Patent ID: 6777420
Filing Date: 2004-08-17
Classification: A61P,C07D

Abstract:
A compound having the formula:P-L-T, wherein P is a segment that is a pyrimidine selected from the group consisting of a uracil substituted with an optionally substituted phenylamino or benzylamino at the 6-position and an isocytosine substituted with an optionally substituted phenylamino or benzylamino at the 6-position, wherein the phenylamino or benzylamino, if substituted, is substituted at the 3-position and/or the 4-position with a lower alkyl, a lower alkenyl, a lower alkynyl or halo; or positions 3 and 4 of the phenylamino or benzylamino are linked to form a fused 5 or 6-membered carbocyclic ring, which is saturated, unsaturated, or aromatic; and further wherein the pyrimidine selectively binds and inhibits bacterial DNA polymerase IIIC in the presence of a DNA template and is linked at the 3-position to linker segment L or directly to segment T, if L is absent; L is absent or is a linker segment comprising 1 to 10 atoms in contiguous linear connectivity that links P and T segments; and segment T is a pyridone that is linked to molecular segment P and that selectively inhibits a type II bacterial topoisomerase; and wherein the compound P-L-T inhibits DNA polymerase IIIC; and pharmaceutically acceptable salts, and hydrates thereof.