New Patents iii

4738973

PHARMACEUTICAL COMPOSITIONS AND MEDICAL

USES OF DIOXOPIPERIDINE DERIVATIVES

and a pharmacologically acceptable acid addi- tion salt thereof. This compound has both effects of the inhibition of gastric acid and the protec- tion of gastric mucosa, which is low in toxicity. Accordingly, it is useful as a therapeutical agent for peptic ulcer disease.

Maurice W Gittos, Plobsheim, France assigned to National Research Development Corpora- tion

Phenyl-3-aminoalkyl-4-methyl-2,6- dioxopiperidines of the Formula I See Patent for Chemical Structure wherein: R1 represents methoxy, ethoxy or hydroxy, R2 represents methoxy, ethoxy, hydroxy or hydrogen; each R3 independently represents methyl or ethyl; R4 represents hydrogen or methyl; R5 represents hydrogen or methyl; and n represents 2 or 3, and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) an- tagonize the anxiogenic activity of ben- zodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarization activation of tryptophan hydro- xylase. Novel compositions comprise the com- pounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

4738985

PHARMACEUTICAL COMPOSITION AND

TREATMENT

Ronal Kluger, Mortimer Mamelak, Don Mills, Canada assigned to The University of Toronto Innovations Foundations

Sleep disorders in mammals, such as insomnia and narcolepsy, are treated by administering an effective amount of ethyl 4-acetoxybutanoate, or a closely related homolog thereof. The com- pounds may also be administered to mammals to cause muscle relaxation and as animal anaesthetics. Moreover the compounds appear to inhibit the release of dopamine in the brain, and are hence useful also in treatment of condi- tions which are associated with abnormalities of dopamine release and dopamine sensitivities, such as Parkinson's disease, schizophrenia and tardive dyskenesia.

4740519

4738977

2-PYRIDYLACETIC ACID DERIVATIVES,

PHARMACEUTICAL COMPOSITION CONTAINING

THE SAME AND THEIR USE IN TREATING ULCERS

Mitsuhito Okitsu, Osaka, Japan assigned to Suntory Limited

A 2-pyridylacetic acid derivative having the for- mula (I): See Patent for Chemical Structure (I) wherein R1 represents an alkyl having 1 to 15 carbon atoms, an alkenyl having 5 to 20 carbon atoms or an aralkyl having 7 to 15 carbon atoms; R2 represents hydrogen, a linear or cyclic alkyl, a hydroxyalkyl group, an alkenyl, an aryl, an aralkyl or a group-(CH2)-A, where n represents an integer of 0 to 3 and A represents a nitrogen- containing heterocyclic group which may be sub- stituted with an alkyl having 1 to 10 carbon atoms or an aralkyl having 7 to 10 carbon atoms

BENZO (B) THIOPHENE CARBOXYLATE DERIVATIVES

AND PHARMACEUTICAL COMPOSITIONS

Braham Shroot, Jacques Eustache, Jean-Miche Bernardon, Antibes, France assigned to Centre International de Recherches Dermatologiques C I R D

Aromatic heterocyclic derivatives have the for- mula See Patent for Chemical Structure wherein R1 represents See Patent for Chemical Structure wherein R3 represents hydrogen, -OR4 wherein R4 represents hydrogen, alkyl having 1-20 car- bon atoms or mono- or polyhydroxyalkyl or R3 represents See Patent for Chemical Structure wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R2 represents hydrogen or -CH3 and Ar represents See Patent for Chemical Structure (A) ZCH3CH3 (B) wherein Z is O or S, See Patent for Chemical Structure (C) wherein R5 is lower alkyl or See Patent for Chemical Structure (D)

iv New Patents

wherein R6 is hydrogen or alkyl having 1-10 car- bon.atoms and R7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or -N-R8 when R8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R6 is alkyl having 1-4 carbon atoms and R7 is branched alkyl having 4-12 atoms useful in veterinary or human therapy and in cosmetic formulations.

4 7 4 0 5 2 2

O X O L A B D A N E S U S E F U L AS P H A R M A C E U T I C A L S F O R

R E D U C I N G I N T R A O C U L A R P R E S S U R E

Nicholas J Hrib assigned to Hoechst-Roussel Pharmaceuticals Inc

Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing com- pounds or compositions thereof are disclosed.

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