Hoechst Aktiengesellschaft

Reinhard Becker

Hansjorg Urbach

Rainer Henning

Volker Teetz

Rolf Geiger

Bernward Scholkens

Wolfgang Ruger

Holger Gaul

Heinrich Christian Englert

Hermann J Gerhards

Adalbert Wagner

Franz Hock

Heinz-Werner Kleemann

Holger Heitsch

Dieter Mania

Wolfgang Linz

Jean-Paul Vevert

Hans Wissmann

Henning: Rainer

John-Claude Caille

Bernward Sch Olkens

Hans Jorg Urbach

Hans Wissman

Hansj/o/ Rg Urbach

The invention relates to combinations of angiotensin-converting enzyme inhibitors with calcium antagonists, processes for their preparation and their use as medicaments.

Combination of angiotensin-converting enzyme inhibitors with calcium

Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain, process for their preparation and their use Compounds of the formula (I) ##STR1## in which R.sup.1 is, for example, ethyl,

Imidazole derivatives with a biphenylsulfonylurea or

Azole derivatives, process for their preparation, and their use Azole derivatives of the formula (I) ##STR1## in which A, L, O, R.sup.1, X, Y, Z and q have the meanings given, process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have for example the following meanings:

Azole derivatives, process for their preparation and their use

A combination of angiotensin-converting enzyme inhibitors and calcium antagonists for the treatment of proteinuria is disclosed. The invention relates to the prevention and therapy of proteinuria by administration of a combination of ACE inhibitor and calcium antagonist.

Use of a combination of angiotensin-converting enzyme inhibitor and

The invention relates to a pharmaceutical composition comprising an angiotensin converting enzyme inhibitor (trandolpril or pamipril) and a loop diuretic (Furosemide or piretanide), and to their use for the treatment of high blood pressure.

Pharmaceutical composition for the treatment of high blood pressure

The invention relates to the prevention and therapy of proteinuria by administration of a combination of ACE inhibitor and calcium antagonist.

New amino acid esters, a process for their preparation, medicaments containing them, and the use thereof The invention relates to amino acid esters of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 denote hydrogen or a defined radical, R.sup.4 together with R.sup.5 and the atoms carrying them form a heterocyclic ring system, to a process for their preparation, to agents containing them, and to the use thereof.

New amino acid esters, a process for their preparation, medicaments

Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0, 1 or 2, R.sub.1 denotes hydrogen (C.sub.1 -C.sub.6)-alkyl which can optionally be substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, [which can be substituted as defined previously in the aryl radical], a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 - C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4 -alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process of the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.

Azabicycloamino carboxylic acid intermediates

Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and 2 denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.

Cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids, a process for

The invention relates to amino acid esters of the formula ##STR1## in which n=1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 denote hydrogen or a defined radical, R.sup.4 together with R.sup.5 and the atoms carrying them form a heterocyclic ring system, processes for their preparation, agents containing them and their use.

Novel amino acid glycerides, learning medicaments containing them and

Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.

Cis, endo-2-azabicyclo-[3.3.0]-octane-5-carboxylic acids

Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0,1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally by substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.2 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C.sub.1 - C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy, hydroxyl, halogen, nitro, amino, (C.sub.1 -C.sub.4)-alkylamino, di-(C.sub.1 -C.sub.4)-alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process for the preparation thereof, agents containing them, their use as a medicine and intermediates for the preparation thereof.

Bicyclic aminoacids as intermediates

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.

Growing community of inventors

Wiesbaden, Germany

Reinhard Becker