Patent ID: 6667330
Filing Date: 2003-12-23
Classification: A61P,C07D

Abstract:
A compound of Formula I wherein:R1 is: â€”C(O)ORâ€²; â€”C(O)NRâ€²Râ€³; â€”CH2ORâ€²â€³; cyano; optionally substituted heterocyclyl; optionally substituted heterocyclyl-alkyl; optionally substituted heteroaryl, or optionally substituted heteroaralkyl; R2 is: optionally substituted alkyl; optionally substituted cycloalkyl; optionally substituted aryl; optionally substituted aralkyl; optionally substituted heterocyclyl; optionally substituted heteroaryl; optionally substituted heteroaralkyl; an optionally substituted nucleoside; an optionally substituted amino acid; or an optionally substituted di-, tri- or tetra-peptide; R3 is: optionally substituted alkyl; optionally substituted cycloalkyl; optionally substituted aryl; optionally substituted aralkyl; optionally substituted heterocyclyl; optionally substituted heteroaryl; optionally substituted heteroaralkyl; an optionally substituted nucleoside; an optionally substituted amino acid; or an optionally substituted di-, tri- or tetra-peptide; R4 is: hydrogen; alkyl; alkylcarbonyl; (poly)alkoxyalkylene; or dialkoxyphosphoryloxy; X is: lower alkylene; â€”N(Râ€²)â€”; â€”Sâ€”; â€”S(O)â€”; â€”S(O)2â€”; or X taken together with R2 is â€”P(O)(ORâ€²)2; Y is: â€”N(Râ€²)â€”; â€”Sâ€”; â€”S(O)â€”; â€”S(O)2â€”; or Y taken together with R3 is â€”P(O)(ORâ€²)2; or Xâ€”R2 taken together with Yâ€”R3 form an optionally substituted aliphatic or aromatic ring; Râ€² is: hydrogen; alkenyl; optionally substituted alkyl; optionally substituted cycloalkyl; phosphoryl; or optionally substituted aryl; Râ€³ is: hydrogen; alkenyl; optionally substituted alkyl; or optionally substituted aryl; or Râ€² and Râ€³ together with the atom to which they are attached form a 5- to 7-membered aromatic, saturated or unsaturated ring, optionally incorporating one or more additional heteroatoms chosen from N, O, or S, and optionally substituted with one or more substituents selected from the group consisting of optionally substituted lower alkyl, halo, cyano, alkylthio, lower alkoxy, carboxy, benzyl, and oxo; Râ€²â€³ is: hydrogen; alkenyl; optionally substituted alkyl; acyl, optionally substituted cycloalkyl; phosphoryl; or optionally substituted aryl; with the proviso that the compound is not 4-hydroxy-3-methanesulfonyl-2-methane-sulfonylmethyl-5-oxo-2,5-dihydro-furan-2-carboxylic acid ethyl ester and further with the proviso that when X is lower alkylene,R2 is not optionally substituted alkyl; including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof.