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1. 发明授权

US4975453A Combination of angiotensin converting enzyme inhibitors with potassium channel modulators and use thereof in pharmaceuticals 失效
标题翻译：血管紧张素转换酶抑制剂与钾通道调节剂的组合及其在药物中的应用
公开(公告)号：US4975453A
公开(公告)日：1990-12-04
申请号：US357822
申请日：1989-05-26
申请人： Reinhard Becker , Rainer Henning , Hansjorg Urbach , Volker Teetz , Heinrich C. Englert , Dieter Mania
发明人： Reinhard Becker , Rainer Henning , Hansjorg Urbach , Volker Teetz , Heinrich C. Englert , Dieter Mania
IPC分类号： A61K31/40 , A61K38/55 , A61K45/06 , A61P25/02
CPC分类号： A61K38/556
摘要： Combination of angiotensin converting enzyme inhibitors with potassium channel modulators and use thereof in pharmaceuticals.The invention relates to combinations of angiotensin converting enzyme inhibitors with potassium channel modulators, processes for their preparation and use thereof as medicaments.
摘要翻译：血管紧张素转换酶抑制剂与钾通道调节剂的组合及其在药物中的应用。本发明涉及血管紧张素转换酶抑制剂与钾通道调节剂的组合，其制备方法和用途作为药物。

2. 发明授权

US4999371A Substituted 3,4-dihydro-2H-benzopyrans, processes for their preparation, their use and pharmaceutical products based on these compounds 失效
标题翻译：取代的3,4-二氢-2H-苯并吡喃，其制备方法及其用途和基于这些化合物的药物产品
公开(公告)号：US4999371A
公开(公告)日：1991-03-12
申请号：US151584
申请日：1988-02-02
申请人： Heinrich C. Englert , Hans-Jochen Lang , Dieter Mania , Bernward Scholkens
发明人： Heinrich C. Englert , Hans-Jochen Lang , Dieter Mania , Bernward Scholkens
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P9/00 , A61P9/08 , A61P9/10 , C07D405/04 , C07D409/14
CPC分类号： C07D405/04 , C07D409/14
摘要： 3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.
摘要翻译：描述了式I的3,4-二氢-2H-苯并[b]吡喃，其中R 1是H，OH，（C 1 -C 2） - 烷氧基，（C 1 -C 2） - 烷基或NR 4 R 5， R4和R5相同或不同，代表H，（C1-C2） - 烷基或（C1-C3） - 烷基羰基，R2和R3相同或不同，是具有1-4个碳原子的烷基，Ar是芳族或杂芳族系统是未取代或取代的，n是1或2，X是可以被杂原子O，S或NR6中间的（CH2）r链，R6是H或（C1-C4） - 烷基，r是编号2,3,4或5.还描述了这些化合物的制备方法及其用途和基于这些化合物的药物产品。

3. 发明授权

US4661636A 6-sulfoxyphenol derivatives, their preparation and their use as cytoprotective agents 失效
标题翻译： 6-磺基苯酚衍生物，其制备及其作为细胞保护剂的用途
公开(公告)号：US4661636A
公开(公告)日：1987-04-28
申请号：US648139
申请日：1984-09-07
申请人： Heinrich C. Englert , Hans-Jochen Lang , Dieter Mania , Martin Bickel
发明人： Heinrich C. Englert , Hans-Jochen Lang , Dieter Mania , Martin Bickel
IPC分类号： A61K31/10 , A61K31/11 , A61K31/135 , A61K31/18 , A61K31/415 , A61K31/60 , A61P1/04 , A61P3/00 , C07C45/56 , C07C67/00 , C07C311/15 , C07C313/00 , C07C315/00 , C07C315/04 , C07C317/00 , C07C317/22 , C07C317/32 , C07C317/46 , C07C323/66 , C07D233/02 , C07D325/00 , C07D327/02 , C07D339/00 , C07C149/00 , C07C149/32
CPC分类号： C07D233/02 , C07C309/00 , C07C313/04 , C07C317/00 , C07C45/565
摘要： Compounds of the formula I ##STR1## where R.sup.1 is hydrogen, lower alkyl, lower alkoxy, amino or dialkylamino; R.sup.2 and R.sup.3 are O-alkyl, N-dialkyl or S-alkyl, or R.sup.2 and R.sup.3 together represent --X--(CH.sub.2).sub.m --X, a carbonyl group or an imino group NR, and m is 2-6; where R.sup.4 is lower alkyl, cycloalkyl, alkenyl or dialkylamino, and where R.sup.5 is lower alkyl or cycloalkyl, and where n is 1 or 2, have excellent cytoprotective effects.They are prepared by reacting compounds II ##STR2## with formaldehyde or a reagent producing formaldehyde.
摘要翻译：式I的化合物其中R 1是氢，低级烷基，低级烷氧基，氨基或二烷基氨基; R 2和R 3是O-烷基，N-二烷基或S-烷基，或者R 2和R 3一起表示-X-（CH 2）m -X，羰基或亚氨基NR，m是2-6; 其中R 4是低级烷基，环烷基，烯基或二烷基氨基，其中R 5是低级烷基或环烷基，并且其中n是1或2，具有优异的细胞保护作用。它们通过使化合物II与甲醛或产生甲醛的试剂反应制备。

4. 发明授权

US5364878A Use of substituted 3,4-dihydro-2H-benzopyrans as remedies for obstructive functional disorders of the lungs 失效
标题翻译：使用取代的3,4-二氢-2H-苯并吡喃作为肺部阻塞性功能障碍的补救措施
公开(公告)号：US5364878A
公开(公告)日：1994-11-15
申请号：US4648
申请日：1993-01-14
申请人： Heinrich C. Englert , Erik Klaus , Dieter Mania , Bernward Scholkens
发明人： Heinrich C. Englert , Erik Klaus , Dieter Mania , Bernward Scholkens
IPC分类号： A61K31/40 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/55
CPC分类号： A61K31/42 , A61K31/40 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61K31/535 , Y10S514/826
摘要： The use of substituted 3,4-dihydro-2H-benzopyrans as remedies for obstructive functional disorders of the lungs and/or disorders of the efferent urinary passagesThe use of 3,4-dihydro-2H-benzo[b]pyrans of the formula I ##STR1## in which R.sup.1 represents H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are identical or different and represent H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkyl-carbonyl,R.sup.2 and R.sup.3 are identical or different and represent alkyl having 1-4 carbon atoms,Ar represents an aromatic or heteroaromatic system which is unsubstituted or substituted by 1 to 3 identical or different radicals (C.sub.1 -C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy, halogen, trifluoromethyl, CN, NO.sub.2, CO--(C.sub.1 -C.sub.2)-alkyl or SO.sub.m --(C.sub.1 -C.sub.2)-alkyl with m=1 or 2,n represents 1 or 2,X represents a chain (CH.sub.2).sub.r which can be interrupted by a heteroatom O, S or NR.sup.6, where R.sup.6 denotes H or (C.sub.1 -C.sub.4)-alkyl, and r represents the numbers 2, 3, 4 or 5,for the preparation of a remedy for obstructive functional disorders of the lungs and/or disorders of the efferent urinary passages, is described.
摘要翻译：使用取代的3,4-二氢-2H-苯并吡喃作为肺部阻塞性功能障碍的补救措施和/或传出的尿道的障碍使用式（I）的3,4-二氢-2H-苯并[b]吡喃其中R 1表示H，OH，（C 1 -C 2） - 烷氧基，（C 1 -C 2） - 烷基或NR 4 R 5，其中R 4和R 5相同或不同并且表示H，（C 1 -C 2） - 烷基或（C 1 -C 3） - 烷基 - 羰基，R 2和R 3相同或不同并且表示具有1-4个碳原子的烷基，Ar表示未被取代或被1至3个相同或不同基团取代的芳族或杂芳族体系（C 1 -C 2） - 烷基，（C 1 -C 2） - 烷氧基，卤素，三氟甲基，CN，NO 2，CO-（C 1 -C 2） - 烷基或SO m-（C 1 -C 2） - 烷基，m = 1或2，X表示可以被杂原子O，S或NR6中断的链（CH 2）r，其中R 6表示H或（C 1 -C 4） - 烷基，r表示数2，3，4或5 ，用于制备肺部阻塞性功能障碍的补救措施描述了传出尿道的d /或紊乱。

5. 发明授权

US5043344A Unsaturated N-benzopyranyllactams 失效
标题翻译：不饱和的N-苯并吡喃内酰胺
公开(公告)号：US5043344A
公开(公告)日：1991-08-27
申请号：US330042
申请日：1989-03-29
申请人： Heinrich C. Englert , Dieter Mania , Bernward Scholkens , Roland Utz
发明人： Heinrich C. Englert , Dieter Mania , Bernward Scholkens , Roland Utz
IPC分类号： C07D405/00 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/455 , A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P21/02 , A61P25/04 , C07C277/00 , C07C279/28 , C07C317/42 , C07C323/35 , C07C323/65 , C07D217/24 , C07D295/18 , C07D405/04
CPC分类号： C07D405/04 , A61K31/40 , A61K31/44 , A61K31/455 , A61K31/505 , C07C279/28 , C07C317/42 , C07D217/24 , C07D295/18 , C07C2101/14 , C07C2102/10
摘要： Compounds I ##STR1## where R.sup.1 is H, alkyl, alkoxy, CO alkyl, COOH, carboxyalkyl, CONR.sub.2, CN, NO.sub.2, alkylsulfi(o)nyl, arylsulfi(i)-nyl; R.sup.2 is H, OH, alkoxy, alkyl or alkylcarbonyl, R.sup.3 /R.sup.4 are alkyl, m is zero or one and X is --CR.sup.6 .dbd.CR.sup.7 -(--CR.sup.8 .dbd.CR.sup.9) (R.sup.6 R.sup.9 are H or alkyl), where n is zero or 1, are described. They are active antihypertensives and spasmolytics for the bladder, intestine, gall bladder, uterus, trachea and ureter.
摘要翻译：化合物Ⅰ其中R 1是H，烷基，烷氧基，CO烷基，COOH，羧基烷基，CONR2，CN，NO2，烷基亚磺酰基（O）nyl，芳基亚磺酰基（ⅰ） R2是H，OH，烷氧基，烷基或烷基羰基，R3 / R4是烷基，m是0或1，X是-CR6 = CR7 - （ - CR8 = CR9）（R6 R9是H或烷基），其中n是0 或1。它们是膀胱，肠，胆囊，子宫，气管和输尿管的主动抗高血压药和解痉药。

6. 发明授权

US4766241A 2-Aminomethyl-6-sulfamoylphenol derivatives with salidiuretic activities 失效
标题翻译： 2-氨基甲基-6-磺酰基苯酚衍生物，具有耐盐水活性
公开(公告)号：US4766241A
公开(公告)日：1988-08-23
申请号：US102793
申请日：1987-09-23
申请人： Heinrich C. Englert , Dieter Mania , Roman Muschaweck , Max Hropot
发明人： Heinrich C. Englert , Dieter Mania , Roman Muschaweck , Max Hropot
IPC分类号： A61K31/18 , A61K31/40 , A61P3/00 , A61P7/10 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/02 , C07C303/38 , C07C303/40 , C07C311/15 , C07C311/37 , C07D295/22 , C07D295/26 , C07C143/80
CPC分类号： C07D295/26 , C07C309/00
摘要： The invention relates to 2-aminomethylphenols of the formula I ##STR1## in which R.sup.1 and R.sup.2 represent hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or benzyl which is optionally substituted by alkyl, alkoxy or halogen, R.sup.3 and R.sup.5 denote hydrogen, halogen, alkyl or alkoxy, R.sup.4 denotes halogen, alkyl or cycloalkyl and R.sup.6 and R.sup.7 represent hydrogen or alkyl, it being possible for the radicals R.sup.1 and R.sup.2, R.sup.6 R.sup.7 and/or two of the radicals R.sup.3, R.sup.4 and R.sup.5 to form an alkylene chain which is optionally substituted by methyl groups and which, in the case of the radicals R.sup.1, R.sup.2, R.sup.6 and R.sup.7, can also be interrupted by oxygen atoms, sulfur atoms and/or imino groups, and to physiologically acceptable salts thereof, a process for their preparation, and their use and to pharmaceutical formulations based on these compounds.
摘要翻译：本发明涉及式I的2-氨基甲基苯酚，其中R 1和R 2表示氢，烷基，烯基，炔基，环烷基或苄基，其任选被烷基，烷氧基或卤素取代，R 3和R 5表示氢，卤素，烷基或烷氧基，R 4表示卤素，烷基或环烷基，R 6和R 7表示氢或烷基，基团R 1和R 2，R 6 R 7和/或基团R 3，R 4和R 5中的两个可以形成亚烷基链，任选被甲基取代，并且在基团R 1，R 2，R 6和R 7的情况下，也可以被氧原子，硫原子和/或亚氨基基团及其生理上可接受的盐中断，制剂及其用途以及基于这些化合物的药物制剂。

7. 发明授权

US5145867A Naphthylalkylamino-substituted sulfamoylbenzoic acid derivatives, and the use thereof as medicines 失效
标题翻译：萘磺酰氨基取代的磺酰苯甲酸衍生物及其作为药物的用途
公开(公告)号：US5145867A
公开(公告)日：1992-09-08
申请号：US505466
申请日：1990-04-06
申请人： John C. Ellory , Heinrich C. Englert , Hans-Jochen Lang , Dieter Mania , Wulf Merkel
发明人： John C. Ellory , Heinrich C. Englert , Hans-Jochen Lang , Dieter Mania , Wulf Merkel
IPC分类号： A61K31/245 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61P7/06 , C07C311/39 , C07C317/48 , C07C323/67 , C07D317/62 , C07D333/24 , C07D333/30
CPC分类号： C07D333/24 , C07C311/39
摘要： Naphthylalkylamino-substituted sulfamoylbenzoic acid derivatives, processes for the preparation thereof and the use thereof as medicines.Compounds I ##STR1## R(1) hydrogen, (C.sub.1 -C.sub.4)-alkyl and Na, K, NH.sub.4, Ca, Mg, R(2) and R(3) hydrogen, alkyl groups which can also be linked together in a ring,X oxygen, sulfur, SO, SO.sub.2, NR(6) [with R(6)=hydrogen-alkyl], CH.sub.2, CO, or a bond,R(4) phenyl, thienyl, which are unsubstituted or substitutedR(5) hydrogen, (C.sub.1 -C.sub.4)-alkyl,n 1, 2, 3 or 4,where the naphthyl system is unsubstituted or substituted like the phenyl radical of R(4),and where X and R(4) together can also be Cl are medicaments for treating sickle-cell anemia.
摘要翻译：萘基烷基氨基取代的氨磺酰基苯甲酸衍生物，其制备方法及其作为药物的用途。化合物I（1）氢，（C 1 -C 4） - 烷基和Na，K，NH 4，Ca，Mg，R（2）和R（3）氢，也可以在环，X氧，硫，SO，SO2，NR（6）[与R（6）=氢 - 烷基]，CH2，CO或键，R（4）苯基，噻吩基，其为未取代或取代的R（ 5）氢，（C 1 -C 4） - 烷基，n 1,2,3或4，其中萘基系统是未取代的或被取代的，如R（4）的苯基，并且其中X和R（4）也可一起是Cl是用于治疗镰状细胞性贫血的药物。

8. 发明授权

US4607030A 2-aminomethyl-6-sulfamoylphenol derivatives, a process for their preparation and their use and also pharmaceutical formulations based on these compounds 失效
标题翻译： 2-氨基甲基-6-氨磺酰基苯酚衍生物，其制备方法及其应用，以及基于这些化合物的药物制剂
公开(公告)号：US4607030A
公开(公告)日：1986-08-19
申请号：US751995
申请日：1985-07-03
申请人： Heinrich C. Englert , Dieter Mania , Roman Muschaweck , Max Hropot
发明人： Heinrich C. Englert , Dieter Mania , Roman Muschaweck , Max Hropot
IPC分类号： A61K31/18 , A61K31/40 , A61P3/00 , A61P7/10 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/02 , C07C303/38 , C07C303/40 , C07C311/15 , C07C311/37 , C07D295/22 , C07D295/26 , C07C143/80 , C07D207/00
CPC分类号： C07D295/26 , C07C309/00
摘要： The invention relates to 2-aminomethylphenols of the formula I ##STR1## in which R.sup.1 and R.sup.2 represent hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or benzyl which is optionally substituted by alkyl, alkoxy or halogen, R.sup.3 and R.sup.5 denote hydrogen, halogen, alkyl or alkoxy, R.sup.4 denotes halogen, alkyl or cycloalkyl and R.sup.6 and R.sup.7 represents hydrogen or alkyl, it being possible for the radicals R.sup.1 and R.sup.2, R.sup.6 and R.sup.7 and/or two of the radicals R.sup.3, R.sup.4 and R.sup.5 to form an alkylene chain which is optionally substituted by methyl groups and which, in the case of the radicals R.sup.1, R.sup.2, R.sup.6 and R.sup.7, can also be interrupted by oxygen atoms, sulfur atoms and/or imino groups, and to physiologically acceptable salts thereof, a process for their preparation, and their use and to pharmaceutical formulations based on these compounds.
摘要翻译：本发明涉及式I的2-氨基甲基苯酚，其中R 1和R 2表示氢，烷基，烯基，炔基，环烷基或苄基，其任选被烷基，烷氧基或卤素取代，R 3和R 5表示氢，卤素，烷基或烷氧基，R 4表示卤素，烷基或环烷基，R 6和R 7表示氢或烷基，基团R 1，R 2，R 6和R 7和/或基团R 3，R 4和R 5中的两个可以形成亚烷基链其任选被甲基取代，并且在基团R 1，R 2，R 6和R 7的情况下，也可以被氧原子，硫原子和/或亚氨基基团及其生理上可接受的盐中断，它们的制备及其用途以及基于这些化合物的药物制剂。

9. 发明授权

US5130310A Substituted benzo[b]pyrans, processes for their preparation, their use and pharmaceutical preparations based on these compounds 失效
标题翻译：取代的苯甲（B）PYRANS，其制备方法，其使用和基于这些化合物的药物制备
公开(公告)号：US5130310A
公开(公告)日：1992-07-14
申请号：US467547
申请日：1990-01-19
申请人： Klaus Weidman , Heinrich C. Englert , Bernward Scholkens , Martin Bickel
发明人： Klaus Weidman , Heinrich C. Englert , Bernward Scholkens , Martin Bickel
IPC分类号： C07D263/22 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/54 , A61P9/12 , C07D405/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
CPC分类号： C07D405/04 , C07D413/04
摘要： Benzo[b]pyran derivatives of the formula I ##STR1## with E--D equal to CH--CHOH or C.dbd.CH;X equal to oxygen or sulfur;Y equal to oxygen, sulfur, SO, SO.sub.2 or NR.sup.9 ;R.sup.1 equal to CN, NO.sub.2, Hal, alkoxycarbonyl, SO.sub.1-2 -alkyl or SO.sub.1-2 -aryl;R.sup.2 equal to H, OH, alkoxy, alkyl, Hal, NR.sup.10 R.sup.11 ;R.sup.3 /R.sup.4 equal to alkyl;R.sup.5 /R.sup.6 equal to alkyl, (CH.sub.2).sub.1-6 COO-alkyl, (CH.sub.2).sub.1-6 CONR.sup.10 R.sup.11, (CH.sub.2).sub.0-6 COOH, (CH.sub.2).sub.1-6 CO-alkyl, CO.sub.2 -alkyl, alkylmercaptoalkyl, alkylsulfi(i)(o)nyl, hydroxyalkyl, mercaptoalkyl, aminoalkyl, N-(di)-alkylaminoalkyl or (CH.sub.2).sub.f Ar with f equal to zero-3;R.sup.7 /R.sup.8 equal to hydrogen, alkyl or phenyl, and m equal to zero-2are outstanding antihypertensives and spasmolytics. Preparation processes and use are described.
摘要翻译：式I的苯并[b]吡喃衍生物，其中E-D等于CH-CHOH或C = CH; X等于氧或硫; Y等于氧，硫，SO，SO2或NR9; R1等于CN，NO2，Hal，烷氧基羰基，SO1-2-烷基或SO1-2-芳基; R2等于H，OH，烷氧基，烷基，Hal，NR10R11; R3 / R4等于烷基; （CH 2）1-6 CONR 10 R 11，（CH 2）0-6COOH，（CH 2）1-6 CO-烷基，CO 2 - 烷基，烷基巯基烷基，烷基亚磺酸（i）（ o）n，羟基烷基，巯基烷基，氨基烷基，N-（二） - 烷基氨基烷基或（CH2）fAr，f等于零-3; R7 / R8等于氢，烷基或苯基，m等于零-2是杰出的抗高血压药和解痉药。描述制备方法和用途。

10. 发明授权

US4994493A N-substituted 5-nitroanthranilic acids, a process for their preparation, their use, and pharmaceutical products based on these compounds 失效
标题翻译： N-取代的5-硝基邻氨基苯甲酸，其制备方法，它们的用途和基于这些化合物的药物产品
公开(公告)号：US4994493A
公开(公告)日：1991-02-19
申请号：US890318
申请日：1986-07-29
申请人： Rainer Greger , Heinrich C. Englert , Hans-Jochen Lang , Max Hropot
发明人： Rainer Greger , Heinrich C. Englert , Hans-Jochen Lang , Max Hropot
IPC分类号： A61K31/195 , A61K31/34 , C07C205/57 , C07C229/56 , C07D307/52
CPC分类号： C07D307/52
摘要： Compounds I ##STR1## with R equal to hydrogen or (C.sub.1 -C.sub.4)-alkyl,X equal to (CH.sub.2).sub.n with n=1-4, unsubstituted or substituted, andAr is equal to an aromatic or heteroaromatic system, optionally substituted,and their pharmaceutically tolerated salts are valuable pharmaceuticals for the treatment of cerebral edema or diarrhea.
摘要翻译：其中R等于氢或（C 1 -C 4） - 烷基，X等于（CH 2）n，其中n = 1-4，未取代或取代的，且Ar等于芳族或杂芳族体系，任选地并且其药学上可耐受的盐是用于治疗脑水肿或腹泻的有价值的药物。

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