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1. 发明申请

US20110190503A1 Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase 审中-公开
标题翻译：噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯胺作为白三烯A4水解酶的调节剂
公开(公告)号：US20110190503A1
公开(公告)日：2011-08-04
申请号：US13039105
申请日：2011-03-02
申请人： Genesis M. BACANI , Diego BROGGINI , Eugene Y. CHEUNG , Christa C. CHROVIAN , Xiaohu DENG , Anne M. FOURIE , Laurent GOMEZ , Cheryl A. GRICE , Aaron M. KEARNEY , Adrienne M. LANDRY-BAYLE , Alice LEE-DUTRA , Jimmy T. LIANG , Susanne LOCHNER , Neelakandha S. MANI , Alejandro SANTILLÁN, JR. , Kathleen SAPPEY , Kia SEPASSI , Virginia M. TANIS , Alvah T. WICKBOLDT , John J. M. WIENER , Hartmut ZINSER
发明人： Genesis M. BACANI , Diego BROGGINI , Eugene Y. CHEUNG , Christa C. CHROVIAN , Xiaohu DENG , Anne M. FOURIE , Laurent GOMEZ , Cheryl A. GRICE , Aaron M. KEARNEY , Adrienne M. LANDRY-BAYLE , Alice LEE-DUTRA , Jimmy T. LIANG , Susanne LOCHNER , Neelakandha S. MANI , Alejandro SANTILLÁN, JR. , Kathleen SAPPEY , Kia SEPASSI , Virginia M. TANIS , Alvah T. WICKBOLDT , John J. M. WIENER , Hartmut ZINSER
IPC分类号： C07D451/02
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
摘要翻译：描述了噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯基胺化合物，其可用作LTA4水解酶（LTA4H）调节剂。这样的化合物可以用于调节LTA4H的药物组合物和方法以及用于治疗由LTA4水解酶活性介导的疾病状态，障碍和病症。

2. 发明申请

US20090258854A1 Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase 有权
标题翻译：噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯胺作为白三烯A4水解酶的调节剂
公开(公告)号：US20090258854A1
公开(公告)日：2009-10-15
申请号：US12421406
申请日：2009-04-09
申请人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Anne M. Fourie , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearny , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillan, JR. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
发明人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Anne M. Fourie , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearny , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillan, JR. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
IPC分类号： A61K31/437 , C07D513/04 , A61K31/506 , A61K31/5377 , A61K31/4985 , A61P29/00 , C12N9/50 , C07D453/02
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
摘要翻译：描述了噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯基胺化合物，其可用作LTA4水解酶（LTA4H）调节剂。这样的化合物可以用于调节LTA4H的药物组合物和方法以及用于治疗由LTA4水解酶活性介导的疾病状态，障碍和病症。

3. 发明申请

US20110159563A1 Thyazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase 有权
标题翻译：噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯胺作为白三烯A4水解酶的调节剂
公开(公告)号：US20110159563A1
公开(公告)日：2011-06-30
申请号：US13039017
申请日：2011-03-02
申请人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Anne M. Fourie , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearney , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillán, JR. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
发明人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Anne M. Fourie , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearney , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillán, JR. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
IPC分类号： C12N9/99 , C07D513/04
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
摘要翻译：描述了噻唑并吡啶-2-基氧基 - 苯基和噻唑并吡嗪-2-基氧基 - 苯基胺化合物，其可用作LTA4水解酶（LTA4H）调节剂。这样的化合物可以用于调节LTA4H的药物组合物和方法以及用于治疗由LTA4水解酶活性介导的疾病状态，障碍和病症。

4. 发明申请

US20070219378A1 Method for Producing Sodium Fosphenytoin 审中-公开
标题翻译：生产苯丙酸钠的方法
公开(公告)号：US20070219378A1
公开(公告)日：2007-09-20
申请号：US10587189
申请日：2004-02-05
申请人： Hartmut Zinser , Guisep Derungs
发明人： Hartmut Zinser , Guisep Derungs
IPC分类号： C07D233/00
CPC分类号： C07F9/6506
摘要： Sodium fosphenytoin, 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione disodium salt, a known anticonvulsive, antiepileptic and antiarrhythmic, can be prepared by reacting 3-hydroxymethyl-5,5-diphenylimidazoline-2,4-dione with a phosphorous acid diester or triester activated by an oxidizing agent, whose ester groups can be selectively cleaved from the reaction product, cleaving the ester groups from the resulting phosphoric acid diester 2,5-dioxo-4,4-diphenyl-imidazolidin-1-ylmethyl ester and converting the resulting 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione to its disodium salt. The oxidizing agent is advantageously a halogenating agent such as elemental bromine or N-bromosuccinimide, and the phosphorous acid ester used is advantageously dibenzyl phosphite. Of particular importance—even taken on its own—is the fact that a phosphoric acid diester 2,5-dioxo-4,4-diphenylimidazolidin-1-ylmethyl ester, whose phosphoric acid diester structural element can be selectively cleaved, can be converted to 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione and the latter converted to its disodium salt in a single operation.
摘要翻译：已知的抗惊厥，抗癫痫和抗心律失常药的5-苯基苯并噻吩钠，5,5-二苯基-3 - [（膦酰氧基）甲基]咪唑烷-2,4-二酮二钠盐可以通过3-羟甲基-5,5-二苯基咪唑啉-2 具有通过氧化剂活化的亚磷酸二酯或三酯的2,4-二酮，其酯基可以从反应产物中选择性地裂解，从所得的磷酸二酯2,5-二氧代-4,4-二酮中切割酯基，并将所得的5,5-二苯基-3 - [（膦酰氧基）甲基]咪唑烷-2,4-二酮转化成其二钠盐。氧化剂有利地是卤化剂如元素溴或N-溴代琥珀酰亚胺，并且所用的亚磷酸酯有利地是亚磷酸二苄酯。特别重要的是甚至独自考虑的事实是，其磷酸二酯结构单元可以选择性地裂解的磷酸二酯2,5-二氧代-4,4-二苯基咪唑烷-1-基甲酯可以转化为 5,5-二苯基-3 - [（膦酰氧基）甲基]咪唑烷-2,4-二酮，后者在一次操作中转化成其二钠盐。

5. 发明授权

US07939527B2 Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase 有权
公开(公告)号：US07939527B2
公开(公告)日：2011-05-10
申请号：US12421406
申请日：2009-04-09
申请人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearney , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillán, Jr. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
发明人： Genesis M. Bacani , Diego Broggini , Eugene Y. Cheung , Christa C. Chrovian , Xiaohu Deng , Laurent Gomez , Cheryl A. Grice , Aaron M. Kearney , Adrienne M. Landry-Bayle , Alice Lee-Dutra , Jimmy T. Liang , Susanne Lochner , Neelakandha S. Mani , Alejandro Santillán, Jr. , Kathleen Sappey , Kia Sepassi , Virginia M. Tanis , Alvah T. Wickboldt , John J. M. Wiener , Hartmut Zinser
IPC分类号： A61K31/5355 , A61K31/4985 , A61K31/516 , A61K31/497 , A61K31/4365 , C07D413/14 , C07D239/34 , C07D513/04
CPC分类号： C07D498/04 , C07D451/02
摘要： Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.

6. 发明申请

US20070060642A1 Process for the preparation of (3r,3as,6ar)-hexahydrofuro [2,3-b] furan-3-yl (1s,2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate 有权
标题翻译：制备（3r，3as，6ar）六氢呋喃并[2,3-b]呋喃-3-基（1s，2r）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1 苄基-2-羟丙基氨基甲酸酯
公开(公告)号：US20070060642A1
公开(公告)日：2007-03-15
申请号：US10596732
申请日：2004-12-23
申请人： Nicolaas Martha Felix Goyvaerts , Piet Wigerinck , Hartmut Zinser , Birgit Ebert
发明人： Nicolaas Martha Felix Goyvaerts , Piet Wigerinck , Hartmut Zinser , Birgit Ebert
IPC分类号： A61K31/343 , C07D493/02
CPC分类号： C07D493/02 , C07D493/04
摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.
摘要翻译：本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸酯以及用于所述方法的中间体。更具体地，本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 使用4-氨基-N - （（2R，3S）-3-氨基-2-羟基-4-苯基丁基）-N-（异丁基）苯磺酰胺的（异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸叔丁酯中间和适用于工业规模化的流程。（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。

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