Novel-prodrugs for phosphorus-containing compounds
作者： K. Raja Reddy , Mark D. Erion , Edward D. Robinson
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摘要: Prodrugs of formula (I), their uses, intermediates, and method manufacture are described, wherein V is selected from the group consisting -H, aralkyl, alicyclic, aryl, substituted heteroaryl, 1-alkenyl, 1-alkynyl, -R9; or together Z connected via 3-5 atoms to form a cyclic group, optionally containing 1 heteroatom, with hydroxy, acyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy attached carbon atom that three an oxygen phosphorus; fused aryl at beta gamma position W 3 6 one substituent alkylthiocarbonyloxy, aryloxycarbonyloxy, W' independently alkyl, -CHR2OH, -CHR?2OC(O)R3, -CHR2OC(S)R3, -CHR2OC(S)OR3, -CHR2OC(O)SR3, -CHR2OCO?2R?3, -OR2, -SR2, -CHR2N?3, -CH2aryl, -CH(aryl)OH, -CH(CH=CR22)OH, -CH(C CR?2)OH, -R2, -NR2?2, -OCOR3, -OCO?2?R?3, -SCOR3?, -SCO?2R?3, -NHCOR2, -NHCO?2?R?3, -CH?2NHaryl, -(CH2)p-OR2, -(CH?2?)p-SR?2; R2? R3 -H; alicyclic; R9 p integer 2 3; provisos a) V, Z, W, not all b) when z then least M PO?3?2-, P2O63-, P?3O9?4- biologically active in vivo, phosphorus (I) carbon, oxygen, nitrogen atom; pharmaceutically acceptable prodrugs salts thereof.
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