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    C10-SUBSTITUTED CAMPTOTHECIN ANALOGS
    1.
    发明公开
    C10-SUBSTITUTED CAMPTOTHECIN ANALOGS 有权
    C10-取代的喜树碱类似物

    公开(公告)号：EP2197279A1

    公开(公告)日：2010-06-23

    申请号：EP07852779.3

    申请日：2007-10-16

    申请人： BIONUMERIK PHARMACEUTICALS, INC.

    发明人： NARKUNAN, Kesavaram ,  CHEN, Xinghai ,  KOCHAT, Harry ,  HAUSHEER, Frederick

    IPC分类号： A01N43/42 ,  A61K31/44

    CPC分类号： A61K31/44

    摘要： 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

    MONOAZOLE LIGAND PLATINUM ANALOGS
    2.
    发明公开
    MONOAZOLE LIGAND PLATINUM ANALOGS 有权
    单偶氮配体铂类似物

    公开(公告)号：EP1896491A2

    公开(公告)日：2008-03-12

    申请号：EP06719723.6

    申请日：2006-01-26

    申请人： BIONUMERIK PHARMACEUTICALS, INC.

    发明人： XIAO, Zejun ,  KOCHAT, Harry ,  HAUSHEER, Frederick

    IPC分类号： C07F15/00 ,  A61K31/555

    CPC分类号： C07F15/0093

    摘要： Disclosed herein are novel platinum-based analogs with a single substituted azole ligand: RN=NR7, wherein the RN=NR7 functional group is covalently bonded to the platinum through nitrogen of NR7. The analogs also have nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA, and one or more leaving groups which can be displaced by water, hydroxide ions or other nucleophiles, which is thought to form active species in vivo, and then, form cross-linked complexes between nucleic acid strands, principally between purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof. These platinum analogs may also be more easily transported into tumor cells, due to their increased lipophilicity and are likely to be useful as anti¬ neoplastic agents, and in modulating or interfering with the synthesis or replication or transcription of DNA or translation or function of RNA in vitro or in vivo, as they are potentially capable of forming a platinum coordinate complex with an intact or nascent DNA or RNA and thereby interfering with cellular synthesis, transcription or replication of nucleic acid polynucleotides.

    摘要翻译： 本文公开了具有单个取代的吡咯配体的新型铂基类似物：RN = NR7，其中RN = NR7官能团通过NR7的氮共价键合至铂。 类似物还具有能够与DNA或RNA中的碱基形成氢键的氮供体配体和可以被水，氢氧根离子或其他亲核试剂取代的一个或多个离去基团，其被认为在体内形成活性物质，并且 然后在核酸链之间形成交联复合物，主要是在DNA（或RNA）中的嘌呤，即在其鸟嘌呤或腺嘌呤碱基之间。 由于其亲脂性增加，这些铂类似物也可以更容易地转运到肿瘤细胞中，并且可能用作抗肿瘤剂，并且调节或干扰DNA的合成或复制或转录或RNA的翻译或功能 因为它们可能能够与完整或新生的DNA或RNA形成铂配位络合物，从而干扰核酸多核苷酸的细胞合成，转录或复制。

    PROCESS FOR COUPLING AMINO ACIDS TO AN ANTIFOLATE SCAFFOLD
    5.
    发明公开
    PROCESS FOR COUPLING AMINO ACIDS TO AN ANTIFOLATE SCAFFOLD 有权
    用于氨基至叶酸拮抗剂框架离合器

    公开(公告)号：EP1373225A1

    公开(公告)日：2004-01-02

    申请号：EP02763863.4

    申请日：2002-03-22

    申请人： BIONUMERIK PHARMACEUTICALS, INC.

    发明人： KOCHAT, Harry ,  WU, Ye

    IPC分类号： C07D239/84 ,  C07D487/04

    CPC分类号： C07D475/04

    摘要： A synthetic process is disclosed for coupling amino acids to a substrate. The process involves dissolving the amino acid and the scaffold in a non-polar aprotic solvent, and agitating the resulting mixture for a predetermined time. The process is specially suited to the synthesis of antifolate compounds having useful applications in the medical fields of oncology, inflammatory diseases and others.

    METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN
    6.
    发明公开
    METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN 有权
    PROCEDURE总化学合成纯对映体7 - （2” - 三甲基硅烷基）乙基喜树碱

    公开(公告)号：EP2920191A1

    公开(公告)日：2015-09-23

    申请号：EP13855448.0

    申请日：2013-11-07

    申请人： BIONUMERIK PHARMACEUTICALS, INC.

    发明人： CHEN, Xinghai ,  HAUSHEER, Frederick, H. ,  MALAKHOV, Andrey ,  KOCHAT, Harry

    IPC分类号： C07F17/02 ,  C07D471/00 ,  C07D491/00

    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.

    C7-SUBSTITUTED CAMPTOTHECIN ANALOGS
    7.
    发明公开
    C7-SUBSTITUTED CAMPTOTHECIN ANALOGS 有权
    C7-取代喜树碱

    公开(公告)号：EP2197879A1

    公开(公告)日：2010-06-23

    申请号：EP07839601.7

    申请日：2007-10-16

    申请人： BIONUMERIK PHARMACEUTICALS, INC.

    发明人： KOCHAT, Harry ,  HAUSHEER, Frederick ,  CHEN, Xinghai ,  NARKUNAN, Kesavaram

    IPC分类号： C07D471/02 ,  A61K31/695

    CPC分类号： C07F9/6561 ,  A61K31/695 ,  C07F7/0812

    摘要： The novel C7-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

    PROCESS FOR COUPLING AMINO ACIDS TO AN ANTIFOLATE SCAFFOLD
    8.
    发明授权
    PROCESS FOR COUPLING AMINO ACIDS TO AN ANTIFOLATE SCAFFOLD 有权
    用于氨基至叶酸拮抗剂框架离合器

    公开(公告)号：EP1373225B1

    公开(公告)日：2006-05-24

    申请号：EP02763863.4

    申请日：2002-03-22

    申请人： BIONUMERIK PHARMACEUTICALS, INC.

    发明人： KOCHAT, Harry ,  WU, Ye

    IPC分类号： C07D239/84 ,  C07D487/04 ,  C07D475/04

    CPC分类号： C07D475/04

    摘要： A synthetic process is disclosed for coupling amino acids to a substrate. The process involves dissolving the amino acid and the scaffold in a non-polar aprotic solvent, and agitating the resulting mixture for a predetermined time. The process is specially suited to the synthesis of antifolate compounds having useful applications in the medical fields of oncology, inflammatory diseases and others.