N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
    11.
    发明授权
    N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors 失效
    N-芳基磺酰基氮杂双环衍生物作为有效的细胞粘附抑制剂

    公开(公告)号:US06855708B2

    公开(公告)日:2005-02-15

    申请号:US10096607

    申请日:2002-03-13

    CPC分类号: C07D401/12 C07D487/04

    摘要: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

    摘要翻译: 式I的化合物是VLA-4和/或α4/β7的拮抗剂,因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物,适用于治疗AIDS相关的痴呆,过敏性结膜炎,过敏性鼻炎,阿尔茨海默病,哮喘,动脉粥样硬化,自体骨髓移植,某些类型的毒性和免疫性肾炎, 接触皮肤过敏,包括溃疡性结肠炎和克罗恩病的炎性肠病,炎症性肺病,病毒感染的炎症后遗症,脑膜炎,多发性硬化,多发性骨髓瘤,心肌炎,器官移植,牛皮癣,肺纤维化,再狭窄,视网膜炎,类风湿性关节炎,败血症 关节炎,中风,肿瘤转移,葡萄膜炎和I型糖尿病。

    Heterocycle amides as cell adhesion inhibitors
    14.
    发明授权
    Heterocycle amides as cell adhesion inhibitors 失效
    杂环酰胺作为细胞粘附抑制剂

    公开(公告)号:US06420418B1

    公开(公告)日:2002-07-16

    申请号:US09638074

    申请日:2000-08-14

    IPC分类号: A61K3134

    摘要: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

    摘要翻译: 式I的化合物是VLA-4和/或α4β7的拮抗剂,因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物,适用于治疗AIDS相关的痴呆,过敏性结膜炎,过敏性鼻炎,阿尔茨海默病,哮喘,动脉粥样硬化,自体骨髓移植,某些类型的毒性和免疫性肾炎, 接触皮肤过敏,包括溃疡性结肠炎和克罗恩病的炎性肠病,炎症性肺病,病毒感染的炎症后遗症,脑膜炎,多发性硬化,多发性骨髓瘤,心肌炎,器官移植,牛皮癣,肺纤维化,再狭窄,视网膜炎,类风湿性关节炎,败血症 关节炎,中风,肿瘤转移,葡萄膜炎和I型糖尿病。

    Triaryl substituted imidazoles as glucagon antagonists
    15.
    发明授权
    Triaryl substituted imidazoles as glucagon antagonists 失效
    三芳基取代的咪唑类作为胰高血糖素拮抗剂

    公开(公告)号:US5880139A

    公开(公告)日:1999-03-09

    申请号:US972023

    申请日:1997-11-17

    申请人: Linda L. Chang

    发明人: Linda L. Chang

    IPC分类号: C07D401/04 A61K31/44

    CPC分类号: C07D401/04

    摘要: 2,4-Diaryl-5-pyridylimidazoles are glucagon antagonists. The compounds block the action of glucagon at its receptor. Thus, the compounds can be used in the prophylaxis or treatment of disease states in mammals mediated by elevated levels of glucagon. Examples of such disease states include diabetes, obesity, hypertension, and cachexia and the like.

    摘要翻译: 2,4-二芳基-5-吡啶基咪唑是胰高血糖素拮抗剂。 该化合物阻断胰高血糖素受体的作用。 因此,这些化合物可用于预防或治疗由升高水平的胰高血糖素介导的哺乳动物的疾病状态。 这种疾病状态的实例包括糖尿病,肥胖症,高血压和恶病质等。

    Substituted pyridyl pyrroles, compositions containing such compounds and
methods of use
    16.
    发明授权
    Substituted pyridyl pyrroles, compositions containing such compounds and methods of use 失效
    取代的吡啶基吡咯,含有这些化合物的组合物和使用方法

    公开(公告)号:US5776954A

    公开(公告)日:1998-07-07

    申请号:US742428

    申请日:1996-10-30

    摘要: The present invention addresses substituted pyridyl pyrroles, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists and inhibitors of the biosynthesis and action of TNF-.alpha. and IL1. The compounds block the action of glucagon at its receptors and thereby decrease the levels of plasma glucose. The instant pyrroles are also inhibitors of TNF-.alpha. and IL1 and may be used as antidiabetic agents as well as other cytokine mediated diseases. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production of one or more cytokines occurs. Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) are cytokines produced by a variety of cells, which are involved in immunoregulation and other physiological conditions, such as inflammation.

    摘要翻译: 本发明涉及取代的吡啶基吡咯,以及含有这些化合物的组合物和处理方法。 本发明中的化合物是胰高血糖素拮抗剂和TNF-α和IL1的生物合成和作用的抑制剂。 该化合物阻断胰高血糖素受体的作用,从而降低血浆葡萄糖的水平。 即时吡咯也是TNF-α和IL1的抑制剂,可用作抗糖尿病药物和其他细胞因子介导的疾病。 细胞因子介导的疾病是指发生一种或多种细胞因子的过量或不稳定的产生的疾病或病症。 白细胞介素-1(IL-1)和肿瘤坏死因子(TNF)是由各种细胞产生的细胞因子,其涉及免疫调节和其它生理条件如炎症。