利索-全球专利检索

  1. Login
  2. Sign Up

Search Results

34 records (took 0.015 seconds)

    C10-substituted camptothecin analogs
    1.
    发明授权
    C10-substituted camptothecin analogs 有权
    C10取代的喜树碱类似物

    公开(公告)号：US07687497B2

    公开(公告)日：2010-03-30

    申请号：US11974756

    申请日：2007-10-16

    Applicant: Kesavaram Narkunan ,  Xinghai Chen ,  Harry Kochat ,  Frederick Hausheer

    Inventor： Kesavaram Narkunan ,  Xinghai Chen ,  Harry Kochat ,  Frederick Hausheer

    IPC: A61K31/4375 ,  A61K31/5377 ,  A61P35/00 ,  C07F7/10

    CPC classification number: C07F7/0812 ,  A61K31/4375 ,  A61K31/5377

    Abstract: The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW

    Abstract translation: 本发明的新颖的C10修饰的喜树碱类似物及其药学上可接受的盐：（i）具有有效的抗肿瘤活性（即纳米摩尔或亚纳摩尔浓度），用于在体外抑制人和动物肿瘤细胞的生长; （ii）是拓扑异构酶I的有效抑制; （iii）对MDR / MRP耐药性不敏感; （iv）不需要代谢药物活化：（v）缺乏A环或B环的葡糖醛酸化; （vi）降低与血浆蛋白质的药物结合亲和力; （vii）维持内酯稳定性; （viii）维持药物效力; 和（ix）具有低分子量（例如MW <600）。

    Process for making camptothecin derivatives
    6.
    发明授权
    Process for making camptothecin derivatives 失效
    制造喜树碱衍生物的方法

    公开(公告)号：US07030243B1

    公开(公告)日：2006-04-18

    申请号：US10976109

    申请日：2004-10-28

    Applicant: Ye Wu ,  Kesavaram Narkunan ,  Jianyan Wang ,  Harry Kochat

    Inventor： Ye Wu ,  Kesavaram Narkunan ,  Jianyan Wang ,  Harry Kochat

    IPC: C07D491/22

    CPC classification number: C07D491/22

    Abstract: A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with a silylated heterocyclic compound in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.

    Abstract translation: 合成喜树碱高亲脂性衍生物的方法。 该方法包括在经修饰的Minisci型烷基化反应中使溶解的，未衍生的喜树碱与甲硅烷基化杂环化合物反应，以产生喜树碱的7-取代衍生物。

    Process for synthesizing antifolates
    8.
    发明申请
    Process for synthesizing antifolates 失效
    合成抗叶酸剂的方法

    公开(公告)号：US20050020833A1

    公开(公告)日：2005-01-27

    申请号：US10627483

    申请日：2003-07-25

    Applicant: Ye Wu ,  Harry Kochat

    Inventor： Ye Wu ,  Harry Kochat

    IPC: C07D239/95 ,  C07D487/02

    CPC classification number: C07D239/95 ,  Y02P20/55

    Abstract: A process for synthesizing antifolate compounds is disclosed. The process includes cyclization of a readily available starting reagent, followed by one or more coupling steps to produce compounds that mimic folic acid. The compounds synthesized have commercial use as drugs in oncology, inflammatory disease, and other medical fields.

    Abstract translation: 公开了合成抗叶酸化合物的方法。 该方法包括容易获得的起始试剂的环化，随后进行一个或多个偶联步骤以产生模拟叶酸的化合物。 合成的化合物在肿瘤学，炎性疾病和其他医学领域具有商业用途。

    Process for synthesizing pharmaceutically active disulfide salts
    9.
    发明授权
    Process for synthesizing pharmaceutically active disulfide salts 有权
    合成药学活性二硫键的方法

    公开(公告)号：US06504049B1

    公开(公告)日：2003-01-07

    申请号：US10135756

    申请日：2002-04-30

    Applicant: Harry Kochat

    Inventor： Harry Kochat

    IPC: C07C30905

    CPC classification number: C07C327/22 ,  C07C319/24 ,  C07F9/3808 ,  C07C323/66

    Abstract: A process for synthesizing pharmaceutically active disulfides, particularly Dimesna and certain derivatives thereof. The process includes reacting an alkylene salt with a sulfurating reagent, then alkalizing the intermediate and flowing oxygen through the mixture to produce the final compound in high yield.

    Abstract translation: 合成药学活性二硫化物，特别是Dimesna及其某些衍生物的方法。 该方法包括使亚烷基盐与硫化试剂反应，然后使中间体碱化并将氧气流过混合物以高产率生成最终化合物。

    Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin
    10.
    发明授权
    Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin 有权
    完全化学合成对映体纯7-（2'-三甲基甲硅烷基）乙基喜树碱的方法

    公开(公告)号：US08722886B1

    公开(公告)日：2014-05-13

    申请号：US13694255

    申请日：2012-11-13

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

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

    IPC: C07F7/02 ,  C07D491/147

    CPC classification number: C07F7/10 ,  C07F7/0812

    Abstract: 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.

    Abstract translation: 本发明公开并要求五（5）种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。

Patent Agency Ranking