Acylated phospholipid drugs
This invention relates to means for improving the efficacy of a drug containing a carboxy group by esterifying the drug to a glycerol phospholipid. The present invention also relates to the product obtained therefrom and the method of using the resulting product to treat various pathological conditi...
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Zusammenfassung: | This invention relates to means for improving the efficacy of a drug containing a carboxy group by esterifying the drug to a glycerol phospholipid. The present invention also relates to the product obtained therefrom and the method of using the resulting product to treat various pathological conditions in animals, especially mammals.
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 Rand Ris 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 andR is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources;Ris hydrogen or lower alkyl andRis 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 RZR;Z is O or S; Rand Rare 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 Rand Rdoes 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. |
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