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    NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS
    1.
    发明公开
    NOVEL PRODRUGS FOR PHOSPHORUS-CONTAINING COMPOUNDS 有权
    含磷化合物的新前药FOR

    公开(公告)号：EP1060182A2

    公开(公告)日：2000-12-20

    申请号：EP99912300.3

    申请日：1999-03-05

    申请人： Metabasis Therapeutics Inc.

    发明人： ERION, Mark, D. ,  REDDY, K., Raja ,  ROBINSON, Edward, D.

    IPC分类号： C07H19/00

    CPC分类号： C07H19/10 ,  C07F9/657154 ,  C07F9/657181 ,  C07F9/65742 ,  C07F9/65744 ,  C07H19/20 ,  C07H19/207

    摘要： 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 -R9; 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 -R9; Z is selected from the group consisting of -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, and -(CH¿2?)p-SR?2; R2¿ is an R3 or -H; R3 is selected from the group consisting of alkyl, aryl, aralkyl, and alicyclic; and R9 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 -R2, then at least one of V and W is not -H, or -R9; and M is selected from the group that attached to PO¿3?2-, P2O63-, or P¿3O9?4- 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.