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1. 发明授权

US06127402A 5-aroylpyrrol-2-ylmethylarene derivatives 失效
标题翻译： 5-芳酰基吡咯-2-基甲基芳烃衍生物
公开(公告)号：US06127402A
公开(公告)日：2000-10-03
申请号：US275540
申请日：1999-03-24
申请人： Denis J. Kertesz , Edvige Galeazzi Toscani , Deborah C. Reuter , Eric B. Sjogren
发明人： Denis J. Kertesz , Edvige Galeazzi Toscani , Deborah C. Reuter , Eric B. Sjogren
IPC分类号： C07D207/32 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/333 , C07D207/34 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D209/52 , A61K31/403
CPC分类号： C07D207/333 , C07D401/06 , C07D405/14 , C07D409/06 , C07D409/14
摘要： Compounds selected from the group of compounds represented by formula I: where:R.sub.10 is represented by the formula (A), (B), or (C): ##STR1## R.sub.20 is represented by the formula (U), (V), or (W): ##STR2## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts;are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.
摘要翻译：选自由式I表示的化合物的化合物：其中：R 10由式（A），（B）或（C）表示：R 20由式（U），（V）或（W ）：其它取代基如说明书中所定义; 及其药学上可接受的盐; 是前列腺素G / H合酶的抑制剂，是抗炎和止痛剂。

2. 发明授权

US5952368A 5-aroylpyrrol-2-ylmethylarene derivatives 失效
公开(公告)号：US5952368A
公开(公告)日：1999-09-14
申请号：US864703
申请日：1997-05-28
申请人： Denis J. Kertesz , Edvige Galeazzi Toscani , Deborah C. Reuter , Eric B. Sjogren
发明人： Denis J. Kertesz , Edvige Galeazzi Toscani , Deborah C. Reuter , Eric B. Sjogren
IPC分类号： C07D207/32 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/333 , C07D207/34 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14
CPC分类号： C07D207/333 , C07D401/06 , C07D405/14 , C07D409/06 , C07D409/14
摘要： Compounds selected from the group of compounds represented by formula I: ##STR1## where: R.sub.10 is represented by the formula (A), (B), or (C): ##STR2## R.sub.20 is represented by the formula (U), (V), or (W): ##STR3## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts; are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.

3. 发明授权

US5554612A 4-amino 6-substitutes mycophenolic acid and derivatives 失效
标题翻译： 4-氨基-6-取代霉酚酸及其衍生物
公开(公告)号：US5554612A
公开(公告)日：1996-09-10
申请号：US452243
申请日：1995-05-26
申请人： John W. Patterson , David Morgans, Jr. , Eric B. Sjogren , David B Smith , Francisco X. Talam as , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fern andez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
发明人： John W. Patterson , David Morgans, Jr. , Eric B. Sjogren , David B Smith , Francisco X. Talam as , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fern andez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
IPC分类号： A61K31/365 , A61K31/38 , A61K31/40 , A61K31/4025 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , C07D307/88 , C07D405/06 , C07D407/06 , C07D409/06 , A61K31/535 , C07D413/12
CPC分类号： C07D307/88
摘要： The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
摘要翻译：公开的霉酚酸衍生物是治疗针对霉酚酸和/或霉酚酸酯和其它免疫抑制剂的疾病状态的治疗剂。

4. 发明授权

US5380879A Derivatives of mycophenolic acid 失效
标题翻译：霉酚酸的衍生物
公开(公告)号：US5380879A
公开(公告)日：1995-01-10
申请号：US198817
申请日：1994-02-18
申请人： Eric B. Sjogren
发明人： Eric B. Sjogren
IPC分类号： C07D307/88 , A61K31/365 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , C07D307/80 , C07D405/12 , C07D417/12
CPC分类号： C07D405/12 , C07D307/80 , C07D417/12
摘要： The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
摘要翻译：公开的霉酚酸衍生物是治疗针对霉酚酸和/或霉酚酸酯和其它免疫抑制剂的疾病状态的治疗剂。

5. 发明授权

US4775752A Process and intermediates for beta-lactam antibiotics 失效
标题翻译： β-内酰胺抗生素的工艺和中间体
公开(公告)号：US4775752A
公开(公告)日：1988-10-04
申请号：US99032
申请日：1987-09-21
申请人： David A. Evans , Eric B. Sjogren
发明人： David A. Evans , Eric B. Sjogren
IPC分类号： C07D205/085 , C07D263/22 , C07D405/06 , C07D413/04 , C07D413/14 , C07D463/00 , C07D205/08 , C07B41/12
CPC分类号： C07D405/06 , C07D205/085 , C07D263/22 , C07D413/04 , C07D413/14
摘要： A process for preparing a .beta.-keto ester of the formula ##STR1## is provided which comprises cycloaddition of an (S)-4-aryloxazolidin-2-one-3-ylacetyl halide with an imine formed with a benzyl amine and an m-alkoxycinnamaldehyde to form the azetidinone ##STR2## hydrogenation of the azetidinone to the 4-[2-(m-alkoxyphenyl)-ethyl]substituted azetidinone; reduction of the hydrogenation product with Li-NH.sub.3 and t-butyl alcohol to form the 3-aminoazetidinone. ##STR3## and N-acylation of the 3-aminoazetidinone followed by ozonolysis of the cyclodiene group; wherein, e.g. alk, is methyl, Ar is phenyl and R.sub.1 is phenoxymethyl.
摘要翻译：提供了制备式“β”的β-酮酯的方法，其包括（S）-4-芳基恶唑烷-2-酮-3-基乙酰卤与由苄基胺形成的亚胺的环加成反应，烷氧基肉桂醛形成氮杂环丁酮将氮杂环丁酮氢化成4- [2-（间 - 烷氧基苯基） - 乙基]取代的氮杂环丁酮; 用Li-NH 3和叔丁醇还原氢化产物以形成3-氨基氮杂环丁酮。 3-氨基氮杂环丁酮的N-酰化反应，然后进行环二烯基的臭氧分解; 其中，例如烷基是甲基，Ar是苯基，R 1是苯氧基甲基。

6. 发明授权

US4665171A Process and intermediates for .beta.-lactam antibiotics 失效
标题翻译： β-内酰胺抗生素的工艺和中间体
公开(公告)号：US4665171A
公开(公告)日：1987-05-12
申请号：US755982
申请日：1985-07-17
申请人： David A. Evans , Eric B. Sjogren
发明人： David A. Evans , Eric B. Sjogren
IPC分类号： C07D471/04 , B01J23/00 , B01J23/46 , C07B53/00 , C07B61/00 , C07D205/08 , C07D205/085 , C07D263/22 , C07D263/24 , C07D401/04 , C07D405/06 , C07D413/04 , C07D413/14 , C07D463/00 , C07F9/653 , C07F9/6561 , C07F9/65
CPC分类号： C07D405/06 , C07D205/085 , C07D263/22 , C07D413/04 , C07D413/14 , C07D463/20
摘要： 1-Benzyl (or substituted benzyl)-3.beta.-[4(S)-aryloxazolidin-2-one-3-yl]-4.beta.-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic .beta.-lactam antibiotics.
摘要翻译： 1-苄基（或取代的苄基）-3β-[4（S） - 芳基恶唑烷-2-酮-3-基]-4β-（2-芳基乙烯基）氮杂环丁烷-2-酮通过环（4） S） - 芳基恶唑烷-2-酮-3-基乙酰卤和由苄胺和3-芳基丙烯醛形成的亚胺，例如肉桂醛。氮杂环丁酮是1-咔唑（1-脱氢）-3-羟基-3-头孢烯-4-羧酸和酯与单环β-内酰胺抗生素不对称合成中有用的手性中间体。

7. 发明授权

US06136844A 5-aroylpyrrol-2-ylmethylarene derivatives 失效
公开(公告)号：US06136844A
公开(公告)日：2000-10-24
申请号：US275542
申请日：1999-03-24
申请人： Denis J. Kertesz , Edvige Galeazzi Toscani , Deborah C. Reuter , Eric B. Sjogren
发明人： Denis J. Kertesz , Edvige Galeazzi Toscani , Deborah C. Reuter , Eric B. Sjogren
IPC分类号： C07D207/32 , A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D207/333 , C07D207/34 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14
CPC分类号： C07D207/333 , C07D401/06 , C07D405/14 , C07D409/06 , C07D409/14
摘要： Compounds selected from the group of compounds represented by formula I: ##STR1## where: R.sub.10 is represented by the formula (A), (B), or (C): ##STR2## R.sub.20 is represented by the formula (U), (V), or (W): ##STR3## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts;are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.

8. 发明授权

US5512568A Method of using 4-amino derivatives of 5-substituted mycophenolic acid 失效
标题翻译：使用5-取代霉酚酸的4-氨基衍生物的方法
公开(公告)号：US5512568A
公开(公告)日：1996-04-30
申请号：US198732
申请日：1994-02-18
申请人： David Morgans, Jr. , Eric B. Sjogren , David B. Smith , Francisco X. Talamas , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fernandez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , John W. Patterson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
发明人： David Morgans, Jr. , Eric B. Sjogren , David B. Smith , Francisco X. Talamas , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fernandez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , John W. Patterson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
IPC分类号： A61K31/34 , A61K31/365 , A61K31/38 , A61K31/40 , A61K31/4025 , A61P17/00 , A61P29/00 , A61P37/06 , C07D307/88 , C07D405/06 , C07D407/06 , C07D409/06 , A61K31/535
CPC分类号： C07D405/06 , C07D307/88 , C07D407/06 , C07D409/06
摘要： The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
摘要翻译：公开的霉酚酸衍生物是治疗针对霉酚酸和/或霉酚酸酯和其它免疫抑制剂的疾病状态的治疗剂。

9. 发明授权

US5034410A Anthelmintically active benzenepropanamide derivatives 失效
标题翻译：驱虫活性苯丙酰胺衍生物
公开(公告)号：US5034410A
公开(公告)日：1991-07-23
申请号：US420076
申请日：1989-10-11
申请人： Eric B. Sjogren , Michael A. Rider
发明人： Eric B. Sjogren , Michael A. Rider
IPC分类号： C07C255/41 , C07C255/57 , C07C255/60 , C07C327/40
CPC分类号： C07C255/41 , C07C255/57 , C07C255/60 , C07C327/40
摘要： This invention is directed to a method for treating helminthiasis in an animal which method comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of the Formula (I): ##STR1## wherein Z is oxygen or sulfur;R.sup.1 is hydrogen or lower alkyl; andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen, halo, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, cyano, halophenoxy, haloalkylphenoxy, thiocyano or isothiocyano, provided that R.sup.2 and R.sup.3 cannot simultaneously be hydrogen and that R.sup.4 and R.sup.5 cannot simultaneously be hydrogen; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions formulated therewith. This invention is also directed to novel anthelmintically active benzenepropanamides of Formula (I) wherein Z is oxygen.
摘要翻译：本发明涉及一种治疗动物蠕虫病的方法，该方法包括向有需要的动物施用驱肠虫有效量的式（I）化合物：其中Z为氧或硫; R1是氢或低级烷基; R2和R3独立地为氢，卤素，低级卤代烷基，低级烷氧基，低级卤代烷氧基，硝基，氰基，卤代苯氧基，卤代烷基苯氧基，硫代氰基或异硫氰基，条件是R2和R3不能同时为氢，R4和R5不能同时是氢; 或其药学上可接受的盐，以及用其配制的药物组合物。本发明还涉及其中Z是氧的式（I）的新型驱虫活性苯丙酰胺。

10. 发明授权

US4734495A Process and intermediates for beta-lactam antibiotics 失效
标题翻译： β-内酰胺抗生素的工艺和中间体
公开(公告)号：US4734495A
公开(公告)日：1988-03-29
申请号：US13521
申请日：1987-02-11
申请人： David A. Evans , Eric B. Sjogren
发明人： David A. Evans , Eric B. Sjogren
IPC分类号： C07D205/085 , C07D263/22 , C07D405/06 , C07D413/04 , C07D413/14 , C07D463/00 , C07D205/08 , C07D409/14
CPC分类号： C07D405/06 , C07D205/085 , C07D263/22 , C07D413/04 , C07D413/14
摘要： 1-Benzyl(or substituted benzyl)-3.beta.-[4(S)-aryloxazolidin-2-one-3-yl]-4.beta.-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic .beta.-lactam antibiotics.
摘要翻译： 1-苄基（或取代的苄基）-3β-[4（S） - 芳基恶唑烷-2-酮-3-基]-4β-（2-芳基乙烯基）氮杂环丁烷-2-酮通过环（4） S） - 芳基恶唑烷-2-酮-3-基乙酰卤和由苄胺和3-芳基丙烯醛形成的亚胺，例如肉桂醛。氮杂环丁酮是1-咔唑（1-脱氢）-3-羟基-3-头孢烯-4-羧酸和酯与单环β-内酰胺抗生素不对称合成中有用的手性中间体。

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