Carboxy containing ester prodrugs of corticosteroids

Details Carboxy containing ester prodrugs of corticosteroids Carboxy containing ester prodrugs of corticosteroids

C - Chemistry, Metallurgy

07

J

260/63

C07J 5/00 (2006.01) C07C 59/347 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01)

Patent

CA 1230328

ABSTRACT A compound of the formula Image wherein St represents a corticosteroid moiety bonded to the carbonyl via the 21-hydroxy group of corticosteroid; wherein Z is a bond or -O-; wherein n is an integer from 4 to 9; wherein Q is (1) Y-CH2COOH wherein Y is -S-, -S(O)-3 -S(O2)-, -SO2N(R)-, or -N(R)SO2; R is hydrogen or lower alkyl(C1-C4) with the proviso that the total carbon atoms in R and (CH2)n is not greater than 10; Image (2) or (3) Image wherein R1 is hydrogen and R2 is H, CH3, CH2COOH, CH2CH2COOH, CH2OH, CH2SH, CH2CH2SCH3, or CH2Ph-(OH) wherein Ph is phenyl and Ph-(OH) is p-hydroxyphenyl; or R1 is CH3 and R2 is H; or R1 and R2 taken together are -CH2CH2CH2-; or N(R1)CH(R2)COOH taken together is NHCH2CONHCH2COOH; and pharmaceutically salts thereof. These prodrug ccmpounds are soluble in aqueous solutions and stable therein in vitro but are rapidly converted in vivo to the active parent drug (St-OH) which are anti-inflammatory agents.

475936

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