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公开(公告)号：US08987437B2
公开(公告)日：2015-03-24
申请号：US13475569
申请日：2012-05-18
申请人： Richard Hung Chiu Yu , Brandon Heath Brown , Richard P. Polniaszek , Benjamin R. Graetz , Keiko Sujino , Duong Duc-Phi Tran , Alan Scott Triman , Kenneth M. Kent , Steven Pfeiffer
发明人： Richard Hung Chiu Yu , Brandon Heath Brown , Richard P. Polniaszek , Benjamin R. Graetz , Keiko Sujino , Duong Duc-Phi Tran , Alan Scott Triman , Kenneth M. Kent , Steven Pfeiffer
IPC分类号： C07H19/00 , C07F9/6561 , C07D473/34 , C07F9/40 , C07F9/44 , C07H19/20 , C07H19/16 , C07H23/00
CPC分类号： C07H19/20 , C07D473/34 , C07F9/4075 , C07F9/4449 , C07F9/65616 , C07H19/02 , C07H19/04 , C07H19/16 , C07H19/173 , C07H23/00
摘要： The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.
摘要翻译： 本发明提供可用于制备具有有效抗HIV特性的化合物的合成方法和合成中间体。
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公开(公告)号：US20120296076A1
公开(公告)日：2012-11-22
申请号：US13475569
申请日：2012-05-18
申请人： Richard Hung Chiu Yu , Brandon Heath Brown , Richard P. Polniaszek , Benjamin R. Graetz , Keiko Sujino , Duong Duc-Phi Tran , Alan Scott Triman , Kenneth M. Kent , Steven Pfeiffer
发明人： Richard Hung Chiu Yu , Brandon Heath Brown , Richard P. Polniaszek , Benjamin R. Graetz , Keiko Sujino , Duong Duc-Phi Tran , Alan Scott Triman , Kenneth M. Kent , Steven Pfeiffer
CPC分类号： C07H19/20 , C07D473/34 , C07F9/4075 , C07F9/4449 , C07F9/65616 , C07H19/02 , C07H19/04 , C07H19/16 , C07H19/173 , C07H23/00
摘要： The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.
摘要翻译： 本发明提供可用于制备具有有效抗HIV特性的化合物的合成方法和合成中间体。
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公开(公告)号：US08173623B2
公开(公告)日：2012-05-08
申请号：US11729522
申请日：2007-03-29
申请人： Kenneth R. Crawford , Eric Dowdy , Arnold Gutierrez , Richard P. Polniaszek , Richard Hung Chiu Yu
发明人： Kenneth R. Crawford , Eric Dowdy , Arnold Gutierrez , Richard P. Polniaszek , Richard Hung Chiu Yu
IPC分类号： A61K31/665
CPC分类号： C07F9/6561 , A61K31/665 , C07C51/412 , C07C253/30 , C07C303/38 , C07C303/40 , C07C311/29 , C07D493/04 , C07F9/4006 , C07F9/4075 , C07F9/4084 , C07C255/60
摘要： A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
摘要翻译： 因此公开了用于制备抗病毒HIV蛋白酶抑制剂化合物的双呋喃中间体的合成方法。
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公开(公告)号：US5856507A
公开(公告)日：1999-01-05
申请号：US786523
申请日：1997-01-21
申请人： Richard P. Polniaszek , Xuebao Wang , Jeffrey S. DePue , Chennagiri R. Pandit , Kumar G. Gadamasetti , Yadagiri Pendri , Eduardo J. Martinez
发明人： Richard P. Polniaszek , Xuebao Wang , Jeffrey S. DePue , Chennagiri R. Pandit , Kumar G. Gadamasetti , Yadagiri Pendri , Eduardo J. Martinez
IPC分类号： C07D263/32 , C07D405/12 , C07D413/12
CPC分类号： C07D405/12 , C07D263/32
摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.
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公开(公告)号：US20120258935A1
公开(公告)日：2012-10-11
申请号：US13401659
申请日：2012-02-21
申请人： Kenneth R. Crawford , Eric D. Dowdy , Arnold Gutierrez , Richard P. Polniaszek , Richard Hung Chiu Yu
发明人： Kenneth R. Crawford , Eric D. Dowdy , Arnold Gutierrez , Richard P. Polniaszek , Richard Hung Chiu Yu
IPC分类号： C07F9/655 , A61P31/18 , A61K31/665 , A61P31/12 , C07C311/47 , C07C311/37
CPC分类号： C07F9/6561 , A61K31/665 , C07C51/412 , C07C253/30 , C07C303/38 , C07C303/40 , C07C311/29 , C07D493/04 , C07F9/4006 , C07F9/4075 , C07F9/4084 , C07C255/60
摘要： A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed
摘要翻译： 因此公开了用于制备抗病毒HIV蛋白酶抑制剂化合物的双呋喃中间体的合成方法
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6.发明授权Process for preparing N-protected amino acid .alpha.-halomethyl ketones and alcohols from N-protected amino acid esters 失效从N-保护的氨基酸酯制备N-保护的氨基酸的α-卤甲基酮和醇的方法
公开(公告)号：US5481011A
公开(公告)日：1996-01-02
申请号：US355373
申请日：1994-12-13
申请人： Ping Chen , Peter T. W. Cheng , Steven H. Spergel , Joel C. Barrish , John K. Thottathil , Robert Zahler , Richard P. Polniaszek , Xuebao Wang
发明人： Ping Chen , Peter T. W. Cheng , Steven H. Spergel , Joel C. Barrish , John K. Thottathil , Robert Zahler , Richard P. Polniaszek , Xuebao Wang
IPC分类号： C07D301/24 , C07C269/06 , C07C271/18 , C07D303/36 , C07D301/02 , C07D303/12
CPC分类号： C07D303/36 , C07C269/06 , C07C271/18
摘要： The present invention relates to a novel method useful for the conversion of amino acids to halomethylketones, which are then converted to amino acid epoxides. Such epoxides are important intermediates for the synthesis of inhibitors of renin and HIV protease, which are particularly useful in the treatment and/or prevention of HIV infection (AIDS).
摘要翻译： 本发明涉及用于将氨基酸转化成卤代甲基酮的新方法，然后将其转化为氨基酸环氧化物。 这种环氧化物是合成肾素和HIV蛋白酶抑制剂的重要中间体，其特别可用于治疗和/或预防HIV感染（AIDS）。
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公开(公告)号：US08431745B2
公开(公告)日：2013-04-30
申请号：US13401659
申请日：2012-02-21
申请人： Kenneth R. Crawford , Eric D. Dowdy , Arnold Gutierrez , Richard P. Polniaszek , Richard Hung Chiu Yu
发明人： Kenneth R. Crawford , Eric D. Dowdy , Arnold Gutierrez , Richard P. Polniaszek , Richard Hung Chiu Yu
IPC分类号： C07C381/00
CPC分类号： C07F9/6561 , A61K31/665 , C07C51/412 , C07C253/30 , C07C303/38 , C07C303/40 , C07C311/29 , C07D493/04 , C07F9/4006 , C07F9/4075 , C07F9/4084 , C07C255/60
摘要： A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
摘要翻译： 因此公开了用于制备抗病毒HIV蛋白酶抑制剂化合物的双呋喃中间体的合成方法。
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![Intermediates in the preparation of the antiviral agent [1S-(1α, 3α, 4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxmethyl)-2-methylenecyclopentyl]-6H-purin-6-one](/abs-image/US/2009/06/23/US07550619B2/abs.jpg.150x150.jpg)
8.发明授权Intermediates in the preparation of the antiviral agent [1S-(1α, 3α, 4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxmethyl)-2-methylenecyclopentyl]-6H-purin-6-one 有权制备抗病毒剂的中间体[1S-（1α，3α，4beta）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] 嘌呤-6-酮公开(公告)号：US07550619B2
公开(公告)日：2009-06-23
申请号：US11311598
申请日：2005-12-19
申请人： Yadagiri R. Pendri , Chung-Pin H. Chen , Jing Liang , Shaopeng Wang , Milan Stojanovic , Richard P. Polniaszek , John Thottathil , Dhileepkumar Krishnamurty
发明人： Yadagiri R. Pendri , Chung-Pin H. Chen , Jing Liang , Shaopeng Wang , Milan Stojanovic , Richard P. Polniaszek , John Thottathil , Dhileepkumar Krishnamurty
CPC分类号： C07F7/083 , C07D473/18 , C07F7/081 , C07F7/0812 , C07F7/0814 , C07F7/0827 , C07F7/1804
摘要： Intermediates useful in the preparation of the antiviral agent entecavir are disclosed. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various processes useful in the preparation of entecavir are also disclosed.
摘要翻译： 公开了用于制备抗病毒剂恩替卡韦的中间体。 还公开了用于恩替卡韦的分离和纯化的树脂吸附方法。 还公开了可用于制备恩替卡韦的各种方法。
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![Process for preparing the antiviral agent [1S-(1alpha,3 alpha,4beta )]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one](/abs-image/US/2006/04/25/US07034152B2/abs.jpg.150x150.jpg)
9.发明授权Process for preparing the antiviral agent [1S-(1alpha,3 alpha,4beta )]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one 有权制备抗病毒剂的方法[1S-（1α，3α，4beta）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤 -6-one公开(公告)号：US07034152B2
公开(公告)日：2006-04-25
申请号：US10734012
申请日：2003-12-11
申请人： Yadagiri R. Pendri , Chung-Pin H. Chen , Sunil S. Patel , Jeffrey M. Evans , Jing Liang , David R. Kronenthal , Gerald L. Powers , Siva Josyula Prasad , Jeffrey T. Bien , Zhongping Shi , Ramesh N. Patel , Amit Banerjee , Yeung Yu Chan , Sushil K. Rijhwani , Ambarish K. Singh , Shaopeng Wang , Milan Stojanovic , David J. Kucera , Richard P. Polniaszek , Charles Lewis , John Thottathil , Dhileepkumar Krishnamurty , Maotang X. Zhou , Purushotham Vemishetti
发明人： Yadagiri R. Pendri , Chung-Pin H. Chen , Sunil S. Patel , Jeffrey M. Evans , Jing Liang , David R. Kronenthal , Gerald L. Powers , Siva Josyula Prasad , Jeffrey T. Bien , Zhongping Shi , Ramesh N. Patel , Amit Banerjee , Yeung Yu Chan , Sushil K. Rijhwani , Ambarish K. Singh , Shaopeng Wang , Milan Stojanovic , David J. Kucera , Richard P. Polniaszek , Charles Lewis , John Thottathil , Dhileepkumar Krishnamurty , Maotang X. Zhou , Purushotham Vemishetti
IPC分类号： C07D473/18 , C07D7/08 , C07D473/40 , C07F7/10 , C07F7/18
CPC分类号： C07F7/083 , C07D473/18 , C07F7/081 , C07F7/0812 , C07F7/0814 , C07F7/0827 , C07F7/1804
摘要： Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.
摘要翻译： 公开了制备抗病毒剂恩替卡韦的方法。 还公开了用于恩替卡韦的分离和纯化的树脂吸附方法。 还公开了可用于制备恩替卡韦的各种中间体。
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公开(公告)号：US06639082B2
公开(公告)日：2003-10-28
申请号：US09967387
申请日：2001-09-28
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07D261/16 , C07F5/025
摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.
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