公开(公告)号：US5811448A

公开(公告)日：1998-09-22

申请号：US760610

申请日：1996-12-04

Applicant: Heinrich Christian Englert ,  Uwe Gerlach ,  Dieter Mania ,  Wolfgang Linz ,  Heinz Gogelein ,  Erik Klaus ,  Peter Crause

Inventor： Heinrich Christian Englert ,  Uwe Gerlach ,  Dieter Mania ,  Wolfgang Linz ,  Heinz Gogelein ,  Erik Klaus ,  Peter Crause

IPC: C07D311/58 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/445 ,  A61P9/00 ,  A61P9/06 ,  A61P9/10 ,  C07D311/64 ,  C07D311/70 ,  C07D405/12 ,  C07D311/60 ,  C07D407/12

CPC classification number: C07D405/12 ,  C07D311/64

Abstract: Substituted chromanylsulfonyl(thio)ureas, processes for their preparation, their use in pharmaceutical preparations, and pharmaceutical preparations comprising them Chromanylsulfonyl(thio)ureas of the formula I ##STR1## are useful pharmaceuticals for the treatment of cardiac arrhythmias and for the prevention of sudden heart death due to arrhythmia. They can be used as antiarrhythmics and are suitable for the prevention of sudden heart death, for the treatment of cardiac insufficiency and also heart failure as a result of the effects of shock.

Abstract translation: 取代的色氨酰基磺酰基（硫代）脲，其制备方法，它们在药物制剂中的应用以及包含它们的药物制剂式I的染料基磺酰基（硫代）脲（I）是用于治疗心律失常的有用药物， 预防因心律失常引起的心脏死亡。 它们可以用作抗心律失常药物，适用于预防心源性猝死，用于治疗心功能不全以及由于休克的作用引起的心力衰竭。

公开(公告)号：US5607976A

公开(公告)日：1997-03-04

申请号：US598319

申请日：1996-02-08

Applicant: Heinrich Englert ,  Uwe Gerlach ,  Peter Crause ,  Dieter Mania ,  Heinz G ogelein ,  Joachim Kaiser

Inventor： Heinrich Englert ,  Uwe Gerlach ,  Peter Crause ,  Dieter Mania ,  Heinz G ogelein ,  Joachim Kaiser

IPC: C07D333/20 ,  A61K31/18 ,  A61K31/34 ,  A61K31/35 ,  A61K31/38 ,  A61K31/381 ,  A61K31/395 ,  A61K31/40 ,  A61K31/425 ,  A61K31/426 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  C07C233/00 ,  C07C303/40 ,  C07C311/58 ,  C07C327/40 ,  C07C335/42 ,  C07D207/32 ,  C07D207/335 ,  C07D213/40 ,  C07D277/28 ,  C07D307/52

CPC classification number: C07C335/42 ,  C07C311/58

Abstract: Substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use for the production of pharmaceutical preparations, and pharmaceutical preparations containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.

Abstract translation: 取代的苯磺酰脲和硫脲，其制备方法，其用于制备药物制剂的用途，以及含有它们的药物制剂。 式I的取代苯磺酰脲和硫脲显示出对心血管系统的作用。

公开(公告)号：US5043344A

公开(公告)日：1991-08-27

申请号：US330042

申请日：1989-03-29

Applicant: Heinrich C. Englert ,  Dieter Mania ,  Bernward Scholkens ,  Roland Utz

Inventor： Heinrich C. Englert ,  Dieter Mania ,  Bernward Scholkens ,  Roland Utz

IPC: 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 classification number: C07D405/04 ,  A61K31/40 ,  A61K31/44 ,  A61K31/455 ,  A61K31/505 ,  C07C279/28 ,  C07C317/42 ,  C07D217/24 ,  C07D295/18 ,  C07C2101/14 ,  C07C2102/10

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4766241A

公开(公告)日：1988-08-23

申请号：US102793

申请日：1987-09-23

Applicant: Heinrich C. Englert ,  Dieter Mania ,  Roman Muschaweck ,  Max Hropot

Inventor： Heinrich C. Englert ,  Dieter Mania ,  Roman Muschaweck ,  Max Hropot

IPC: 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 classification number: C07D295/26 ,  C07C309/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06335467B1

公开(公告)日：2002-01-01

申请号：US09490078

申请日：2000-01-24

Applicant: Heinrich Englert ,  Dieter Mania ,  Jens Hartung ,  Heinz Gögelein ,  Joachim Kaiser ,  Wolfgang Linz ,  David Wettlauper

Inventor： Heinrich Englert ,  Dieter Mania ,  Jens Hartung ,  Heinz Gögelein ,  Joachim Kaiser ,  Wolfgang Linz ,  David Wettlauper

IPC: C07C31116

CPC classification number: C07C311/46 ,  C07C311/58 ,  C07C335/42 ,  Y10S514/821

Abstract: Benzenesulfonylureas and -thioureas of the formula I where R(1) in N or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S, Y is —[CR(3)2]n—, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO2 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract translation: 苯基磺酰脲和硫脲，其中R（1）在N或（氟）甲基中，R（2）是H，Hal或（氟）（巯基）烷（氧）），E是O或S，Y是 - [CR（3）2] n-，其中R（3）= H或烷基，n = 1-4，X为H，Hal或烷基，Z为Hal，NO 2或烷基（yl） 化合物I用于治疗心律紊乱和预防心律失常引起的心源性猝死，因此可用作抗心律失常药物。 它们特别适用于心律失常是冠状血管狭窄（如心绞痛或急性心肌梗死）的结果的情况。

公开(公告)号：US5849755A

公开(公告)日：1998-12-15

申请号：US969794

申请日：1997-11-13

Applicant: Heinrich Christian Englert ,  Uwe Gerlach ,  Dieter Mania ,  Wolfgang Linz ,  Heinz Gogelein ,  Erik Klaus

Inventor： Heinrich Christian Englert ,  Uwe Gerlach ,  Dieter Mania ,  Wolfgang Linz ,  Heinz Gogelein ,  Erik Klaus

IPC: C07D311/04 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/355 ,  A61K31/40 ,  A61K31/4025 ,  A61P9/00 ,  A61P9/06 ,  C07D207/26 ,  C07D209/34 ,  C07D211/76 ,  C07D217/24 ,  C07D227/02 ,  C07D311/16 ,  C07D311/18 ,  C07D311/42 ,  C07D311/58 ,  C07D311/70 ,  C07D405/12

CPC classification number: C07D405/12 ,  C07D311/58 ,  C07D311/70

Abstract: 3-amidochromanylsulfonyl(thio)ureas of the formula (I): ##STR1## which are valuable pharmaceutically active compounds for the treatment of disturbances of the cardiovascular system, in particular for the treatment of arrhythmias, for preventing sudden cardiac death or for influencing a reduced contractility of the heart, and processes for their preparation, their use and pharmaceutical preparations comprising them.

Abstract translation: 式（I）的3-酰氨基苯并二氢吡喃基磺酰基（硫代）脲：作为治疗心血管系统紊乱的有价值的药物活性化合物，特别是用于治疗心律不齐的有用的药物活性化合物，用于预防心源性猝死或 用于影响心脏收缩力的降低，及其制备方法及其用途以及包含它们的药物制剂。

公开(公告)号：US5698596A

公开(公告)日：1997-12-16

申请号：US707103

申请日：1996-09-03

Applicant: Heinrich Englert ,  Dieter Mania ,  Jens Hartung ,  Heinz Gogelein ,  Joachim Kaiser ,  Wolfgang Linz ,  David Wettlaufer

Inventor： Heinrich Englert ,  Dieter Mania ,  Jens Hartung ,  Heinz Gogelein ,  Joachim Kaiser ,  Wolfgang Linz ,  David Wettlaufer

IPC: A61K31/18 ,  A61K31/64 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  C07C303/40 ,  C07C311/46 ,  C07C311/58 ,  C07C323/67 ,  C07C335/42 ,  A61K31/17

CPC classification number: C07C311/46 ,  C07C311/58 ,  C07C335/42 ,  Y10S514/821

Abstract: Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticals Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --�CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.

Abstract translation: 取代的苯磺酰脲和硫脲 - 其制备方法及其作为药物的用途式I的苯磺酰脲和硫脲其中R（1）为H或（氟）甲基，R（2）为H，Hal或（ 氟）（巯基）烷（氧）基，E是O或S; Y是 - [CR（3）2] n - ，其中R（3）= H或烷基，n = 1-4，X是H，Hal或烷基，Z是Hal，NO 2或烷基（yl） 描述。 化合物I用于治疗心律紊乱和预防心律失常引起的心源性猝死，因此可用作抗心律失常药物。 它们特别适用于心律失常是冠状血管狭窄（如心绞痛或急性心肌梗死）的结果的情况。

公开(公告)号：US5476850A

公开(公告)日：1995-12-19

申请号：US353263

申请日：1994-12-05

Applicant: Heinrich Englert ,  Dieter Mania ,  Jens Hartung ,  Heinz Gogelein ,  Joachim Kaiser

Inventor： Heinrich Englert ,  Dieter Mania ,  Jens Hartung ,  Heinz Gogelein ,  Joachim Kaiser

IPC: A61K31/64 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07C303/36 ,  C07C311/57 ,  C07C335/42 ,  C07D295/135 ,  C07C311/58 ,  C07D295/155

CPC classification number: C07D295/135 ,  C07C335/42

Abstract: There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.

Abstract translation: 描述了式I的氨基取代的苯磺酰脲和硫脲。化合物I用于治疗心律不齐，并用于预防由心律失常引起的心跳骤停，因此可用作抗心律失常药。 它们特别适合于心律不齐是冠状血管收缩的结果，例如心绞痛或急性心肌梗死的病例。

公开(公告)号：US4999371A

公开(公告)日：1991-03-12

申请号：US151584

申请日：1988-02-02

Applicant: Heinrich C. Englert ,  Hans-Jochen Lang ,  Dieter Mania ,  Bernward Scholkens

Inventor： Heinrich C. Englert ,  Hans-Jochen Lang ,  Dieter Mania ,  Bernward Scholkens

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D405/04 ,  C07D409/14

CPC classification number: C07D405/04 ,  C07D409/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4393072A

公开(公告)日：1983-07-12

申请号：US418649

申请日：1982-09-16

Applicant: Wulf Merkel ,  Dieter Bormann ,  Dieter Mania ,  Roman Muschaweck

Inventor： Wulf Merkel ,  Dieter Bormann ,  Dieter Mania ,  Roman Muschaweck

IPC: A61K31/38 ,  A61K31/381 ,  A61P7/10 ,  A61P9/12 ,  C07D333/20 ,  C07D333/24 ,  C07D333/28 ,  C07D409/12

CPC classification number: C07D333/24 ,  Y10S514/87

Abstract: The invention provides thienylbenzoic acid derivatives of the formula I ##STR1## in which R.sup.1 is an alkyl radical having from 1 to 3 carbon atoms, a phenyl, thienyl or furyl radical optionally substituted by halogen, CF.sub.3, CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydrogen, halogen or CH.sub.3 ; R.sup.3 is hydrogen or alkyl having from 1 to 4 carbon atoms or benzyl; and n is 1 or 2; and the pharmaceutically tolerable salts thereof with acids or bases.

Abstract translation: 本发明提供式I（I）的噻吩基苯甲酸衍生物，其中R 1是具有1至3个碳原子的烷基，任选被卤素，CF 3，CH 3或OCH 3取代的苯基，噻吩基或呋喃基; R2是氢，卤素或CH3; R3是氢或具有1至4个碳原子的烷基或苄基; n为1或2; 及其与酸或碱的药学上可接受的盐。