Ciba-geigy Corporation

Novartis Ag

Santhera Pharmaceuticals Ag

Andreas Von Sprecher

Andreas Beck

Marc Gerspacher

Robert Mah

Robert W Lang

Silvio Roggo

Werner Breitenstein

Walter Schilling

Konrad Oertle

Silvio Ofner

Siem J Veenstra

Stefan Stutz

Pier G Ferrini

Georges Haas

Yves Auberson

Ivan Ernest

Cyrille Lescop

Claudia Betschart

Alan J Main

Bruno Schaub

Hansjurg Wetter

Marco Henneböhle

Philipp Weyermann

Michael Soeberdt

Sonja Nordhoff

Holger Deppe

Stephan Bulat

Acylaminoalkenylene-amide derivatives as NK1 and NK2 antagonists

1-aryl-2-acylamino-ethane compounds and their use as neurokinin

Compounds of formula I ##STR1## wherein rings A and B are as defined in the specification, have valuable pharmacological properties and are particularly effective as NK1 antagonists and substance P antagonists. Said compounds are prepared in a manner known per se.

Chromone Derivatives

Compounds of formula I ##STR1## wherein R.sub.1 -R.sub.5, X, Ar and Y are as defined in the description, have valuable pharmaceutical properties and are especially effective as leukotriene antagonists. They are prepared in a manner known per se.

Quinoline compound

Benzocycloalkenecarboxylic acid and process for its preparation

Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.

Alkanophenones useful for treating allergies

Substituted alkanophenones of the general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is a 5-membered heteroaryl radical that contains 1N, O or S atom as hetero atom and is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterfied or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties can e used as antiallergic active ingredients in medicaments.

Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,

.alpha.-Hydroxy thioethers

Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,

Aromatic thioethers

Novel asymmetric thioethers of the formula ##STR1## in which R.sup.1 represents a C.sub.1-3 -alkyl radical or a C.sub.1-3 -hydroxyalkyl radical of which the hydroxy group may be in esterified form,

Aliphatic thioethers

Substituted benzophenones of the formula ##STR1## in which Ph represents unsubstituted or substituted phenyl and R represents free, esterified or amidated carboxy, have anti-inflammatory and/or analgesic properties and can be used as active ingredients in medicaments. They are manufactured, for example, as follows: a compound or a mixture of compounds of the formula ##STR2## in which X.sub.1 and X.sub.2 together represent a group of the formula --C(.dbd.O)--O that is bonded via the carbonyl group to the radical Ph and X.sub.3 represents hydrogen, or one of the radicals X.sub.1 and X.sub.3 represents a group of the formula --C(.dbd.O)--Z, the other represents hydrogen and X.sub.2 represents a group R'O-- in which R' represents hydrogen or a hydroxy-protecting group, is subjected to acid treatment and the primary product is decomposed solvolytically.

Benzophenones

Growing community of inventors

Oberwil, Switzerland

Andreas Von Sprecher