NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS
Prodrugs of formula (I), their uses, their intermediates, and their method of manufacture are described, wherein V is selected from the group consisting of -H, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; or together V and Z are conne...
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Sprache: | eng ; fre ; ger |
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Zusammenfassung: | Prodrugs of formula (I), their uses, their intermediates, and their method of manufacture are described, wherein V is selected from the group consisting of -H, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, substituted with hydroxy, acyloxy, alkoxycarbonyloxy, or aryloxycarbonyloxy attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; or together V and Z are connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, that is fused to an aryl group at the beta and gamma position to the oxygen attached to the phosphorus; or together V and W are connected via 3 carbon atoms to form an optionally substituted cyclic group containing 6 carbon atoms and substituted with one substituent selected from the group consisting of hydroxy, acyloxy, alkoxycarbonyloxy, alkylthiocarbonyloxy, and aryloxycarbonyloxy, attached to a carbon atom that is three atoms from an oxygen attached to the phosphorus; W and W' are independently selected from the group consisting of -H, alkyl, aralkyl, alicyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, and -R ; Z is selected from the group consisting of -CHR OH, -CHR OC(O)R , -CHR OC(S)R , -CHR OC(S)OR , -CHR OC(O)SR , -CHR OCO2R , -OR , -SR , -CHR N3, -CH2aryl, -CH(aryl)OH, -CH(CH=CR 2)OH, -CH(CCR )OH, -R , -NR 2, -OCOR , -OCO2R , -SCOR , -SCO2R , -NHCOR , -NHCO2R , -CH2NHaryl, -(CH2)p-OR , and -(CH2)p-SR ; R is an R or -H; R is selected from the group consisting of alkyl, aryl, aralkyl, and alicyclic; and R is selected from the group consisting of alkyl, aralkyl, and alicyclic; p is an integer from 2 to 3; with the provisos that a) V, Z, W, and W' are not all -H; and b) when z is -R , then at least one of V and W is not -H, or -R ; and M is selected from the group that attached to PO3, P2O6, or P3O9 is biologically active in vivo, and that is attached to the phosphorus in formula (I) via a carbon, oxygen, or nitrogen atom; and pharmaceutically acceptable prodrugs and salts thereof. |
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