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公开(公告)号：US07989653B2
公开(公告)日：2011-08-02
申请号：US12505079
申请日：2009-07-17
申请人： George G. Wu , Anantha Sudhakar , Tao Wang , Ji Xie , Frank X. Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , Daw-Iong Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia 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-Iong Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam , Jing Liao , Ilia Zavialov , Hoa N. Nguyen , Ngiap Kie Lim
IPC分类号： C07C69/608
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：US08258319B2
公开(公告)日：2012-09-04
申请号：US13168029
申请日：2011-06-24
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 , Ilia 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 , Ilia 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：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：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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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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7.发明授权Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof 失效黄嘌呤磷酸二酯酶V抑制剂及其前体的制备方法公开(公告)号：US07786301B2
公开(公告)日：2010-08-31
申请号：US11429719
申请日：2006-05-08
IPC分类号： C07D473/06 , C07D473/08 , C07D233/90
CPC分类号： C07C257/12 , C07D233/90 , C07D473/06
摘要： A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9.
摘要翻译： 一种制备黄嘌呤磷酸二酯酶V抑制剂的方法，以及用于所述方法的化合物。 该方法包括用于无中间纯化或分离的化合物5的有效合成的五步方法，合成化合物7的二卤化步骤和产生化合物9的偶联反应。
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![Process and intermediates for the preparation of (1R,2S,5S)-3-azabicyclo[3,1,0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[1,1-dimethylethyl]amino]carbonylamino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl](/abs-image/US/2008/02/05/US07326795B2/abs.jpg.150x150.jpg)
8.发明授权Process and intermediates for the preparation of (1R,2S,5S)-3-azabicyclo[3,1,0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[1,1-dimethylethyl]amino]carbonylamino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl 失效制备（1R，2S，5S）-3-氮杂双环[3,1,0]己烷-2-甲酰胺，N- [3-氨基-1-（环丁基甲基）-2,3-二氧代丙基] -3 - [（2S）-2 - [[[1,1-二甲基乙基]氨基]羰基氨基] -3,3-二甲基-1-氧代丁基] -6,6-二甲基公开(公告)号：US07326795B2
公开(公告)日：2008-02-05
申请号：US10867600
申请日：2004-06-15
申请人： Anantha Sudhakar , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Orr , Hoa N. Nguyen , Juergen Weber , Ingyu Jeon , Minzhang Chen , Michael D. Green , George S. Wong , Jeonghan Park , Tetsuo Iwama
发明人： Anantha Sudhakar , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Orr , Hoa N. Nguyen , Juergen Weber , Ingyu Jeon , Minzhang Chen , Michael D. Green , George S. Wong , Jeonghan Park , Tetsuo Iwama
IPC分类号： C07D209/52 , C07C233/08
CPC分类号： C07K5/0202 , C07C271/22 , C07C2601/04
摘要： In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.
摘要翻译： 在一个实施方案中，本申请涉及制备式I化合物的方法以及在制备式I化合物的方法中制备的某些中间体化合物。
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公开(公告)号：US07728135B2
公开(公告)日：2010-06-01
申请号：US11326154
申请日：2006-01-05
申请人： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecelia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
发明人： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecelia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
IPC分类号： C07D401/14 , C07D403/12 , A61K31/506 , A61K31/18
CPC分类号： C07D211/96 , C07D211/26 , C07D401/14
摘要： The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
摘要翻译： 本发明涉及4- [4 - [（R） - [1- [环丙基磺酰基] -4-哌啶基]（3-氟苯基）甲基] -3（S） - 甲基-1-哌嗪基] 1 - [（4,6-二甲基-5-嘧啶基）羰基] -4-甲基哌啶]，以及通过新途径从容易获得的起始原料中间产物。
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公开(公告)号：US20100036125A1
公开(公告)日：2010-02-11
申请号：US12580855
申请日：2009-10-16
申请人： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
发明人： Xiongwei Shi , Man Zhu , William Leong , Vilas Dahanukar , Ilia A. Zavialov , Cecilia Proietti , Shannon Zhao , Hong-Chang Lee , Yi Liu , Hoa N. Nguyen , Wenxue Wu , Bosco D'Sa , Feng Liang , Loc Thanh Tran
IPC分类号： C07D401/06 , C07D211/30
CPC分类号： C07D211/96 , C07D211/26 , C07D401/14
摘要： The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.
摘要翻译： 本发明涉及4- [4 - [（R） - [1- [环丙基磺酰基] -4-哌啶基]（3-氟苯基）甲基] -3（S） - 甲基-1-哌嗪基] 1 - [（4,6-二甲基-5-嘧啶基）羰基] -4-甲基哌啶]，以及通过新途径从容易获得的起始原料中间产物。
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