Aromatase inhibiting pyrimidine derivatives

A - Human Necessities – 61 – K

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A61K 31/505 (2006.01) C07D 239/26 (2006.01)

Patent

CA 1211050

Abstract Pyrimidine derivatives of the formula Image I or a pharmaceutically acceptable salt thereof, wherein R is Image 2-chloroethyl, C3-C8 cycloalkyl, phenoxy-substituted C1-C4 alkyl, or norbornan-2-yl, R1 is methyl, trifluoromethyl, methoxy, fluoro, chloro, bromo, or nitro; R2 is hydrogen, methyl, trifluoromethyl, methoxy, fluoro, chloro, bromo, or nitro; each of R3 and R4 is independently hydrogen, methyl, methoxy, fluoro, or chloro; and X is hydrogen, hydroxy, methyl, or halo, with the proviso that if R1 is methoxy, R must be substituted phenyl with at least one of R3 and R4 being other than hydrogen inhibit aromatase and are useful in treating or preventing estrogen-dependent diseases in mammals.

446363

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