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1. 发明授权

US5529995A Aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE 失效
标题翻译：氨基乙酰巯基衍生物可用作脑啡肽酶和ACE的抑制剂
公开(公告)号：US5529995A
公开(公告)日：1996-06-25
申请号：US397294
申请日：1995-03-01
申请人： Gary A. Flynn , Robert J. Cregge , Thomas L. Fevig , Shyam Sunder , Patrick W. Shum
发明人： Gary A. Flynn , Robert J. Cregge , Thomas L. Fevig , Shyam Sunder , Patrick W. Shum
IPC分类号： C07D487/04 , A61K31/55 , A61K38/00 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/04 , A61P29/00 , A61P43/00 , C07D471/04 , C07D498/04 , C07D513/04 , C07K5/078 , C12N9/99 , A61K31/35 , C07D495/06
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.
摘要翻译：本发明涉及可用作脑啡肽酶和ACE抑制剂的新型氨基乙酰巯基衍生物。

2. 发明授权

US5488048A Aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ace 失效
公开(公告)号：US5488048A
公开(公告)日：1996-01-30
申请号：US396999
申请日：1995-03-01
申请人： Gary A. Flynn , Robert J. Cregge , Thomas L. Fevig , Shyam Sunder , Patrick W. Shum
发明人： Gary A. Flynn , Robert J. Cregge , Thomas L. Fevig , Shyam Sunder , Patrick W. Shum
IPC分类号： C07D487/04 , A61K31/55 , A61K38/00 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/04 , A61P29/00 , A61P43/00 , C07D471/04 , C07D498/04 , C07D513/04 , C07K5/078 , C12N9/99
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.

3. 发明授权

US6140511A Fungicidal compositions and methods of making thereof 有权
标题翻译：杀真菌组合物及其制备方法
公开(公告)号：US6140511A
公开(公告)日：2000-10-31
申请号：US326225
申请日：1999-06-04
申请人： Wendell G. Phillips , Michael K. Mao , Chun Ma , Thomas L. Fevig
发明人： Wendell G. Phillips , Michael K. Mao , Chun Ma , Thomas L. Fevig
IPC分类号： A01N43/10 , A01N55/00 , A01N55/10 , A01P3/00 , C07D333/38 , C07F7/08 , C07D333/30
CPC分类号： C07F7/083 , C07D333/38 , C07F7/0814
摘要： The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I) shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg. Therefore, the compounds having Formula (III): ##STR1## or an agronomic salts and compositions thereof are expected to provide such control as well; wherein:Q is --NH, S, or O;W is O, or S;X is --OH, --OAc, --OR, where R is lower alkyl;Y is S, O, or --NH;Z is --Si(R).sub.3, --C(R).sub.3, where R is lower alkyl;R.sub.1 is a lower alkyl, allyl, or propargyl;R.sub.2 is a lower alkyl or aryl; andR.sub.3 and R.sub.4 are independently chosen from hydrogen, a lower alkyl and aryl;optionally, R.sub.2 and R.sub.3 together form a 5- or 6-membered ring.
摘要翻译：杀真菌化合物4,5-二甲基-N-2-丙烯基-2-（三甲基甲硅烷基）-3-噻吩甲酰胺（式（I））显示出对土壤真菌Gaeumannomyces graminis（Gg）的生长的优异和意想不到的控制。本发明提供用于合成使用化合物4-羟基-4,5-二甲基-2-三甲基硅烷基 - 二氢噻吩-3-甲酸烯丙基酰胺（式（II））的式（I）化合物的新化合物以及新颖的此外，意外地发现式（II）本身提供了对Gg的控制。因此，具有式（III）的化合物或其农艺盐及其组合物也预期也提供这样的控制; 其中：Q是-NH，S或O; W是O或S; X是-OH，-OAc，-OR，其中R是低级烷基; Y是S，O或-NH; Z是-Si （R）3，-C（R）3，其中R是低级烷基; R 1是低级烷基，烯丙基或炔丙基; R 2是低级烷基或芳基; R 3和R 4独立地选自氢，低烷基和芳基; 任选地，R 2和R 3一起形成5-或6-元环。

4. 发明授权

US5962469A Cyclic nitrones 失效
标题翻译：环状硝酮
公开(公告)号：US5962469A
公开(公告)日：1999-10-05
申请号：US978971
申请日：1997-11-26
申请人： Craig E. Thomas , Thomas L. Fevig , Stephen M. Bowen , Robert A. Farr , Albert A. Carr , David A. Janowick
发明人： Craig E. Thomas , Thomas L. Fevig , Stephen M. Bowen , Robert A. Farr , Albert A. Carr , David A. Janowick
IPC分类号： A61K31/00 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4427 , A61K31/4436 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/4747 , A61K31/55 , A61P39/00 , A61P39/06 , C07D209/44 , C07D217/08 , C07D217/24 , C07D221/10 , C07D221/20 , C07D223/14 , C07D223/16 , C07D491/04 , C07D491/048 , C07D491/10 , C07D491/107 , C07D495/04 , C07D221/06 , C07D491/02
CPC分类号： C07D221/20 , C07D209/44 , C07D217/08 , C07D217/24 , C07D221/10 , C07D223/14 , C07D223/16 , C07D491/04 , C07D491/10 , C07D495/04
摘要： The present invention is directed to novel cyclic nitrones and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in which radicals either damage or destroy tissues via oxidation, and pharmaceutical compositions containing these cyclic nitrones.
摘要翻译：本发明涉及新的环状硝酮及其用于预防自由基的氧化组织损伤，其用于治疗许多疾病状态，其中自由基通过氧化损伤或破坏组织，以及含有这些的药物组合物环状硝酮。

5. 发明授权

US5424425A Aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ace 失效
标题翻译：可用作脑啡肽酶抑制剂的氨基乙酰巯基衍生物
公开(公告)号：US5424425A
公开(公告)日：1995-06-13
申请号：US119924
申请日：1993-09-10
申请人： Gary A. Flynn , Robert J. Cregge , Thomas L. Fevig , Shyam Sunder , Patrick W. Shum
发明人： Gary A. Flynn , Robert J. Cregge , Thomas L. Fevig , Shyam Sunder , Patrick W. Shum
IPC分类号： C07D487/04 , A61K31/55 , A61K38/00 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/04 , A61P29/00 , A61P43/00 , C07D471/04 , C07D498/04 , C07D513/04 , C07K5/078 , C12N9/99 , A61K38/55
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.
摘要翻译：本发明涉及可用作脑啡肽酶和ACE抑制剂的新型氨基乙酰巯基衍生物。

6. 发明授权

US06291513B1 Fungicidal compositions and methods of making thereof 有权
标题翻译：杀真菌组合物及其制备方法
公开(公告)号：US06291513B1
公开(公告)日：2001-09-18
申请号：US09609211
申请日：2000-07-05
申请人： Wendell G. Phillips , Michael K. Mao , Chun Ma , Thomas L. Fevig
发明人： Wendell G. Phillips , Michael K. Mao , Chun Ma , Thomas L. Fevig
IPC分类号： A01N4306
CPC分类号： C07F7/083 , C07D333/38 , C07F7/0814
摘要： The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I)) has shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg. Therefore, the compounds having Formula (III): or an agronomic salts and compositions thereof are expected to provide such control as well; wherein: Q is —NH, S, or O; W is O, or S; X is —OH, —OAc, —OR, where R is lower alkyl; Y is S, O, or —NH; Z is —Si(R)3, —C(R)3, where R is lower alkyl; R1 is a lower alkyl, allyl, or propargyl; R2 is a lower alkyl or aryl; and R3 and R4 are independently chosen from hydrogen, a lower alkyl and aryl; optionally, R2 and R3 together form a 5- or 6-membered ring.
摘要翻译：杀真菌化合物4,5-二甲基-N-2-丙烯基-2-（三甲基甲硅烷基）-3-噻吩甲酰胺（式（I））显示出对土壤真菌Gaeumannomyces graminis（Gg）生长的优异和意想不到的控制，。本发明提供用于合成式（I）的化合物的新型化合物，其使用化合物4-羟基-4,5-二甲基-2-三甲基硅烷基 - 二氢噻吩-3-甲酸烯丙基酰胺（式（II））以及合成烯丙基酰胺的新型化合物。此外，公式（II）本身意外地被发现提供了GG的控制。因此，具有式（III）的化合物或其农艺盐及其组合物预期也提供这种控制; 其中：Q是-NH，S或O; W是O或S; X是-OH，-OAc，-OR，其中R是低级烷基; Y是S，O或-NH; Z是-Si （R）3，-C（R）3，其中R是低级烷基; R 1是低级烷基，烯丙基或炔丙基; R 2是低级烷基或芳基; R 3和R 4独立地选自氢，低级烷基和芳基;任选地，R 2和R 3一起形成5-或6-元环。

7. 发明授权

US6084108A Synthesis of 3-carbomethoxy-4,5-dimethylthiophene 有权
标题翻译： 3-甲酯基-4,5-二甲基噻吩的合成
公开(公告)号：US6084108A
公开(公告)日：2000-07-04
申请号：US170441
申请日：1998-10-13
申请人： Thomas L. Fevig , Patrick H. Lau , Wendell G. Phillips
发明人： Thomas L. Fevig , Patrick H. Lau , Wendell G. Phillips
IPC分类号： C07D333/32 , C07D333/38 , C07D333/40 , C07D333/60 , C07D333/56
CPC分类号： C07D333/38 , C07D333/32 , C07D333/40
摘要： Fungicides having thiophene rings may be made from the intermediate compound 3-carbomethoxy-4,5-dimethylthiophene. That compound, and related compounds, may be produced by reacting an alpha mercaptoketone, e.g., 3-mercapto-2-butanone, with an acrylate, e.g., methyl-3-methoxy acrylate, in the presence of an alkoxide base, e.g., NaOMe, to form the substituted tetrahydrothiophene, followed by conversion to the aromatic thiophene with an acid treatment. The substituted tetrahydrothiophene is a novel compound.
摘要翻译：具有噻吩环的杀真菌剂可以由中间体化合物3-甲酯基-4,5-二甲基噻吩制备。该化合物和相关化合物可以通过使α-巯基酮（例如3-巯基-2-丁酮）与丙烯酸酯例如甲基-3-甲氧基丙烯酸酯在醇盐碱例如NaOMe 形成取代的四氢噻吩，然后用酸处理转化成芳香族噻吩。取代的四氢噻吩是一种新型化合物。

8. 发明授权

US6037478A Synthesis of 3-carbomethoxy-4,5-dimethylthiophene 有权
公开(公告)号：US6037478A
公开(公告)日：2000-03-14
申请号：US394760
申请日：1999-09-13
申请人： Thomas L. Fevig , Patrick H. Lau , Wendell G. Phillips
发明人： Thomas L. Fevig , Patrick H. Lau , Wendell G. Phillips
IPC分类号： C07D333/32 , C07D333/38 , C07D333/40 , C07D333/60 , C07D333/26
CPC分类号： C07D333/38 , C07D333/32 , C07D333/40
摘要： Fungicides having thiophene rings may be made from the intermediate compound 3-carbomethoxy-4,5-dimethylthiophene. That compound, and related compounds, may be produced by reacting an alpha mercaptoketone, e.g., 3-mercapto-2-butanone, with an acrylate, e.g., methyl-3-methoxy acrylate, in the presence of an alkoxide base, e.g., NaOMe, to form the substituted tetrahydrothiophene, followed by conversion to the aromatic thiophene with an acid treatment. The substituted tetrahydrothiophene is a novel compound.

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