Lactam tachykinin receptor antagonists
    12.
    发明申请
    Lactam tachykinin receptor antagonists 失效
    内酰胺速激肽受体拮抗剂

    公开(公告)号:US20050282886A1

    公开(公告)日:2005-12-22

    申请号:US11135240

    申请日:2005-05-23

    CPC分类号: C07D207/27 C07D207/273

    摘要: The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

    摘要翻译: 本发明涉及可用作神经激肽-1(NK-1)受体拮抗剂,速激肽抑制剂,特别是物质P的某些内酰胺化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病,包括呕吐,尿失禁,抑郁和焦虑。

    Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors
    15.
    发明申请
    Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors 审中-公开
    趋化因子受体的苯并恶嗪基酰胺基环戊基 - 杂环调节剂

    公开(公告)号:US20070238723A1

    公开(公告)日:2007-10-11

    申请号:US10536092

    申请日:2004-10-15

    摘要: Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.

    摘要翻译: 通过使用苯并恶嗪的环氮通过酰胺部分连接到苯并恶嗪基的环戊基化合物,并进一步被杂环部分取代,由式I表示的化合物:其用于调节CCR-2趋化因子受体以预防或治疗炎症 和免疫调节性疾病和疾病,过敏性疾病,特应性病症,包括过敏性鼻炎,皮炎,结膜炎和哮喘,以及自身免疫性病态如类风湿性关节炎和动脉粥样硬化; 和包含这些化合物的药物组合物以及这些化合物和组合物的用途。

    Substituted imidazoles as cannabinoid receptor modulators

    公开(公告)号:US20060089356A1

    公开(公告)日:2006-04-27

    申请号:US11265850

    申请日:2005-11-03

    CPC分类号: C07D405/12 C07D233/90

    摘要: The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.

    Selective s1p1/edg1 receptor agonists
    18.
    发明申请
    Selective s1p1/edg1 receptor agonists 审中-公开
    选择性s1p1 / edg1受体激动剂

    公开(公告)号:US20050070506A1

    公开(公告)日:2005-03-31

    申请号:US10501176

    申请日:2003-01-14

    摘要: The present invention encompasses a method of treating an immunoregulatory abnormality in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said immunoregulatory abnormality, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor, said compound administered in an amount effective for treating said immunoregulatory abnormality. Pharmaceutical compositions are included. The invention also encompasses a method of identifying candidate compounds that are agonists of the S1P1/Edg1 receptor and which possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor. The invention further encompasses a method of treating a respiratory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said respiratory disease or condition, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor.

    摘要翻译: 本发明包括在需要这种治疗的哺乳动物患者中治疗免疫调节异常的方法,包括以有效治疗所述免疫调节异常的量向所述患者施用作为S1P1 / Edg1受体激动剂的化合物,其中所述化合物 对S1P1 / Edg1受体具有S1PR3 / Edg1受体的选择性,所述化合物以有效治疗所述免疫调节异常的量给药。 包括药物组合物。 本发明还包括鉴定作为S1P1 / Edg1受体的激动剂的候选化合物的方法,并且其具有S1P1 / Edg1受体超过S1PR3 / Edg3受体的选择性。 本发明还包括治疗需要这种治疗的哺乳动物患者的呼吸系统疾病或病症的方法,包括向所述患者施用有效治疗所述呼吸系统疾病或病症的S1P1 / Edg1受体激动剂的化合物 其中所述化合物对S1P1 / Edg1受体具有超过S1PR3 / Edg3受体的选择性。

    Tetrahydropyranyl Cyclopentyl Tetrahydropyridopyridine Modulators of Chemokine Receptor Activity
    19.
    发明申请
    Tetrahydropyranyl Cyclopentyl Tetrahydropyridopyridine Modulators of Chemokine Receptor Activity 失效
    四氢吡喃基环戊基四氢吡啶并吡啶调节剂趋化因子受体活性

    公开(公告)号:US20080021061A1

    公开(公告)日:2008-01-24

    申请号:US11587288

    申请日:2005-04-22

    CPC分类号: C07D309/14 C07D405/12

    摘要: Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

    摘要翻译: 式I化合物:其中n,R 1,R 3,R 4,R 5,R 5, R 6,R 7,R 8,R 9,R 10,R 10,R 9, 15,15,Y和Z如本文所定义),其是趋化因子受体活性的调节剂,并且可用于预防或治疗某些炎性和免疫调节性疾病和疾病 过敏性疾病,过敏性疾病,包括过敏性鼻炎,皮炎,结膜炎和哮喘,以及自身免疫性疾病如类风湿性关节炎和动脉粥样硬化。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。