4-[(Carboxyl- and sulfamyl-substituted alkyl)-amino] benzoic acids and analogs

DETAILED DESCRIPTION OF THE INVENTION The compounds of the invention are new and novel 4-[(carboxyl- and sulfamyl-substituted alkyl)amino]benzoic acids and analogs which have therapeutically useful biological and pharmacological properties.
No hypolipemic activity has been reported in the literature for these compounds and they are different in structure and superior in action to other hypolipemic agents.
The compounds of this invention lower serum-lipid concentration and also decrease the deposition of lipids in the aorta.
The novel compounds of this invention are reliably absorbed from the gastrointestinal tract and cause little, if any gastrointesinal irritation.
4-Alkylaminobenzoic acids and esters thereof are described in our U.
S.
Pat.
No.
3,868,416.
We have now found that certain members of this class of compound can safely and effectively lower both serum sterols and triglycerides in warm-blooded mammals.
Such actions on serum-lipid components are considered to be very useful in the treatment of atherosclerosis, especially in contrast to available drugs whose action is much more limited.
For some time it has been considered desirable to lower serum-lipid levels and to correct lipoprotein imbalance in mammals as a preventive measure against atherosclerosis.
The compounds of the present invention do not act by blocking late stages of cholesterol biosyntheses and thus do not produce accumulation of intermediates such as desmosterol, as equally undesirable as cholesterol itself.
Compounds with the combination of therapeutically favorable characteristics possessed by those of the present invention can be safely administered to warm-blooded mammals for the treatment of hyperlipidemic and atherosclerotic states found in patients with or prone to heart attacks, to peripheral or cerebral vascular disease, and to stroke.
The 4-[(carboxy- and sulfamyl-substituted alkyl)amino]benzoic acids and analogs of the present invention are, in general, white crystalline solids having characteristic melting points and absorption spectra