US 5,627,057 A · Inhibitor compounds of farnesyl-protein transferase and chemotherapeutic compositions containing the same, produced by strain ATCC 55532

Abstract

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras. Furthermore, Actinoplanes sp. ATCC 55532 and Streptomces sp. ATCC 55550 are microorganisms which are capable of producing the disclosed compounds which are classified as carboxylic acid esters. In addition a method for preparing the compounds is disclosed which includes cultivating strain ATCC 55532 or strain ATCC 55550. The strains are independently capable of producing the carboxylic acid ester compounds.

Claims3

Dependent claims

A biologically pure culture of Actinoplanes sp. MA 7066 (ATCC 55532), or an active mutant thereof capable of producing in recoverably amounts a compound selected from the group consisiting of:

1,2,3-propanetricarboxylic acid 1-[10-[4-carboxy-19-(6-carboxy-4-ethyl-3-oxoheptyl)-12-hydroxy-11,13,15,17 -tetramethyl-2,6-dioxo-1,7-dioxacycloeiocosa-14,18-dien-8yl]-1,4-dimethyl-5 -decenyl]ester having the structure:
##STR11##
and 1. 2,3-propanetricarboxylic acid 1-[28-carboxy-11-[[3,4-dicarboxy-1-oxopentyl]oxy]-26-ethyl-15-hydroxy-1,4, 14,16,18,20,22-heptamethyl-25-ox-5,17,21-nonacosatrienyl]ester having the structure:
##STR12##

1 more element

Dependencies are inferred from the claim text.

Facts

Application

08/611,700Filed 6 Mar 1996 · division

Priority

6 Jun 1994

Granted

6 May 1997

Term ends

Not estimatedThe source records don’t support an estimate.

Classification17 codes

C12N 1/205
Bacteria; Culture media therefor: bacterial isolates
A61K 31/225
Of acyclic acids, e.g. pravastatin: polycarboxylic acids
A61K 31/231
Of acids having a carboxyl group bound to a chain of seven or more carbon atoms: having one or two double bonds
A61K 31/232
Of acids having a carboxyl group bound to a chain of seven or more carbon atoms: having three or more double bonds, e.g. etretinate

Inhibitor compounds of farnesyl-protein transferase and chemotherapeutic compositions containing the same, produced by strain ATCC 55532

Life of this patent

Inhibitor compounds of farnesyl-protein transferase and chemotherapeutic compositions containing the same, produced by strain ATCC 55532

Life of this patent

Abstract

Claims3