New Patents v aryl, halogen, or oxygen function; except that R4 and R5 are not both hydrogen; and except for the compounds when R5 is hydrogen and R is methyl, i-propyl, branched butyl, methoxy methyl, 2-phenylethyl, or 2-phenylethylene; chromans and dihydrobenzofurans derived from these compounds; pharmaceutically acceptable salts, and metabolites and metabolic precursors of these compounds; processes for preparing the aforementioned types of compounds; use of the aforementioned types of compounds as anti- bacterial and/or antimycotic agents; and pharmaceutical compositions of such compounds. enoxy, halogen, cyano, carboxyamido or ureido group optionally separated from the phenyl ring by a methylene or ethylene bridge; R2 is hydrogen, halogen, lower alkyl or alkoxy; R3 is hydrogen, halogen, lower alkyl, lower alkoxy or R2 and R3, taken together, are a methylendioxy group; R4 is hydrogen or lower alkyl, endowed with remarkable cardioselective beta- adrenolytic properties, are described. The pro- cess for their preparation and pharmaceutical compositions containing them are also described. 4579730 PHARMACEUTICAL COMPOSITIONS CONTAINING INSULIN Miriam Kidron, Ehud Ziv, Hanoch Bar-On, Amiram Eldor, Jerusalem, Israel assigned to Hadassah Medical Organization The invention provides a pharmaceutical composition for the oral administration of insulin comprising insulin, a bile acid or alkali metal salt thereof, the bile acid being selected from the group consisting of cholic acid, chenodeoxy- cholic acid, taurocholic acid, taurochenodeoxy- cholic acid, glycocholic acid, glycochenocholic acid, 3 beta-hydroxy-12-ketocholic acid, 12 alpha-3 beta-dihydrocholic acid, and ursodesox- ycholic acid, and a protease inhibitor, the composition being provided with an enterocoating to assure passage through the stomach and release in the intestine. 4579861 ARYLOXYPROPANOLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND ADRENEGIC THEREOF Cesare Casagrande, Massimo Nicola, Arese, Italy assigned to Pierrel S p A Compounds having general formula I See Pa- tent for Chemical Structure I wherein R1 is hydrogen, lower alkyl, lower alkoxy, alkyl 4579867 STABLE PHARMACEUTICAL COMPOSITIONS OF SHORT- ACTING BETA-ADRENERGIC RECEPTOR BLOCKING AGENTS Agustin Escobar, Dietmar M Wagenknecht, Abu S Alam assigned to American Hospital Supply Corporation A pharmaceutical composition for parenteral administration is disclosed which comprises from about 0.01~o to about 30~o of a beta- adrenergic blocking compound of the formula See Patent for Chemical Structure I wherein Ar represents a substituted or unsubstituted aromatic group or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents -NR2CORI, NR2CONR 1R3, -NR2SO2R 1, NR2SO2NR2R3, 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 or W and B together denote Z which represents lower alkyl or aralkyl; or a pharmaceutically acceptable salt thereof in a hydroalcoholic solution including from about 5~ to about 50~o ethanol by volume of a phys- iologically acceptable polyhydric compound; from about 0.05 to about 2 molar phys- iologically acceptable buffering agent; said hydroalcoholic solution having a pH of from about 2.0 to about 4.0. The pharmaceutical compositions are useful in the treatment or prophylaxis of cardiac disorders.

4579867 Stable pharmaceutical compositions of short-acting beta-adrenergic receptor blocking agents

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Page 1: 4579867 Stable pharmaceutical compositions of short-acting beta-adrenergic receptor blocking agents

New Patents v

aryl, halogen, or oxygen function; except that R4 and R5 are not both hydrogen; and except for the compounds when R5 is hydrogen and R is methyl, i-propyl, branched butyl, methoxy methyl, 2-phenylethyl, or 2-phenylethylene; chromans and dihydrobenzofurans derived from these compounds; pharmaceutically acceptable salts, and metabolites and metabolic precursors of these compounds; processes for preparing the aforementioned types of compounds; use of the aforementioned types of compounds as anti- bacterial and/or antimycotic agents; and pharmaceutical compositions of such compounds.

enoxy, halogen, cyano, carboxyamido or ureido group optionally separated from the phenyl ring by a methylene or ethylene bridge; R2 is hydrogen, halogen, lower alkyl or alkoxy; R3 is hydrogen, halogen, lower alkyl, lower alkoxy or R2 and R3, taken together, are a methylendioxy group; R4 is hydrogen or lower alkyl, endowed with remarkable cardioselective beta- adrenolytic properties, are described. The pro- cess for their preparation and pharmaceutical compositions containing them are also described.

4579730

PHARMACEUTICAL COMPOSITIONS CONTAINING

INSULIN

Miriam Kidron, Ehud Ziv, Hanoch Bar-On, Amiram Eldor, Jerusalem, Israel assigned to Hadassah Medical Organization

The invention provides a pharmaceutical composition for the oral administration of insulin comprising insulin, a bile acid or alkali metal salt thereof, the bile acid being selected from the group consisting of cholic acid, chenodeoxy- cholic acid, taurocholic acid, taurochenodeoxy- cholic acid, glycocholic acid, glycochenocholic acid, 3 beta-hydroxy-12-ketocholic acid, 12 alpha-3 beta-dihydrocholic acid, and ursodesox- ycholic acid, and a protease inhibitor, the composition being provided with an enterocoating to assure passage through the stomach and release in the intestine.

4579861

ARYLOXYPROPANOLAMINE DERIVATIVES,

PHARMACEUTICAL COMPOSITIONS AND

ADRENEGIC THEREOF

Cesare Casagrande, Massimo Nicola, Arese, Italy assigned to Pierrel S p A

Compounds having general formula I See Pa- tent for Chemical Structure I wherein R1 is hydrogen, lower alkyl, lower alkoxy, alkyl

4579867

STABLE PHARMACEUTICAL COMPOSITIONS OF SHORT- ACTING BETA-ADRENERGIC

RECEPTOR BLOCKING AGENTS

Agustin Escobar, Dietmar M Wagenknecht, Abu S Alam assigned to American Hospital Supply Corporation

A pharmaceutical composition for parenteral administration is disclosed which comprises from about 0.01~o to about 30~o of a beta- adrenergic blocking compound of the formula See Patent for Chemical Structure I wherein Ar represents a substituted or unsubstituted aromatic group or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents -NR2CORI, NR2CONR 1R3, -NR2SO2R 1, NR2SO2NR2R3, 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 or W and B together denote Z which represents lower alkyl or aralkyl; or a pharmaceutically acceptable salt thereof in a hydroalcoholic solution including from about 5~ to about 50~o ethanol by volume of a phys- iologically acceptable polyhydric compound; from about 0.05 to about 2 molar phys- iologically acceptable buffering agent; said hydroalcoholic solution having a pH of from about 2.0 to about 4.0. The pharmaceutical compositions are useful in the treatment or prophylaxis of cardiac disorders.