Hoffmann-la Roche Inc.

Jean-Marie Cassal

Georges Hirth

Kaspar Burri

Henri Ramuz

Werner Neidhart

Martine Clozel

Volker Breu

Marcel Muller

Bernd-Michael Loffler

Richard Barner

Paul Hadvary

Klaus Muller

Andor Furst

Albrecht Edenhofer

Werner Meier

Albert E Fischli

Andre Szente

Hans Lengsfeld

Eva-Maria Gutknecht

Marcel M Uller

Kasper F Burri

Nigel Gains

Bernd-Michael L Offler

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

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

Steroids of the formula ##STR1## wherein R.sup.1 to R.sup.4, X and n have the significance given in the description, which lower the intestinal resorption of cholesterol and plasma cholesterol and a process of making same from corresponding steroids having an alcohol residue of the formula --O--X--OH in the 3-position.

Steroids

Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, and their hydrates, which inhibit blood platelet activating factor (PAF), are described.

Glycerin derivatives

Glycerol derivatives of the formula ##STR1## wherein one of the residues R.sup.1, R.sup.2 and R.sup.3 is a group U of the formula OY.sup.1 or --X.sup.1 --CO--(A.sup.1).sub.n --Z.sup.1, another residue is a group V of the formula OY.sup.2 or --X.sup.2 --CO--(A.sup.2).sub.p --Z.sup.2, and the remaining residue is a group W of the formula --X.sup.3 T--(C.sub.2-6 -alkylene)-N.sup.+ R A.sup.- in which one of X.sup.1, X.sup.2 and X.sup.3 is oxygen or NQ.sup.1 and the other two are oxygen and the remaining symbols have the significance given below, and their hydrates are described and are prepared by introducing or generating the residues R.sup.1, R.sup.2 and R.sup.3 in corresponding glycerol derivatives. The compounds of formula I are active as inhibitors of blood platelet activating factor or as inhibitors of the growth of tumors.

Glycerol derivatives

Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.

Glycerin derivatives and inhibition of blood PAF

Phenyl-pyrimidinium, thiazolium or imidazolium salts and use in

Steroids of the formula ##STR1## wherein n represents the number 2, 3 or 4; R.sup.1 represents hydrogen, lower-alkyl or lower-alkylidene; R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or lower-alkyl and the dotted C--C bonds in the 5(6)-, 7(8)-, 22(23)-, 24(28)- and 25(26)-position are optional, whereby the B-ring can contain only one double bond and the side-chain is either saturated or is mono-unsaturated or is di-unsaturated in the 22(23), 25(26)-position; and whereby R.sup.1 is lower-alkyl or lower-alkylidene when a 5(6)-double bond is present, n is 2 and R.sup.2, R.sup.3 and R.sup.4 are methyl, and pharmaceutically acceptable salts of these steroids have activity inhibiting the intestinal resorption of cholesterol. They can be manufactured from steroids which are otherwise substituted in the 3.beta.-position.

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Mulhouse, France

Jean-Marie Cassal