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    • 9. 发明申请
    • SUBSTITUTED BENZANILIDES AS MODULATORS OF THE CCR5 RECEPTOR
    • 作为CCR5受体的调节剂的替代苯扎林
    • WO2004010943A2
    • 2004-02-05
    • PCT/US2003/023524
    • 2003-07-28
    • SMITHKLINE BEECHAM CORPORATIONBONDINELL, William, E.NEEB, Michael, J.
    • BONDINELL, William, E.NEEB, Michael, J.
    • A61K
    • C07D413/12C07D207/08C07D211/22C07D211/26C07D211/34C07D211/58C07D211/72C07D401/12
    • 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.
    • 本发明涉及作为CCR5受体的调节剂,激动剂或拮抗剂的取代的苯甲酰苯胺。 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(例如特应性皮炎和过敏),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和炎症性肠病,全部在哺乳动物中,通过使用作为CCR5受体拮抗剂的取代的苯甲酰苯胺。 此外,由于CD8 + T细胞与COPD有牵连,因此CCR5可能在其募集中发挥作用,因此CCR5拮抗剂可为COPD治疗提供潜在的治疗方法。 此外,由于CCR5是HIV进入细胞的共同受体,因此选择性受体调节剂可用于治疗HIV感染。
    • 10. 发明申请
    • SUBSTITUTED HETEROCYCLIC COMPOUNDS AS MODULATORS OF THE CCR5 RECEPTOR
    • 作为CCR5受体的调节剂的取代的杂环化合物
    • WO2004010942A2
    • 2004-02-05
    • PCT/US2003/023523
    • 2003-07-28
    • SMITHKLINE BEECHAM CORPORATIONBONDINELL, William, E.NEEB, Michael, J.
    • BONDINELL, William, E.NEEB, Michael, J.
    • A61K
    • C07D295/215A61K31/435A61K31/495A61K31/497
    • This invention relates to substituted heterocyclic compounds 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, or idiopathic pulmonary fibrosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, treating and/or preventing rejection of transplanted organs, and inflammatory bowel disease, all in mammals, by the use of substituted heterocyclic compounds 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.
    • 本发明涉及作为CCR5受体的调节剂,激动剂或拮抗剂的取代的杂环化合物。 此外,本发明涉及由CCR5介导的疾病状态的治疗和预防,包括但不限于哮喘和特应性疾病(例如特应性皮炎和过敏),类风湿性关节炎,结节病或特发性肺纤维化等 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,治疗和/或预防移植器官的排斥,以及哺乳动物的炎症性肠病,都是使用CCR5受体拮抗剂的取代的杂环化合物。 此外,由于CD8 + T细胞与COPD有牵连,因此CCR5可能在其募集中发挥作用,因此CCR5拮抗剂可为COPD治疗提供潜在的治疗方法。 此外,由于CCR5是HIV进入细胞的共同受体,因此选择性受体调节剂可用于治疗HIV感染。