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1. 发明授权

US06307066B1 Process for producing simvastatin 失效
标题翻译：辛伐他汀生产工艺
公开(公告)号：US06307066B1
公开(公告)日：2001-10-23
申请号：US08754677
申请日：1996-11-21
申请人： K. S. Keshava Murthy , Stephen E. Horne , Gamini Weeratunga , Shawn Young
发明人： K. S. Keshava Murthy , Stephen E. Horne , Gamini Weeratunga , Shawn Young
IPC分类号： C07D30930
CPC分类号： C07D309/30 , C07F5/025
摘要： A process for manufacturing Simvastatin is provided comprising reacting lovastatin with an organic boronic acid to produce a derivative of lovastatin (lovastatin phenylboronate) methylating the 2-methylbutyryloxy group on the lovastatin derivative to form a 2,2-dimethylbutyryloxy group on the lovastatin derivative and thereafter removing the boronate group to produce simvastatin.
摘要翻译：提供了一种制造辛伐他汀的方法，其包括使洛伐他汀与有机硼酸反应，以产生洛伐他汀衍生物甲基化2-甲基丁酰氧基的洛伐他汀（洛伐他汀苯基硼酸酯）的衍生物，从而在洛伐他汀衍生物上形成2,2-二甲基丁酰氧基去除硼酸盐组产生辛伐他汀。

2. 发明授权

US07767843B2 Process for the preparation of phenylcarbamates 失效
标题翻译：苯基氨基甲酸酯的制备方法
公开(公告)号：US07767843B2
公开(公告)日：2010-08-03
申请号：US11365596
申请日：2006-03-02
申请人： Zhi-Xian Wang , Stephen E. Horne , K. S. Keshava Murthy
发明人： Zhi-Xian Wang , Stephen E. Horne , K. S. Keshava Murthy
IPC分类号： C07C269/04
CPC分类号： C07C269/04 , C07C271/44
摘要： A process for the preparation of aminoalkyl phenyl carbamate compounds of Formula I, wherein R1 and R2 independently are hydrogen or a C1-6 alkyl; R3 and R4 are the same or different and each is a C1-6 alkyl; or R3 and R4 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; R5 and R6 independently are hydrogen, linear, branched or cyclic C1-6 alkyl; or R5 and R6 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; the carbon centre designated “*” can be racemic or enantiomerically enriched in the (R)- or (S)- configuration; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：制备式I氨基烷基苯基氨基甲酸酯化合物的方法，其中R 1和R 2独立地是氢或C 1-6烷基; R3和R4相同或不同，各自为C1-6烷基; 或者R 3和R 4与它们所连接的氮一起形成具有或不具有氮或氧的杂原子的环状三元至八元环; R 5和R 6独立地是氢，直链，支链或环状C 1-6烷基; 或R 5和R 6与它们所连接的氮一起形成具有或不具有杂原子如氮或氧的环状三元至八元环; 指定为“*”的碳中心可以是（R） - 或（S） - 构型的外消旋或对映异构体富集; 及其药学上可接受的酸加成盐。

3. 发明授权

US08471011B2 Preparation of acid addition salts of amine bases by solid phase—gas phase reactions 有权
标题翻译：通过固相气相反应制备胺碱的酸加成盐
公开(公告)号：US08471011B2
公开(公告)日：2013-06-25
申请号：US11168523
申请日：2005-06-29
申请人： Allan W. Rey , Lotfi Derdour , K. S. Keshava Murthy , Probal Kanti Datta , Martin Ehlert , Stephen E. Horne
发明人： Allan W. Rey , Lotfi Derdour , K. S. Keshava Murthy , Probal Kanti Datta , Martin Ehlert , Stephen E. Horne
IPC分类号： C07D239/72
CPC分类号： C07D405/12 , C07D211/28 , C07D307/52 , C07D401/14
摘要： A process for the preparation of an acid addition salt of an organic base comprising exposing the organic base in solid form to a gaseous acid, with the proviso that ziprasidone, its acid addition salts and intermediates thereof are excluded.
摘要翻译：一种制备有机碱的酸加成盐的方法，包括将固体形式的有机碱暴露于气态酸，条件是排除了齐拉西酮，其酸加成盐和中间体。

4. 发明授权

US07193090B2 Preparation of atorvastatin 失效
标题翻译：阿托伐他汀的制备
公开(公告)号：US07193090B2
公开(公告)日：2007-03-20
申请号：US10800741
申请日：2004-03-16
申请人： Bhaskar Reddy Guntoori , Daqing Che , Fan Wang , Yajun Zhao , K. S. Keshava Murthy , Stephen E. Horne
发明人： Bhaskar Reddy Guntoori , Daqing Che , Fan Wang , Yajun Zhao , K. S. Keshava Murthy , Stephen E. Horne
IPC分类号： C07D207/00
CPC分类号： C07D207/416 , C07D207/34
摘要： A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester.
摘要翻译：制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5 - 羟基-3-氧代-1-庚酸叔丁酯包括：（a）还原5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -3-氧代-1-戊酸，（R）-2-羟基-1,2,2-三苯乙基酯; （b）（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] 3-羟基-1-戊酸，（R）-2-羟基-1,2,2-三苯基乙基酯，使用碱在溶剂中形成酸; （c）酸形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基吡啶-3-基] -5-羟基-3-氧代-1-庚酸叔丁酯。

5. 发明授权

US06380388B1 1,3-oxathiolan-5-ones useful in the production of antiviral nucleoside analogues 失效
标题翻译：可用于生产抗病毒核苷类似物的1,3-氧硫杂环戊烷-5-酮
公开(公告)号：US06380388B1
公开(公告)日：2002-04-30
申请号：US09572867
申请日：2000-05-18
申请人： K. S. Keshava Murthy , Stephen E. Horne , Gurijala V. Reddy , Chandrawansha B. W. Senanayake , Bruno K. Radatus
发明人： K. S. Keshava Murthy , Stephen E. Horne , Gurijala V. Reddy , Chandrawansha B. W. Senanayake , Bruno K. Radatus
IPC分类号： C07D32704
CPC分类号： C07D411/04 , C07D327/04
摘要： A compound of the formula A, wherein R* is a chiral auxiliary, and where the configuration at the asymmetric carbon atom between oxygen and sulfur is (R), (S), or combinations of (R) and (S), useful in the preparation of enantiomerically enriched 1,3-oxathiolane nucleoside analogues, for example (−)-FTC and 3TC.
摘要翻译：式A化合物，其中R *是手性助剂，其中氧和硫之间不对称碳原子上的构型是（R），（S）或（R）和（S）的组合，可用于制备对映体富集的1,3-氧硫杂环戊烷核苷类似物，例如（ - ） - FTC和3TC。

6. 发明授权

US07049399B2 Process for the preparation of polypeptide 1 失效
标题翻译：多肽1的制备方法
公开(公告)号：US07049399B2
公开(公告)日：2006-05-23
申请号：US10326994
申请日：2002-12-24
申请人： Elena Bejan , Gamini Weeratunga , Stephen E. Horne
发明人： Elena Bejan , Gamini Weeratunga , Stephen E. Horne
IPC分类号： C07K1/00 , C07K2/00
CPC分类号： C07K14/001 , A61K38/00 , C07K14/195
摘要： A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutically acceptable salts thereof, comprising the steps of: (a) polymerization of a mixture of the N-carboxyanhydrides of L-alanine, L-tyrosine, a protected L-glutamate and a protected L-lysine to obtain protected copolymer 6 or salt thereof; (b) deprotection of the protected copolymer 6 (or salt thereof) to produce polypeptide 1 or a pharmaceutically acceptable salt thereof in one single step; (c) separation and purification of the polypeptide 1 (or a pharmaceutically acceptable salt) to obtain a purified polypeptide 1
摘要翻译：制备本发明中指定的多肽的方法为1，由以下结构中的氨基酸单元组成，即随机排列在多肽中的L-丙氨酸，L-谷氨酸，L-赖氨酸和L-酪氨酸 1或其药学上可接受的盐，包括以下步骤：（a）将L-丙氨酸，L-酪氨酸，受保护的L-谷氨酸和受保护的L-赖氨酸的N-羧酸酐的混合物聚合，得到被保护的共聚物6 或其盐; （b）在一个单一步骤中保护的共聚物6（或其盐）去保护以产生多肽1或其药学上可接受的盐; （c）分离和纯化多肽1（或其药学上可接受的盐）以获得纯化的多肽1

7. 发明授权

US06495691B1 Process for the preparation of tetrahydrothieno[3,2-c]pyridine derivatives 失效
标题翻译：四氢噻吩并[3,2-c]吡啶衍生物的制备方法
公开(公告)号：US06495691B1
公开(公告)日：2002-12-17
申请号：US09902165
申请日：2001-07-11
申请人： Stephen E. Horne , Gamini Weeratunga , Bogdan M. Comanita , Jaipal Reddy Nagireddy , Laura Kaye McConachie
发明人： Stephen E. Horne , Gamini Weeratunga , Bogdan M. Comanita , Jaipal Reddy Nagireddy , Laura Kaye McConachie
IPC分类号： C07D49102
CPC分类号： C07D413/04 , C07D333/20 , C07D333/22 , C07D495/04
摘要： A process for the preparation of tetrahydrothieno[3,2-c]pyridine derivatives of general formula I: or their pharmaceutically acceptable salts, wherein the meaning of X is hydrogen, carboxyl, alkoxycarbonyl, aryloxycarbonyl, nitrile, or carbamoyl of formula wherein R1 and R2 can be individually or simultaneously hydrogen, alkyl or part of a heterocyclic structure; Z can be hydrogen, halogen, alkyl, aryl, aryloxy or alkoxy group.
摘要翻译：制备通式I的四氢噻吩并[3,2-c]吡啶衍生物的方法：或其药学上可接受的盐，其中X的含义是式I和R 2的氢，羧基，烷氧基羰基，芳氧基羰基，腈或氨基甲酰基可以单独或同时地氢，烷基或部分杂环结构; Z可以是氢，卤素，烷基，芳基，芳氧基或烷氧基。

8. 发明申请

US20080009639A1 Preparation of oseltamivir phosphate (Tamiflu) and intermediates starting from D-glucose or D-xylose 审中-公开
标题翻译：从D-葡萄糖或D-木糖开始制备磷酸奥司他韦（Tamiflu）和中间体
公开(公告)号：US20080009639A1
公开(公告)日：2008-01-10
申请号：US11709658
申请日：2007-02-23
申请人： Bruno Konrad Radatus , K.S. Keshava Murthy , Gamini Weeratunga , Stephen E. Horne , Kiran Kumar Kothakonda , Eckardt C.G. Wolf , Zhongyi Wang
发明人： Bruno Konrad Radatus , K.S. Keshava Murthy , Gamini Weeratunga , Stephen E. Horne , Kiran Kumar Kothakonda , Eckardt C.G. Wolf , Zhongyi Wang
IPC分类号： C07C229/00 , C07C311/01 , C07D203/26 , C07D307/02 , C07F7/04 , C07F9/28
CPC分类号： C07C229/48 , C07C233/52 , C07C247/14 , C07C303/30 , C07C2601/16 , C07D203/26 , C07F7/1804 , C07F7/1892 , C07F9/65515 , C07F9/6561 , C07C309/73
摘要： Novel processes for the preparation of the anti-viral agent, Oseltamivir Phosphate and novel intermediates prepared in such processes. The novel processes use as starting materials D-glucose or D-xylose in the preparation of Oseltamivir Phosphate.
摘要翻译：用于制备抗病毒剂，奥司他韦磷酸盐和在这些方法中制备的新型中间体的新方法。该新方法在制备奥司他韦磷酸盐时用作原料D-葡萄糖或D-木糖。

9. 发明申请

US20100324298A1 Novel Process for the Preparation of Esomeprazole and Salts Thereof 失效
标题翻译：用于制备艾美拉唑及其盐的新方法
公开(公告)号：US20100324298A1
公开(公告)日：2010-12-23
申请号：US12855667
申请日：2010-08-12
申请人： Fan Wang , Laura Kaye Montemayor , Daqing Che , Stephen E. Horne
发明人： Fan Wang , Laura Kaye Montemayor , Daqing Che , Stephen E. Horne
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , Y02P20/55
摘要： A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.
摘要翻译：一种用于制备奥美拉唑及其对映异构体的新方法，例如艾美拉唑，以及相关的2-（2-吡啶基甲基 - 亚磺酰基）-1H-苯并咪唑（包括泮托拉唑，兰索拉唑和雷贝拉唑）作为受体或单一对映异构体的制备，并开发了它们的碱金属盐或碱金属盐。该新方法涉及令人惊奇的发现：在相应的硫化物氧化后，通过与烷基，芳基或氯甲酸烷基酯反应来保护游离碱性苯并咪唑亚砜（例如奥美拉唑或埃索美拉唑）消除了对其直接分离的需要。随后用碱金属或碱土金属醇溶液在C1-C4醇中除去保护基团直接提供相应的盐。通过消除处理游离碱性苯并咪唑亚砜的需要，与本领域中描述的方法相比，该有利的方法提供了增加的化学产率。

10. 发明申请

US20090182146A1 Process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3')quiniclidine hydrochloride 失效
标题翻译：顺式-2-甲基螺（1,3-氧硫杂环戊烷-5,3'）奎宁啶盐酸盐的制备和纯化方法
公开(公告)号：US20090182146A1
公开(公告)日：2009-07-16
申请号：US12007394
申请日：2008-01-10
申请人： Svetoslav S. Bratovanov , Elena Bejan , David A. Stradiotto , Abbulu Kante , Zhi-Xian Wang , Stephen E. Horne
发明人： Svetoslav S. Bratovanov , Elena Bejan , David A. Stradiotto , Abbulu Kante , Zhi-Xian Wang , Stephen E. Horne
IPC分类号： C07D497/20
CPC分类号： C07D497/20
摘要： An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine from a cisitrans mixture of isomers. Treatment of the mixture with an organic sulfonice acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3′)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.
摘要翻译：从异构体的顺式异构体混合物制备和纯化顺式-2-甲基螺（1,3-氧硫杂环戊烷-5,3'）奎宁啶的工业上可接受的方法。用有机磺酸处理混合物产生富含顺式异构体的较不溶性的酸加成盐。使用各种有机溶剂的重结晶或制浆允许通过过滤富集顺式异构体。根据本发明制备的2-甲基螺旋（1,3-氧硫杂环戊烷-5,3'）奎宁啶的顺式异构体的这些新的磺酸盐可以通过任何已知的方法进一步转化成盐酸盐，例如用碱，然后与盐酸形成盐酸盐或与盐酸交换磺酸盐。

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