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1. 发明授权

US4424355A Resolution of substituted dibenzo�b,f!thiepin-3-carboxylic acid-5-oxides with brucine or ephedrine 失效
标题翻译：取代二苯并[b，f]硫杂-3-羧酸-5-氧化物与布鲁丁或麻黄碱的拆分
公开(公告)号：US4424355A
公开(公告)日：1984-01-03
申请号：US351708
申请日：1982-02-24
申请人： Patrice C. Belanger , Haydn W. R. Williams , Joshua Rokach
发明人： Patrice C. Belanger , Haydn W. R. Williams , Joshua Rokach
IPC分类号： C07D337/14 , C07D405/14
CPC分类号： C07D337/14 , Y02P20/582
摘要： The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo�b,f!thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with brucine or ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer. The compounds obtained in high yield by this process are highly active prostaglandin antagonists which are useful in treating a variety of conditions such as allergic asthma.
摘要翻译：本发明涉及一种制备具有结构式“IMAGE”II的（ - ）7或8-氟二苯并[b，f]硫杂-3-羧酸-5-氧化物的高活性光学异构体的改进方法，其中氟取代基取代7或8位的氢。由式II表示的两种活性异构体是S（ - ）7-氟二苯并[b，f]硫杂-3-羧酸-5-氧化物和R（ - ）8-氟二苯并[b，f]硫杂-3-羧酸 -5-氧化物。特别关注外消旋的7或8氟二苯并[b，f]硫杂环庚烷-3-羧酸-5-氧化物的拆分，首先通过与酪氨酸或麻黄碱的盐形成形成和分离所述外消旋羧酸的非对映异构体，随后结晶并再生所需的（ - ）异构体并通过再生异构体的外消旋再循环（+）异构体。通过该方法以高产率获得的化合物是可用于治疗多种病症如过敏性哮喘的高活性前列腺素拮抗剂。

2. 发明授权

US4435579A Resolution of substituted dibenzo[b,f]thiepin-3-carboxylic acid-5-oxides with ephedrine 失效
标题翻译：取代二苯并[b，f]硫杂-3-羧酸-5-氧化物与麻黄碱的拆分
公开(公告)号：US4435579A
公开(公告)日：1984-03-06
申请号：US397253
申请日：1982-07-12
申请人： Patrice C. Belanger , Haydn W. R. Williams , Joshua Rokach
发明人： Patrice C. Belanger , Haydn W. R. Williams , Joshua Rokach
IPC分类号： C07D337/14
CPC分类号： C07D337/14
摘要： The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer. The compounds obtained in high yield by this process are highly active prostaglandin antagonists which are useful in treating a variety of conditions such as allergic asthma.
摘要翻译：本发明涉及一种制备具有结构式“IMAGE”II的（ - ）7或8-氟二苯并[b，f]硫杂-3-羧酸-5-氧化物的高活性光学异构体的改进方法，其中氟取代基取代7或8位的氢。由式II表示的两种活性异构体是S（ - ）7-氟二苯并[b，f]硫杂-3-羧酸-5-氧化物和R（ - ）8-氟二苯并[b，f]硫杂-3-羧酸 -5-氧化物。特别关注外消旋的7或8氟二苯并[b，f]硫杂-3-羧酸-5-氧化物的拆分，首先通过与麻黄碱形成盐形成和分离所述外消旋羧酸的非对映异构体，随后结晶和再生的所需（ - ）异构体，并通过再生异构体的外消旋再循环（+）异构体。通过该方法以高产率获得的化合物是可用于治疗多种病症如过敏性哮喘的高活性前列腺素拮抗剂。

3. 发明授权

US4453005A Process for preparing substituted phenylalkenoic acids 失效
标题翻译：取代苯基烯酸的制备方法
公开(公告)号：US4453005A
公开(公告)日：1984-06-05
申请号：US446910
申请日：1982-12-06
申请人： Patrice C. Belanger , Claude Dufresne , John W. Gillard , Haydn W. R. Williams
发明人： Patrice C. Belanger , Claude Dufresne , John W. Gillard , Haydn W. R. Williams
IPC分类号： C07C57/42 , C07C57/60 , C07C59/84 , C07C59/88 , C07C59/90 , C07C63/33
CPC分类号： C07C59/84 , C07C57/42 , C07C57/60 , C07C59/88 , C07C59/90
摘要： Substituted phenylalkenoic acids and esters of the formula: ##STR1## having useful pharmaceutical activity and processes for their preparation are disclosed.
摘要翻译：公开了具有有用的药物活性的取代的苯基烯酸和下式的具有下式的酯：＆lt; IMAGE＆gt;其制备方法。

4. 发明授权

US4448786A 4-Naphthyl and substituted naphthyl-3-hydroxy-3-pyrroline-2,5-diones and their use as inhibitors of glycolic acid oxidase 失效
标题翻译： 4-萘基和取代的萘基-3-羟基-3-吡咯啉-2,5-二酮及其作为乙醇酸氧化酶抑制剂的用途
公开(公告)号：US4448786A
公开(公告)日：1984-05-15
申请号：US392191
申请日：1982-06-25
申请人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
发明人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
IPC分类号： C07D207/44 , C07D207/456 , C07D321/10 , C07D207/416 , A61K31/40 , C07D405/10
CPC分类号： C07D207/456 , C07D321/10 , Y10S514/877 , Y10S514/891
摘要： Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
摘要翻译：公开了新的4-取代-3-羟基-3-吡咯啉-2,5-二酮，其抑制乙醇酸氧化酶，因此可用于治疗和预防草酸钙肾结石形成。还公开了一种新的制备方法。

5. 发明授权

US4428956A 4-Hydroxy-5-substituted-3-(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis 失效
标题翻译：用于治疗尿路草酸钙结石症的4-羟基-5-取代-3-（2H） - 异噻唑酮-1,1-二氧化物衍生物
公开(公告)号：US4428956A
公开(公告)日：1984-01-31
申请号：US221173
申请日：1980-12-29
申请人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
发明人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
IPC分类号： C07D275/02 , C07D275/03 , A61K31/44
CPC分类号： C07D275/03 , C07C309/00 , Y10S514/878 , Y10S514/891
摘要： 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and n is 0 or 1;or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
摘要翻译：具有下式的4-羟基-5-取代-3（2H） - 异噻唑酮-1,1-二氧化物衍生物：其中X和Y独立地选自氢，卤素和C1 -6烷基; 取代的苯基部分的位置2和6可以不被取代; 并且n为0或1; 或其药学上可接受的盐; 可用于治疗尿道，特别是肾性草酸钙结石。

6. 发明授权

US4249021A Indanacetic acid compounds 失效
标题翻译：茚满乙酸化合物
公开(公告)号：US4249021A
公开(公告)日：1981-02-03
申请号：US15095
申请日：1979-02-26
申请人： Edward J. Cragoe, Jr. , Haydn W. R. Williams , Otto W. Woltersdorf, Jr.
发明人： Edward J. Cragoe, Jr. , Haydn W. R. Williams , Otto W. Woltersdorf, Jr.
IPC分类号： C07C59/88
CPC分类号： C07C59/88 , Y10S514/869
摘要： Substituted 1-oxo-2,2-disubstituted-5-indanacetic acids and their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity.
摘要翻译：公开了取代的1-氧代-2,2-二取代-5-二氢茚酸及其盐，酯和酰胺。该产品显示出双重药物效用，因为它们具有利尿，盐析和尿酸活性。

7. 发明授权

US4432992A 4-[5(and 4)-Substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase 失效
标题翻译：乙醇酸氧化酶的4- [5（和4） - 取代-2-噻吩基] -3-羟基-3-吡咯啉-2,5-二酮抑制剂
公开(公告)号：US4432992A
公开(公告)日：1984-02-21
申请号：US91448
申请日：1979-11-05
申请人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
发明人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
IPC分类号： C07D333/22 , C07D333/24 , C07D409/04
CPC分类号： C07D409/04 , C07D333/22 , C07D333/24 , Y10S514/891
摘要： Novel 4-[5(and 4)-substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
摘要翻译：公开了新的4- [5（和4） - 取代-2-噻吩基] -3-羟基-3-吡咯啉-2,5-二酮，其抑制乙醇酸氧化酶，因此可用于治疗和预防草酸钙石块形成。还公开了一种新的制备方法。

8. 发明授权

US4431652A 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis 失效
标题翻译：用于治疗尿路草酸钙结石症的4-羟基-5-取代-3（2H） - 异噻唑酮-1,1-二氧化物衍生物
公开(公告)号：US4431652A
公开(公告)日：1984-02-14
申请号：US221172
申请日：1980-12-29
申请人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
发明人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
IPC分类号： C07D277/22 , C07D277/26 , C07D417/04 , A61K31/44 , C07D275/02
CPC分类号： C07D277/22 , C07D277/26 , C07D417/04 , Y10S514/877 , Y10S514/891
摘要： 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted by C.sub.3-6 alkyl; or a pharmaceutically acceptable salt thereof;useful in treating urinary tract, especially renal calcium oxalate lithiasis.
摘要翻译：具有下式的4-羟基-5-取代-3（2H） - 异噻唑酮-1,1-二氧化物衍生物：其中X和Y独立地选自氢，卤素和 C 1-6烷基; 取代的苯基部分的位置2和6不能被C 3-6烷基取代; 或其药学上可接受的盐; 可用于治疗尿道，特别是肾性草酸钙结石。

9. 发明授权

US4256758A 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase 失效
标题翻译： 4-取代的3-羟基-3-吡咯啉-2,5-二酮抑制剂的乙醇酸氧化酶
公开(公告)号：US4256758A
公开(公告)日：1981-03-17
申请号：US47413
申请日：1979-06-11
申请人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
发明人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
IPC分类号： A61K31/40 , A61K31/4015 , A61P13/02 , A61P15/00 , C07C45/46 , C07D207/44 , C07D207/456 , C07D207/40 , C07D207/416
CPC分类号： C07D207/456 , C07C45/46 , Y10S514/891
摘要： Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
摘要翻译：公开了新的4-取代-3-羟基-3-吡咯啉-2,5-二酮，其抑制乙醇酸氧化酶，因此可用于治疗和预防草酸钙肾结石。

10. 发明授权

US4537902A 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase 失效
标题翻译： 4-取代的3-羟基-3-吡咯啉-2,5-二酮抑制剂的乙醇酸氧化酶
公开(公告)号：US4537902A
公开(公告)日：1985-08-27
申请号：US47412
申请日：1979-06-11
申请人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
发明人： Edward J. Cragoe, Jr. , Clarence S. Rooney , Haydn W. R. Williams
IPC分类号： C07D207/44 , C07D207/456 , C07D403/10 , C07D403/02 , A61K31/40 , C07D207/40
CPC分类号： C07D207/456 , C07D403/10
摘要： Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
摘要翻译：公开了新的4-取代-3-羟基-3-吡咯啉-2,5-二酮，其抑制乙醇酸氧化酶，因此可用于治疗和预防草酸钙肾结石。

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