Amide derivatives

Details Amide derivatives Amide derivatives

C - Chemistry, Metallurgy

07

C

260/550, 260/476

C07C 205/56 (2006.01) C07C 59/56 (2006.01) C07D 263/44 (2006.01) C07D 303/48 (2006.01)

Patent

CA 1161850

ABSTRACT Novel 3,4-disubstituted-N-acylanilines of the formula: Image wherein R1, R2 and ring A are defined in claim 1; wherein R3 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R5 as stated below; wherein R4 is alkyl of 2 to 4 carbon atoms, or has the formula -CX1X2X3 wherein X1, X2 and X3, which may be the same or different, each is hydrogen, fluorine or chlorine; wherein R5 is hydrogen, hydroxy or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R3 to form an oxycarbonyl group such that together with the -N-CO-?- part of the molecule it forms an oxazolidinedione group; and wherein R6 is hydrogen or halogen. These compounds possess antiandrogenic activity and are useful for the treatment of androgen dependent or prostatic diseases. Representative of the compounds is 3,4-dichloro-N-(2- hydroxy-2-p-nitrophenylpropionyl)aniline. Also disclosed are processes for the manufacture of the compounds and pharmaceutical and veterinary compositions containing them.

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