知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

104 条记录 (耗时 0.034 秒)

    INHIBITION OF CELL PROLIFERATION
    1.
    发明申请
    INHIBITION OF CELL PROLIFERATION 有权
    抑制细胞增殖

    公开(公告)号：US20140221658A1

    公开(公告)日：2014-08-07

    申请号：US14171273

    申请日：2014-02-03

    申请人： University of South Florida

    发明人： Said M. Sebti ,  Srikumar Chellappan ,  Nicholas James Lawrence

    IPC分类号： C07C323/45 ,  C07D213/53 ,  C07D215/12 ,  C07D235/28 ,  C07D277/40 ,  C07D249/12 ,  C07D249/14 ,  C07D233/84 ,  C07D317/58 ,  C07C279/06

    CPC分类号： C07C323/45 ,  C07C279/06 ,  C07C335/32 ,  C07D213/53 ,  C07D215/12 ,  C07D233/30 ,  C07D233/84 ,  C07D235/28 ,  C07D249/12 ,  C07D249/14 ,  C07D277/40 ,  C07D277/42 ,  C07D317/56 ,  C07D317/58

    摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

    摘要翻译： 所公开的Rb：Raf-1相互作用的调节剂是Rb：Raf-1结合的有效的选择性破坏剂，IC 50值范围为80nM至500nM。 此外，这些化合物令人惊奇地有效地抑制多种癌细胞，包括骨肉瘤，上皮性肺癌，非小细胞肺癌，三种不同的胰腺癌细胞系，两种不同的胶质母细胞瘤细胞系，转移性乳腺癌，黑素瘤和 前列腺癌。 此外，所公开的化合物有效地破坏了血管发生，并显着抑制了源自人上皮性肺癌肿瘤的裸鼠中的肿瘤。 因此，提供了所公开的化合物，包含该化合物的药物组合物，抑制细胞增殖的方法，治疗患有癌症的受试者的方法以及制备所公开的化合物的方法。

    Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
    5.
    发明授权
    Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use 失效

    公开(公告)号：US06825185B2

    公开(公告)日：2004-11-30

    申请号：US10730979

    申请日：2003-12-10

    申请人： Subhash P. Khanapure ,  David S. Garvey ,  Richard A. Earl ,  Maiko Ezawa ,  Xinqin Fang ,  Ricky D. Gaston

    发明人： Subhash P. Khanapure ,  David S. Garvey ,  Richard A. Earl ,  Maiko Ezawa ,  Xinqin Fang ,  Ricky D. Gaston

    IPC分类号： A61K3133

    CPC分类号： C07D319/08 ,  A61K45/06 ,  C07D317/56 ,  C07D319/18 ,  C07D319/20 ,  C07D405/06

    摘要： The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

    Sulfated metaaminophenol compounds
    8.
    发明授权
    Sulfated metaaminophenol compounds 失效
    硫酸偏氨基苯酚化合物

    公开(公告)号：US5616809A

    公开(公告)日：1997-04-01

    申请号：US428619

    申请日：1995-04-25

    申请人： Alex Junino ,  Alain Lagrange ,  Alain Genet

    发明人： Alex Junino ,  Alain Lagrange ,  Alain Genet

    IPC分类号： A61K8/00 ,  A61K8/33 ,  A61K8/40 ,  A61K8/41 ,  A61K8/46 ,  A61K8/49 ,  A61Q5/10 ,  C07C323/20 ,  C07C323/36 ,  C07D317/56 ,  C07D317/62 ,  C09B53/00 ,  D06P3/08 ,  C07C215/28

    CPC分类号： A61K8/46 ,  A61Q5/10 ,  C07C323/20 ,  C07C323/36 ,  C07D317/56

    摘要： Sulfated metaaminophenols are disclosed and have the formula ##STR1## where: Z is alkyl, aralkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, aminoalkyl;R.sub.1 is hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, monocarbamylalkyl, dicarbamylalkyl, aminoalkyl, acylaminoalkyl, carbalkoxyalkyl, carbamyl, or monoalkylcarbamyl;R.sub.2 is hydrogen, alkyl, monohydroxyalkyl, alkoxy;and their acid salts.Intermediate products used for their preparation are also disclosed.These sulfated metaaminophenols are used to dye keratinous fibers.

    摘要翻译： 公开了硫酸偏氨基苯酚，并具有式（I）其中：Z是烷基，芳烷基，一羟基烷基，多羟基烷基，芳基，氨基烷基; R1是氢，烷基，单羟基烷基，多羟基烷基，单链烷基烷基，二氨基烷基，氨基烷基，酰基氨基烷基，碳烷氧基烷基，氨基甲酰基或单烷基氨基甲酰基; R2是氢，烷基，单羟基烷基，烷氧基; 和它们的酸盐。 还公开了用于其制备的中间产物。 这些硫酸偏氨基苯酚用于染色角质纤维。