New Patents iii

group; whereas Y stands for -NH- when R5 stands for a hydrogen atom and a valence bond exists between the C2, and C7, atoms, as well as their acid addition salts and pharmaceutical pre- parations containing these compounds. Further on, the invention relates to a process for pre- paring these compounds and preparations. The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.

4746671

P H A R M A C E U T I C A L U S E O F ( 3 - P Y R I D I N Y L - M E T H Y L E N -

A M I N O - O X Y ) A L K A N O I C A C I D S A N D E S T E R S

Eddy J Freyne, Alfons H M Raeymaekers, Vic- tor Sipido, Marc G Venet, Rumst, Belgium as- signed to Janssen Pharmaceutica N V

Novel (3-pyridinyl-methylen-amino- oxy)alkanoic acids and esters, compositions con- taining the same, and methods of treating clinical conditions related with the production of thromboxane A2, prostacyclin and/or pros- taglandins D2, E2 and F2 alpha.

4746667

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 C O N T A I N I N G

2 - ( 2 - B E N Z I M I D A Z O L Y L T H I O M E T H Y L ) P Y R I D I N E

Enar I Carlsson, Hakan S Larsson, Sundell Gun- hild W yon Wittken, Viola Samuelsson- Junggren, Kenneth Lundstrom, VFr Sweded assigned to Aktiebolaget Hassle

A pharmaceutical preparation containing as ac- tive ingredient a compound of the formula See Patent for Chemical Structure or a therapeutically acceptable salt thereof in which formula R1 and R2 are the same or different and each selected from the group consisting of H, CF3, NO2, -COOCH3, -COOC2H5, alkyl con- taining 1-7 carbon atoms, halogen, alkoxy, con- taining 1-5 carbon atoms, and alkanoyl containing 1-4 carbon atoms; R is selected from the group consisting of H, alkanoyl containing 1- 4 carbon atoms, and carboalkoxy containing 2-6 carbon atoms; and R3, R4 and RS, which are the same or different, are each selected from the group consisting of H, CH3, C2H5, OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3; provided that (a) at least one of R3, R4 and R5 is selected from the group consisting of CH3, C2H5, OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3, and (b) when two of R3, R4 and R5 are H, then the remaining radical R3, R4 or R5 is selected from the group consisting of OCH3, OC2H5, OCH2CH2OCH3, and OCH2CH2OCH2CH3; the use of the compounds for inhibiting gastric acid secretion; compounds included in the for- mula I, and processes for their preparation.

4746672

O X I D E S O F 1 , 2 , 5 - T H I A D I A Z O L E S , T H E I R U S E I N

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

Tobias O Yellin, Philip Edwards, Michael Large assigned to ICI Americas Inc

Sulphur derivatives which are histamine H-2 an- tagonists and which inhibit gastric acid secretion of the formula I: See Patent for Chemical Struc- ture I in which R1 and R2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4- 14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, CI or Br atoms, provided that one of R 1 and R2 is halogen substituted; ring X is a heterocyclie ring as defined in the specification; A is pheny- lene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R3 is a variety of radicals described in the specification; and the pharmaceuticaUy-aggqftable acid-addition salts thereof. M a~md~cturing processes for the derivatives, :-'-rmediates and pharmaceutical compositions are also part of the invention.

4746675

E X T E R N A L 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

Yuji Makino, Yoshiki Suzuki, Hino, Japan as- signed to Teijin Limited

A pharmaceutical composition for external use with the enhanced penetration of a pharma-