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    PHARMACEUTICAL COMPOSITIONS OF SILICON-CONTAINING SUBSTITUTED ADENOSINE NUCLEOSIDE AMIDE ANALOGS
    6.
    发明申请
    PHARMACEUTICAL COMPOSITIONS OF SILICON-CONTAINING SUBSTITUTED ADENOSINE NUCLEOSIDE AMIDE ANALOGS 审中-公开
    含硅取代腺苷核苷酰胺类似物的药物组合物

    公开(公告)号：WO2007019221A3

    公开(公告)日：2007-06-28

    申请号：PCT/US2006030246

    申请日：2006-08-02

    申请人： RND PHARMACEUTICALS INC ,  GATELY STEPHEN

    发明人： GATELY STEPHEN

    IPC分类号： C07H19/00 ,  A01N43/04 ,  A61K31/70 ,  C07H19/167 ,  C07H19/173 ,  C07H19/22

    CPC分类号： C07H19/167 ,  C07H19/173

    摘要： Novel compositions of silicon-containing anti-metabolite compounds, their preparation and use in methods for treating cancer are described. The silyl group confers lipophilicity that can enhance the penetration of the compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The triorganosilyl group provides compounds having improved pharmacokinetics and anti-tumor activity. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

    摘要翻译： 描述了含硅抗代谢物化合物的新型组合物，其制备方法和在治疗癌症的方法中的用途。 甲硅烷基赋予亲脂性，其可以增强化合物穿过肠壁，细胞膜和血脑屏障的渗透，从而改善治疗性质，包括生物利用度，代谢和/或药代动力学。 三有机甲硅烷基提供具有改善的药代动力学和抗肿瘤活性的化合物。 本发明包括新化合物，类似物，前药和药学上可接受的盐，用于治疗涉及癌症等的疾病和其他疾病或病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及用于这些方法的中间体。

    ANTI-MICROBIAL AGENTS AND USES THEREOF
    7.
    发明申请
    ANTI-MICROBIAL AGENTS AND USES THEREOF 审中-公开
    抗微生物剂及其用途

    公开(公告)号：WO2006113615A3

    公开(公告)日：2007-01-11

    申请号：PCT/US2006014394

    申请日：2006-04-14

    申请人： SLOAN KETTERING INST CANCER ,  CORNELL RES FOUNDATION INC ,  TAN DEREK SHIEH ,  QUADRI LUIS E N ,  RYU JAE-SANG ,  CISAR JUSTIN SCOTT ,  FERRERAS JULIAN ALBERTO ,  LU XUEQUAN

    发明人： TAN DEREK SHIEH ,  QUADRI LUIS E N ,  RYU JAE-SANG ,  CISAR JUSTIN SCOTT ,  FERRERAS JULIAN ALBERTO ,  LU XUEQUAN

    IPC分类号： C07H19/00 ,  C07H19/22

    CPC分类号： C07H19/24 ,  C07H19/00 ,  C07H19/22

    摘要： Many pathogens, including Mycobacterium tuberculosis and Yersinia pestis, rely on an iron acquisition system based on siderophores, secreted iron-chelating compounds with extremely high Fe(III) affinity. The compounds of the invention are inhibitors of domain salicylation enzymes, which catalyze the salicylation of an aroyl carrier protein (ArCP) domain to form a salicyl-ArCP domain thioester intermediate via a two-step reaction. The compounds include the intermediate mimic 5 '-O- [N- (salicyl)sulfamoyl] -adenosine (salicyl-AMS) and analogs thereof. These compounds are inhibitors of the salicylate activity of MbtA, YbtE, PchD, and other domain salicylation enzymes involved in the biosynthesis of siderophores. Therefore, these compounds may be used in the treatment of infection caused by microorganisms which rely on siderphore-based iron acquisition systems. Pharmaceutical composition and methods of using these compounds to treat or prevent infection are also provided as well as methods of preparing the inventive compounds.

    摘要翻译： 许多病原体，包括结核分枝杆菌和鼠疫耶尔森氏菌，依赖于铁铁获取系统，其基于铁载体，分泌的铁螯合化合物具有极高的Fe（III）亲和力。 本发明的化合物是结构域水解酶的抑制剂，其催化芳酰基载体蛋白（ArCP）结构域的水杨酸化以通过两步反应形成水杨酰-ArCP结构域的硫酯中间体。 这些化合物包括中间体5'-O- [N-（水杨基）氨磺酰基] - 腺苷（水杨基-AMS）及其类似物。 这些化合物是参与铁载体生物合成的MbtA，YbtE，PchD和其他结构域水杨酸酶的水杨酸盐活性的抑制剂。 因此，这些化合物可用于治疗由依赖于白藜芦醇的铁采集系统的微生物引起的感染。 还提供了使用这些化合物治疗或预防感染的药物组合物和方法以及制备本发明化合物的方法。

    [<18>F]-FURANOSYLPURINE DERIVATIVES AND USES THEREOF
    9.
    发明申请
    [<18>F]-FURANOSYLPURINE DERIVATIVES AND USES THEREOF 审中-公开
    [18 F] - 呋喃并吡啶衍生物及其用途

    公开(公告)号：WO2004096138A3

    公开(公告)日：2005-01-06

    申请号：PCT/US2004012576

    申请日：2004-04-23

    申请人： UNIV SOUTHERN CALIFORNIA ,  CONTI PETER S ,  ALAUDDIN MIAN M ,  FISSEKIS JOHN D

    发明人： CONTI PETER S ,  ALAUDDIN MIAN M ,  FISSEKIS JOHN D

    IPC分类号： A61K20060101 ,  A61K31/355 ,  A61K51/00 ,  C07H19/22

    CPC分类号： A61K51/00 ,  A61K51/0491

    摘要： 2'-Deoxy-2'- [ F] -labeled and 3'-deoxy-3'- [ F] -labeled purine nucleoside analogs such as [ F]-FAA and [ F]­FXA have been found to have desirable properties for use as imaging agents. The analogs are particularly useful for in vivo imaging of biological material including organ tissues (e.g., heart, liver, brain and kidneys) and tumors. Methods for the preparation of the [ F]-FAA and [ F]-FXA are also provided.

    摘要翻译： 2'-脱氧-2'[18 F]标记和3'-脱氧-3'- [18 F]标记的嘌呤核苷类似物如[18 F] -FAA和[18 > F] FXA已被发现具有用作成像剂的期望性质。 类似物对于包括器官组织（例如心脏，肝脏，脑和肾）和肿瘤的生物材料的体内成像特别有用。 还提供了制备[18 F] -FAA和[18 F] -FXA的方法。