ALKANOLAMINE DERIVATIVES

摘要

1312055 Pharmaceutical compositions IMPERIAL CHEMICAL INDUSTRIES Ltd 19 April 1971 [20 April 1970] 18738/70 Addition to 1269775 Heading A5B [Also in Division C2] Pharmaceutical compositions, suitable for oral or parenteral administration, contain novel alkanolamines of the formula: wherein R1 is H or alkyl; R2 is H or alkyl which may optionally be substituted by one or more substituents selected from OH, aryl and aryloxy, or cycloalkyl; wherein R3 is H or alkyl; R4 is branched chain butyl; R5 is H, halogen, acylamino, alkyl, alkenyl, nitro, alkylthio, alkoxy, alkenyloxy or acyl; or esters thereof; or acid acid addition salts thereof: or compounds of the formula: wherein R7 is alkyl, hydroxyalkyl, alkoxyalkyl cycloalkyl, alkenyl, aralkyl or substituted aralkyl; and R8 is H, halogen, alkyl, alkenyl, nitro, alkylthio, alkoxy, alkenyloxy or acyl; or esters thereof; or acid addition salts thereof; or one of the following compounds: 1-[2-chloro-4-(N-n-butyl carbamoyl) phenoxy]-3-t-butyl-amino-2-propanol, 1-[2-chloro-4-(N-n-pentylcarbamoyl)-phenoxy]-3-t-butylamino - 2 - propanol, 1-(2-chloro-4-N-cyclohexylcarbamoylphenoxy)-3-t-butylamino-2-propanol, 1-(2-chloro-4- N-cyclohexycarbamoyl phenoxy)-3-isopropylamino-2-propanol, 1-[2-bromo-4-(N-n-hexylcarbamoylphenoxy]-3-t-butylamino - 2 - propanol, 1-(4-N-isopropylcarbamoyl- 2 - methoxyphenoxy)-3-t-butylamino-2-propanol; or 1-[4-N-nbutyl-carbamoyl)-2-methoxyphenoxy] - 3 - tbutylamino-2-propanol; or the esters thereof or the acid addition salts thereof in association with pharmaceutically acceptable diluents or carriers therefor. The compositions may be used in the treatment or prophylaxis of heart diseases, and some of the compounds possess selective #-adrenergic blocking activity. The above compositions may also contain one or more drugs selected from sedatives, for example phenobarbitone, meprobate and chlorpromazine; vasodilators, for example glyceryl trinitrate, pentaerythritol tetranitrate and isosorbide dinitrate; diuretics, for example chlorothiazide; hypotensive agents, for example reserpine, bethanidine and guanethidine; myocardial depressants, for example quinidine; agents used in the treatment of Parkinson's disease, for example benzhexol; cardiotonic agents, for example digitalis preparations; and sympathomimetic bronchodilators, for example isoprenaline, orciprenaline, adrenaline and ephedrine.