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1. 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。

2. 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。

3. 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。

4. 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。

5. 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.

6. 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。

7. 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.

8. 发明授权

US5998463A Glycogen phosphorylase inhibitors 失效
标题翻译：糖原磷酸化酶抑制剂
公开(公告)号：US5998463A
公开(公告)日：1999-12-07
申请号：US251141
申请日：1999-02-16
申请人： Bernard Hulin , Reinhard Sarges
发明人： Bernard Hulin , Reinhard Sarges
IPC分类号： A61K45/06 , C07D209/34 , A01N43/38
CPC分类号： A61K45/06 , C07D209/34
摘要： This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.
摘要翻译：本发明涉及可用作糖原磷酸化酶抑制剂的某些5-酰基-2-氧代 - 吲哚-3-甲酰胺，用这些化合物治疗糖原磷酸化酶依赖性疾病或病症的方法和包含这些化合物的药物组合物。本发明还涉及包含5-酰基-2-氧代 - 吲哚-3-甲酰胺与抗糖尿病药物的组合物的药物组合物以及用这些组合物治疗糖原磷酸化酶依赖性疾病或病症的方法。

9. 发明授权

US4977178A Method of treating anxiety and depression with 1-phenyl-2(1H,3H)-indolone psycho-therapeutic agents 失效
标题翻译：用1-苯基-2（1H，3H） - 吲哚酮心理治疗剂治疗焦虑和抑郁症的方法
公开(公告)号：US4977178A
公开(公告)日：1990-12-11
申请号：US382614
申请日：1989-07-19
申请人： Harry R. Howard, Jr. , Reinhard Sarges
发明人： Harry R. Howard, Jr. , Reinhard Sarges
IPC分类号： C07C43/225 , C07D209/08 , C07D209/34 , C07D209/38
CPC分类号： C07D209/08 , C07C43/225 , C07D209/34 , C07D209/38
摘要： Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.
摘要翻译：某些取代的1-苯基-3-（氨基亚烷基）-2（1H，3H） - 吲哚酮是非常有效的gabaergic试剂，在治疗患有精神分裂症或逆转先前或同时施用的精神抑制剂的副作用的个体中是有价值的; 或治疗癫痫。更广泛类别的取代的1-苯基-3-（氨基亚烷基）-2（1H，3H） - 吲哚酮与1-苯基-3-（2-吡咯烷亚基）-2（1H，3H） - 吲哚酮及其同系物，在治疗焦虑方面是有价值的。

10. 发明授权

US4960785A Indolinone derivatives 失效
标题翻译：吲哚啉酮衍生物
公开(公告)号：US4960785A
公开(公告)日：1990-10-02
申请号：US346115
申请日：1988-12-16
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 , C07D491/056
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. Said oxindole-1-alkanoic acid compounds are of the formulae: ##STR1## wherein X is hydrogen and X.sup.1 is hydrogen, hydroxy, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or X and X.sup.1, when taken separately, are each chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and when taken together are --OCH.sub.2 (CH.sub.2).sub.n O-- at the 4,5-, 5,6- or 6,7-positions of the molecule wherein n is zero or one; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or phenylalkyl having up to three carbon atoms in the alkyl moiety wherein said phenylalkyl is optionally substituted with up to two chlorine substituents on the phenyl ring; R.sub.3 is naphthylmethyl, furfuryl, thenyl, benzothienylmethyl, benzoxazolylmethyl, benzothiazolylmethyl or phenylalkyl having up to three carbon atoms in the alkyl moiety wherein said phenylalkyl is optionally substituted with up to two identical or non-identical substituents on the phenyl ring, said identical substituents being fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy and said non-identical substituents being chlorine, methyl, methoxy or trifluoromethyl; and Y is hydrogen, fluorine, chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 -alkoxy.
摘要翻译： PCT No.PCT / US86 / 01429 Sec。 371日期：1988年12月16日 102（e）1988年12月16日PCT PCT 1986年6月10日。一系列新型3-单（取代甲基） - 和3,3-二（取代甲基）-2-氧代 - 二氢吲哚-1-链烷酸已经制备了酸化合物，包括其低级烷基酯和未取代的酰胺衍生物，以及所述酸与药理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。所述羟吲哚-1-链烷酸化合物具有下式：其中X是氢，X 1是氢，羟基，氟，氯，溴，C 1 -C 4烷基或C 1 -C 4烷氧基; 或X和X 1分别为氯，C 1 -C 4烷基或C 1 -C 4烷氧基，并且当在4,5-，5,6-或6,7时共同为-OCH 2（CH 2）n O- 分子的位置，其中n为0或1; R1是氢或甲基; R2是氢，C1-C4烷基或在烷基部分具有至多三个碳原子的苯基烷基，其中所述苯基烷基任选被苯环上最多两个氯取代基取代; R3是在烷基部分中具有至多三个碳原子的萘甲基，糠基，噻吩基，苯并噻吩基甲基，苯并恶唑基甲基，苯并噻唑基甲基或苯基烷基，其中所述苯基烷基任选被苯环上最多两个相同或不相同的取代基取代，所述相同的取代基是氟，氯，溴，三氟甲基，C 1 -C 4烷基或C 1 -C 4烷氧基，所述不相同的取代基是氯，甲基，甲氧基或三氟甲基; Y是氢，氟，氯，C1-C4烷基或C1-C4-烷氧基。

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