Robert J Markovich

US Patent:

6602861, Aug 5, 2003

Filed:

Apr 16, 1992

Appl. No.:

07/869697

Inventors:

Charles Pidgeon - West LaFayette IN
Robert J. Markovich - Franklin Park NJ

Assignee:

Research Corporation Technologies, Inc. - Tucson AZ

International Classification:

A61K 31685

US Classification:

514 77, 514 78, 514 885, 554 78, 554 79, 554 80, 554 81

Abstract:

This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: or pharmaceutically acceptable salts thereof wherein one of R and R is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources; R is hydrogen or lower alkyl and R is hydrogen, hydrocarbyl containing from 1-18 carbon atoms in a principal chain and up to a total of 23 carbon atoms, said principal chain may contain 1-5 double bonds or 1-2 triple bonds; phenyl which may be unsubstituted or substituted with lower alkyl; naphthyl which may be unsubstituted or substituted with lower alkoxy; or R ZR ; Z is O or S; R and R are independently a hydrocarbyl chain containing from 1-18 carbon atoms in the principal chain and up to a total of 23 carbon atoms, said chain may be completely saturated or may contain 1-5 double bonds or 1-2 triple bonds; and the sum of the carbon atoms in R and R does not exceed 23. This invention also relates to the compounds prepared therefrom as well as the use of the compounds to treat diseases in animals.

US Patent:

58469559, Dec 8, 1998

Filed:

Jun 6, 1995

Appl. No.:

8/469312

Inventors:

Charles Pidgeon - West LaFayette IN
Robert J. Markovich - Franklin Park NJ

Assignee:

Research Corporation Technologies, Inc. - Tucson AZ

International Classification:

A61K 31685

US Classification:

514 77

Abstract:

This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: ##STR1## or pharmaceutically acceptable salts thereof wherein one of R. sub. 1 and R. sub. 2 is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or ##STR2## and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources; R. sub. 3 is hydrogen or lower alkyl and R. sub. 4 is hydrogen, hydrocarbyl containing from 1-18 carbon atoms in a principal chain and up to a total of 23 carbon atoms, said principal chain may contain 1-5 double bonds or 1-2 triple bonds; phenyl which may be unsubstituted or substituted with lower alkyl; naphthyl which may be unsubstituted or substituted with lower alkoxy; or R. sub. 5 ZR. sub. 6 ; Z is O or S; R. sub. 5 and R. sub.