1
New Patents xix New compounds of general formula See Patent for Chemical Structure I and salts therewith of pharmaceutically acceptable acids, wherein R and R1 independently represent a hydrogen atom or a straight or branched alkyl group having from 1 to 5 carbon atoms, and n is an in- teger from 4 to 12; and of general formula See Patent for Chemical Structure II wherein R'I represents a straight or branched alkyl group having from 2 to 4 carbon atoms, W represents hydroxymethyl or the COOM group in which M stands for a hydrogen atom, an alkali metal or an equivalent of an alkali earth metal and n is an in- teger from 6 to 8. The compounds are useful in treating hyperlipidaemia. 4454155 PHARMACEUTICAL COMPOSITIONS CONTAINING A MONO-SUBSTITUTED DERIVATIVE OF 4-PHENYL-4- OXOBUTEN-2-OIC ACID, AND METHODS OF USING THEM IN TREATING GASTRIC AND GASTRODUODENAL AILMENTS Yan Chrisridis, Fernando Barzaghi, Paris, France assigned to Roussel UCLAF R! ~ C~ ]cH~.~C~C~OR II I II O R20 Pharmaceutical compositions containing a com- pound of the formula (I): See Patent for Chem- ical Structure (I) in which R represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms, R1 represents a hydroxy radical in 2-posirion or an alkoxy radical in 4-position containing from 1 to 8 car- bon atoms, and R2 represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms. Pharmaceutically acceptable alkali metal, alkaline earth metal, ammonium or amine salts of the compounds of formula (I) in which R represents a hydrogen atom may also be in- cluded in the compositions. Such compositions are useful in treating hyperchlorhydria, gastric or gastroduodenal ulcers, gastritis, hiatal her- nias, and gastric or gastroduodenal ailments accompanied by gastric hyperacidity. 4455298 PHARMACEUTICAL PREPARATIONS WITH GASTRO- PROTECTIVE ACTION Stuart J McFarlane, John E Croft, Auckland, New Zealand The invention concerns novel pharmaceutical preparations containing (A) an extract of the mollusc Perna canaliculus, a mussel which is found on the shores of New Zealand, and (B) a pharmaceutically active substance, especially medicaments having anti-phlogistic, antipyretic and/or analgetic action, which, when taken per se, may cause as a side effect irritation of the gastro-intestinal mucosae and possibly the for- marion of ulcers. The addition of a mollusc extract according to (A) to the said medicaments has a gastro-protective action, in that the oc- curence of the said side effects is prevented or diminished. The component (A) is preferably used as a dry powder of the whole of the flesh of the mollusc or a dry powder obtained from the gonads thereof. In a typical preparation ac- cording to the invention an extract of the gonads is e.g. combined with acetyl-salicylic acid. The preparations may contain the 2 components in one and the same dosage unit form, e.g. a capsule or in 2 different ones, e.g. a capsule and a tablet. The invention also includes a method for pre- venting, alleviating or treating gastro-intestinal irritation or ulcer formation by administering an effective amount of the mollusc extract as defined under A. 4455422 CARBOSTYRIL DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME Kazuo Banno, Takafum Fujioka, Masaaki Osaki, Kazuyuki Nakagawa, Tokushima, Japan assigned to Otsuka Pharmaceutical Co Ltd Novel carbostyril derivatives and their salts, having antihistaminic effect and central nervous system controlling effect, are represented by the general formula (1), See Patent for Chemical Structure (1) wherein R1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, a lower alkynyl group; A is a group of the formula See Patent for Chemical Structure (wherein R2 is a hydrogen atom or a

4455298 Pharmaceutical preparations with gastro-protective action

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New Patents xix

New compounds of general formula See Patent for Chemical Structure I and salts therewith of pharmaceutically acceptable acids, wherein R and R1 independently represent a hydrogen atom or a straight or branched alkyl group having from 1 to 5 carbon atoms, and n is an in- teger from 4 to 12; and of general formula See Patent for Chemical Structure II wherein R'I represents a straight or branched alkyl group having from 2 to 4 carbon atoms, W represents hydroxymethyl or the COOM group in which M stands for a hydrogen atom, an alkali metal or an equivalent of an alkali earth metal and n is an in- teger from 6 to 8. The compounds are useful in treating hyperlipidaemia.

4454155

PHARMACEUTICAL COMPOSITIONS CONTAINING A

MONO-SUBSTITUTED DERIVATIVE OF 4-PHENYL-4- OXOBUTEN-2-OIC ACID, AND

METHODS OF USING THEM IN TREATING GASTRIC AND

GASTRODUODENAL AILMENTS

Yan Chrisridis, Fernando Barzaghi, Paris, France assigned to Roussel UCLAF

R!

~ C~ ]cH~..~C~C~OR II I II O R20

Pharmaceutical compositions containing a com- pound of the formula (I): See Patent for Chem- ical Structure (I) in which R represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms, R1 represents a hydroxy radical in 2-posirion or an alkoxy radical in 4-position containing from 1 to 8 car- bon atoms, and R2 represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms. Pharmaceutically acceptable alkali metal, alkaline earth metal, ammonium or amine salts of the compounds of formula (I) in which R represents a hydrogen atom may also be in- cluded in the compositions. Such compositions are useful in treating hyperchlorhydria, gastric or gastroduodenal ulcers, gastritis, hiatal her- nias, and gastric or gastroduodenal ailments accompanied by gastric hyperacidity.

4455298

PHARMACEUTICAL PREPARATIONS WITH GASTRO-

PROTECTIVE ACTION

Stuart J McFarlane, John E Croft, Auckland, New Zealand

The invention concerns novel pharmaceutical preparations containing (A) an extract of the mollusc Perna canaliculus, a mussel which is found on the shores of New Zealand, and (B) a pharmaceutically active substance, especially medicaments having anti-phlogistic, antipyretic and/or analgetic action, which, when taken per se, may cause as a side effect irritation of the gastro-intestinal mucosae and possibly the for- marion of ulcers. The addition of a mollusc extract according to (A) to the said medicaments has a gastro-protective action, in that the oc- curence of the said side effects is prevented or diminished. The component (A) is preferably used as a dry powder of the whole of the flesh of the mollusc or a dry powder obtained from the gonads thereof. In a typical preparation ac- cording to the invention an extract of the gonads is e.g. combined with acetyl-salicylic acid. The preparations may contain the 2 components in one and the same dosage unit form, e.g. a capsule or in 2 different ones, e.g. a capsule and a tablet. The invention also includes a method for pre- venting, alleviating or treating gastro-intestinal irritation or ulcer formation by administering an effective amount of the mollusc extract as defined under A.

4455422

CARBOSTYRIL DERIVATIVES AND PHARMACEUTICAL

COMPOSITION CONTAINING THE SAME

Kazuo Banno, Takafum Fujioka, Masaaki Osaki, Kazuyuki Nakagawa, Tokushima, Japan assigned to Otsuka Pharmaceutical Co Ltd

Novel carbostyril derivatives and their salts, having antihistaminic effect and central nervous system controlling effect, are represented by the general formula (1), See Patent for Chemical Structure (1) wherein R1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, a lower alkynyl group; A is a group of the formula See Patent for Chemical Structure (wherein R2 is a hydrogen atom or a