Amidic derivatives of nicotinic acid as therapeutics

Information

  • Patent Grant
  • 4100289
  • Patent Number
    4,100,289
  • Date Filed
    Monday, December 27, 1976
    48 years ago
  • Date Issued
    Tuesday, July 11, 1978
    46 years ago
  • Inventors
  • Original Assignees
  • Examiners
    • Friedman; Stanley J.
    Agents
    • Burns; Robert E.
    • Lobato; Emmanuel J.
    • Adams; Bruce L.
Abstract
A novel cysteine thiolactone of nicotinamide is disclosed having the formula: ##STR1## The compounds, homo-cysteine thiolactone of nicotinamide, and its pharmacologically acceptable salts have the useful pharmacological activity of lowering cholesterol, free fatty acid and triglyceride plasma level in the case of altered lipid metabolism and improving BSP clearance ratio in cases of liver injury.A synthesis of the compound from nicotinoyl chloride, hydrochloride or nicotinic acid esters is described as well as modes for the administration of the compound.
Description
Claims
  • 1. A Pharmaceutical composition for the treatment of elevated serum cholesterol, elevated serum free fatty acid levels, elevated serum lipids and/or impaired BSP clearance containing as an active component thereof an effective amount of the compound homocysterine thiolactone nicotinamide: ##STR4## and a non-toxic, pharmacologically acceptable salt thereof.
  • 2. A method of treating elevated serum cholesterol, elevated serum free fatty acid levels, elevated serum lipids and/or impaired BSP clearance which comprises administering to animals, having such malfunction, effective amounts of the composition of claim 1.
RELATED APPLICATIONS

This application is a divisional of application Ser. No. 668,498 filed Mar. 19, 1976 now U.S. Pat. 4,021,433 and which is a Continuation-in-Part of patent application Ser. No. 451,694 filed Mar. 15, 1974 and herewith abandoned. This invention relates to the novel homocysteine thiolactone of nicotinamide and its salts and more particularly to its synthesis, utility and modes for its useful administration. The compound: homocysteine thiolactone of nicotinamide having the formula: ##STR2## and its pharmacologically acceptable salts have useful pharmacological activity related to liver function and indicated therapeutic activity in lowering cholesterol, free fatty acid, and triglyceride, plasma levels and in improving BSP clearance in conditions where such effects are indicated.

US Referenced Citations (2)
Number Name Date Kind
3155672 Pasini et al. Nov 1964
3758485 Biniecki et al. Sep 1973
Divisions (1)
Number Date Country
Parent 668498 Mar 1976
Continuation in Parts (1)
Number Date Country
Parent 451694 Mar 1974