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1. 发明授权

US07470810B2 Alkyl and aryl-thiotrifluoroacetates and process 有权
标题翻译：烷基和芳基 - 三油酰氯酸盐和方法
公开(公告)号：US07470810B2
公开(公告)日：2008-12-30
申请号：US11032734
申请日：2005-01-11
申请人： Padam N. Sharma , Edward J. Gublo , Susan D. Boettger , Saibaba Racha , John Usher
发明人： Padam N. Sharma , Edward J. Gublo , Susan D. Boettger , Saibaba Racha , John Usher
IPC分类号： C07C321/04
CPC分类号： C07C327/22 , C07C231/02 , C07C2603/74 , Y02P20/55 , C07C233/48
摘要： Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate.In addition, a process for protecting a primary or secondary amino group or a primary or secondary hydroxyl group or an amino alcohol with a trifluoroacetyl protecting group is provided wherein a primary or secondary amine, amino acid, a primary or secondary alcohol or an amino alcohol is treated with a C3 to C19 alkyl- or aryl-thiotrifluoroacetate in basic aqueous solution.
摘要翻译：提供新的C3-C19烷基 - 和芳基 - 三油酸乙酯，其具有其中Q是C9-C19烷基或芳基的结构，并且是胺，氨基酸或伯或仲醇或氨基的氨基或羟基官能团的有用的保护剂醇，以在肽或蛋白质中形成酰胺键，其可用作筛选剂，药物和化妆品。还提供了制备C 3 -C 19烷基 - 和芳基 - 三硫代三氟乙酸盐的方法，其中在有机碱如吡啶，溶剂如二氯甲烷（DCM））存在下，用三氟乙酸酐（TFAA）处理C 3 -C 19烷基硫醇或芳基硫醇，和二甲基氨基吡啶（DMAP）作为催化剂形成所需的C 3 -C 19烷基 - 或芳基 - 三硫代三氟乙酸盐。另外，提供了用三氟乙酰基保护基保护伯或仲氨基或伯或仲羟基或氨基醇的方法，其中伯胺或仲胺，氨基酸，伯或仲醇或氨基醇在碱性水溶液中用C3至C19烷基 - 或芳基 - 三硫代三氟乙酸盐处理。

2. 发明授权

US07420063B2 Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein 有权
标题翻译：制备二肽基肽酶IV抑制剂的方法及其中使用的中间体
公开(公告)号：US07420063B2
公开(公告)日：2008-09-02
申请号：US11668641
申请日：2007-01-30
申请人： Padam N. Sharma , Edward J. Gublo , Gabriel M. Galvin , Susan D. Boettger , Saibaba Racha
发明人： Padam N. Sharma , Edward J. Gublo , Gabriel M. Galvin , Susan D. Boettger , Saibaba Racha
IPC分类号： C07C69/013 , C07D209/52
CPC分类号： C07C233/47 , C07C2603/74 , C07D209/02
摘要： A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reaget and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicabonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.
摘要翻译：提供了一种制备二肽基肽酶IV抑制剂的方法，其结构在乙酸异丙酯中用TFAA处理以保护作为三氟乙酸基团的叔羟基以形成4（其是新的中间体），其转化为酰氯化合物5（其是一种新型化合物），使用Vilsmeier试剂或其它氯代催化剂，并与化合物6在乙酸乙酯和二硼酸氢钠水溶液的非均相混合物中偶联，得到化合物7将化合物7的N，O-双（三氟乙酰基）基团去保护，碱化合物10。

3. 发明授权

US07186846B2 Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein 有权
标题翻译：制备二肽基肽酶IV抑制剂的方法及其中使用的中间体
公开(公告)号：US07186846B2
公开(公告)日：2007-03-06
申请号：US11091183
申请日：2005-03-28
申请人： Padam N. Sharma , Edward J. Gublo , Gabriel M. Galvin , Susan D. Boettger , Saibaba Racha
发明人： Padam N. Sharma , Edward J. Gublo , Gabriel M. Galvin , Susan D. Boettger , Saibaba Racha
IPC分类号： C07C69/013 , C07D209/52
CPC分类号： C07C233/47 , C07C2603/74 , C07D209/02
摘要： A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure wherein is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.
摘要翻译：提供了一种用于制备结构的二肽基肽酶IV抑制剂的方法，其中用TFAA在乙酸异丙酯中处理以保护作为三氟乙酸基团的叔羟基形成4（其是新的中间体），其转化为酰氯化合物5 （其是新型化合物），使用Vilsmeier试剂或其它氯试剂，并与化合物6在乙酸乙酯和碳酸氢水溶液的非均相混合物中偶联，得到化合物7化合物7的N，O-双（三氟乙酰基）基团脱保护，得到游离碱化合物10。

4. 发明申请

US20050159612A1 Novel alkyl- and aryl-thiotrifluoroacetates and process 有权
标题翻译：新型烷基 - 和芳基 - 三硫代三氟乙酸盐和方法
公开(公告)号：US20050159612A1
公开(公告)日：2005-07-21
申请号：US11032734
申请日：2005-01-11
申请人： Padam Sharma , Edward Gublo , Susan Boettger , Saibaba Racha , John Usher
发明人： Padam Sharma , Edward Gublo , Susan Boettger , Saibaba Racha , John Usher
IPC分类号： C07C231/02 , C07C233/48 , C07C323/22 , C07C327/22 , C07C333/02 , C07C233/58
CPC分类号： C07C327/22 , C07C231/02 , C07C2603/74 , Y02P20/55 , C07C233/48
摘要： Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate. In addition, a process for protecting a primary or secondary amino group or a primary or secondary hydroxyl group or an amino alcohol with a trifluoroacetyl protecting group is provided wherein a primary or secondary amine, amino acid, a primary or secondary alcohol or an amino alcohol is treated with a C3 to C19 alkyl- or aryl-thiotrifluoroacetate in basic aqueous solution.
摘要翻译：提供新的C 3 -C 20烷基 - 和芳基 - 三油酸乙酯，其具有其中Q为C 9 -C 19的结构并且是用于胺，氨基酸或伯或仲醇或氨基醇的氨基或羟基官能团的有用的保护剂，以使肽或蛋白质中的酰胺键能够形成，其可用作筛选剂，药品和化妆品。还提供了制备C 3 -C 20 - 烷基 - 和芳基 - 三硫代三氟乙酸盐的方法，其中C 3 -C 19 - 在有机碱如吡啶，溶剂如二氯甲烷（DCM）和二甲基氨基吡啶（DMAP）等催化剂存在下，用三氟乙酸酐（TFAA）处理烷基硫醇或芳基硫醇，形成所需的C 3 烷基 - 或芳基 - 三硫代三氟乙酸盐。另外，提供了用三氟乙酰基保护基保护伯或仲氨基或伯或仲羟基或氨基醇的方法，其中伯胺或仲胺，氨基酸，伯或仲醇或氨基醇在碱性水溶液中用C 3〜C 19烷基 - 或芳基 - 三硫代三氟乙酸酯处理。

5. 发明申请

US20150112070A1 PROCESSES FOR PREPARING HETEROCYCLIC COMPOUNDS INCLUDING TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE AND SALTS THEREOF 审中-公开
标题翻译：制备包含转-7-氧代-6-（磺酰基）-1,6-二氮杂双环[3,2,1]二氧化碳酰胺及其盐的杂环化合物的方法
公开(公告)号：US20150112070A1
公开(公告)日：2015-04-23
申请号：US14589194
申请日：2015-01-05
申请人： Melanie Simone Ronsheim , Saibaba Racha , Graham Richard Lawton , Shao Hong Zhou , Yuriy B. Kalyan , Michael Golden , David Milne , Alexander Telford , Janette Cherryman , Alistair Boyd , Andrew Phillips , Mahendra G. Dedhiya
发明人： Melanie Simone Ronsheim , Saibaba Racha , Graham Richard Lawton , Shao Hong Zhou , Yuriy B. Kalyan , Michael Golden , David Milne , Alexander Telford , Janette Cherryman , Alistair Boyd , Andrew Phillips , Mahendra G. Dedhiya
IPC分类号： C07D471/08 , C07D211/60
CPC分类号： C07D211/60 , A61K31/439 , A61K31/445 , C07D211/56 , C07D471/08 , Y02P20/55
摘要： The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
摘要翻译：本发明涉及制备式（I）化合物的化合物和方法，包括化合物如反式-7-氧代-6-（磺酰氧基）-1,6-二氮杂双环[3,2,1]辛烷-2-甲酰胺及其盐（如NXL-104）。

6. 发明授权

US06329542B1 Preparation of (S)-2-amino-6,6-dimethoxyhexanoic acid methyl ester via novel dioxolanes 失效
标题翻译：通过新型二氧戊环制备（S）-2-氨基-6,6-二甲氧基己酸甲酯
公开(公告)号：US06329542B1
公开(公告)日：2001-12-11
申请号：US09689215
申请日：2000-10-12
申请人： Jollie D. Godfrey, Jr. , David R. Kronenthal , Mark D. Schwinden , Sushil K. Srivastava , Keith Ramig , John J. Venit , Paul A. Jass , Saibaba Racha , John L. Dillon, Jr. , Nachimuthu Soundararajan , Gerald L. Powers , Atul S. Kotnis
发明人： Jollie D. Godfrey, Jr. , David R. Kronenthal , Mark D. Schwinden , Sushil K. Srivastava , Keith Ramig , John J. Venit , Paul A. Jass , Saibaba Racha , John L. Dillon, Jr. , Nachimuthu Soundararajan , Gerald L. Powers , Atul S. Kotnis
IPC分类号： C07C6966
CPC分类号： C07C229/22 , C07D317/30
摘要： The glycinamide of the formula is reacted with the dioxolane of the formula wherein L is a leaving group such as iodo, bromo, alkylsulfonyloxy, or arylsulfonyloxy to give the dioxolane of the formula Treating the dioxolane of formula III under aqueous refluxing conditions followed by exchanging the dioxolane acetal with a dimethoxy acetal and introduction of the methyl ester gives (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester which is an intermediate in the preparation of the dual inhibitor [4S-[4&agr;(R*),7&agr;,10a&bgr;]]-octahydro-4-[(2-mercapto-1-oxo-3-phenylpropyl)-amino]-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid. Also disclosed are storage stable salts of (S)-2-amino-6, 6-dimethoxyhexanoic acid, methyl ester.
摘要翻译：式中的甘氨酰胺与二氢呋喃的反应是离去基团如碘，溴，烷基磺酰氧基或芳基磺酰氧基，得到下式的二氧戊环：在含水回流条件下，将式III的二氧戊环，然后与二氧戊环缩醛交换，得到（S）-2-氨基-6,6-二甲氧基己酸甲酯，其是制备双重抑制剂[4S- [4α（R *），7α， 10]] - 八氢-4 - [（2-巯基-1-氧代-3-苯基丙基） - 氨基] -5-氧代-7H-吡啶并[2,1-b] [1,3]硫氮杂-7-羧酸酸。还公开了（S）-2-氨基-6,6-二甲氧基己酸甲酯的储存稳定的盐。

7. 发明申请

US20060035954A1 Ammonolysis process for the preparation of intermediates for DPP IV inhibitors 审中-公开
标题翻译：用于制备DPP IV抑制剂中间体的分解方法
公开(公告)号：US20060035954A1
公开(公告)日：2006-02-16
申请号：US11199539
申请日：2005-08-08
申请人： Padam Sharma , Gabriel Galvin , Susan Boettger , Saibaba Racha , Jingyang Zhu , Jack Melton , Boguslaw Mudryk
发明人： Padam Sharma , Gabriel Galvin , Susan Boettger , Saibaba Racha , Jingyang Zhu , Jack Melton , Boguslaw Mudryk
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D207/277 , C07D209/52
摘要： A process is provided for preparing the intermediate A in accordance with the following reaction sequence The intermediate A is used in preparing DPP IV inhibitors which are useful in treating diabetes.
摘要翻译：提供了根据以下反应顺序制备中间体A的方法。中间体A用于制备可用于治疗糖尿病的DPP IV抑制剂。

8. 发明申请

US20050222242A1 Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein 有权
标题翻译：制备二肽基肽酶IV抑制剂的方法及其中使用的中间体
公开(公告)号：US20050222242A1
公开(公告)日：2005-10-06
申请号：US11091183
申请日：2005-03-28
申请人： Padam Sharma , Edward Gublo , Gabriel Galvin , Susan Boettger , Saibaba Racha
发明人： Padam Sharma , Edward Gublo , Gabriel Galvin , Susan Boettger , Saibaba Racha
IPC分类号： A61K31/198 , A61K31/403 , C07C233/47 , C07C233/84 , C07D209/02
CPC分类号： C07C233/47 , C07C2603/74 , C07D209/02
摘要： A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure wherein is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.
摘要翻译：提供了一种用于制备结构的二肽基肽酶IV抑制剂的方法，其中用TFAA在乙酸异丙酯中处理以保护作为三氟乙酸基团的叔羟基形成4（其是新的中间体），其转化为酰氯化合物5 （其是新型化合物），使用Vilsmeier试剂或其它氯试剂，并与化合物6在乙酸乙酯和碳酸氢水溶液的非均相混合物中偶联，得到化合物7化合物7的N，O-双（三氟乙酰基）基团脱保护，得到游离碱化合物10。

9. 发明授权

US08829191B2 Processes for preparing heterocyclic compounds including trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof 有权
标题翻译：包括反式-7-氧代-6-（磺酰氧基）-1,6-二氮杂双环[3,2,1]辛烷-2-甲酰胺及其盐的制备方法
公开(公告)号：US08829191B2
公开(公告)日：2014-09-09
申请号：US13524007
申请日：2012-06-15
申请人： Melanie Simone Ronsheim , Saibaba Racha , Graham Richard Lawton , Shao Hong Zhou , Yuriy B. Kalyan , Michael Golden , David Milne , Alexander Telford , Janette Cherryman , Alistair Boyd , Andrew John Phillips , Mahendra G. Dedhiya
发明人： Melanie Simone Ronsheim , Saibaba Racha , Graham Richard Lawton , Shao Hong Zhou , Yuriy B. Kalyan , Michael Golden , David Milne , Alexander Telford , Janette Cherryman , Alistair Boyd , Andrew John Phillips , Mahendra G. Dedhiya
IPC分类号： C07D471/08 , C07D211/98
CPC分类号： C07D211/60 , A61K31/439 , A61K31/445 , C07D211/56 , C07D471/08 , Y02P20/55
摘要： The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
摘要翻译：本发明涉及制备式（I）化合物的化合物和方法，包括化合物如反式-7-氧代-6-（磺酰氧基）-1,6-二氮杂双环[3,2,1]辛烷-2-甲酰胺及其盐（如NXL-104）。

10. 发明申请

US20120323010A1 PROCESSES FOR PREPARING HETEROCYCLIC COMPOUNDS INCLUDING TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE AND SALTS THEREOF 有权
标题翻译：制备包含转-7-氧代-6-（磺酰基）-1,6-二氮杂双环[3,2,1]二氧化碳酰胺及其盐的杂环化合物的方法
公开(公告)号：US20120323010A1
公开(公告)日：2012-12-20
申请号：US13524007
申请日：2012-06-15
申请人： Melanie Simone Ronsheim , Saibaba Racha , Graham Richard Lawton , Shao Hong Zhou , Yuriy B. Kalyan , Michael Golden , David Milne , Alexander Telford , Janette Cherryman , Alistair Boyd , Andrew John Phillips , Mahendra G. Dedhiya
发明人： Melanie Simone Ronsheim , Saibaba Racha , Graham Richard Lawton , Shao Hong Zhou , Yuriy B. Kalyan , Michael Golden , David Milne , Alexander Telford , Janette Cherryman , Alistair Boyd , Andrew John Phillips , Mahendra G. Dedhiya
IPC分类号： C07D471/08 , C07D211/98
CPC分类号： C07D211/60 , A61K31/439 , A61K31/445 , C07D211/56 , C07D471/08 , Y02P20/55
摘要： The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
摘要翻译：本发明涉及制备式（I）化合物的化合物和方法，包括化合物如反式-7-氧代-6-（磺酰氧基）-1,6-二氮杂双环[3,2,1]辛烷-2-甲酰胺及其盐（如NXL-104）。

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