vi New Patents

Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: See Patent for Chemical Structure (1) in which R1 is hydrogen or hydroxy; R2 is hydrogen or alkyl; R3 is C3-6 alkyl; R4 is hydrogen, alkyl, -CH2-Z where Z is optionally substituted phenyl or heteroaryl, or R4 is a group See Patent for Chemical Structure where R8 is hydrogen, alkyl or -CH2-Ph where Ph is optionally substituted phenyl, and R9 is hydrogen or alkyl; and R5 is hydrogen or alkyl.

4935421

2-HYDROXYPROPYLAMINE ARYL ESTER DERIVATIVES AND

PHARMACEUTICAL USE

Sheung T Kam, William Matier assigned to E I Du Pont de Nemours and Company

Novel compounds of the general formula See Patent for Chemical Structure wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from I to about I0 carbon atoms; and B represents -NR2COR 1, -NR2CONR1R3, -NR2SO2R 1, -NR2SO2NR 1R3, or - NR2COOR1 wherein R1, R2 and R3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R1 is not hydrogen when B is -NR2SO2R1 or - NR2COOR1, or R1 and R3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit beta- adrenergic blocking activity and are also useful in the treatment of glaucoma.

4935432

INDOLYLPIPERIDINE COMPOUNDS, PROCESSES FOR THE PREPARATION THEREOF

AND PHARMACEUTICAL COMPOSITION COMPRISING

THE SAME

Masaaki Matsuo, Takashi Manabe, Shinji Shigenaga, Hiroshi Matsuda, Osaka, Japan as- signed to Fujisawa Pharmaceutical Co Ltd

The invention relates to new compounds, of antiallergic activity, of the formula: See Patent for Chemical Structure wherein R1 is aryl sub-

stituted with substituent(s) selected from group consisting of hydroxy, protected hydro halogen and lower alkoxy, A is lower alkyl¢ and B is lower alkenylene, or a pharmaceutic~ acceptable salt thereof.

4935433

2-(ACYLTHIO)METHYL DIHYDROPYRIDINES, AND

PHARMACEUTICAL COMPOSITIONS CONTAININ(

THEM

Marco Frigerio, Carlo Riva, Andrea Zali~ Carmelo A Gandolfi, Odoard Tofanetti, Ser Tognella, Milan, Italy assigned to Boehrin Mannheim Italia S p A

Compounds of formula I wherein R1 is alkoxy carbonyl, aminocarbonyl, acetyl, ben; cyano or nitro group; R2 is as optionally s stituted phenyl, aryl, hetaryl residue; R3 is alkoxy-carbonyl group, X is an oxygen or ~, phur atom, R4 is hydrogen, an optionally s stituted alkyl, cycloalkyl, alkenyl group, Y i single bond oxygen, sulphur or substitu nitrogen atom. Compounds of formula I are r pared by acylation from a 2-mercaptometh3 4-dihydropyridine and are useful in therapy.

4935441

FLAVENE AND THIOFLAVEN[ DERIVATES, PROCESSES FOR

THEIR MANUFACTURE, PHARMACEUTICAL

PREPARATIONS THAT CONTAI SUCH COMPOUNDS, AND TH]

USE OF THE LATTER

Christian Rimbault, Gran Lancy, Switzed~ assigned to Zyma SA

Compounds of the formula I See Patent Chemical Structure (I) wherein rings A and B each unsubstituted or substituted; Y is oxy8 sulfur, sulfinyl or sulfonyl; one of the symbols and Z2 is halogen and the other formyl; pharmaceutically acceptable salts of such cc pounds that contain a salt-forming group useful for the treatment of diseases of respiratory tract and of liver diseases. They prepared by methods known per se.