Alkanolamine derivatives as {62 -adrenergic blocking agents

Claim 2

A PHARMACEUTICAL COMPOSITION FOR B-ADRENERGIC BLOCKING WHICH CONTAINS AS ACTIVE INGREDIENT AN EFFECTIVE B-ADRENERGIC BLOCKING AMOUNT OF AN ALKANOLAMINE DERIVATIVE SELECTED FROM THE GROUP CONSISTING OF COMPOUNDS OF THE FORMULA:

Claim 3

The composition as claimed in claim 1 wherein in the alkanolamine derivative used as active ingredient R1 is alkyl of 3,4 or 5 carbon atoms which is branched at the Alpha -carbon atom and which in unsubstituted or which bears one hydroxy or phenyl substituent attached to a carbon atom other than the Alpha -carbon atom.

Claim 4

The pharmaceutical composition as claimed in claim 1 wherein the active ingredient is selected from the group consisting of compounds of the formula given in claim 1, wherein R1 is isopropyl, s-butyl, t-butyl, cyclopropyl, cyclobutyl, cyclopentyl, 2-hydroxy-1,1-dimethylethyl, 1,1-dimethyl-2-phenylethyl, 1-methyl-2-phenylethyl, 1-methyl-3-phenylpropyl or 1-methyl-2-(p-methoxyphenyl)-ethyl, wherein R2 is hydrogen or methyl, wherein R3 is formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, pivaloyl, hexanoyl, heptanoyl, decanoyl, hydroxyacetyl, chloroacetyl, acryloyl, crotonoyl, ethoxycarbonyl, methane-sulphonyl, ethanesulphonyl, cyclopropanecarbonyl, cyclohexane-carbonyl, phenylacetyl, phenoxyacetyl, cinnamoyl, benzoyl, o-chlorobenzoyl, p-chlorobenzoyl, m-nitrobenzoyl, p-toluoyl, p-t-butylbenzoyl, p-acetamidobenzoyl, 2-furoyl, benzenesulphonyl or toluene-p-sulphonyl, and whereIn R4 is hydrogen, fluorine, chlorine, bromine, iodine, hydroxy, nitro, cyano, acetamido, trifluoro-methyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, s-butyl, t-butyl, t-pentyl, 1-methylheptyl, methoxymethyl, benzyl, Alpha -methylbenzyl, benzyloxy, phenyl, p-tolyl, phenoxy, p-tolyloxy, cyclohexyl, hydroxymethyl, methoxy, ethoxy, allyloxy, allyl, methylthio, ethylthio, acetyl, propionyl, methoxycarbonyl or ethoxycarbonyl; and the non-toxic, pharmaceutically acceptable hydrochloride or oxalate salts thereof.

Claim 5

The pharmaceutical composition as claimed in claim 1 wherein said active ingredient is selected from the group consisting of compounds of the formula:-

Claim 6

The pharmaceutical composition as claimed in claim 4 wherein R1 is isopropyl or t-butyl and R4 has the meaning stated in claim 3.

Claim 7

The pharmaceutical composition as claimed in claim 1 wherein the active ingredient is 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol or a non-toxic, pharmaceutically-acceptable acid-addition salt thereof.

Claim 8

The pharmaceutical composition as claimed in claim 1 wherein the active ingredient is 1-(2-nitro-4-propionamidophenoxy)-3-t-butylamino-2-propanol or a non-toxic, pharmaceutically-acceptable acid-addition salt thereof.

Claim 9

The pharmaceutical composition as claimed in claim 1 which is in the form of a tablet, capsule, aqueous or oily solution or suspension, emulsion, dispersible powder, granule, syrup, elixir, sterile injectable aqueous or oily solution or suspension, suppository, aerosol, spray or snuff.

Claim 10

A pharmaceutical composition which comprises a tablet containing a Beta -adrenergic blocking amount of between 25 mg. and 200 mg. of the compound 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol.

Claim 11

A pharmaceutical composition which comprises a tablet containing a Beta -adrenergic blocking amount of between 25 mg. and 200 mg. of the compound 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol.

Claim 12

A pharmaceutical composition which comprises a sterile aqueous solution containing a Beta -adrenergic blocking amount of between 0.05 percent and 1 percent w/v of the compound 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol or a non-toxic, pharmaceutically acceptable acid-addition salt thereof.

Claim 13

A pharmaceutical composition which comprises a sterile aqueous solution containing a Beta -adrenergic blocking amount of between 0.05 percent and 1 percent w/v of the compound 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol or a non-toxic, pharmaceutically acceptable acid-addition salt thereof.

Claim 14

A pharmaceutical composition which comprises, in combination, a cardioselective Beta -adrenergic blocking amount of an agent selected from the group consisting of 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol and the non-toxic, pharmaceutically acceptable acid-addition salts thereof and an effective amount of a sympathomimetic bronchodilator seclected from the group consisting of isoprenaline, orciprenaline, adrenaline and ephedrine and the non-toxic, pharmaceutically acceptable acid-addition salts thereof.

Claim 15

A pharmaceutical composition which comprises, in combination, a cardioselective Beta -adrenergic blocking amount of an agent selected from the group consisting of 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol and the non-toxic, pharmaceutically acceptable acid-addition salts thereof and an effective amount of a sympathomimetic bronchodilator seclected from the group consisting of isoprenaline, orciprenaline, adrenaline and ephedrine and the non-toxic, pharmaceutically acceptable acid-addition salts thereof.

Claim 16

The pharmaceutical composition according to claim 11 which is in the form of a sterile injectable aqueous solution, a sublingual tablet or an inhalation composition.

Claim 17

A method for effecting coronary Beta -adrenergic blockade in a warm-blooded animal, in need of such blockade, which comprises administering to said animal an effective Beta -adrenergic blocking amount of an alkanolamine derivative or salt thereof as defined in claim 1.

Claim 18

The method according to claim 13 wherein the compound administered is 1-(4-acetamidophenoxy)-3-isopropylamino-2-propanol or a non-toxic, pharmaceutically-accepTable acid-addition salt thereof.

Claim 19

The method according to claim 14 wherein the compound administered is 1-(2-nitro-4-propionamidophenoxy)-3-t-butylamino-2-propanol or a non-toxic, pharmaceutically-acceptable acid-addition salt thereof.