2,6-Dichlorophenyl-substituted amino-imidazole derivatives and u

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...

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548315, 548337, A61K 31415, C07D23354

Patent

active

042750725

ABSTRACT:
The 2,6-dichlorophenyl-substituted amino-imidazole derivatives 1-(2',6'-dichlorophenyl)-2-amino-4-methyl-imidazole, 2-(2',6'-dichloroanilino)-4-methyl-imidazole, their non-toxic, pharmaceutically acceptable, acid addition salts and mixtures thereof, exhibit excellent anti-hypertensive activity which makes the derivatives particularly suitable for treatment of high blood pressure in mammals.
The derivatives may be prepared in either of two processes. The first process involves the sequential reaction of a known starting material with ammonia and a halogenated acetone which may be followed by separation of the formed isomers. The second process involves the decarboxylation of the novel intermediates 4-[1-(2',6'-dichlorophenyl)-2-amino)]-imidazoleacetic acid or 4-[2-(2',6'-dichloroanilino)]-imidazoleacetic acid or mixtures thereof. Such intermediates, their lower alkyl esters, their non-toxic, pharmaceutically acceptable acid addition salts or mixtures thereof may also be employed as a diuretic agent.
The derivatives are employed in an effective amount and are typically combined with a pharmaceutical carrier. Administration of the derivatives may be accomplished either orally or parenterally.

REFERENCES:
Jen. et al., Journal of Medicinal Chemistry, vol. 18, No. 1, (1975) pp. 90-99.

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