Antihypertension treatment

A - Human Necessities – 61 – K

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167/208, 167/246

A61K 31/13 (2006.01) A61K 31/395 (2006.01)

Patent

CA 1175749

-a- ABSTRACT OF THE DISCLOSURE The present specification discloses a class of chemical compounds the members of which when introduced by ingestion, injection, absorption, or otherwise into a mammal (including man), produce avoidance, amelioration and/or inprovement of a hyper- tensive conditon in mammals and man when used in an antihyper- tensively effective amount as taught herein. The active anti- hypertensive agents used in the compositions of the present invention fall into four broad categories. They are: (1) the inorganic salts of sulfurous acid which display anti- hypertensive activity, specifically the alkali metal, alkaline earth metal, and ammonium salts of sulfites and bisulfites (including metabisulfites) and mixtures thereof. Alkali metal, particularly sodium and potassium bisulfites are preferred active agents, and, of these, sodium bisulfite is a presently most pre- ferred active agent. Also, because of similar toxicological considerations, the calcium, magnesium, and ammonium compounds are also preferred. (2) A compound of the formula: Image in which R is hydrogen or hydroxymethyl, R1 is hydrogen, a straight chain alkyl containing 2 to 5 hydroxylated carbon atoms, or residue of a polysaccharide capable of reducing Fehling's solution, while X is an alkali metal or ammonium. Illustrative compounds include sodium glucose bisulfite and sodium formaldehyde bisulfite. (3) A lower alkyl amine sulfite compound of the formula: - b - Image where R1 is lower alkyl, cycloalkly containing from 6 to 10 carbon atoms each, lower monohydroxyalkyl or aralkyl, R2 is hydrogen, lower alkyl or lower monohydroxyalkyl, or R1 and R2 together constitute a morpholine, piperidine, or hexamethyleneimine ring, provided that each such ring can be substituted on one of its carbon atoms by lower alkyl radical, R3 is lower aalkyl, lower monohydroxyalkyl, hydrogen, or a compound of the formula: Image in which R4 is a divalent saturated lower aliphatic radical, m and n are intergers, the sum of m and n is 2, and n is eithr 0 or 1.

417902

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