Phosphocholine linked prodrug derivatives

Details Phosphocholine linked prodrug derivatives Phosphocholine linked prodrug derivatives

2006-06-13

2006-06-13

Kishore, Gollamudi S. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

C514S078000, C514S079000, C514S100000, C540S456000, C540S460000, C540S478000, C544S243000, C544S337000, C546S023000, C548S113000, C548S119000

Reexamination Certificate

active

07060290

ABSTRACT:
Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.

REFERENCES:
patent: 5534499 (1996-07-01), Ansell
patent: 5703063 (1997-12-01), Chasalow
patent: 5776915 (1998-07-01), Peterson
patent: 5830432 (1998-11-01), Chasalow
patent: 96/16680 (1996-06-01), None
patent: WO 98/11906 (1998-03-01), None

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