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公开(公告)号：US20120302745A1
公开(公告)日：2012-11-29
申请号：US13564966
申请日：2012-08-02
申请人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： C07C269/06 , C07D307/92 , C07D405/08 , C07D317/72 , C07D413/12
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
摘要翻译： 本申请公开了一种用于合成烟肼类似物的新方法，以及由此制备的化合物。 合成通过包括环状缩酮酰胺途径，手性氨基甲酸酯酰胺路线和手性氨基甲酸酯路线的替代途径进行。 由此制备的化合物可用作凝血酶受体拮抗剂。 本文公开的化学例如以下合成顺序：
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公开(公告)号：US20120142914A1
公开(公告)日：2012-06-07
申请号：US13370768
申请日：2012-02-10
申请人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： C07D413/12 , C07D307/92 , C07D405/08 , C07D317/72 , C07C269/06
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
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公开(公告)号：US20110251392A1
公开(公告)日：2011-10-13
申请号：US13168029
申请日：2011-06-24
申请人： George Wu , Anantha R. Sudhakar , Mingsheng Huang , Tao Wang , Vijay Sabesan , Ji Xie , Frank Xing Chen , Marc Poirier , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie. Lim
发明人： George Wu , Anantha R. Sudhakar , Mingsheng Huang , Tao Wang , Vijay Sabesan , Ji Xie , Frank Xing Chen , Marc Poirier , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie. Lim
IPC分类号： C07F9/141 , C07C205/56 , C07C309/16 , C07D213/02 , C07C235/00 , C07C205/44 , C07D307/77 , C07D277/64
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译： 本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。 该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。 本文教导的化学结构可以举例说明如下：
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公开(公告)号：US20090281321A1
公开(公告)日：2009-11-12
申请号：US12505079
申请日：2009-07-17
申请人： George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
发明人： George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
IPC分类号： C07C69/608 , C07D405/08 , C07F9/40 , C07D307/92 , C07D417/08 , C07D277/64
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译： 本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。 该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。 本文教导的化学结构可以举例说明如下：
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公开(公告)号：US20120296093A1
公开(公告)日：2012-11-22
申请号：US13563136
申请日：2012-07-31
申请人： George Wu , Anantha R. SUDHAKAR , Tao WANG , Ji XIE , Frank Xing CHEN , Marc POIRIER , Mingsheng HUANG , Vijay SABESAN , Daw-long KWOK , Jian CUI , Xiaojing YANG , Tiruvettipuram K. THIRUVENGADAM , Jing LIAO , Ilia A. Zavialov , Hoa N. NGUYEN , Ngiap Kie LIM
发明人： George Wu , Anantha R. SUDHAKAR , Tao WANG , Ji XIE , Frank Xing CHEN , Marc POIRIER , Mingsheng HUANG , Vijay SABESAN , Daw-long KWOK , Jian CUI , Xiaojing YANG , Tiruvettipuram K. THIRUVENGADAM , Jing LIAO , Ilia A. Zavialov , Hoa N. NGUYEN , Ngiap Kie LIM
IPC分类号： C07D405/08 , C07C205/56 , C07D417/08 , C07D307/77 , C07C69/732 , C07F7/18 , C07C205/44 , C07C309/08 , C07C205/55 , C07D277/64 , C07F9/58 , C07C233/09
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译： 本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。 该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。 本文教导的化学结构可以举例说明如下：
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公开(公告)号：US08273790B2
公开(公告)日：2012-09-25
申请号：US13370768
申请日：2012-02-10
申请人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： A61K31/335
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
摘要翻译： 本申请公开了一种用于合成烟肼类似物的新方法，以及由此制备的化合物。 合成通过包括环状缩酮酰胺途径，手性氨基甲酸酯酰胺路线和手性氨基甲酸酯路线的替代途径进行。 由此制备的化合物可用作凝血酶受体拮抗剂。 本文公开的化学例如以下合成顺序：
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公开(公告)号：US08138180B2
公开(公告)日：2012-03-20
申请号：US12827000
申请日：2010-06-30
申请人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： A61K31/535
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
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公开(公告)号：US08618314B2
公开(公告)日：2013-12-31
申请号：US13563136
申请日：2012-07-31
申请人： George G. Wu , Anantha Sudhakar , Tao Wang , Ji Xie , Frank X. Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Illia Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
发明人： George G. Wu , Anantha Sudhakar , Tao Wang , Ji Xie , Frank X. Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Illia Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
IPC分类号： C07D307/92
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译： 本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。 该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。 本文教导的化学结构可以举例说明如下：
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公开(公告)号：US07772276B2
公开(公告)日：2010-08-10
申请号：US11330521
申请日：2006-01-12
申请人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap-Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap-Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： A61K31/34
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
摘要翻译： 本申请公开了一种用于合成烟肼类似物的新方法，以及由此制备的化合物。 合成通过包括环状缩酮酰胺途径，手性氨基甲酸酯酰胺路线和手性氨基甲酸酯路线的替代途径进行。 由此制备的化合物可用作凝血酶受体拮抗剂。 本文公开的化学例如以下合成顺序：
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公开(公告)号：US07605275B2
公开(公告)日：2009-10-20
申请号：US11331324
申请日：2006-01-12
申请人： Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam
发明人： Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07D307/92
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译： 本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。 该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。 本文教导的化学结构可以举例说明如下：
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