Hypocholesteremic fermentation products

• US 4,342,767 A
• Filed: 06/16/1980
• Issued: 08/03/1982
• Est. Priority Date: 01/23/1980
• Status: Expired due to Term

• Current Assignee: MSD Techology L.P.
• Original Assignee: Merck & Co., Inc.
• Inventors: Monaghan, Richard L., Albers-Schonberg, George, Alberts, Alfred W., Hoffman, Carl H.
• Primary Examiner(s): Trousof, Natalie
• Assistant Examiner(s): Pepper, Frederick W.
• Application Number:
  US06/159,983
• Time in Patent Office: 778 Days
• Field of Search: 560/119, 560/252, 560/256, 548/327, 544/358, 424/305, 424/311, 424/289, 424/273 B, 424/250, 260/429.9, 260/448 R
• US Class Current: 514/548
• CPC Class Codes: C07D 309/30 Oxygen atoms, e.g. delta-lactones
• CPC Class Codes: C12P 17/06 containing a six-membered hetero ring, e.g. fluorescein
• CPC Class Codes: C12P 7/62 Carboxylic acid esters

Abstract

Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise compounds which have structures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.

Claims

1. The compound:

##STR6## or a pharmaceutically acceptable salt or a lower alkyl ester or a substituted lower alkyl ester wherein the substituent is phenyl, dimethylamino, or acetylamino.

2. The pharmaceutically acceptable salts of the compounds of claim 1, wherein the cation is derived from ammonia, ethylenediamine, N-methylglucamine, lysine, arginine or ornithine.

3. The ammonium salt of compound II of claim 1.

4. The ethylenediamine salt of compound II of claim 1.

5. The lower alkyl esters and substituted lower alkyl esters of the compound of claim 1.

6. The ethyl ester of compound II of claim 1.

7. An antihypercholesteremic pharmaceutical composition comprising a pharmaceutical carrier and an effective amount of the compound:

##STR7## or a pharmaceutically acceptable salt or a lower alkyl ester or a substituted lower alkyl ester wherein the substituent is phenyl, dimethylamino, or acetylamino.

8. The composition of claim 7 wherein the compound is a pharmaceutically acceptable salt wherein the cation is derived from ammonia, ethylenediamine, N-methylglucamine, lysine, arginine or ornithine.

9. The composition of claim 7 wherein the compound is the ammonium salt of compound II.

10. The composition of claim 7 wherein the compound is the ethylenediamine salt of compound II.

11. The composition of claim 7 wherein the compound is a lower alkyl ester or substituted lower alkyl ester.

12. The composition of claim 7 wherein the compound is the ethyl ester of compound II.