Hoechst Aktiengesellschaft

Clariant Corporation

Roussel Uclaf

Aventis Pharma Deutschland, Gmbh

Adalbert Wagner

Holger Heitsch

Bernward Scholkens

Heinz-Werner Kleemann

Hermann J Gerhards

Klaus Wirth

Rainer Henning

Jean Buendia

Jean-Paul Vevert

Neerja Bhatnagar

Christine Griffoul

Gerhard Nolken

Reinhard Becker

Wolfgang Linz

Gabriele Wiemer

Jean-Claude Caille

Hans-Jerg Kleiner

Martin Bickel

Heinrich Christian Englert

Dieter Regnat

Max Hropot

Dieter Ruppert

Herbert Vojacek

Maximilian Simon

Bernward Sch&ouml;lkens

Frank Ebmeyer

John-Claude Caille

Georg Stuhlm&uuml;ller

Bernward Sch Olkens

Terpene ethers and their use

Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer's disease. This application describes such compounds, as well as processes for their preparation and use. The compounds according to this invention include compounds of formula (I)

Benzyloxy-substituted, fused N-heterocycles, processes for their preparation, and their use as bradykinin receptor antagonists

Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B.sub.2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) ##STR1## in which R.sup.1,R.sup.2,R.sup.3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, CO--O-alkyl, COOH; R.sup.4, R.sup.5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R.sup.6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R.sup.7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.

Aminoalkyl and acylaminoalkyl ethers, process for their preparation, and

Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process or their preparation, and their use Heterocyclic fluoroalkyl derivatives and fluoroalkoxy derivatives of the formula (I) having bradykinin-antagonistic action ##STR1## in which X.sub.1 -X.sub.3 are N or CR.sup.5, R.sup.1 and R.sup.2 are H or halogen, R.sup.3 and R.sup.4 are H, halogen, alkyl or alkenyl, R.sup.5 is H, halogen, (substituted) alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (substituted) aryl, (substituted)aryl-alkyl, --C(O)--OR.sup.6 or --C(O)--H, R.sup.6 and R.sup.8 H, alkyl, alkenyl or aryl-alkyl, R.sup.7 is (substituted) alkyl or (substituted) alkoxy, B is an aminocarboxylic acid, D is alkenediyl, alkanediyl or --(CH.sub.2).sub.n --Y.sub.p --(CH.sub.2).sub.m --, E is oxygen or sulfur, Y is oxygen, sulfur or NR.sup.8, n and m are a number 0-3, o is a number 1-3 and p is 0 or 1, and their physiologically tolerable salts and a process for their preparation are described.

Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin

Sulfur-containing heterocyclic bradykinin antagonists, process for their preparation, and their use Compounds of the formula (I) ##STR1## in which one of the radicals X.sub.1, X.sub.2 or X.sub.3 is C--O--R.sup.2 and the other X.sub.1, X.sub.2, and X.sub.3, in each case, and X.sub.4, are then, identically or differently, N or CR.sup.1 ; R.sup.1 and R.sup.3 are, identically or differently, H, halogen, (C.sub.1 -C.sub.6)-alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (C.sub.6 -C.sub.12)-aryl, (C.sub.6 -C.sub.12)-aryl-(C.sub.1 -C.sub.3)-alkyl, C(O)--OR.sup.6, C(O)--H, (C.sub.2 -C.sub.5)-alkenyl, NO.sub.2, SO.sub.3 R.sup.7, CN or C(O)--NHR.sup.8, where alkyl, aryl and alkenyl can optionally be substituted.

Sulfur-containing heterocyclic bradykinin antagonists, process for their

The invention relates to the use of nonpeptide bradykinin antagonists for the production of pharmaceuticals for the treatment of chronic fibrogenetic liver disorders (hepatic cirrhosis and hepatic fibrosis), acute liver disorders and for the prevention of complications, in particular for the prophylaxis or treatment of portal hypertension, decompensation symptoms such as ascites, edema formation, hepatorenal syndrome, hypertensive gastropathy and colopathy, splenomegaly and hemorrhagic complications in the gastrointestinal tract due to portal hypertension, collateral circulation and hyperemia and a cardiopathy as a result of a chronically hyperdynamic circulatory situation and its consequences.

Use of nonpeptide bradykinin antagonists for the treatment and

Aromatic bromomethyl compounds play a major role in the synthesis of active substances. They can be obtained in particularly pure form by the free-radical bromination of aromatic methyl compounds in the solvent chlorobenzene.

Process for the preparation of aromatic bromomethyl compounds

A compound of the formula ##STR1## in which the symbols have the following meaning: X is a monocyclic radical having 3, 4 or 5 ring atoms,

Benzimidazole derivatives as angiotensin II receptor antagonists,

The invention relates to a process for the preparation of a compound of the formula (I) ##STR1## in which X is an optionally protected formyl group and

Process for the preparation of biphenyl derivatives

Biphenyl derivatives and processes for the preparation of biphenyl derivatives are described. A compound of formula (I) is disclosed ##STR1## in which the substituent X is --CHO or --CH(OR.sup.1)OR.sup.2, where R.sup.1 and R.sup.2 independently of one another are (C.sub.1 -C.sub.6)-alkyl or R.sup.1 and R.sup.2 together are an alkylene group (--CH.sub.2).sub.n --, where n is 2, 3 4 or 5 and R is --F, --Cl, --NO.sub.2, --(CH.sub.2).sub.m --COOR.sup.3, --(CH.sub.2).sub.m --CONHR.sup.3, --(CH.sub.2).sub.m --CN, --SO.sub.2 NH--COOR.sup.3, --SO.sub.2 NH--CO--NHR.sup.3, --SO.sub.2 NH--SO.sub.2 --R.sup.3, --NHSO.sub.2 R.sup.3, ##STR2## --PO.sub.3 R.sup.3, --NH--SO.sub.2 --CF.sub.3, --SO.sub.2 NR.sup.4 where R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.6)cycloalkyl, or (C.sub.1 -C.sub.6)-alkyl-(C.sub.3 -C.sub.6)cycloalkyl and R.sup.4 is a group .dbd.C--N(CH.sub.3).sub.2, and m is 0, 1, 2, 3, or 4. The invention also relates to a process for the preparation of a compound of the formula (I) in which X is an optionally protected formyl group and R is a group which is itself inert to the reaction conditions of the synthesis, which comprises reacting a compound of the formula (II) ##STR3## with a substituted phenyl-halogen compound of the formula (III) ##STR4## wherein the substituent Hal is a halogen group.

Angiotensin II receptor antagonists for the treatment and prophylaxis of coronary heart disease. Antagonists for angiotensin II receptors of the AT.sub.1 subtype can be employed for the prophylaxis and combating of coronary heart disease. Furthermore these compounds, such as, for example, azoles of the formula (I) ##STR1## can also be used for the therapy of cognitive and erectile dysfunction.

Angiotensin II receptor antagonists for the treatment and prophylaxis of

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

A novel process for the preparation of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the text.

Process for the preparation of

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

Antagonists for angiotensin II receptors of the AT.sub.1 subtype can be employed for the prophylaxis and combating of coronary heart disease. Furthermore these compounds, such as, for example, azoles of the formula (I) ##STR1## can also be used for the therapy of cognitive and erectile dysfunction.

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Hattersheim am Main, Germany

Adalbert Wagner