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    COMPOUNDS AND METHODS
    1.
    发明公开
    COMPOUNDS AND METHODS 有权
    组合物和方法

    公开(公告)号：EP1140072A1

    公开(公告)日：2001-10-10

    申请号：EP99967619.0

    申请日：1999-12-28

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： BONDINELL, William, E. ,  KU, Thomas, W. ,  WANG, Ning

    IPC分类号： A61K31/41 ,  A61K31/36 ,  A61K31/135

    CPC分类号： A61K31/167

    摘要： This invention relates to substituted benzanilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

    COMPOUNDS AND METHODS
    2.
    发明授权
    COMPOUNDS AND METHODS 有权
    化合物和方法

    公开(公告)号：EP1140072B1

    公开(公告)日：2004-04-14

    申请号：EP99967619.0

    申请日：1999-12-28

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： BONDINELL, William, E. ,  KU, Thomas, W. ,  WANG, Ning

    IPC分类号： A61K31/41 ,  A61K31/36 ,  A61K31/135 ,  A61K31/165

    CPC分类号： A61K31/167

    摘要： This invention relates to substituted benzanilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

    摘要翻译： 本发明涉及取代的苯甲酰苯胺类化合物，它们是CCR5受体的调节剂，激动剂或拮抗剂。 此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和变态反应），类风湿性关节炎，结节病和其他纤维化疾病，动脉粥样硬化， 牛皮癣，自身免疫性疾病如多发性硬化症和炎症性肠病，都是在哺乳动物中，通过使用取代的苯甲酰苯胺类（它们是CCR5受体拮抗剂）。 此外，由于CD8 + T细胞与COPD有关，CCR5可能在其募集中发挥作用，因此CCR5的拮抗剂可为COPD的治疗提供潜在治疗。 而且，因为CCR5是HIV进入细胞的辅助受体，所以选择性受体调节剂可用于治疗HIV感染。