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    Lactone stable formulation of 7-ethyl camptothecin and methods for uses thereof
    26.
    发明授权
    Lactone stable formulation of 7-ethyl camptothecin and methods for uses thereof 失效
    内酯稳定配方的7-乙基喜树碱及其应用方法

    公开(公告)号：US5604233A

    公开(公告)日：1997-02-18

    申请号：US234131

    申请日：1994-04-28

    申请人： Frederick H. Hausheer ,  Kochat Haridas

    发明人： Frederick H. Hausheer ,  Kochat Haridas

    IPC分类号： A61K9/107 ,  A61K9/48 ,  A61K31/47 ,  A61K47/18 ,  A61K47/26 ,  A61K31/44

    CPC分类号： A61K47/26 ,  A61K31/47 ,  A61K47/18 ,  A61K9/0019 ,  A61K9/4858 ,  A61K9/1075

    摘要： 7-ethyl camptothecin (ECPT), an active metabolite of the camptothecin analog CPT-11, is poorly soluble in water. Because of its poor water solubility, ECPT has not been directly administered by parenteral or oral routes in human patients for the purpose of inhibiting the growth of cancer cells. There is also unpredictable interpatient variability in the metabolic production of ECPT from CPT-11 which limits the utility of CPT-11. This invention overcomes these limitations by teaching novel pharmaceutically acceptable lactone stable ECPT formulations for the direct administration of ECPT. The claimed invention also describes novel dosages, schedules, and routes of administration of the lactone stable ECPT formulations to patients with various forms of cancer.

    摘要翻译： 喜树碱喜树碱（ECPT）是喜树碱类似物CPT-11的活性代谢物，难溶于水。 由于其水溶性差，ECPT尚未通过肠胃外或口服途径直接施用于人类患者，目的是抑制癌细胞的生长。 来自CPT-11的ECPT的代谢生成也存在不可预测的患者间变异，这限制了CPT-11的功效。 本发明通过教导用于直接施用ECPT的新型药学上可接受的内酯稳定的ECPT制剂来克服这些限制。 所要求保护的发明还描述了具有各种形式的癌症的患者的内酯稳定的ECPT制剂的新型剂量，时间表和途径。

    METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN
    27.
    发明申请
    METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN 有权
    全氟化合物7-（2'-三甲基甲硅烷基）乙基氨基甲酸酯的总体化学合成方法

    公开(公告)号：US20140135499A1

    公开(公告)日：2014-05-15

    申请号：US13694255

    申请日：2012-11-13

    申请人： Xinghai Chen ,  Frederick H. Hausheer ,  Andrey Malakhov ,  Harry Kochat

    发明人： Xinghai Chen ,  Frederick H. Hausheer ,  Andrey Malakhov ,  Harry Kochat

    IPC分类号： C07F7/10

    CPC分类号： C07F7/10 ,  C07F7/0812

    摘要： The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.

    摘要翻译： 本发明公开并要求用于全合成对映体纯（即99％）7-（2'-三甲基甲硅烷基）乙基喜树碱（BNP1350; Karenitecin; CositECAN））的五（5）种新型高效合成途径。 这些上述合成方案是首先使用高度新颖的直接，非线性和收敛的合成策略来公开7-（2'-三甲基甲硅烷基）乙基喜树碱的总合成，其涉及关键的C7-（三甲基甲硅烷基）乙基侧链 - 带有A对键合物到对映体纯的三环吡啶酮; 而不是通过在全合成的喜树碱母体化合物上结合C7-（三甲基甲硅烷基）乙基侧链作为最终合成步骤的常规方法。 由于利用预先安装的三甲基甲硅烷基乙基侧链所需的官能化的A环，本文报道的目前新的合成方法，通过将期望的官能化硝基或被保护的取代基取代了较宽范围的药学上相关的A环取代的BNP1350类似物 氨基苯基羧基A环作为起始原料。

    Compositions and methods of use of compounds to increase cancer patient survival time
    29.
    发明申请
    Compositions and methods of use of compounds to increase cancer patient survival time 有权
    使用化合物增加癌症患者生存时间的组合物和方法

    公开(公告)号：US20090232827A1

    公开(公告)日：2009-09-17

    申请号：US12218470

    申请日：2008-07-15

    申请人： Frederick H. Hausheer

    发明人： Frederick H. Hausheer

    IPC分类号： A61K39/395 ,  A61K31/105 ,  A61K31/095 ,  A61K31/505 ,  A61K31/7064 ,  A61K31/7076 ,  A61K31/337 ,  A61K31/282 ,  C12Q1/02 ,  A61P35/00 ,  C12Q1/68 ,  A61K33/24 ,  A61K31/704 ,  A61K31/437 ,  A61K38/43 ,  A61K38/16 ,  A61K38/02

    CPC分类号： A61K33/24 ,  A61K31/095 ,  A61K31/105 ,  A61K31/282 ,  A61K31/337 ,  A61K31/437 ,  A61K31/505 ,  A61K31/704 ,  A61K31/7064 ,  A61K31/7076 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  G01N33/57407 ,  G01N2333/90212 ,  A61K2300/00

    摘要： The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in time of survival in cancer patients, wherein the cancer either: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer. Further, the present invention discloses and claims novel pharmaceutical compositions, methods, and kits used for the treatment of patients with medical conditions and disease where there is the overexpression of thioredoxin and/or glutaredoxin, and wherein this overexpression is associated with deleterious physiological effects in the patients.

    摘要翻译： 本发明公开并要求组合物，治疗方法和试剂盒，其导致癌症患者的存活时间增加，其中所述癌症或者：（i）过表达硫氧还蛋白或谷氧还蛋白和/或（ii）显示硫氧还蛋白或 对一种或多种化学治疗干预的谷氧还蛋白介导的抗性。 本发明还公开并要求用于施用所述组合物以适当治疗癌症患者的方法和试剂盒。 此外，本发明公开并说明了用于定量测定癌症患者癌细胞中硫氧还蛋白或谷氧还蛋白表达水平的方法和试剂盒，在初始诊断和/或规划后续治疗方法中使用确定水平的方法 所述癌症患者以及确定特定癌症的潜在增长“侵略性”和特定类型癌症的治疗反应性。 此外，本发明公开并要求用于治疗患有硫氧还蛋白和/或谷氧还蛋白过表达的医学病症和疾病的患者的新型药物组合物，方法和试剂盒，并且其中所述过表达与有害的生理作用相关 病人。

    Platinum complexes with mononitrile-containing ligands
    30.
    发明授权
    Platinum complexes with mononitrile-containing ligands 失效
    铂配合物与含有单腈的配体

    公开(公告)号：US07569606B2

    公开(公告)日：2009-08-04

    申请号：US11405141

    申请日：2006-04-17

    申请人： Zejun Xiao ,  Frederick H. Hausheer ,  Pavankumar Petluru

    发明人： Zejun Xiao ,  Frederick H. Hausheer ,  Pavankumar Petluru

    IPC分类号： A61K31/28 ,  C07F15/00

    CPC分类号： C07F15/0093

    摘要： Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L1 and L2 )which can be hydrolyzed iii vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.

    摘要翻译： 本文公开了具有与铂共价连接的一个腈取代基（单腈）的新型铂基络合物，能够与DNA或RNA中的碱形成氢键的离子基团（即L1和L2）的一个或多个氮供体配体 ），其可以体内水解成活性物质，其然后可以在鸟嘌呤或腺嘌呤碱基上与DNA或RNA形成配位加合物。 本文还公开了用于合成所述铂络合物的反应方案，以及通过施用药学有效剂量的所述新型铂络合物治疗各种类型的癌症的方法。