Antiproliferative substituted naphthalene compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 209/00 (2006.01) A61K 31/40 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 209/90 (2006.01) C07D 209/92 (2006.01) C07D 239/70 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07F 9/547 (2006.01)

Patent

CA 2091688

2091688 9205153 PCTABS00011 The present invention relates to certain naphthalene compounds which inhibit the enzyme thymidylate synthase ("TS"), pharmaceutical compositions containing these cyclic compounds, and the use of these compounds to inhibit TS, including all effects derived from the inhibition of TS. Effects derived from the inhibiton of TS include the inhibition of the growth and proliferation of the cells of higher organisms and of microorganisms, such as yeast and fungi. Such effects include antitumor activity. Processes for the preparation of the naphthalene compounds of the invention are also disclosed. (I) wherein: Z and W are independently nitrogen, sulfur, or substituted or unsubstituted alkylene groups with the proviso that, when either of Z or W is nitrogen or sulfur, the other is a substituted or unsubstituted alkylene group; Ar is a group comprising one or more rings selected from the group consisting of (1) substituted or unsubstituted aryl rings and (2) substituted or unsubstituted heterocyclic rings; X and Y together form a nitrogen-containing, five- or six-membered heterocyclic ring which itself may be substituted or unsubstituted.

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