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36 条记录 (耗时 0.036 秒)

    Substituted 2-pyrrolidinone activators of PKC
    26.
    发明授权
    Substituted 2-pyrrolidinone activators of PKC 失效
    PKC的取代的2-吡咯烷酮激活剂

    公开(公告)号：US5962504A

    公开(公告)日：1999-10-05

    申请号：US149609

    申请日：1998-09-08

    申请人： Alan P. Kozikowski ,  Shaomeng Wang ,  Lixin Qiao

    发明人： Alan P. Kozikowski ,  Shaomeng Wang ,  Lixin Qiao

    IPC分类号： A61K31/4015 ,  A61P35/00 ,  A61P43/00 ,  C07D207/26 ,  C07D498/04 ,  A61K31/40

    CPC分类号： C07D207/26

    摘要： Compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.

    摘要翻译： 式I化合物：其中R 1和R 2具有说明书中定义的任何值及其药学上可接受的盐，是PKC激活剂，并且可用于治疗疾病，例如癌症。 还公开了包含式I化合物，式I化合物的方法和可用于制备式I化合物的中间体的药物组合物。

    Bifunctional synthetic molecules
    27.
    发明授权
    Bifunctional synthetic molecules 有权
    双功能合成分子

    公开(公告)号：US08354116B2

    公开(公告)日：2013-01-15

    申请号：US11820172

    申请日：2007-06-18

    申请人： Stephen G. Carter ,  Kanu Patel ,  Zhen Zhu ,  Lixin Qiao

    发明人： Stephen G. Carter ,  Kanu Patel ,  Zhen Zhu ,  Lixin Qiao

    IPC分类号： A61K9/00 ,  A61K8/02

    CPC分类号： C07D213/80 ,  C07C69/612 ,  C07C233/87 ,  C07C2601/14 ,  C07D207/16 ,  C07D217/26 ,  C07D233/06 ,  C07D233/24 ,  C07D233/50 ,  C07D417/04

    摘要： The synthesis and use of bifunctional molecules to improve the topical and transdermal delivery efficiency of various types of therapeutic agents or agents designed to promote the transdermal delivery of those therapeutic agents either into the skin tissue or into the systemic circulation. Three major classes of molecules are covalently joined as bifunctional substances; chemical vasodilators, passive dermal penetration enhancers and therapeutic or diagnostic drugs. Chemical vasodilators may be delivered into the skin to increasing the blood flow in a tissue that has compromised circulation or they may be used as part of a delivery vehicle to promote the delivery of the drug. Passive dermal penetration enhancers are those chemicals that promote the passive penetration of drugs and other chemicals through the stratum corneum and epidermis of the skin tissue. Drugs and diagnostic agents are the third group of chemicals that are candidates for the linkage of molecules.

    摘要翻译： 双功能分子的合成和使用以改善各种类型治疗剂或试剂的局部和透皮递送效率，所述治疗剂或试剂旨在促进将这些治疗剂透皮递送至皮肤组织或进入体循环。 三大类分子共价连接成双功能物质; 化学血管扩张剂，被动皮肤渗透增强剂和治疗或诊断药物。 化学血管扩张剂可以被递送到皮肤中以增加已经损害循环的组织中的血液流动，或者它们可以用作递送载体的一部分以促进药物的递送。 被动皮肤渗透增强剂是促进药物和其他化学物质通过角质层和皮肤组织表皮的被动穿透的化学物质。 药物和诊断剂是作为分子连接的候选物的第三组化学品。

    Inhibitors of phosphatidyl myo-inositol cycle
    28.
    发明授权
    Inhibitors of phosphatidyl myo-inositol cycle 失效
    磷脂酰肌醇周期抑制剂

    公开(公告)号：US06667340B1

    公开(公告)日：2003-12-23

    申请号：US09879765

    申请日：2001-06-12

    申请人： Alan P. Kozikowski ,  Lixin Qiao ,  Garth Powis

    发明人： Alan P. Kozikowski ,  Lixin Qiao ,  Garth Powis

    IPC分类号： A61K31215

    CPC分类号： C07F9/117 ,  C07C69/013 ,  C07C69/96 ,  C07C2601/14 ,  C07F9/4081

    摘要： The present invention relates to the preparation and biological activity of 3-deoxy-Dmyo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor 5 agents which effectively inhibit the growth of mammalian cells.

    摘要翻译： 本发明涉及作为磷脂酰肌醇-3-激酶信号传导和癌细胞生长抑制剂的3-脱氧-Dmyo-inositol醚脂质类似物的制备和生物学活性。 本发明的化合物可用作有效抑制哺乳动物细胞生长的抗肿瘤剂5。

    Inhibiting EPH B-3 Kinase
    30.
    发明申请
    Inhibiting EPH B-3 Kinase 有权
    抑制EPH B-3激酶

    公开(公告)号：US20120238597A1

    公开(公告)日：2012-09-20

    申请号：US13260990

    申请日：2010-03-30

    申请人： Lixin Qiao ,  Marcie Glicksman ,  Thomas Gainer ,  Donald C. Lo ,  Ross L. Stein ,  Sungwoon Choi ,  Gregory D. Cuny

    发明人： Lixin Qiao ,  Marcie Glicksman ,  Thomas Gainer ,  Donald C. Lo ,  Ross L. Stein ,  Sungwoon Choi ,  Gregory D. Cuny

    IPC分类号： A61K31/437 ,  A61P35/02 ,  A61P25/00 ,  C07D471/04 ,  A61P35/00

    CPC分类号： A61K31/437 ,  A61K31/00

    摘要： EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.

    摘要翻译： 包括某些吡唑并[1,5-a]吡啶和咪唑并[1,2-a]吡啶化合物的EphB3激酶抑制剂化合物抑制EphB3激酶。 与一般激酶抑制剂相比，EphB3激酶抑制剂化合物对EphB3激酶的抑制作用可能更大。 还提供了包含EphB3激酶抑制剂化合物的药物组合物，例如神经保护剂。 EphB3激酶抑制剂化合物和药物组合物可用于例如在缺血事件（例如中风）期间损伤的神经元组织的神经保护和/或修复。