Antioestrogenic phenol derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 211/34 (2006.01) C07D 231/12 (2006.01) C07D 271/10 (2006.01) C07D 295/088 (2006.01) C07D 295/14 (2006.01) C07D 295/15 (2006.01)

Patent

CA 1280416

A B S T R A C T A phenol derivative of the formula NU-A-X-R1 wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxy- indanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or cycloalkylene which is interrupted by a heterocyclene linkage, wherein R1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R1 is joined to R2, and wherein X is -CONR2-, -CSNR2-, -NR12CO-, -NR12CS-, -NR12CONR2-, Image , -SO2NR2- or -CO-, or, when R1 is not hydrogen, is -NR12COO-, -S-, -SO- or -SO2-, wherein R2 is hydrogen or alkyl, or R1 and R2 together form alkylene; wherein R12 is hydrogen or alkyl, and wherein R22 is hydrogen, cyano or nitro; or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumours or of anovulatory infertility.

480152

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