New Patents vii

stereoselective hydrolysis of compound (II) into compound (I), having at least 80% by weight the S-configuration, and if desired converting com- pound (I) into the pharmaceutically acceptable salt or ester thereof.

high hydrophilicity and are soluble at approx- imately pH 4, compared to prior art compounds which are water-soluble only at higher pH and enhanced stability.

4886785

P Y R I M I D I N E D E R I V A T I V E S , P H A R M A C E U T I C A L

C O M P O S I T I O N S A N D M E T H O D O F U S I N G S A M E

Robert W Lambert, Joseph A Martin, Gareth J Thomas, Welwyn, United Kingdom assigned to Hoffmann-La Roche Inc

Compounds of the formula See Patent for Chemical Structure I wherein A is C l-8-alkylene, Ri is halogen, C1-4-alkyl or halo-(C1-4-alkyl), R2 is hydrogen, hydroxy or acyloxy, R3 is hydrogen or Cl-4-alkyl, R4 is aryl or aryloxy and X is O or NH, and tautomers thereof are described. The compounds of formula I and their tautomers possess antiviral activity and can be used in the form of medicaments for the con- trol and prevention of viral infections.

4886792

1 0 - D I H Y D R O - 1 0 - D E O X O I1- A Z A E R Y T H R O N O L I D E A

C O M P O U N D S , M E T H O D S A N D I N T E R M E D I A T E S F O R T H E

M A N U F A C T U R E T H E R E O F A N D T H E I R U S E IN

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

Giorgio Pifferi, Nevenka Lopotar, Gabrijela Kobrehel, KrnjevicHrvoje , CarevicOlga , Zagreb, Yugoslavia assigned to Sour Pliva

10-dihydro-10-deoxo 1 l-azaerythronolide A compounds and pharmaceutically acceptable acid addition salts of said compounds; methods and intermediates for the manufacture thereof; their use as antiinflammatory agents and pro- cesses for their preparation.

4886791

S O L U B L E D E R I V A T I V E S O F S I L Y B I N , A M E T H O D O F P R E P A R I N G T H E M , A N D

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

T H E M

Raffaell Giorgi, Marisa Conti, Oiorgio Pifferi, Milan, Italy assigned to Inverni della Beffa S p A

Novel water-soluble derivatives of silybin of en- hanced activity are provided as well as methods of preparing the derivatives and pharmaceutical compositions containing them. The novel derivatives according to the invention have the following general formula (I); See Patent for Chemical Structure See Patent for Tabular Pre- sentation where: R = H or PO(OH)2 and R' = PO(OH)2 The compounds of the invention are useful inter alia in therapy of liver disorders and other applications where an anti-radical ef- fect is required. They have the advantages of

4886806

F L A V O N E - 3 - C A R B O X Y L I C A C I D S C O M P O U N D S A N D

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

T H E M

Rainer Walenta, Reine Muller-Peddinghaus, Ivan Ban, Michael Wurl, Ulf Preuschoff, Wedemark, Federal Republic Of Germany as- signed to Kali-Chemie Pharma GmbH

Falvone-3-carboxylic acid compounds cor- responding to the Formula I: See Patent for Chemical Structure I wherein Ri, R2, R3, R4 and R5 represent hydrogen, lower alkyl, halogen, hydroxy, or etherified or esterified hydroxy, and Z-R6 stands for a basically sub- stituted alkoxy or amino group, as well as pro- cesses and intermediate products for their production. The compounds exhibit inflammation-inhibiting pharmacological ac- tivity.