Importance

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Abstract

This invention discloses pyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof, of the following formula: ##STR1## wherein L and M are selected from the group consisting of carbon and CH, the chemical bond between L and M is selected from the group consisting of a single bond and a double bond, wherein Z.sub.4 and Z.sub.5 are different and are selected from the group consisting of R.sub.14 and ##STR2## where Z.sub.4 is R.sub.14 when Z.sub.5 is ##STR3## and Z.sub.4 is ##STR4## when Z.sub.5 is R.sub.14 ; wherein A.sub.1 is CH; wherein B.sub.1 is CH; wherein R.sub.17 is selected from the group consisting of aryl, diaryl, triaryl, mono-, di- or tri-substituted aryl, mono-, di- or tri-substituted diaryl, mono-, di- or tri- substituted triaryl, a substituted or unsubstituted heteroaryl and p-aroyl-L-glutamate; wherein R.sub.18 is a lower akyl group; and said compound capable of inhibiting dihydrofolate reductase and thymidylate synthase. These compounds are useful in the treatment of certain illnesses, including cancer and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients.

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First Claim