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1. 发明授权

US3961067A Composition comprising a benzenesulfonylurea hypoglycemic agent and method of treatment 失效
标题翻译：包含苯磺酰脲降血糖剂和治疗方法的组合物
公开(公告)号：US3961067A
公开(公告)日：1976-06-01
申请号：US516372
申请日：1974-10-21
申请人： Donald E. Kuhla , Reinhard Sarges , Hans E. Wiedermann
发明人： Donald E. Kuhla , Reinhard Sarges , Hans E. Wiedermann
IPC分类号： A61K31/425
CPC分类号： A61K31/425 , Y10S514/866
摘要： Several benzenesulfonylurea compounds derived from 4-methyl-5-thiazolecarboxylic acid have been prepared by reacting 4-[2-(4-methyl-5-thiazolecarboxamido)ethyl]benzenesulfonamide with an appropriate organic isocyanate or a trisubstituted urea equivalent thereof. The sulfonylureas so obtained are useful in therapy as oral hypoglycemic agents. 1-Cyclohexyl-3-{4-[2-(4-methyl-5-thiazolecarboxamido)ethyl]benzenesulfonyl}urea represents a preferred embodiment.
摘要翻译：通过使4- [2-（4-甲基-5-噻唑基甲酰氨基）乙基]苯磺酰胺与合适的有机异氰酸酯或其三取代的脲等价物反应制备了由4-甲基-5-噻唑羧酸衍生的几种苯磺酰脲化合物。如此获得的磺酰脲可用作作为口服降血糖剂的治疗。 1-环己基-3- {4- [2-（4-甲基-5-噻唑基甲酰氨基）乙基]苯磺酰基}脲代表优选的实施方案。

2. 发明授权

US3987172A Piperidinesulfonylurea derivatives 失效
标题翻译：哌啶酮衍生物（PIPERIDINESULFONYLUREA DERIVATIVES）
公开(公告)号：US3987172A
公开(公告)日：1976-10-19
申请号：US598746
申请日：1975-07-25
申请人： George R. Evanega , Donald E. Kuhla , Reinhard Sarges
发明人： George R. Evanega , Donald E. Kuhla , Reinhard Sarges
IPC分类号： A61K31/445 , A61K31/47
CPC分类号： A61K31/445 , Y10S514/866
摘要： A series of novel 1-piperidinesulfonylurea compounds derived from a nitrogen-containing monocarboxylic acid have been prepared by reacting an appropriate sulfamide with an organic isocyanate or a trisubstituted urea equivalent thereof. The sulfamylureas so obtained are useful in therapy as oral hypoglycemic agents. Typical members include those compounds derived from 2-methoxynicotinic acid, of which 1-(bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl)-3-{4-[2-(2-methoxynicotinamido)ethyl]-1-piperidinesulfonyl}-urea is a most preferred embodiment.

3. 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。

4. 发明授权

US3944524A 4-Substituted-1-piperidinesulfonamides 失效
标题翻译： 4-取代的1-哌啶磺酰胺
公开(公告)号：US3944524A
公开(公告)日：1976-03-16
申请号：US544838
申请日：1975-01-28
申请人： George R. Evanega , Donald E. Kuhla , Reinhard Sarges
发明人： George R. Evanega , Donald E. Kuhla , Reinhard Sarges
IPC分类号： C07D211/26
摘要： A series of novel 1-piperidinesulfonylurea compounds derived from a nitrogen-containing monocarboxylic acid have been prepared by reacting an appropriate sulfamide with an organic isocyanate or a trisubstituted urea equivalent thereof. The sulfamylureas so obtained are useful in therapy as oral hypoglycemic agents. Typical members include those compounds derived from 2-methoxynicotinic acid, of which 1-(bicyclo[2.2.1]hept-5-en-2-yl-endomethyl)-3-{4-[2-(2-methoxynicotinamido)ethyl]-1-piperidinesulfonyl}urea is a most preferred embodiment.
摘要翻译：已经通过使适当的磺酰胺与有机异氰酸酯或其三取代的尿素当量反应来制备一系列由含氮一元羧酸衍生的新颖的1-哌啶磺酰脲化合物。如此得到的磺胺类药物可用作口服降糖药的治疗。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-（双环[2.2.1]庚-5-烯-2-基 - 内甲基）-3- {4- [2-（2-甲氧基烟酰氨基）乙基] -1-哌啶磺酰基}脲是最优选的实施方案。

5. 发明授权

US4980357A Azolidinedione derivatives 失效
标题翻译：氮杂二酮衍生物
公开(公告)号：US4980357A
公开(公告)日：1990-12-25
申请号：US474722
申请日：1990-03-01
申请人： Steven W. Goldstein , Reinhard Sarges
发明人： Steven W. Goldstein , Reinhard Sarges
IPC分类号： C07D491/20
CPC分类号： C07D491/20
摘要： A series of novel spiro-deteroazolones derived from a 2,3-dihydropryrano[2,3-b]pyridine ring system have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical member compounds include spiro-imides, spiro-oxazolidinediones, spiro-thiazolidinediones and spiro-imidazolidinediones derived from the aforesaid ring system. (4'S) (2'R)-6'-Chloro-2',3'-dihydro-2'-methyl-spiro-[imidazolidine-4,4'-4'H-pyrano[2,3-b]pyridine]-2,5-dione represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列衍生自2,3-二氢丙氨酸[2,3-b]吡啶环体系的新型螺 - 脱苯罗唑酮，包括其药学上可接受的盐。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。典型的成员化合物包括衍生自上述环系的螺 - 酰亚胺，螺恶唑烷二酮，螺 - 噻唑烷二酮和螺 - 咪唑烷二酮。（4'S）（2'R）-6'-氯-2'，3'-二氢-2'-甲基 - 螺 - [咪唑烷-4,4'-4'H-吡喃并[2,3-b]吡啶 ] -2,5-二酮代表典型和优选的成员化合物。提供了从已知原料制备所有这些化合物的方法。

6. 发明授权

US4273775A Hydantoin derivatives, anti-diabetic compositions thereof, and method of use thereof 失效
标题翻译：乙内酰脲衍生物，其抗糖尿病组合物及其使用方法
公开(公告)号：US4273775A
公开(公告)日：1981-06-16
申请号：US153154
申请日：1980-05-27
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： C07D471/10 , C07D471/20 , A61K31/42
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。

7. 发明授权

US4248882A Treating diabetes-associated complications with hydantoin amines 失效
标题翻译：用乙内酰胺治疗与糖尿病相关的并发症
公开(公告)号：US4248882A
公开(公告)日：1981-02-03
申请号：US120944
申请日：1980-02-12
申请人： Reinhard Sarges , Rodney C. Schnur
发明人： Reinhard Sarges , Rodney C. Schnur
IPC分类号： A61K31/415 , A61K31/435 , A61P25/02 , A61P27/02 , C07D471/10 , C07D491/10 , C07D491/107 , C07D495/10 , A61K31/47
CPC分类号： C07D471/10 , C07D491/10 , C07D495/10 , Y10S514/866
摘要： A series of amino-and alkylamino-substituted spirohydantoins and pharmaceutically acceptable salts thereof useful as inhibitors of the enzyme aldose reductase and as therapeutic agents for the treatment of chronic complications associated with diabetes are disclosed. Preferred compounds include 6-chloro-8-amino-spiro[4H-2,3-dihydro-1-benzopyran-4,4'-imidazolidine]-2',5'-dione, the 6-fluoro and 8-methylamino- analogs thereof and the corresponding dihydrobenzothiopyran analogs of these compounds. The optical isomers of these compounds having the 4S-configuration are especially preferred.
摘要翻译：公开了用作酶醛糖还原酶的抑制剂的一系列氨基和烷基氨基取代的螺乙内酰脲及其药学上可接受的盐，以及用于治疗与糖尿病相关的慢性并发症的治疗剂。优选的化合物包括6-氯-8-氨基 - 螺[4H-2,3-二氢-1-苯并吡喃-4,4'-咪唑烷] -2'，5'-二酮，6-氟和8-甲基氨基 - 其类似物和这些化合物的相应的二氢苯并噻喃类似物。具有4S构型的这些化合物的光学异构体是特别优选的。

8. 发明授权

US4147797A Spiro-furanohydantoin derivatives 失效
标题翻译：螺 - 呋喃乙内酰脲衍生物
公开(公告)号：US4147797A
公开(公告)日：1979-04-03
申请号：US932990
申请日：1978-08-11
申请人： Paul R. Kelbaugh , Reinhard Sarges
发明人： Paul R. Kelbaugh , Reinhard Sarges
IPC分类号： A61K31/415 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/02 , A61P27/02 , A61P27/12 , C07D491/10 , C07D491/107
CPC分类号： C07D491/10 , Y10S514/866
摘要： Novel spiro-furanohydantoin derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. The compounds include 2-methyl-spiro-[cyclohexa(b)furan-4,4'-imidazolidine]-2',5'-dione, 2-fluoro-spiro-[cyclohexa(b)furan-4,4'-imidazolidine]-2',5'-dione, 2-chloro-spiro-[cyclohexa(b)furan-4,4'-imidazolidine]-2',5'-dione, 2-bromo-spiro-[cyclohexa(b)furan-4,4'-imidazolidine]-2',5'-dione and spiro-[cyclohexa(b)furan-4,4'-imidazolidine]-2',5'-dione.
摘要翻译：公开了可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PG（PG），1新型螺 - 呋喃乙内酰脲衍生物。化合物包括2-甲基 - 螺 - {8环己烷（b）呋喃-4,4（40-咪唑烷）{9-2 {40,5 {40-二酮，2-氟 - 螺 - {8环己烷（b）呋喃 -4,4 {40-咪唑烷{9-2 {40,5 {40-二酮，2-氯 - 螺 - {8环己烷（b）呋喃-4,4 {40-咪唑烷{9-2 {40,5 {40-二酮，2-溴 - 螺 - {8环己烷（b）呋喃-4,4 {40-咪唑烷{9-2 {40,5 {40-二酮和螺 - {8环己烷（b）呋喃-4 ，4 {40-咪唑烷{9-2 {40,5 {40-二酮。

9. 发明授权

US4045488A Aminophenyltetralin compounds 失效
公开(公告)号：US4045488A
公开(公告)日：1977-08-30
申请号：US690709
申请日：1976-05-27
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： C07C87/64
摘要： A series of novel 4-phenyl-1,2,3,4-tetrahydro-1-naphthylamines, including their pharmaceutically acceptable acid addition salts and their cis- and trans-isomers, have been prepared. The trans-isomers are useful in the field of mental health as antidepressant agents and/or as psychomotor stimulants. The trans-isomer of N-methyl-4-phenyl-1,2,3,4-tetrahydro-1-naphthylamine represents a preferred embodiment.

10. 发明授权

US4029731A Aminophenyltetralin compounds 失效
标题翻译：氨基苯基四氢化萘化合物
公开(公告)号：US4029731A
公开(公告)日：1977-06-14
申请号：US692764
申请日：1976-06-04
申请人： Reinhard Sarges
发明人： Reinhard Sarges
IPC分类号： A01N9/20 , A01N9/24 , C07C87/64
摘要： A series of novel 4-phenyl-1,2,3,4-tetrahydro-1-naphthylamines, including their pharmaceutically acceptable acid addition salts and their cis- and trans-isomers, have been prepared. The trans-isomers are useful in the field of mental health as antidepressant agents and/or as psychomotor stimulants. The trans-isomer of N-methyl-4-phenyl-1,2,3,4-tetrahydro-1-naphthylamine represents a preferred embodiment.
摘要翻译：已经制备了一系列新的4-苯基-1,2,3,4-四氢-1-萘胺，包括它们的药学上可接受的酸加成盐及其顺式和反式异构体。反式异构体在心理健康领域中可用作抗抑郁剂和/或作为精神运动兴奋剂。 N-甲基-4-苯基-1,2,3,4-四氢-1-萘胺的反式异构体是优选的实施方案。

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