| 摘要 |
Compounds of the general formulas (Ia and Ib), wherein R1 is a group of the formula (II): R3 - CO - A - wherein R3 is alkyl; mono- or polyhalogenated lower alkyl; phenyl; or substituted phenyl or R3 is an aromatic 5- or 6-membered heterocyclic ring containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; and A is a single bond or a group of the formula (IIa): - O - CR6R7 - wherein the carbon atom is attached to the nitrogen atom of the parent ring system, and wherein R6 and R7 are the same or different and each represent hydrogen or have the same meaning as R3 or R1 is a group of the formula (III): R8R9N - Y - CO - A - wherein R8 and R9 are ther same or different and each represent hydrogen or have the same meaning as R3; or R8 and R9 together with the adjacent nitrogen form a 5- or 6-membered heterocyclic ring, which in addition to the nitrogen may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; Y is a single bond or a group of the formula (IIIa): (- CR6R7 -)n wherein n is an integer from 1 to 5 and A, R6 and R7 are as defined above; or R1 is a group of the formula (IV): R'3 - O - CO - A - wherein A is as defined above and R'3 has the same meaning as R3 defined above, with the proviso that R'3 is not ethyl when A is a bond; or R1 is a group of the formula (VII): R13 - CO - (CH2)n - CO - A - wherein n and A are as defined above, and R13 is hydroxy or a group of the formula -NR8R9 are as defined above; or R1 is a group of the formula (IX): (HO)2PO2 - CR6R7 - wherein R6 and R7 are as defined above; R2 is any of the groups II, III, IV and VII as defined above with the proviso that A solely is the group (IIa) as defined above; and R5 is hydrogen or has the same meaning as R2 as defined above, and salts thereof. The compounds of the formula (Ia and Ib) are prodrugs of allopurinol and have i.a. a much higher solubility in water and/or a higher lipophilicity than allopurinol. |
