Signal transduction inhibitor compounds
    34.
    发明授权
    Signal transduction inhibitor compounds 失效
    信号转导抑制剂化合物

    公开(公告)号:US5705514A

    公开(公告)日:1998-01-06

    申请号:US455825

    申请日:1995-05-31

    摘要: A method of inhibiting the invasion and metastasis of malignant solid tumors in mammals, said method comprising administering to said mammal an anti-proliferative, anti-invasive and anti-metastasis effective amount of a compound selected from the group of formulas consisting of: ##STR1## wherein: p is an integer of from 0 to 4; Ar.sup.1 is a moiety selected from the group consisting of --Ar.sup.2 --X--Ar.sup.3, phenyl, trioxaadamantyl, anthracenyl, anthraquinonyl, naphthyl, phenanthryl, and substituted versions thereof; Ar.sup.2 and Ar.sup.3 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, and substituted versions thereof; X is a linking moiety selected from the group consisting of O, S, SO.sub.2 2, CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; and Z is a nitrogen-containing heterocyclic moiety selected from the group consisting of imidazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl and substituted versions thereof, said heterocyclic moieties being attached to the --(CH.sub.2).sub.p -- portion of the molecule at the N1 position of the heterocycle.

    摘要翻译: 一种抑制哺乳动物恶性实体瘤侵袭和转移的方法,所述方法包括对所述哺乳动物施用抗增殖,抗侵袭和抗转移的有效量的选自下组的化合物:Z( CH 2)pAr 1(I)和(II)其中:p是0至4的整数; Ar1是选自-Ar2-X-Ar3,苯基,三氧杂金刚烷基,蒽基,蒽醌基,萘基,菲基及其取代形式的部分; Ar 2和Ar 3各自独立地选自苯基,萘基及其取代形式的芳族部分; X是选自O,S,SO22,CO,CHCN,直链烷基,烷氧基和烷氧基烷基的连接部分; 并且Z是选自咪唑基,1,2,3-三唑基,1,2,4-三唑基及其取代形式的含氮杂环部分,所述杂环部分连接到 - (CH 2)p - 分子在杂环的N1位的部分。

    Method for inhibiting metalloproteinase expression
    35.
    发明授权
    Method for inhibiting metalloproteinase expression 失效
    抑制金属蛋白酶表达的方法

    公开(公告)号:US5602156A

    公开(公告)日:1997-02-11

    申请号:US209089

    申请日:1994-03-10

    IPC分类号: A61K31/41 A61K31/415

    CPC分类号: A61K31/415 A61K31/41

    摘要: Calcium homeostasis is an important regulator of MMP-2 transcription, activation and activity. Disclosed herein are compounds which inhibit the expression of matrix metalloproteinases in cells. Pharmaceutical application of these compounds to inhibit the expression of MMPs offers a new approach to cancer treatment as well as treatment for nerve healing, degenerative cartilagenous diseases, decubitus ulcers, arthritis, Alzheimer's disease, wound healing, proliferative retinopathy, proliferative renal diseases, corneal ulcers and fertility problems.

    摘要翻译: 钙稳态是MMP-2转录,激活和活性的重要调节因子。 本文公开了抑制细胞中基质金属蛋白酶表达的化合物。 这些化合物抑制MMP表达的药物应用提供了一种新的治疗方法,以及治疗神经愈合,退行性软骨疾病,褥疮性溃疡,关节炎,阿尔茨海默氏病,伤口愈合,增殖性视网膜病变,增殖性肾病,角膜溃疡 和生育问题。

    Method for Predicting Response to Tamoxifen
    40.
    发明申请
    Method for Predicting Response to Tamoxifen 审中-公开
    对他莫昔芬反应的预测方法

    公开(公告)号:US20100317740A1

    公开(公告)日:2010-12-16

    申请号:US12669833

    申请日:2008-07-28

    CPC分类号: G01N33/57415 G01N2800/52

    摘要: This invention relates, e.g., to a method for predicting the response of a subject having, or at risk of developing, breast cancer to Tamoxifen therapy. The method comprises measuring the amount of phosphorylation at residues S70 of Bcl-2, Y992 of EGFR, and/or Y527 of Src in a suitable sample from the subject, wherein a statistically significantly elevated level of phosphorylation at one or more of the three residues compared to a baseline value indicates that the subject is likely to be responsive to Tamoxifen therapy.

    摘要翻译: 本发明涉及例如用于预测具有或有发展为乳腺癌患有他莫昔芬治疗的风险的受试者的反应的方法。 该方法包括在来自受试者的合适样品中测量在Bcl-2,Y992的EGFR和/或Src的残基S70处的磷酸化量,其中三个残基中的一个或多个的统计学上显着升高的磷酸化水平 与基线值相比表明受试者可能对他莫昔芬治疗有反应。