译: 本发明涉及包含由式(I)表示的化合物(其中所有符号具有与说明书中定义相同的含义)的CXCR3拮抗剂,其盐,其季铵盐,其N-氧化物形式或 其溶剂合物或其前药。 该拮抗剂可用作CXCR3介导的疾病如免疫或过敏性疾病[例如特应性疾病,自身免疫疾病(例如多发性硬化症,类风湿性关节炎,系统性的)的预防,治疗和/或进展抑制剂 红斑狼疮,I型糖尿病,肾小球肾炎,干燥综合征等),全身炎症反应综合征(SIRS),移植器官,组织和/或细胞等的排斥反应],胃肠疾病[例如炎性肠 疾病等]或呼吸系统疾病[例如哮喘,慢性阻塞性肺病等]。

    Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient
    12.
    发明授权
    Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient 失效
    三氮杂螺[5.5]十一烷衍生物和包含与活性成分相同的药物组合物

    公开(公告)号:US07262193B2

    公开(公告)日:2007-08-28

    申请号:US11135272

    申请日:2005-05-24

    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 R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 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〜 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,关节炎或类风湿关节炎 等等

    Heterocyclic compound containing nitrogen atom and use thereof
    13.
    发明申请
    Heterocyclic compound containing nitrogen atom and use thereof 审中-公开
    含氮原子的杂环化合物及其用途

    公开(公告)号:US20070043079A1

    公开(公告)日:2007-02-22

    申请号:US10553704

    申请日:2004-04-16

    摘要: The present invention relates to a medicament comprising the compound of formula (I) wherein all symbols have the same meanings as defined in the specification, a salt thereof or a prodrug thereof. The compound of the present invention is useful for the prevention and/or treatment of immune diseases such as various types of inflammation, autoimmune disease, allergic diseases, etc.; infection concerning inflammation or HIV infections (e.g. asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), organ transplantation rejection, immunosuppression, psoriasis, multiple sclerosis, optic neuritis, polymyalgia rheumatica syndrome, uveitis, vasculitis, human immunodeficiency virus infection (acquired immunodeficiency syndrome etc.), atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, osteoarthritis, ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacteria infection, diabetes, cancer metastasis, atherosclerosis, etc.).

    摘要翻译: 本发明涉及包含式(I)化合物的药物,其中所有符号具有与说明书中定义的相同的含义,其盐或其前药。 本发明的化合物可用于预防和/或治疗各种类型的炎症,自身免疫性疾病,过敏性疾病等免疫疾病; 关于炎症或HIV感染的感染(例如哮喘,肾炎,肾病,肝炎,关节炎,类风湿性关节炎,鼻炎,结膜炎,溃疡性结肠炎等),器官移植排斥反应,免疫抑制,牛皮癣,多发性硬化症,视神经炎,多发性肌痛风湿综合征, 葡萄膜炎,血管炎,人类免疫缺陷综合症等,特应性皮炎,荨麻疹,过敏性支气管肺曲霉病,过敏嗜酸性胃肠炎,骨关节炎,缺血再灌注损伤,急性呼吸窘迫综合征,伴随细菌感染的休克,糖尿病,癌症转移, 动脉粥样硬化等)。

    Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient
    15.
    发明授权
    Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient 失效
    三氮芥[5.5]十一烷衍生物和含有与活性成分相同的药物

    公开(公告)号:US07053090B2

    公开(公告)日:2006-05-30

    申请号:US10472555

    申请日:2002-03-18

    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 R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 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〜 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,关节炎或类风湿关节炎 等等

    Pharmaceutical composition for treatment of disease due to vascular constriction or vasodilation
    17.
    发明申请
    Pharmaceutical composition for treatment of disease due to vascular constriction or vasodilation 失效
    用于治疗由血管收缩或血管舒张引起的疾病的药物组合物

    公开(公告)号:US20060148844A1

    公开(公告)日:2006-07-06

    申请号:US10519113

    申请日:2003-06-25

    IPC分类号: A61K31/4745 C07D471/02

    摘要: A therapeutic and/or preventing agent for a disease due to vascular constriction or vasodilation comprising a EDG-5 modulator. Since EDG-5 modulator specifically binds EDG-5 and shows antagonistic or agonistic action, EDG-5 antagonist is useful for treating and/or preventing for a disease due to vascular constriction, for example, cerebrovascular spasmodic disorder after subarachnoid hemorrhage or stroke, cardiovasucular spasmodic disorder, hypertension, renal disease, cardiac infarction, cardiac angina, arrhythmia, facilitation of the portal blood pressure involved in liver cirrhosis, varicosity involved in liver cirrhosis and the like, or EDG-5 agonist is useful for treating and/or preventing for a disease due to vasodilation of blood vessels, for example, chronic headache (such as migraine, tension-type headache, mixed-type headache thereof, or migrainous neuralgia), haemorrhoid, congestive disorder and the like.

    摘要翻译: 由于包含EDG-5调节剂的血管收缩或血管扩张引起的疾病的治疗和/或预防剂。 由于EDG-5调节剂特异性结合EDG-5并且具有拮抗作用或激动作用,因此EDG-5拮抗剂可用于治疗和/或预防由于血管收缩引起的疾病,例如蛛网膜下腔出血或中风后的脑血管性痉挛障碍,心脏血管 痉挛性疾病,高血压,肾脏疾病,心肌梗死,心脏心绞痛,心律失常,肝硬化引起的门静脉血压便利化,参与肝硬化的静脉曲张等,或EDG-5激动剂可用于治疗和/或预防 由于血管血管扩张引起的疾病,例如慢性头痛(如偏头痛,紧张型头痛,混合型头痛或偏头痛神经痛),痔疮,充血性障碍等。