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1.发明授权Enantioconvergent chemoenzymatic synthesis of (R)-γ-amino-β-hydroxybutyric acid ((R)-GABOB) 有权（R） - 氨基-β-羟基丁酸（（R）-GABOB）的光化学转化化学酶合成公开(公告)号：US07374926B2
公开(公告)日：2008-05-20
申请号：US11022275
申请日：2004-12-23
CPC分类号： C12P13/005 , C12P13/002 , C12P41/004
摘要： The present invention particularly relates to a chemoenzymatic process for the stereoselective preparation of both enantiomers of 3-hydroxy-4-trityloxy butanenitrile key intermediates for the preparation of (R)-GABOB by lipase mediated kinetic resolution of its racemates and their effective application in the enantioconvergent synthesis of (R)-GABOB.
摘要翻译： 本发明特别涉及用于通过脂肪酶介导的其外消旋物的动力学拆分制备（R）-GABOB的3-羟基-4-三苯甲氧基丁腈关键中间体的两种对映体的立体选择性制备的化学酶学方法及其在 （R）-GABOB的对映异构体合成。
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2.发明申请Enantioconvergent chemoenzymatic synthesis of (R)-gamma-amino-beta-hydroxybutyric acid ((R)-GABOB) 有权（R） - 氨基-β-羟基丁酸（（R）-GABOB）的光化学转化化学酶合成公开(公告)号：US20060141606A1
公开(公告)日：2006-06-29
申请号：US11022275
申请日：2004-12-23
IPC分类号： C12P41/00
CPC分类号： C12P13/005 , C12P13/002 , C12P41/004
摘要： The present invention particularly relates to a chemoenzymatic process for the stereoselective preparation of both enantiomers of 3-hydroxy-4-trityloxy butanenitrile key intermediates for the preparation of (R)-GABOB by lipase mediated kinetic resolution of its racemates and their effective application in the enantioconvergent synthesis of (R)-GABOB.
摘要翻译： 本发明特别涉及用于通过脂肪酶介导的其外消旋物的动力学拆分制备（R）-GABOB的3-羟基-4-三苯甲氧基丁腈关键中间体的两种对映体的立体选择性制备的化学酶学方法及其在 （R）-GABOB的对映异构体合成。
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3.发明授权Chemoenzymatic process for stereoselective preparation of R and S enatiomers of 2-hydroxy-3-(2-thienyl) propanenitrile 有权用于立体选择性制备2-羟基-3-（2-噻吩基）丙腈的R和S对映体的化学酶法公开(公告)号：US07045341B2
公开(公告)日：2006-05-16
申请号：US10393406
申请日：2003-03-20
IPC分类号： C12P41/00
CPC分类号： C12P41/004 , C12P11/00
摘要： A chemoenzymatic process for the stereoselective preparation of both the (R) and (S) enantiomers of 3-hydroxy-3-(2-thienyl) propanenitrile has been developed. These optically pure key intermediates were prepared by enzymatic resolution of (±)3-hydroxy-3-(2-thienyl) propanenitrile both by transesterification and by hydrolysis reaction which were then transformed to both enantiomers of duloxetine.
摘要翻译： 已经开发了用于立体选择性制备3-羟基-3-（2-噻吩基）丙腈的（R）和（S）对映异构体的化学酶法。 这些光学纯的关键中间体通过酯交换和水解反应的酶解分解（±）3-羟基-3-（2-噻吩基）丙腈来制备，然后将其转化成度洛西汀的两种对映异构体。
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![Pyrrolo [2,1-c][1,4]benzodiazepine-anthraquinone conjugates useful as antitumour agents](/abs-image/US/2007/02/06/US07173026B2/abs.jpg.150x150.jpg)
4.发明授权Pyrrolo [2,1-c][1,4]benzodiazepine-anthraquinone conjugates useful as antitumour agents 有权吡咯并[2,1-c] [1,4]苯并二氮杂 - 蒽醌共轭物可用作抗肿瘤剂公开(公告)号：US07173026B2
公开(公告)日：2007-02-06
申请号：US11024240
申请日：2004-12-27
IPC分类号： C07D487/04 , A61K31/551 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to synthesis of pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone hybrids (V) wherein n=3,4; R=H, OH and to their use as antitumour agents.
摘要翻译： 本发明涉及吡咯并[2,1-c] [1,4]苯并二氮杂蒽醌杂合物（Ⅴ）的合成，其中n = 3,4; R = H，OH和它们作为抗肿瘤剂的用途。
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![Pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide conjugates linked through piperazine moiety and process for preparation thereof](/abs-image/US/2005/12/27/US06979684B1/abs.jpg.150x150.jpg)
5.发明授权Pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide conjugates linked through piperazine moiety and process for preparation thereof 失效通过哌嗪部分连接的吡咯并[2,1-c] [1,4]苯并二氮杂 - 萘二甲酰亚胺缀合物及其制备方法公开(公告)号：US06979684B1
公开(公告)日：2005-12-27
申请号：US10881729
申请日：2004-06-30
IPC分类号： A61K31/5517 , A61P35/00 , C07D403/14
CPC分类号： C07D403/14
摘要： The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety as potential antitumour agents. The present invention also relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety useful as potential antitumour agents.
摘要翻译： 本发明涉及通过哌嗪部分连接的新的吡咯并[2,1-c] [1,4]苯并二氮杂 - 萘二酰亚胺杂化物作为潜在的抗肿瘤剂。 本发明还涉及通过可用作潜在的抗肿瘤剂的哌嗪部分连接的新的吡咯并[2,1-c] [1,4]苯并二氮杂 - 萘二酰亚胺杂化物的制备方法。
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![Pyrrolo [2, 1-c] [1, 4] benzodiazepine-anthraquinone conjugates useful as antitumour agents](/abs-image/US/2006/06/29/US20060142272A1/abs.jpg.150x150.jpg)
6.发明申请Pyrrolo [2, 1-c] [1, 4] benzodiazepine-anthraquinone conjugates useful as antitumour agents 有权吡咯并[2,1-c] [1,4]苯并二氮杂蒽醌共轭物可用作抗肿瘤剂公开(公告)号：US20060142272A1
公开(公告)日：2006-06-29
申请号：US11024240
申请日：2004-12-27
IPC分类号： A61K31/551 , C07D487/12
CPC分类号： C07D487/04
摘要： The present invention relates to synthesis of pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone hybrids (V) wherein n=3,4; R═H, OH and to their use as antitumour agents
摘要翻译： 本发明涉及吡咯并[2,1-c] [1,4]苯并二氮杂蒽醌杂合物（Ⅴ）的合成，其中n = 3,4; R-H，OH和它们作为抗肿瘤剂的用途
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![PYRROLO[2,1-C][1,4]BENZODIAZEPINE-NAPTHALIMIDE CONJUGATES LINKED THROUGH PIPERAZINE MOIETY AND PROCESS FOR PREPARATION THEREOF](/abs-image/US/2006/01/05/US20060003994A1/abs.jpg.150x150.jpg)
7.发明申请PYRROLO[2,1-C][1,4]BENZODIAZEPINE-NAPTHALIMIDE CONJUGATES LINKED THROUGH PIPERAZINE MOIETY AND PROCESS FOR PREPARATION THEREOF 失效PYRROLO [2,1-C] [1,4]通过哌嗪环连接的苯并二氮杂萘并 - 联吡啶及其制备方法公开(公告)号：US20060003994A1
公开(公告)日：2006-01-05
申请号：US10881729
申请日：2004-06-30
申请人： Ahmed Kamal , Ramu Rondla , Gollpalli Khanna
发明人： Ahmed Kamal , Ramu Rondla , Gollpalli Khanna
IPC分类号： A61K31/551 , C07D487/04
CPC分类号： C07D403/14
摘要： The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety as potential antitumour agents. The present invention also relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety useful as potential antitumour agents.
摘要翻译： 本发明涉及通过哌嗪部分连接的新的吡咯并[2,1-c] [1,4]苯并二氮杂 - 萘二酰亚胺杂化物作为潜在的抗肿瘤剂。 本发明还涉及通过可用作潜在的抗肿瘤剂的哌嗪部分连接的新的吡咯并[2,1-c] [1,4]苯并二氮杂 - 萘二酰亚胺杂化物的制备方法。
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