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53 条记录 (耗时 0.071 秒)

    Compositions useful as inhibitors of ERK
    49.
    发明授权
    Compositions useful as inhibitors of ERK 失效
    可用作ERK抑制剂的组合物

    公开(公告)号：US06849267B2

    公开(公告)日：2005-02-01

    申请号：US09971533

    申请日：2001-10-05

    申请人： Guy Bemis ,  Xiaoling Xie

    发明人： Guy Bemis ,  Xiaoling Xie

    IPC分类号： A61K31/4155 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61F2/02 ,  A61F6/06 ,  A61F13/02 ,  A61K9/70 ,  A61L9/04

    CPC分类号： A61K31/501 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53

    摘要： This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp1, Grp2 and Grp3:Grp 1 is an optionally substituted aryl or aliphatic group; Grp 2 is a heteroaromatic ring having one to three nitrogens, said ring comprising a hydrogen bond acceptor HBA2 optionally bonded to a hydrogen bond donor HBD2, and Grp3 is a heteroaromatic ring comprising a hydrogen bond donor HBD1, with distances between the pharmacophoric features defined in the specification. The method is useful for treating cancer, stroke, diabetes, hepatomegaly, cardiovascular disease, Alzheimer's disease, cystic fibrosis, viral disease, autoimmune diseases, atherosclerosis, restenosis, psoriasis, allergic reactions, inflammation, neurological disorders or a hormone-related disease.

    摘要翻译： 本发明提供一种治疗哺乳动物疾病状态的方法，其通过用蛋白激酶抑制剂，特别是ERK抑制剂治疗而减轻，该方法包括给予具有药学特征的化合物Grp1，Grp2和Grp3：Grp1是任选取代的 芳基或脂族基; Grp 2是具有一至三个氮的杂芳环，所述环包含任选地键合到氢键供体HBD2的氢键受体HBA2，Grp3是包含氢键供体HBD1的杂芳环，其中定义的药效特征之间的距离 规格。 该方法可用于治疗癌症，中风，糖尿病，肝肿大，心血管疾病，阿尔茨海默病，囊性纤维化，病毒性疾病，自身免疫性疾病，动脉粥样硬化，再狭窄，牛皮癣，过敏反应，炎症，神经障碍或激素相关疾病。

    Inhibitors of p38
    50.
    发明授权
    Inhibitors of p38 失效
    p38的抑制剂

    公开(公告)号：US06800626B2

    公开(公告)日：2004-10-05

    申请号：US10327020

    申请日：2002-12-20

    申请人： Francesco Salituro ,  Guy Bemis ,  John Cochran

    发明人： Francesco Salituro ,  Guy Bemis ,  John Cochran

    IPC分类号： C07D21716

    CPC分类号： C07D239/96 ,  C07D217/24 ,  C07D239/60 ,  C07D239/80

    摘要： The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: or pharmaceutically acceptable salts thereof, wherein R, R1, Q1, Q2, X, Y, Z, A, and n are as described in the specification. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

    摘要翻译： 本发明涉及p38的抑制剂，其涉及细胞增殖，细胞死亡和对细胞外刺激的反应的哺乳动物蛋白激酶。 本发明涉及具有下式的化合物：或其药学上可接受的盐，其中R，R 1，Q 1，Q 2，X，Y，Z，A和n如说明书中所述。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。