Hoffmann-la Roche Inc.

Arpida Ag

Kaspar Burri

Georges Hirth

Jean-Marie Cassal

Henri Ramuz

Martine Clozel

Werner Neidhart

Volker Breu

Bernd-Michael Loffler

Marcel Muller

Khalid Islam

Sorana Greiveldinger-Poenaru

Richard Barner

Paul Hadvary

Klaus Muller

Dieter Gillessen

Walter Fischli

Laurent Schmitt

Marcel M Uller

Johannes Hoffner

Bernd M Loffler

Bernd-Michael L Offler

Jurgen Jaeger

The invention concerns a novel process for the preparation of 2H-chromenes of formula I and formula 5 and valuable intermediates of formulae 3 and 4 of this process.

Process for the preparation of 2H-chromenes

The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.

Benzofuran derivatives and their use in the treatment of microbial infections

The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds, and especially their use as anti-infectives.

Selected benzofuran derivatives

The invention relates to novel tetrahydroisoquinoline derivatives of general formula I and theirs use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as anti-infectives, wherein R, Rand Rare as defined in claim 1.

3-substituted 6,7-dihydroxytetrahydroisoquinoline derivatives for use as antibacterial agents

The invention relates to novel benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.

Benzofuran derivatives and their use as antibacterial agents

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

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.

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

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.

Growing community of inventors

Binningen, Switzerland

Kaspar Burri