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31. 发明授权

US4258054A Hydantoin derivatives as therapeutic agents 失效
标题翻译：乙内酰脲衍生物作为治疗剂
公开(公告)号：US4258054A
公开(公告)日：1981-03-24
申请号：US71871
申请日：1979-09-04
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： A61K31/415 , C07D235/02 , C07D311/22 , C07D487/10 , C07D491/10 , C07D495/10
CPC分类号： C07D235/02 , C07C323/00 , C07D311/22 , C07D487/10 , C07D491/10 , C07D495/10
摘要： A series of spiro-hydantoin compounds has been prepared by condensing the appropriate carbonyl ring compound, such as the corresponding 1-indanone, 1-tetralone, 4-chromanone, thiochroman-4-one, 7,8-dihydroquinolin-5(6H)-one, 6,7-dihydropyrindin-5(5H)-one, thiondane-3-one-1,1-dioxide and 4-oxoisothiochroman-2,2-dioxide, respectively, with potassium cyanide and ammonium carbonate. The resulting hydantoin derivatives are found to be useful in preventing or alleviating chronic diabetic complications. Preferred member compounds include spiro-[imidazolidine-4,1'-indan]-2,5-dione, 6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6-chloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,7-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,8-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6'-fluoro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione and 6',7'-dichloro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione.
摘要翻译：通过将适当的羰基环化合物如相应的1-二氢茚酮，1-四氢萘酮，4-苯并二氢吡喃酮，二氢苯并噻喃-4-酮，7,8-二氢喹啉-5（6H）（5H） - 酮，硫杂环戊烷-3-酮-1,1-二氧化物和4-氧代异硫苯并二氢吡喃-2,2-二氧化物分别与氰化钾和碳酸铵反应。发现所得乙内酰脲衍生物可用于预防或缓解慢性糖尿病并发症。优选的成员化合物包括螺 - [咪唑烷-4,1'-二氢化茚] -2,5-二酮，6-氟 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮， 2-氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，6,7-二氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮， 6,8-二氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，6'-氟 - 螺 - [咪唑烷-4,4'-二氢苯并噻喃] -2,5-二酮和6'，7'-二氯 - 螺 - [咪唑烷-4,4'-二氢苯并噻喃] -2,5-二酮。

32. 发明授权

US4235911A Hydantoin derivatives 失效
标题翻译：乙内酰脲衍生物
公开(公告)号：US4235911A
公开(公告)日：1980-11-25
申请号：US48004
申请日：1979-06-13
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： A61K31/435 , A61K31/47 , A61P3/08 , A61P25/02 , A61P27/02 , C07D471/10 , C07D471/20
CPC分类号： C07D471/10
摘要： A series of novel tetrahydroquinoline-derived spiro-hydantoin compounds has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Preferred member compounds include 1'-methyl-1',2',3',4'-tetrahydro- spiro-[imidazolidine-4,4'-quinoline]-2,5-dione, 6'-chloro-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5-dione, 7'-chloro-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5-dione and 1'-methyl-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-pyrido(2,3-b)pyridine]-2,5-dione. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的四氢喹啉衍生的螺 - 乙内酰脲化合物，包括其药学上可接受的酸加成盐。这些特定化合物可用于治疗某些慢性糖尿病并发症的醛糖还原酶抑制剂。优选的成员化合物包括1'-甲基-1'，2'，3'，4'-四氢 - 螺 - [咪唑烷-4,4'-喹啉] -2,5-二酮，6'-氯-1' 2'，3'，4'-四氢 - 螺 - [咪唑烷-4,4'-喹啉] -2,5-二酮，7'-氯-1'，2'，3'，4'-四氢 - 螺 - [咪唑烷-4,4'-喹啉] -2,5-二酮和1'-甲基-1'，2'，3'，4'-四氢 - 螺 - [咪唑烷-4,4'-吡啶并（2 ，b）吡啶] -2,5-二酮。提供了从已知原料制备这些化合物的方法。

33. 发明授权

US4210756A Tetrahydroquinoline hydantoins for chronic diabetic complications 失效
标题翻译：四氢喹啉乙内酰脲用于慢性糖尿病并发症
公开(公告)号：US4210756A
公开(公告)日：1980-07-01
申请号：US961256
申请日：1978-11-16
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： C07D235/02 , C07D311/22 , C07D487/10 , C07D491/10 , C07D495/10
CPC分类号： C07D235/02 , C07C323/00 , C07D311/22 , C07D487/10 , C07D491/10 , C07D495/10
摘要： A series of spiro-hydantoin compounds has been prepared by condensing the appropriate carbonyl ring compound, such as the corresponding 1-indanone, 1-tetralone, 4-chromanone, thiochroman-4-one, 7,8-dihydroquinolin-5(6H)-one, 6,7-dihydropyridin-5(5H)-one, thiondane-3-one-1,1-dioxide and 4-oxoisothiochroman-2,2-dioxide, respectively, with potassium cyanide and ammonium carbonate. The resulting hydantoin derivatives are found to be useful in preventing or alleviating chronic diabetic complications. Preferred member compounds include spiro-[imidazolidine-4,1'-indan]-2,5-dione, 6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6-chloro-spiro-[chroman-4,4'-imidazolidine]-2',5.dbd.-dione, 6,7-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,8-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6'-fluoro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione and 6',7'-dichloro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione.
摘要翻译：通过将适当的羰基环化合物如相应的1-二氢茚酮，1-四氢萘酮，4-苯并二氢吡喃酮，二氢苯并噻喃-4-酮，7,8-二氢喹啉-5（6H） - 酮，6,7-二氢吡啶-5（5H） - 酮，硫杂环丁烷-3-酮-1,1-二氧化物和4-氧代异硫苯并二氢吡喃-2,2-二氧化物分别与氰化钾和碳酸铵反应。发现所得乙内酰脲衍生物可用于预防或缓解慢性糖尿病并发症。优选的成员化合物包括螺 - [咪唑烷-4,1'-二氢化茚] -2,5-二酮，6-氟 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮， 5-氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5 =二酮，6,7-二氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮， 6,8-二氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，6'-氟 - 螺 - [咪唑烷-4,4'-二氢苯并噻喃] -2,5-二酮和6'，7'-二氯 - 螺 - [咪唑烷-4,4'-二氢苯并噻喃] -2,5-二酮。

34. 发明授权

US4210667A Pharmaceutical preparations containing coumarin carboxylic acid derivatives 失效
标题翻译：含香豆素羧酸衍生物的药物制剂
公开(公告)号：US4210667A
公开(公告)日：1980-07-01
申请号：US31564
申请日：1979-04-19
申请人： Reinhard Sarges , John L. Belletire , Rodney C. Schnur
发明人： Reinhard Sarges , John L. Belletire , Rodney C. Schnur
IPC分类号： A61K31/37
CPC分类号： A61K31/37
摘要： Preparations useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. The preparations contain substituted and unsubstituted coumarin-4-carboxylic or acetic acid derivatives as the active ingredients.
摘要翻译：公开了用作醛糖还原酶抑制剂和用作治疗慢性糖尿病并发症的治疗剂的制剂。制剂含有取代和未取代的香豆素-4-羧酸或乙酸衍生物作为活性成分。

35. 发明授权

US4209630A Hydantoin derivatives as therapeutic agents 失效
标题翻译：乙内酰脲衍生物作为治疗剂
公开(公告)号：US4209630A
公开(公告)日：1980-06-24
申请号：US923105
申请日：1978-07-10
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： C07D235/02 , C07D311/22 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D495/10
CPC分类号： C07D235/02 , C07C323/00 , C07D311/22 , C07D487/10 , C07D491/10 , C07D495/10
摘要： A series of spiro-hydantoin compounds has been prepared by condensing the appropriate carbonyl ring compound, such as the corresponding 1-indanone, 1-tetralone, 4-chromanone, thiochroman-4-one, 7,8-dihydroquinolin-5(6H)-one, 6,7-dihydropyrindin-5(5H)-one, thiondane-3-one-1,1-dioxide and 4-oxoisothiochroman-2,2-dioxide, respectively, with potassium cyanide and ammonium carbonate. The resulting hydantoin derivatives are found to be useful in preventing or alleviating chronic diabetic complications. Preferred member compounds include spiro-[imidazolidine-4,1'-indan]-2,5-dione, 6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6-chloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,7-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6,8-dichloro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione, 6'-fluoro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione and 6',7'-dichloro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione.
摘要翻译：通过将适当的羰基环化合物如相应的1-二氢茚酮，1-四氢萘酮，4-苯并二氢吡喃酮，二氢苯并噻喃-4-酮，7,8-二氢喹啉-5（6H）（5H） - 酮，硫杂环戊烷-3-酮-1,1-二氧化物和4-氧代异硫苯并二氢吡喃-2,2-二氧化物分别与氰化钾和碳酸铵反应。发现所得乙内酰脲衍生物可用于预防或缓解慢性糖尿病并发症。优选的成员化合物包括螺 - [咪唑烷-4,1'-二氢化茚] -2,5-二酮，6-氟 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮， 2-氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，6,7-二氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮， 6,8-二氯 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，6'-氟 - 螺 - [咪唑烷-4,4'-二氢苯并噻喃] -2,5-二酮和6'，7'-二氯 - 螺 - [咪唑烷-4,4'-二氢苯并噻喃] -2,5-二酮。

36. 发明授权

US3961065A Benzenesulfonylurea derivatives 失效
标题翻译：苯磺酰脲衍生物
公开(公告)号：US3961065A
公开(公告)日：1976-06-01
申请号：US545741
申请日：1975-01-30
申请人： Donald E. Kuhla , Reinhard Sarges
发明人： Donald E. Kuhla , Reinhard Sarges
IPC分类号： A61K31/455
CPC分类号： A61K31/455 , C07C2101/14 , C07C2102/42 , Y10S514/866
摘要： Certain novel benzenesulfonylurea compounds derived from a nitrogen-containing carboxylic acid have been prepared by reacting an appropriate sulfonamide with an organic isocyanate or a tri-substituted urea equivalent thereof. The sulfonylureas so obtained are useful in therapy as oral hypoglycemic agents. Typical members include those compounds derived from 2-methoxy-nicotinic acid, of which 1-cyclohexyl-3-{4-[2-(5-bromo-2-methoxynicotinamido)ethyl]benzenesulfonyl}urea is a most preferred embodiment.
摘要翻译：通过使合适的磺酰胺与有机异氰酸酯或其三取代的脲等价物反应制备了一些衍生自含氮羧酸的新的苯磺酰脲化合物。如此获得的磺酰脲可用作作为口服降血糖剂的治疗。典型的成员包括衍生自2-甲氧基 - 烟酸的那些化合物，其中1-环己基-3- {4- [2-（5-溴-2-甲氧基烟酰氨基）乙基]苯磺酰基脲是最优选的实施方案。

37. 发明授权

US5064852A Indolinone derivatives 失效
标题翻译：吲哚啉酮衍生物
公开(公告)号：US5064852A
公开(公告)日：1991-11-12
申请号：US561040
申请日：1990-08-01
申请人： Harry R. Howard, Jr. , Reinhard Sarges
发明人： Harry R. Howard, Jr. , Reinhard Sarges
IPC分类号： C07D209/34 , C07D209/96
CPC分类号： C07D209/34 , C07D209/96 , Y10S514/866
摘要： A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical members include those compounds derived from 2-oxo-indoline-1-acetic acid wherein a 3,4-dichlorobenzyl or 3,4-dichloro-.alpha.-methylbenzyl moiety is substituted at 3-position of the molecule. Preferred member compounds include 3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 5-chloro-3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-methoxy-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-hydroxy-2-oxo-indoline-1-acetic acid and 3-(3,4-dichloro-.alpha.-methylbenzyl)-2-oxo-indoline-1-acetic acid. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的3-单（取代的甲基） - 和3,3-二（取代的甲基）-2-氧代 - 二氢吲哚-1-链烷酸化合物，包括其低级烷基酯和未取代的酰胺衍生物，以及作为所述酸与药学上可接受的阳离子的碱式盐。这些化合物可用于治疗某些慢性糖尿病并发症的醛糖还原酶抑制剂。典型的成员包括衍生自2-氧代 - 二氢吲哚-1-乙酸的那些化合物，其中3,4-二氯苄基或3,4-二氯-α-甲基苄基部分在分子的3位被取代。优选的成员化合物包括3-（3,4-二氯苄基）-2-氧代 - 二氢吲哚-1-乙酸，5-氯-3-（3,4-二氯苄基）-2-氧代 - 二氢吲哚-1-乙酸， 3-（3,4-二氯苄基）-6-甲氧基-2-氧代 - 二氢吲哚-1-乙酸，3-（3,4-二氯苄基）-6-羟基-2-氧代 - 二氢吲哚-1-乙酸和 3-（3,4-二氯-α-甲基苄基）-2-氧代 - 二氢吲哚-1-乙酸。提供了从已知原料制备这些化合物的方法。

38. 发明授权

US4471124A Spiro-imide derivatives 失效
标题翻译：螺酰亚胺衍生物
公开(公告)号：US4471124A
公开(公告)日：1984-09-11
申请号：US564599
申请日：1983-12-22
申请人： John L. Belletire , Reinhard Sarges
发明人： John L. Belletire , Reinhard Sarges
IPC分类号： C07C55/30 , C07D209/96 , C07D221/20 , C07D311/58 , C07D333/54 , C07D491/10 , C07D495/10 , C07D491/107 , C07D491/20 , C07D495/20
CPC分类号： C07D221/20 , C07C255/00 , C07C55/30 , C07D209/96 , C07D311/58 , C07D333/54 , C07D491/10 , C07D495/10
摘要： A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2', 5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2', 6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：公开了一系列螺酰亚胺化合物及其与药理学上可接受的阳离子的碱盐。这些特定化合物可用于治疗某些慢性糖尿病并发症的药物。优选的成员化合物包括2,3-二氢螺 - [1H-茚-1,3'-吡咯烷酮] -2 + 40,5'-二酮，2,3-二氢螺 - [1H-茚-2,3 ' - 吡咯烷] -2'，5'-二酮，3,4-二氢螺 - [2H-萘-1,3'-吡咯烷] -2'，5'-二酮，3,4-二氢 - 螺 - [2H-萘-1,3'-哌啶] -2'，6'-二酮，6-氯-2,3-二氢螺 - [4H-1-苯并吡喃-4,3'-吡咯烷] -2' ，5'-二酮和6,7-二氢 - 螺 - [5H-苯并（b）噻吩-4,3'-吡咯烷] -2'，5'-二酮。提供了从已知原料制备这些化合物的方法。

39. 发明授权

US4442114A Imide derivatives 失效
标题翻译：酰亚胺衍生物
公开(公告)号：US4442114A
公开(公告)日：1984-04-10
申请号：US458700
申请日：1983-01-17
申请人： John L. Belletire , Reinhard Sarges
发明人： John L. Belletire , Reinhard Sarges
IPC分类号： C07C55/30 , C07D209/96 , C07D221/20 , C07D311/58 , C07D333/54 , C07D491/10 , C07D495/10 , C07D211/88 , A61K31/445
CPC分类号： C07D221/20 , C07C255/00 , C07C55/30 , C07D209/96 , C07D311/58 , C07D333/54 , C07D491/10 , C07D495/10 , Y10S514/866
摘要： A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2',5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2',6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：公开了一系列螺酰亚胺化合物及其与药理学上可接受的阳离子的碱盐。这些特定化合物可用于治疗某些慢性糖尿病并发症的药物。优选的成员化合物包括2,3-二氢螺 - [1H-茚-1,3'-吡咯烷酮] -2'，5'-二酮，2,3-二氢螺 - [1H-茚-2,3' - 吡咯烷] -2'，5'-二酮，3,4-二氢螺 - [2H-萘-1,3'-吡咯烷] -2'，5'-二酮，3,4-二氢螺 - 2H-萘-1,3'-哌啶] -2'，6'-二酮，6-氯-2,3-二氢 - 螺 - [4H-1-苯并吡喃-4,3'-吡咯烷] -2' 5'-二酮和6,7-二氢 - 螺 - [5H-苯并（b）噻吩-4,3'-吡咯烷] -2'，5'-二酮。提供了从已知原料制备这些化合物的方法。

40. 发明授权

US4348526A Intermediates in the preparation of chiral hydantoins 失效
标题翻译：中间体在制备手性乙内酰脲
公开(公告)号：US4348526A
公开(公告)日：1982-09-07
申请号：US320051
申请日：1981-11-12
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： C07D311/68 , C07D491/04 , C07D491/107
CPC分类号： C07D491/04 , C07D311/68
摘要： A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity.The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.
摘要翻译：描述了从结构图（II）的相应的6-卤代-4-苯并二氢吡喃合成其中X为氟或氯的结构的手性乙内酰脲的新方法。化合物I在治疗由糖尿病引起的某些慢性并发症中是有价值的。此外，其中X是氯的式I化合物具有互补的降血糖活性。该方法包括卤代色素（II）与S - （ - ） - α-甲基苄胺的脱水偶联的顺序，形成结构式（III）的亚胺，加入氰化氢以形成结构的腈（IMAGE） IV）与氯代磺酰基异氰酸酯（或其等同物）缩合形成结构式（Ⅴ）的α-甲基苄氧羰尿苷，最后将其溶解于结构I的手性乙内酰脲。

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