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1. 发明申请

US20110294777A1 BETA-LACTAMASE INHIBITORS 有权
标题翻译： BETA-LACTAMASE抑制剂
公开(公告)号：US20110294777A1
公开(公告)日：2011-12-01
申请号：US12812763
申请日：2009-01-15
申请人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Sookhee Ha , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
发明人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Sookhee Ha , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
IPC分类号： A61K31/4545 , C07D487/08 , C07D519/00 , A61K31/55 , A61K31/454 , A61P31/04 , A61K31/439 , A61K31/553 , A61K31/496 , C07D401/12 , A61P31/00 , C07D471/08 , A61K31/4439
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于治疗与β-内酰胺抗生素组合的细菌感染。特别地，由于β-内酰胺酶的存在，这些化合物可以与抗β-生物抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

2. 发明授权

US08487093B2 β-lactamase inhibitors 有权
标题翻译： β-内酰胺酶抑制剂
公开(公告)号：US08487093B2
公开(公告)日：2013-07-16
申请号：US12812763
申请日：2009-01-15
申请人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
发明人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
IPC分类号： C07D243/00 , A61K31/551
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于与β-内酰胺抗生素联合治疗细菌感染。特别地，由于β-内酰胺酶的存在，该化合物可与β-内酰胺抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

3. 发明授权

US07829699B2 Process for the preparation of CGRP antagonist 失效
标题翻译：制备CGRP拮抗剂的方法
公开(公告)号：US07829699B2
公开(公告)日：2010-11-09
申请号：US12226244
申请日：2007-04-06
申请人： Kevin Belyk , Nelo Rivera
发明人： Kevin Belyk , Nelo Rivera
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.
摘要翻译：制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] -4- （3R，6S）-3-氨基-6-（2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺，（2,2-二氟苯基）-1-（2,2,2-三氟乙基）氮杂环庚烷-2-酮和2-氧代-1-（4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b] 吡啶二盐酸盐与1,1'-羰基二咪唑（“CDI”）作为羰基源; 并且有效制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] - 4-（2-氧代-2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺。

4. 发明申请

US20090281306A1 Process for the Preparation of Cgrp Antagonist 失效
标题翻译： Cgrp拮抗剂的制备方法
公开(公告)号：US20090281306A1
公开(公告)日：2009-11-12
申请号：US12226244
申请日：2007-04-06
申请人： Kevin Belyk , Nelo Rivera
发明人： Kevin Belyk , Nelo Rivera
IPC分类号： C07D401/14
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.
摘要翻译：制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] -4- （3R，6S）-3-氨基-6-（2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺，（2,2-二氟苯基）-1-（2,2,2-三氟乙基）氮杂环庚烷-2-酮和2-氧代-1-（4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b] 吡啶二盐酸盐与1,1'-羰基二咪唑（“CDI”）作为羰基源; 并且有效制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] - 4-（2-氧代-2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺。

5. 发明申请

US20080058522A1 Process For The Preparation Of Enantiomerically Enriched Beta Amino Acid Derivatives 有权
标题翻译：对映体富含β-氨基酸衍生物的制备方法
公开(公告)号：US20080058522A1
公开(公告)日：2008-03-06
申请号：US11547183
申请日：2005-04-05
申请人： Yi Xiao , Yongkui Sun , Thorsten Rosner , Nelo Rivera , Shane Krska , Andrew Clausen , Joseph Armstrong , Felix Spindler , Christophe Malan
发明人： Yi Xiao , Yongkui Sun , Thorsten Rosner , Nelo Rivera , Shane Krska , Andrew Clausen , Joseph Armstrong , Felix Spindler , Christophe Malan
IPC分类号： C07D487/04 , C07C229/28 , C07D211/94
CPC分类号： C07C227/32 , C07C227/16 , C07C231/18 , C07D213/55 , C07D213/64 , C07D487/04 , C07C229/34 , C07C229/36
摘要： The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.
摘要翻译：本发明涉及有效制备对映体富集的β氨基酸衍生物的方法，其中氨基未被保护。产物手性β氨基酸衍生物可用于生物活性分子的不对称合成。该方法包括在与手性单膦或双膦配体配合的铑金属前体的存在下，对胺未未保护的前手性β-氨基丙烯酸或其衍生物进行对映选择性氢化。

6. 发明申请

US20060194977A1 Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation 有权
标题翻译：通过不对称氢化制备手性β氨基酸衍生物的方法
公开(公告)号：US20060194977A1
公开(公告)日：2006-08-31
申请号：US10549425
申请日：2004-03-15
申请人： Yi Xiao , Joseph Armstrong III , Shane Krska , Eugenia Njolito , Nelo Rivera , Yongkui Sun , Thorsten Rosner
发明人： Yi Xiao , Joseph Armstrong III , Shane Krska , Eugenia Njolito , Nelo Rivera , Yongkui Sun , Thorsten Rosner
IPC分类号： C07C327/22 , C07C231/12
CPC分类号： B01J31/2295 , B01J31/24 , B01J31/2409 , B01J2231/645 , B01J2531/0263 , B01J2531/0286 , B01J2531/822 , B01J2531/842 , C07C227/16 , C07C231/12 , C07C231/18 , C07D487/04 , C07C237/20
摘要： The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.
摘要翻译：本发明涉及有效制备对映体富集的β氨基酸衍生物的方法，其可用于生物活性分子的不对称合成。该方法包括前手性β-氨基丙烯酸衍生物底物在与手性二茂铁基二膦配体络合的过渡金属前体存在下的对映选择性氢化。

7. 发明申请

US20160040201A1 Biocatalytic Transamination Process 有权
标题翻译：生物催化转氨法
公开(公告)号：US20160040201A1
公开(公告)日：2016-02-11
申请号：US14649308
申请日：2013-12-03
申请人： Paul Gerard BULGER , Birgit KOSJEK , Nelo RIVERA , MERCK SHARP & DOHME CORP.
发明人： Paul Gerard Bulger , Birgit Kosjek , Nelo Rivera
IPC分类号： C12P17/12
CPC分类号： C12P17/12 , C07D211/02 , C12N9/1096 , C12P13/001 , C12Y206/01
摘要： A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: employing dynamic kinetic resolution (DKR). The DKR process involves an enzymatic enantioselective amination reaction catalyzed by transaminases. The process can be used to manufacture key intermediates in the preparation of poly (ADP-ribose) polymerase (PARP) inhibitors which may be useful for the treatment of cancer.
摘要翻译：提供了一种新颖的方法来有效制备结构式I的不对称化合物：采用动态动力学拆分（DKR）。 DKR方法涉及由转氨酶催化的酶对映选择性胺化反应。该方法可用于制备可用于治疗癌症的聚（ADP-核糖）聚合酶（PARP）抑制剂的制备中的关键中间体。

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