Hoffmann-la Roche Inc.

Henri Ramuz

Werner Neidhart

Jean-Claude Muller

Martine Clozel

Georges Hirth

Jean-Marie Cassal

Kaspar Burri

Volker Breu

Quirico Branca

Wolfgang Wostl

Bernd-Michael Loffler

Marcel Muller

Anna Krasso

Heinz Stadler

Roland Jaunin

Urs O Hengartner

Albrecht Edenhofer

Albert E Fischli

Walter Fischli

Andre Szente

Hans P Marki

James F Eliason

Hans Peter Wessel

Peter Vogt

Eva-Maria Gutknecht

S&eacute;bastien Roux

Philippe Coassolo

Marquard Imfeld

Marcel M Uller

Franzi Marti

Hans P Maki

Bernd M Loffler

Franz A Kaufmann-Schmid, Deceased

Rolf Huber

Franz A Kaufman-Schmid, Deceased

Jenri Ramuz

Bernd-Michael L Offler

Heterocyclic sulfamides

Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;

Aryl-  and hetaryl-sulfonamide derivatives, their preparation and their

Sulfonamides

Aryl- and hetaryl-sulfonamide derivatives, their preparation and their

Compounds of formula I: ##STR1## are disclosed. The compounds inhibit the binding of endothelin to its receptors.

Sulfonylaminopyrimidine carboxylic acid derivatives having endothelin

Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.

Sulphonamides

The compounds of the formula ##STR1## in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.

Amino acid derivatives having renin inhibiting activity

A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.

Sulfonylaminopyrimidines

The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;

Phenylsulfonylamide pyrimidine

Compounds of the formula. ##STR1## wherein R is a residue of the formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and Z are as described, with the exception of rac-N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-.beta.,N-dimethyl-m -dithiane-2-propanamine, as well as their acid addition salts, in particular for use in eliminating cytostatic resistance in tumor treatment and chloroquine resistance in malaria.

Multidrug resistance modifying dithianes

The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth above, are described. The compounds of formula I have an inhibitory activity on the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations for the control or prevention of high blood pressure and cardiac insufficiency.

Amino acid derivatives

Compounds of the formula ##STR1## wherein R is a residue of the formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and Z are as described, with the exception of rac-N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-.beta.,N-dimethyl-m -dithiane-2-propanamine, as well as their acid addition salts, in particular for use in eliminating cytostatic resistance in tumor treatment and chloroquine resistance in malaria.

The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.

Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.-naphthyl, Y is a bivalent residue in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the control or prevention of high blood pressure and cardiac insufficiency.

Amino acid derivatives useful for treating high blood pressure

Sulfonamides of formula I, in which the symbols R.sup.1 -R.sup.6, X, Y and n have the significance given in the description and which are in part novel compounds, and salts thereof, which can be used as active ingredients for the manufacture of medicaments for the treatment of circulatory disorders, especially hypertension, ischemia, vasospasms and angina pectoris, are described.

Sulfonamides and uses

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Birsfelden, Switzerland

Henri Ramuz