Roussel Uclaf

Other

Hoechst Marion Roussel

Aventis Pharma S.a.

Jacques Guillaume

Lucien Nedelec

Claude Dumont

Francois Clemence

Gilles Hamon

Michel Fortin

Alain Corbier

Pierre Deprez

Jean-Luc Haesslein

Jean-Paul Vevert

Bertrand Heckmann

Jacques Dumas

Francoise Delevallee

Marie-Claude Fournie-Zaluski

Andre Allais

Robert Fournex

Hans H Sedlacek

Jorg Czech

Pierre Henri Derible

Neil L Brown

Christian Marchandeau

Bernard Pierre Roques

Lucien Ledelec

Products of formula (1), wherein R is particularly phonyl or biphenyl optionally substituted by halogen n1 and n2 are 0 or 1, R is particularly hydrogen or methyl substituted by phenyl, which may in turn be substituted, and A is partcularly carboxy or alkyl substituted particularly by phenoxy, as well as all isomers and organic and inorganic base addition salts therof, are disclosed.

Sulphur derivatives with a retroamide bond as endothelin-converting enzyme inhibitors

Sulphur derivatives comprising an amide bond, method for preparing same,

Products of formula (1), wherein R.sub.1 is particularly ##STR1## alkyl, alkylthio or alkoxy; R.sub.2 is particularly halogen, --S--R, --O--R or --C(OH)(R)--COOH, where R is alkyl or alkenyl; R.sub.3 is particularly carboxy, acyl, halogen, alkyl, alkenyl or alkylthio; and R.sub.4 is particularly --(CH.sub.2).sub.m1 --COOR.sub.4, --(CH.sub.2).sub.m1 --CONHR.sub.14, --(CH.sub.2).sub.m1 --CN, --SO.sub.2 --NH--SO.sub.2 --R.sub.14, 13 NH--SO.sub.2 --R.sub.14, --PO.sub.3 R.sub.14, or --NH--SO.sub.2 --CF.sub.3, where m1 is 0-4 and R.sub.14 is hydrogen, alkyl or alkenyl; are useful for preparing pharmaceutical compositions for treating disorders resulting from abnormal stimulation of angiotensin II receptors AT.sub.1 and AT.sub.2.

Imidazole-5-carboxamides

Method of preventing abnormal stimulation of AT.sub.1 and AT.sub.2

Tetrasubstituted imidazoles

The bicyclic derivatives of pyridines of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts and a process and intermediates for their preparation which compounds are inhibitors of angiotensin II effects, particularly a vasoconstrictor activity.

Method for inhibiting vasoconstriction

Method of inhibiting angiotensin effects

Bicyclic pyridines which are angiotensin II inhibitors

Novel indole-carboxamides of the formula ##STR1## and their non-toxic pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.

Indole carboxamides

Use of derivatives of 9,10-dihydrophenanthrene for the preparation of an

Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having anti-arhythmic activity.

4-Benzyl-1H-indole derivatives

Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having antiarhythmic activity.

4-benzyl-1H-indoles and anti-arrthymic use thereof

Novel indole-carboxamides of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine --NO.sub.2, --NH.sub.2, acylamide of an aliphatic carboxylic acid of 2 to 5 carbon atoms and mono and dialkylamino with alkyl of 1 to 5 carbon atoms, a and b form .dbd.0 and c is hydrogen or a and c form a carbon-carbon bond and b is hydrogen, A is selected from the group consisting of --(CH.sub.2).sub.n -- and ##STR3## n is an integer from 2 to 5, m is an integer from 1 to 3, B is ##STR4## R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-arrhythmic properties.

Novel indole carboxamides

Novel indole carboxamides of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine, --NO.sub.2, --NH.sub.2, acylamide of an aliphatic carboxylic acid of 2 to 5 carbon atoms and mono and dialkylamino with alkyl of 1 to 5 carbon atoms, a and b form .dbd.O and c is hydrogen or a and c form a carbon-carbon bond and b is hydrogen, A is selected from the group consisting of --(CH.sub.2).sub.n -- and ##STR3## n is an integer from 2 to 5, m is an integer from 1 to 3, B is ##STR4## R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.

N-(1H-indole-4-yl)-benzamides

Novel 4-phenylpropyl-indoles of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, linear alkyl of 1 to 5 carbon atoms, branched alkyl of 3 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms cycloalkylalkyl of 4 to 7 carbon atoms and optionally substituted aralkyl of 7 to 12 carbon atoms or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle containing another heteroatom selected from the group consisting of oxygen, sulfur and nitrogen optionally substituted with a member of the group consisting of alkyl of 1 to 5 carbon atoms, phenyl, naphthyl and aralkyl of 7 to 12 carbon atoms, a together with b forms .dbd.0 or a together with c form a carbon-carbon bond, b is hydrogen or with a forms .dbd.0, c is hydrogen or with a forms a carbon-carbon bond, the dotted line is an optional carbon-carbon bond, A is --(CH.sub.2).sub.n --, is an integer from 2 to 5, R.sub.2 is selected from the group consisting of hydrogen, linear alkyl of 1 to 5 carbon atoms and branched alkyl of 3 to 5 carbon atoms, x is hydrogen or -OH or together with y forms .dbd.0 and y is hydrogen or together with x forms .dbd.0 and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable antiarythmic properties and blocking of slow calcicosodic canals.

4-phenylpropyl-indoles having antiarythmic activity

Growing community of inventors

Sevran, France

Jacques Guillaume