New Patents XV

5015659

THIENYLACETIC ACID DERIVATIVES, PROCESS FOR

THE PREPARATION THEREOF, THE USE THEREOF, AND

PHARMACEUTICALS CONTAINING THESE AND THE

PREPARATION THEREOF

Karl Schonafinger, Rudi Beyerle, Ursula Schin- dler, Bernd Jablonka, Jeffery Troke, Alzenau, Federal Republic Of Germany assigned to Cas- sella Aktiengesellschaft

The present invention relates to thienylacetic acid derivatives of the general formula I See Pa- tent for Chemical Structure (I) in which X denotes -O- or -NH-; Rl denotes hydrogen, the group -CH2-CO-R3 or the group -CO-CHZ- NH2; R2 denotes hydrogen, (Cl-C4)-alkyl or the radical Rl and R3 denotes (Cl-C4)-alkoxy, hydroxyl or amino, it not being possible for both Rl and R2 to represent hydrogen when X denotes 0, as well as the pharmaceutically tolerated salts thereof, process for the prepara- tion thereof, the use thereof, and pharma- ceuticals containing these and the preparation thereof.

5015661

CHROMANES AND THEIR PHARMACEUTICAL

COMPOSITIONS AND METHODS

Armin Walser assigned to Hoffmann-La Roche Inc

Racemic Compounds of the formula See Patent for Chemical Structure I A is -C triple bondCR6, -CH2-CH2-R7 or See Patentfor Chemical Struc- ture Rl is hydrogen or lower alkanoyl, R2, R3, and R4 independently are hydrogen or lower alkyl, R5 is lower alkyl, R6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di- lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl,

lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be See Pa- tent for Chemical Structure wherein R’ is hydro- gen, lower alkanoyl, trifluoroacetyl and R” hydrogen or lower alkyl, R7 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl-lower alkoxy of 2-7 carbon atoms, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, amino, amino-lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino- lower alkyl, lower alkanoylamino, amino- carbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy or pyridyl, or on adja- cent carbons can be See Patent for Chemical Structure wherein R’ is hydrogen, lower alkanoyl, trifluoroacetyl and R” hydrogen or lower alkyl, R8, R9, RlO, independently, are hydrogen, hydroxy, lower alkyl, lower alkoxy, hydroxy lower alkyl, fluorine, chlorine or lower alkanoyl provided that no more than one of R8, R9, and RlO is hydroxy, lower alkoxy, lower hydroxyalkyl, fluorine, chlorine or lower alkanoyl, and Y is CH or N, and their enan- tiomer and salts thereof are described. The com- pounds of formula I exhibit activity as inhibitors of 5-lipoxygenase and inhibit lipid peroxidation. They are, therefore, useful in the treatment of diseases caused or aggravated by excess oxida- tive metabolism of arachidonic acid via the 5- lipoxygenase pathway and in the treatment of inflammation, arthritis, allergies, asthma and psoriasis. The compounds of formula I can also be used to prevent peroxidation of lipids and thus protect lipid membranes from oxidative stress.

5017366

PHARMACEUTICAL COMPOSITIONS

Werner Stiefel, Charles F Breunig assigned to Stiefel Laboratories Inc

A topical pharmaceutical composition com- prising a mixture of(i) at least one topically ac- ceptable UV absorber in a concentration sufficient to block a substantial quantity of sun- generated UV radiation and (ii) an anti- bacterially effective amount of erythromycin in (iii) an pharmaceutically acceptable topical car-