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1.发明授权Biocatalytic processes for the preparation of stereomerically pure fused bicyclic proline compounds 有权用于制备立体异构纯的稠合双环脯氨酸化合物的生物催化方法公开(公告)号：US08574876B2
公开(公告)日：2013-11-05
申请号：US13436506
申请日：2012-03-30
申请人： Benjamin Mijts , Sheela Muley , Jack Liang , Lisa M. Newman , Xiyun Zhang , James Lalonde , Michael D. Clay , Jun Zhu , John M. Gruber , Jeffrey Colbeck , John D. Munger, Jr. , Jagadeesh Mavinahalli , Roger Sheldon
发明人： Benjamin Mijts , Sheela Muley , Jack Liang , Lisa M. Newman , Xiyun Zhang , James Lalonde , Michael D. Clay , Jun Zhu , John M. Gruber , Jeffrey Colbeck , John D. Munger, Jr. , Jagadeesh Mavinahalli , Roger Sheldon
CPC分类号： C07D403/04 , C07D209/02 , C07D403/12 , C07D487/04 , C12P13/24 , C12P17/10 , C12P17/188 , C12Y104/03004
摘要： The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M′, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
摘要翻译： 本公开提供了基本上对映体纯的以下结构式的杂双环化合物，其中A，M，M'和R 5如本文所述，以及其制备的生物催化方法，以及用于这些方法的酶。
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2.发明授权Stereomerically pure fused bicyclic proline compounds useful for preparing hepatitis C protease inhibitors 有权用于制备丙型肝炎蛋白酶抑制剂的立体异构纯合并双环脯氨酸化合物公开(公告)号：US08859784B2
公开(公告)日：2014-10-14
申请号：US13294930
申请日：2011-11-11
申请人： Jack Liang , James Lalonde , Jun Zhu , John M. Gruber , John D. Munger, Jr.
发明人： Jack Liang , James Lalonde , Jun Zhu , John M. Gruber , John D. Munger, Jr.
IPC分类号： C07D209/02 , C07D403/04 , C07D403/12 , C07D487/04 , C12P13/24 , C12P17/10 , C12P17/18
CPC分类号： C07D403/04 , C07D209/02 , C07D403/12 , C07D487/04 , C12P13/24 , C12P17/10 , C12P17/188 , C12Y104/03004
摘要： The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M′, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
摘要翻译： 本公开提供了基本上对映体纯的以下结构式的杂双环化合物，其中A，M，M'和R 5如本文所述，以及其制备的生物催化方法，以及用于这些方法的酶。
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3.发明授权Biocatalytic processes for the preparation of substantially stereomerically pure fused bicyclic proline compounds 有权用于制备基本上立体异构纯的稠合双环脯氨酸化合物的生物催化方法公开(公告)号：US08178333B2
公开(公告)日：2012-05-15
申请号：US12490190
申请日：2009-06-23
申请人： Benjamin Mijts , Sheela Muley , Jack Liang , Lisa M. Newman , Xiyun Zhang , James Lalonde , Michael D. Clay , Jun Zhu , John M. Gruber , Jeffrey Colbeck , John D. Munger, Jr. , Jagadeesh Mavinahalli , Roger Sheldon
发明人： Benjamin Mijts , Sheela Muley , Jack Liang , Lisa M. Newman , Xiyun Zhang , James Lalonde , Michael D. Clay , Jun Zhu , John M. Gruber , Jeffrey Colbeck , John D. Munger, Jr. , Jagadeesh Mavinahalli , Roger Sheldon
CPC分类号： C07D403/04 , C07D209/02 , C07D403/12 , C07D487/04 , C12P13/24 , C12P17/10 , C12P17/188 , C12Y104/03004
摘要： The present disclosure provides monoamine oxidase enzymes and methods of their use in biocatalytic processes for the preparation of substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M′, and R5 are as described herein.
摘要翻译： 本公开内容提供单胺氧化酶及其在生物催化方法中用于制备基本上对映异构体纯的以下结构式的杂双环化合物的方法，其中A，M，M'和R 5如本文所述。
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公开(公告)号：US5859284A
公开(公告)日：1999-01-12
申请号：US701942
申请日：1996-08-23
申请人： Kenneth M. Kent , Choung U. Kim , Lawrence R. McGee , John D. Munger, Jr. , Ernest J. Prisbe , Michael J. Postich , John C. Rohloff , Daphne E. St. John , Matthew A. Williams , Lijun Zhang
发明人： Kenneth M. Kent , Choung U. Kim , Lawrence R. McGee , John D. Munger, Jr. , Ernest J. Prisbe , Michael J. Postich , John C. Rohloff , Daphne E. St. John , Matthew A. Williams , Lijun Zhang
IPC分类号： B05B7/12 , C07C227/08 , C07D203/26 , C07D303/40 , C07D317/46 , C07C69/757 , C07D307/00
CPC分类号： C07D303/40 , B05B7/1209 , C07C227/08 , C07D203/26 , C07D317/46 , C07C2101/16 , Y02P20/55
摘要： The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
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公开(公告)号：US6057459A
公开(公告)日：2000-05-02
申请号：US175744
申请日：1998-10-20
申请人： Kenneth M. Kent , Choung U. Kim , Lawrence R. McGee , John D. Munger, Jr. , Ernest J. Prisbe , Michael J. Postich , John C. Rohloff , Daphne E. St. John , Matthew A. Williams , Lijun Zhang
发明人： Kenneth M. Kent , Choung U. Kim , Lawrence R. McGee , John D. Munger, Jr. , Ernest J. Prisbe , Michael J. Postich , John C. Rohloff , Daphne E. St. John , Matthew A. Williams , Lijun Zhang
IPC分类号： B05B7/12 , C07C227/08 , C07D203/26 , C07D303/40 , C07D317/46 , C07D317/68
CPC分类号： C07D303/40 , B05B7/1209 , C07C227/08 , C07D203/26 , C07D317/46 , C07C2101/16 , Y02P20/55
摘要： The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
摘要翻译： 本发明提供了新的合成方法和组合物。 特别地，提供了可用于合成神经氨酸酶抑制剂的中间体的新方法和可用作中间体的组合物，其本身可用于神经氨酸酶抑制剂的合成。
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公开(公告)号：US06451340B1
公开(公告)日：2002-09-17
申请号：US09950031
申请日：2001-09-10
申请人： Murty N. Arimilli , Daphne E. Kelly , Thomas T. K. Lee , Lawrence V. Manes , John D. Munger, Jr. , Ernest J. Prisbe , Lisa M. Schultze
发明人： Murty N. Arimilli , Daphne E. Kelly , Thomas T. K. Lee , Lawrence V. Manes , John D. Munger, Jr. , Ernest J. Prisbe , Lisa M. Schultze
IPC分类号： A61K920
CPC分类号： A61K31/675 , C07F9/65616
摘要： The invention provides crystalline forms of adefovir dipivoxil and methods to prepare the crystals. The compositions and methods of the present invention have desirable properties for large scale synthesis of crystalline adefovir dipivoxil or for its formulation into therapeutic dosages. Invention compositions include an anhydrous crystal form of adefovir dipivoxil.
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公开(公告)号：US5935946A
公开(公告)日：1999-08-10
申请号：US900752
申请日：1997-07-25
IPC分类号： C07D473/34 , C07F9/6561 , A61K31/675
CPC分类号： C07D473/34 , C07F9/65616
摘要： The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxyphosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.
摘要翻译： 本发明提供包含双（POC）PMPA和富马酸（1:1）的组合物。 该组合物可用作制备抗病毒化合物的中间体，或可用于给患者施用抗病毒治疗或预防。 当口服给药时，组合物特别有用。 本发明还提供了在PMPA合成中制备PMPA和中间体的方法。 实施方案包括在有机溶剂如DMF中的叔丁醇锂，9-（2-羟丙基）腺嘌呤和对甲苯磺酰基甲氧基膦酸二乙酯。 与通过现有方法制备的二乙基PMPA相比，反应产生含有改进的副产物谱图的二乙基PMPA制剂。
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