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    Germanium-containing camptothecin analogues
    1.
    发明申请
    Germanium-containing camptothecin analogues 审中-公开
    含锗喜树碱类似物

    公开(公告)号：US20140073793A1

    公开(公告)日：2014-03-13

    申请号：US13573294

    申请日：2012-09-07

    申请人： Xinghai Chen ,  Harry Kochat ,  Pavankumar N.V. Petluru ,  Aulma Parker ,  Frederick H. Hausheer

    发明人： Xinghai Chen ,  Harry Kochat ,  Pavankumar N.V. Petluru ,  Aulma Parker ,  Frederick H. Hausheer

    IPC分类号： C07F7/30

    CPC分类号： C07F7/30

    摘要： The present invention discloses: (i) the novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof; (ii) methods of synthesis of said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts; (iii) pharmaceutically-acceptable formulations comprising said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof; and (iv) methods of administration of said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof to subjects in need thereof, including subjects with cancer.

    摘要翻译： 本发明公开：（i）新颖的含锗喜树碱化合物，7 [2'-三甲基甲酰基]乙基-20（S）喜树碱及其药学上可接受的盐; （ii）合成所述新颖的含锗喜树碱化合物的方法，7 [2'-三甲基麦角糖基]乙基-20（S）喜树碱及其药学上可接受的盐; （iii）包含所述新颖的含锗喜树碱化合物，7 [2'-三甲基麦角糖基]乙基-20（S）喜树碱的药学上可接受的制剂及其药学上可接受的盐; 和（iv）将所述新颖的含锗喜树碱化合物，7 [2'-三甲基甲酰基]乙基-20（S）喜树碱及其药学上可接受的盐给予需要的受试者，包括患有癌症的受试者的方法。

    METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN
    3.
    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。

    Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin
    4.
    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

    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： C07F7/02 ,  C07D491/147

    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。

    Deuterated analogs of (4S)-4-ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3′, 4′:6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof
    5.
    发明授权
    Deuterated analogs of (4S)-4-ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3′, 4′:6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof 有权
    （4S）-4-乙基-4-羟基-11- [2-（三甲基甲硅烷基）乙基] -1H-吡喃并[3'，4'：6,7]中氮茚并[1,2-b] 3,4（4H，12H） - 二酮及其使用方法

    公开(公告)号：US08569265B2

    公开(公告)日：2013-10-29

    申请号：US13068244

    申请日：2011-05-06

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

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

    IPC分类号： A61K31/695 ,  C07F7/02

    CPC分类号： C07B59/004 ,  A61K38/00 ,  C07F7/0812

    摘要： The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.

    摘要翻译： 本发明公开了：（i）两种新型氘代Karenitecin？类似物，其药学上可接受的盐和/或衍生物; （ii）合成所述新型氘化Karenitecin®类似物，其药学上可接受的盐和/或衍生物的方法; （iii）药学上可接受的制剂，其包含所述新型氘代Karenitecin？类似物，其药学上可接受的盐，衍生物; 和/或任选的一种或多种另外的化学治疗剂; 和（iv）所述新型氘化Karenitecin®类似物，其药学上可接受的盐，衍生物的给药方法; 和/或任选的一种或多种另外的化学治疗剂给予有需要的受试者。

    C10-substituted camptothecin analogs
    7.
    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

    申请人： Kesavaram Narkunan ,  Xinghai Chen ,  Harry Kochat ,  Frederick Hausheer

    发明人： Kesavaram Narkunan ,  Xinghai Chen ,  Harry Kochat ,  Frederick Hausheer

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

    CPC分类号： C07F7/0812 ,  A61K31/4375 ,  A61K31/5377

    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

    摘要翻译： 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）。

    Medicinal disulfide salts
    9.
    发明授权
    Medicinal disulfide salts 有权
    药用二硫化物盐

    公开(公告)号：US07282602B2

    公开(公告)日：2007-10-16

    申请号：US10945809

    申请日：2004-09-21

    申请人： Qiuli Huang ,  Harry Kochat ,  Xinghai Chen

    发明人： Qiuli Huang ,  Harry Kochat ,  Xinghai Chen

    IPC分类号： C07C309/00

    CPC分类号： C07C323/66

    摘要： This invention relates to novel salts of medicinal disulfides. The compounds include a terminal sulfonate or phosphonate moiety, and have many uses, such as toxicity reducing agents when administered with many antineoplastic agents.

    摘要翻译： 本发明涉及药物二硫化物的新型盐。 化合物包括末端磺酸盐或膦酸盐部分，并且当与许多抗肿瘤剂一起施用时具有许多用途，例如毒性降低剂。

    C7- substituted camptothecin analogs
    10.
    发明申请
    C7- substituted camptothecin analogs 有权
    C7-取代的喜树碱类似物

    公开(公告)号：US20090099224A1

    公开(公告)日：2009-04-16

    申请号：US11974754

    申请日：2007-10-16

    申请人： Kesavaram Narkunan ,  Xinghai Chen ,  Harry Kochat ,  Frederick Hausheer

    发明人： Kesavaram Narkunan ,  Xinghai Chen ,  Harry Kochat ,  Frederick Hausheer

    IPC分类号： A61K31/4375 ,  A61P35/00 ,  C07F7/10

    CPC分类号： C07F7/0812 ,  A61K31/4375

    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

    摘要翻译： 本发明的新颖的C7-改性的喜树碱类似物及其药学上可接受的盐：（i）具有用于在体外抑制人和动物肿瘤细胞生长的有效抗肿瘤活性（即纳摩尔或亚纳摩尔浓度） （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）。