Hoffmann-la Roche Inc.

Pierre-Charles Wyss

Synese Jolidon

Ivan Kompis

Ekkehard Weiss

Rita Locher

Werner Bollag

Hans Lengsfeld

Philippe Guerry

Joseph Kiss

Willy Schuep

Karl Friedrich Gey

Willy Burkard

Christian N Hubschwerlen

Henri Stalder

Jean-Luc Specklin

Hans Johann Mayer

Ulf Fischer

Anna Krasso

Wolfgang Pirson

Richard D'Souza

Charles Stanford Harmon

Markus Kamber

The invention is concerned with compounds of formula ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is hydroxy or lower-alkoxy, R.sup.3 is hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aryl-Q-alkyl, or a group of the formula --CR.sup.4 R.sup.4 'COR.sup.5 --, Q is --SO-- or --SO.sub.2 --; R.sup.4, R.sup.4 ' are each independently hydrogen, alkyl, aryl or heterocyclyl, R.sup.5 is hydrogen, alkyl, alkoxy, hydroxy, aryl or heterocycyl, or R.sup.4 and R.sup.5 together form --(CH.sub.2).sub.n --, and n is a whole number between 2 to 5 inclusive and the enantiomers, epimers, and diastereomers thereof, as well as pharmaceutically acceptable salts thereof. These compounds have valuable antibacterial activity.

Substituted 2,4-diaminopyrimidines

Imidazol derivatives

Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.

Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Quinoline derivatives

Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.

The novel retinoids of the formula ##STR1## wherein R represents a residue of a sugar attached ester-wise or a residue of an amino-sugar attached amide-wise or of derivatives of such sugars and n is 1 or 2, can be used as medicaments, e.g. for the treatment of neoplasms, acne and psoriasis. These compounds are obtained by reacting a sugar or an aminosugar or a derivative thereof with a reactive derivative of 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoic acid, optionally followed by the modification of reactive groups present in the reaction product.

Retinoid carbohydrates

The invention relates to novel sugar esters and glycosides especially derivatives of D-glucopyranoside and D-glucopyranaronate suitable for the treatment of neoplasms, acne, psoriasis and dermatoses.

Neoplasmic compounds: sugar esters and glycosides

Thiobenzamides of the formula ##STR1## wherein X' is bromine, fluorine, iodine, trifluoromethyl or C.sub.3-4 alkyl prepared from N-(2-aminoethyl)-morpholine and a compound of the formula ##STR2## wherein X' is as hereinbefore set forth and;

Method of treating depression

Benzamides of the formula ##STR1## wherein X is halogen, trifluoromethyl or C.sub.3-4 -alkyl and Y is hydrogen, halogen or nitro, and N-oxides thereof, prepared inter alia from N-(2-aminoethyl)-morpholine and an acid of the formula ##STR2## wherein X and Y are as hereinbefore set forth, are described. The end products are useful in the treatment of depressive conditions, that is, are useful as antidepressants.

Morpholino containing benzamides

The present invention relates to a process for the manufacture of esters. More particularly, the invention is concerned with a process for the manufacture of esters of 2,2'-anhydro-1.beta.-D-arabinofuranosyl-5-fluorocytosine.

Process for the preparation of esters

Ribofuranoysl-imidazole derivatives of the formula ##STR1## wherein R, X, Y and Z have one of the meanings set forth hereinafter, are described. The ribofuranosyl-imidazole derivatives have cardiac and circulatory-dynamic properties and are useful in the treatment of angina pectoris.

Ribofuranosyl-imidazole derivatives

A novel class of glucose derivatives, i.e., 3,4,6-tri-o-acyl-2-deoxy-2-nicotinamido-1-0-nicotinoyl-D-glucopyranoses are disclosed. These compounds are pharmaceutically active and are useful as plasma lypid lowering agents.

D-glucose-1-0-nicotinoyl-2-deoxy-2-nictinamido derivatives

N-nicotinoylglucosamine as a lipid level lowering agent in plasma.

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Muttenz, Switzerland

Pierre-Charles Wyss