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1. 发明授权

US08569265B2 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
标题翻译：（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。

2. 发明授权

US08722886B1 Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin 有权
标题翻译：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。

3. 发明申请

US20140135499A1 METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN 有权
标题翻译：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。

4. 发明申请

US20120282261A1 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
标题翻译：（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：US20120282261A1
公开(公告)日：2012-11-08
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 , A61K31/7064 , A61K31/7076 , A61K33/24 , A61P35/02 , A61K38/43 , A61K39/395 , A61K38/02 , A61P35/00 , A61P35/04 , C07F7/10 , A61K38/22
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。

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