SUBSTITUTED BENZO(1,2-b:5,4-b')DIPYRAN-4-AMINES AS CCR5 MODULATORS
    1.
    发明授权
    SUBSTITUTED BENZO(1,2-b:5,4-b')DIPYRAN-4-AMINES AS CCR5 MODULATORS 有权
    取代的苯并(1,2-B:5,4-B“)dipyran -4-胺作为CCR5调节剂

    公开(公告)号:EP1156801B1

    公开(公告)日:2004-07-07

    申请号:EP00913848.8

    申请日:2000-03-10

    摘要: This invention relates to substituted benzo[1,2-b:5,4-b']dipyran-4-amines 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 benzo[1,2-b:5,4-b']dipyran-4-amines 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
    3.
    发明公开
    COMPOUNDS AND METHODS 失效
    ZUSAMMENSETZUNGEN UND METHODEN

    公开(公告)号:EP1001766A1

    公开(公告)日:2000-05-24

    申请号:EP98934245.6

    申请日:1998-07-01

    摘要: This invention relates to substituted benzanilides which are ligands, 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 ligands may be useful in the treatment of HIV infection.

    摘要翻译: 本发明涉及作为CCR5受体的配体,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,均在哺乳​​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拮抗剂可以为治疗COPD提供潜在的治疗药物。 此外,由于CCR5是HIV进入细胞的共同受体,因此选择性受体配体可用于治疗HIV感染。

    COMPOUNDS FOR THE TREATMENT OF CCR5-MEDIATED DISEASES
    5.
    发明授权
    COMPOUNDS FOR THE TREATMENT OF CCR5-MEDIATED DISEASES 失效
    ZUSAMMENSETZUNGEN ZUR BEHANDLUNG VON DURCH CCR5 MEDIATIERTEN ERKRANKUNGEN

    公开(公告)号:EP1001766B1

    公开(公告)日:2003-04-09

    申请号:EP98934245.6

    申请日:1998-07-01

    摘要: This invention relates to substituted benzanilides which are ligands, 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 ligands may be useful in the treatment of HIV infection.

    摘要翻译: 本发明涉及作为CCR5受体的配体,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,均在哺乳​​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拮抗剂可以为治疗COPD提供潜在的治疗药物。 此外,由于CCR5是HIV进入细胞的共同受体,因此选择性受体配体可用于治疗HIV感染。

    COMPOUNDS AND METHODS
    6.
    发明公开
    COMPOUNDS AND METHODS 有权
    取代的苯并(1,2-B:5,4-B“)dipyran -4-胺作为CCR5调节剂

    公开(公告)号:EP1156801A1

    公开(公告)日:2001-11-28

    申请号:EP00913848.8

    申请日:2000-03-10

    IPC分类号: A61K31/35

    摘要: This invention relates to substituted benzo[1,2-b:5,4-b']dipyran-4-amines 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 benzo[1,2-b:5,4-b']dipyran-4-amines 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.