Patent GB-974522-A (GB)
Title: Pharmaceutical compositions for the treatment of coronary artery disease
Inventor: STEPHENSON JOHN STUART
IPC: A61K31/00
Filed: 1962-01-15
Abstract: 974,522. Pharmaceutical compositions for the treatment of coronary artery disease. IMPERIAL CHEMICAL INDUSTRIES Ltd. Dec. 17, 1962 [Jan. 15, 1962], No. 1354/6.2. Heading A5B. Pharmaceutical compositions possessing #- adrenergic blocking activity contain as active ingredient at least one compound of the formula wherein R stands for hydrogen or for a lower alkyl radical containing not more than 5 carbon atoms, and R<SP>1</SP> stands for hydrogen when R<SP>2</SP> stands for hydrogen or an unbranched alkyl radical containing not more than 4 carbon atoms or for a benzyl radical, a #-phenylethyl radical, a cyclohexyl radical, or a 1,2,3;4-tetrahydro-2- naphthyl radical, or R<SP>1</SP> stands for a methyl radical when R<SP>2</SP> stands for an unbranched alkyl radical containing not more than 4 carbon atoms, or for a branched alkyl radical containing 3 or 4 carbon atoms, or a benzyl radical, a #- phenylethyl radical, a cyclohexyl radical, or a 1,2,3,4-tetrahydro-2-naphthyl radical, or R<SP>1</SP> stands for a branched or unbranched alkyl radical containing 2, 3 or 4 carbon atoms when R<SP>2</SP> stands for an alkyl radical containing 2, 3 or 4 carbon atoms, or R<SP>1</SP> and R<SP>2</SP>, together with the adjacent nitrogen atom, form a heterocyclic ring and wherein the naphthalene nucleus may optionally bear one or more additional substituents, or a pharmaceutically-acceptable salt thereof, in admixture with one or more pharmaceutically-acceptable diluents or carriers therefor. The optional substituents in the naphthalene nucleus may be halogen and lower alkyl and alkoxy radicals containing not more than 5 carbon atoms. The active salts may be derived from hydrochloric, hydrobromic, phosphoric, sulphuric, oxalic, lactic, tartaric, acetic, salicylic and citric acids. Active ingredients specified are 1-(21-naphthyl)-2-amino-, 1-(2<SP>1</SP>- naphthyl) - 2 - methylamino-, 1 - (2<SP>1</SP>- naphthyl)- 2 - ethylamino-, 1 - (2<SP>1</SP>- naphthyl) - 2 - n - propylamino-, 1 - (2<SP>1 </SP>- naphthyl) - 2 - n - butylamino-, 1 - (2<SP>1</SP> - naphthyl) - 2 - cyclohexylamino-, 1-(21- naphthyl) - 2 - dimethylamino- and 1 - (2<SP>1</SP>-naphthyl) - 2 - di - isopropylamino - ethanol, 1 - (2<SP>1</SP>- naphthyl) - 2 - piperidinoethanol, 1 - (2<SP>1 </SP>- naphthyl) - 2 - aminopropanol, 1 - (2<SP>1</SP> - naphthyl)-2- benzylaminoethanol, 1 - (2<SP>1</SP> - naphthyl) - 2 - (2<SP>1</SP>- phenylethylamino) - ethanol, 1 - (2<SP>1 </SP>- naphthyl)- 2 - diethylaminoethanol, 1 - (2<SP>1 </SP>- naphthyl) - 2 - morpholinoethanol, 1 - (1<SP>1</SP> - methoxy - 2<SP>1</SP>- naphthyl) - 2 - aminopropanol, 1 - (5<SP>1</SP> - bromo- 61 - methoxy - 2<SP>1</SP> - naphthyl) - 2 - di - n - butylaminoethanol, 1 - (2<SP>1</SP> - naphthyl) - 2 - (1<SP>1</SP>,2<SP>1</SP>,3<SP>1</SP>,4<SP>1</SP>- tetrahydroisoquinolino) - ethanol and 1 - (2<SP>1</SP>- naphthyl) - 2 - (1<SP>1</SP>,2<SP>1</SP>,3<SP>1</SP>,4<SP>1</SP> - tetrahydro - 21- naphthylamino)-ethanol and pharmaceutically acceptable salts thereof. The compositions may take the form of tablets, pills, capsules, aqueous or oily solutions, aqueous or oily suspensions, emulsions, injectable aqueous or oily solutions or suspensions, and dispersible powders. According to the definition of the active ingredients in the Provisional Specification, when R<SP>1</SP> stands for hydrogen or for a methyl radical, R<SP>2</SP> may be a cycloalkyl radical in the general formula given above.