Method for minimizing the uterotrophic effect of tamoxifen...

A - Human Necessities – 61 – K

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A61K 31/55 (2006.01) A61K 31/38 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 31/445 (2006.01) A61K 31/4535 (2006.01)

Patent

CA 2148302

The present invention provides a method of minimizing the uterotrophic effect of non-steroidal antiestrogen compounds of formula II Image II wherein either R4 is H or a lower alkyl radical and R5 is a lower alkyl radical, or R4 and R5 are joined together with the adjacent nitrogen atom to form a heterocyclic radical; R6 is H or a lower alkyl radical; R7 is H, halo, OH, a lower alkyl radical, or is a buta-1,3-dienyl radical which together with the adjacent benzene ring forms a naphthyl radical; R8 is H or OH; and n is 2; or a pharmaceutically acceptable salt thereof, wherein said formula II compound is administered to a woman for the treatment or prevention of breast carcinoma, comprising concurrently or sequentially administering to said woman a compound of formula I Image I wherein R1 and R3 are independently hydrogen, -CH3, -CO-(C1-C6 alkyl), or -CO-Ar, in which Ar is optionally substituted phenyl; and R2 is selected from the group consisting of pyrrolidino, hexamethyleneimino, and piperidino; or pharmaceutically acceptable salt or solvate thereof. The present invention further provides pharmaceutical compositions comprising a compound of formula I and a compound of formula II together with a pharmaceutically acceptable carrier, excipient, or diluent.

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