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New Patents iii with alkaline and/or alkaline-earth metals, am- monium salts, salts formed with compatible amines, with amino acids or with physiologically acceptable acids. A process is also described for their preparation. 4562061 PHARMACEUTICAL PREPARATION Curt Appelgren, Conny B Bogentoft, Gunnar H Ekenved, Kungsbacka, Sweden assigned to Ak- tiebolaget Hassle According to the present invention an oral pharmaceutical preparation of acetylsalicylic acid is provided which consists of cores con- taining acetylsalicylic acid as pharmaceutically active component, which cores are coated with a polymer membrane to the formation of coated granules. The preparation is characterized in that the polymer membrane comprises at least one polymer selected from the group consisting of cellulose acetate phtalate and methyl esterified methacrylic acid polymers having a degree of esterification of 45-55%, whereby the amount of such polymer forms 60-45% of the weight of the membrane, and at least one methyl esterified methacrylic acid polymer having a degree of esterification of 65-75% and forming 45-25% of the weight of the membrane, and a plasticizer selected from fatty alcohols and fatty acids forming 4-12% of the weight of the mem- brane, whereby the membrane represents 5-12 weight % of the composition. With this composi- tion a reduced effect on the gastric mucosa as compared with previously known preparations but retaining good absorbtion properties and a controlled release. alkanesulfonyl or arenesulfonyl; R3, R4 and R5 are each lower alkyl; n is 0 or 1 A is lower alky- lene optionally interrupted by a -NHCO- group; and Q is oxido or lower alkoxy; provided that n is 0 or A is lower alkylene interrupted by a - NHCO- group, or Q is lower alkoxy, when R1 is alkoxy and R2 is lower alkyl; and pharma- ceutically acceptable salts thereof, which exhibit antitumor activity. 4562186 (1,2,4-OXADIAZOL-3- YL)ARYLMETHANONES, COMPOSITIONS AND PHARMACEUTICAL USE John J Tegeler, Craig J Diamond assigned to Hoechst-Roussel Pharmaceuticals Inc There are disclosed novel compounds having the formula See Patent for Chemical Structure where X is hydrogen, halogen (F, CI, Br or I), loweralkyl or loweralkoxy; and R is -CH, - CONH2, -COOCH(CH3)2, -COOH, - COO(CH2)4CI, See Patent for Chemical Structure See Patent for Tabular Presentation RI and R2 being independently hydrogen or lower alkyl and R3 being See Patent for Chemical Structure See Patent for Tabular Presentation an optical antipode thereof or a pharmaceutically acceptable acid addition salt thereof, which are useful as antihypertensive, analgesic and anti- inflammatory agents, methods for synthesizing them, and pharmaceutical compositions com- prising an effective amount of such a compound. 4562187 4562179 PHOSPHOLIPID DERIVATIVES, AND PHARMACEUTICAL COMPOSITION OF THE SAME (ISOXAZOL-3- YL)ARYLMETHANONES, COMPOSITIONS AND PHARMACEUTICAL USE John J Tegeler, Craig J Diamond assigned to Hoechst-Roussel Pharmaceuticals Inc Tsutom Teraji, Eishiro Todo, Norihiko Shimazaki, Teruo Oku, Takayuki Namiki, Osaka, Japan assigned to Fujisawa Pharma- ceutical Co Ltd New phospholipid derivatives represented by the formula: See Patent for Chemical Structure (I) wherein R1 is alkyl, alkoxy or alkanoylamino; R2 is lower alkyl, lower There are disclosed novel compounds having the formula See Patent for Chemical Structure where each X is independently hydrogen, halogen (F, C1, Br or I), loweralkyl or loweralkoxy; m is 1 or 2; R' is hydrogen or loweralkyl; and R is See Pa- tent for Chemical Structure See Patent for Tabular Presentation See Patent for Tabular Pre- sentation n being 1, 2 or 3, each of R1 and R2 being independently hydrogen or loweralkyl and

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Page 1: 4562061 Pharmaceutical preparation

New Patents iii

with alkaline and/or alkaline-earth metals, am- monium salts, salts formed with compatible amines, with amino acids or with physiologically acceptable acids. A process is also described for their preparation.

4562061

PHARMACEUTICAL PREPARATION

Curt Appelgren, Conny B Bogentoft, Gunnar H Ekenved, Kungsbacka, Sweden assigned to Ak- tiebolaget Hassle

According to the present invention an oral pharmaceutical preparation of acetylsalicylic acid is provided which consists of cores con- taining acetylsalicylic acid as pharmaceutically active component, which cores are coated with a polymer membrane to the formation of coated granules. The preparation is characterized in that the polymer membrane comprises at least one polymer selected from the group consisting of cellulose acetate phtalate and methyl esterified methacrylic acid polymers having a degree of esterification of 45-55%, whereby the amount of such polymer forms 60-45% of the weight of the membrane, and at least one methyl esterified methacrylic acid polymer having a degree of esterification of 65-75% and forming 45-25% of the weight of the membrane, and a plasticizer selected from fatty alcohols and fatty acids forming 4-12% of the weight of the mem- brane, whereby the membrane represents 5-12 weight % of the composition. With this composi- tion a reduced effect on the gastric mucosa as compared with previously known preparations but retaining good absorbtion properties and a controlled release.

alkanesulfonyl or arenesulfonyl; R3, R4 and R5 are each lower alkyl; n is 0 or 1 A is lower alky- lene optionally interrupted by a -NHCO- group; and Q is oxido or lower alkoxy; provided that n is 0 or A is lower alkylene interrupted by a - NHCO- group, or Q is lower alkoxy, when R1 is alkoxy and R2 is lower alkyl; and pharma- ceutically acceptable salts thereof, which exhibit antitumor activity.

4562186

(1,2,4-OXADIAZOL-3- YL)ARYLMETHANONES,

COMPOSITIONS AND PHARMACEUTICAL USE

John J Tegeler, Craig J Diamond assigned to Hoechst-Roussel Pharmaceuticals Inc

There are disclosed novel compounds having the formula See Patent for Chemical Structure where X is hydrogen, halogen (F, CI, Br or I), loweralkyl or loweralkoxy; and R is -CH, - CONH2, -COOCH(CH3)2, -COOH, - COO(CH2)4CI, See Patent for Chemical Structure See Patent for Tabular Presentation RI and R2 being independently hydrogen or lower alkyl and R3 being See Patent for Chemical Structure See Patent for Tabular Presentation an optical antipode thereof or a pharmaceutically acceptable acid addition salt thereof, which are useful as antihypertensive, analgesic and anti- inflammatory agents, methods for synthesizing them, and pharmaceutical compositions com- prising an effective amount of such a compound.

4562187

4562179

PHOSPHOLIPID DERIVATIVES, AND PHARMACEUTICAL

COMPOSITION OF THE SAME

(ISOXAZOL-3- YL)ARYLMETHANONES,

COMPOSITIONS AND PHARMACEUTICAL USE

John J Tegeler, Craig J Diamond assigned to Hoechst-Roussel Pharmaceuticals Inc

Tsutom Teraji, Eishiro Todo, Norihiko Shimazaki, Teruo Oku, Takayuki Namiki, Osaka, Japan assigned to Fujisawa Pharma- ceutical Co Ltd

New phospholipid derivatives represented by the formula: See Patent for Chemical Structure (I) wherein R1 is alkyl, alkoxy or alkanoylamino; R2 is lower alkyl, lower

There are disclosed novel compounds having the formula See Patent for Chemical Structure where each X is independently hydrogen, halogen (F, C1, Br or I), loweralkyl or loweralkoxy; m is 1 or 2; R' is hydrogen or loweralkyl; and R is See Pa- tent for Chemical Structure See Patent for Tabular Presentation See Patent for Tabular Pre- sentation n being 1, 2 or 3, each of R1 and R2 being independently hydrogen or loweralkyl and