New Patents v

4567195

AZAPROSTACYCLINS, THEIR PREPARATION AND

PHARMACEUTICAL USE

Norbert Schwarz, Werner Skuballa, Helmut Vorbrueggen, Jorge Casals-Stenzel, Ekkehard Schillinger, Michael H Town, Berlin, Federal Republic Of Germany assigned to Schering Ak- tiengesellschaft

Azaprostacyclins of Formula I See Patent for Chemical Structure (I) wherein R1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dia- lkoxy, W is a free or functionally modified car- bonyl group or a See Patent for Chemical Structure wherein R8 is hydrogen or alkyl of 1-5 carbon atoms and R9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR9-group can be in the alpha- or beta-position, R2 is a free or functionally modified hydroxy group, R3 and R4 each independently is hydro- gen, alkyl of 1-5 carbon atoms, or fluorine, D is alkylene of 1-2 carbon atoms which can be sub- stituted by alkyl groups of 1-5 carbon atoms, R5 is hydrogen or alkyl of 1-2 carbon atoms or, when D is alkylene of 1 or 2 carbon atoms, R5, together with R6, represents a bond, R6 and R7 each independently is hydrogen or alkyl of 1-2 carbon atoms, wherein R6(R7) is halogen when R7(R6), respectively, is alkyl of 1-2 carbon atoms or R5 and R7 each independently is hydrogen or alkyl of 1-2 carbon atoms when D and R6 together form a carbocyclic ring closed via (CH2)1-3 with D as -CH( and R6 as -CH2-, and, when R1 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties, e.g., blood-pressure-lowering and bronchodilatory activities.

4567200

ESTERS OF MERCAPTO ACYL- CARNITINES AND

PHARMACEUTICAL COMPOSITIONS CONTAINING

SAME

Maria Tinti, Emm Quaresima, Carl Bagolini, Paolo deWitt, Rome, Italy assigned to Sigma- Tau Industrie Farmaceutiche Riunite S p A

A novel class of esters of mercapto acyl- carnitines is disclosed, wherein the mercapto acyl

radical is the radical of saturated mercapto acids having from 2 to 10 carbon atoms. These esters of mercapto acyl-carnitines are prepared e.g. by first preparing the corresponding ester of halogen acyl-carnitine and then substituting therein, by nucleophylic substitution, the -SH group for the halogen atom. These esters of mer- capto acyl-carnitines are useful therapeutic a- gents, e.g. for the treatment of intoxications and burns, and as mucolytic agents.

4567202

PHARMACEUTICAL AMITRIPTYLIN OXIDE

PREPARATION AND PROCESS FOR ITS MANUFACTURE

Manfred Durr, Benedikt Gajdos, Klaus-Dieter Gneuss, Ekkehard Harhausen, Jurgen Seidel, Pulheim Dansweiler, Federal Republic Of Ger- many assigned to A Nattermann & Cie GmbH

Stable pharmaceutical preparations comprising amitriptylin oxide dihydrate as an active sub- stance and an organic acid from the group of hydroxy carboxylic acids, ketocarboxylic acids or amino acids as a stabilizer besides conven- tional pharmaceutical auxiliaries and carrier substances.

4567295

COMPOSITION ACTIVE AGAINST MITES, WHITEFLY AND THRIPS,

PHARMACEUTICAL COMPOSITION, AND NEW

BENZOYLUREA COMPOUNDS

Marius S Brouwer, Arnoldus Grosscurt, Weesp, Netherlands assigned to Duphar International Research B V

The invention relates to a composition active against mites, whitefly and thrips, which com- prises, in addition to a liquid or solid inert carrier material, a benzoylurea compound of the gene- ral formula See Patent for Chemical Structure wherein R1 is hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluoromethyl, R2 is an alkyl group having 2-4 carbon atoms or a cycloalkyl group having 3 or 4 carbon atoms, R3 is a hydrogen atom or represents 1-3 substituents which are selected from the group consisting of halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy having 1-4