FIELD: chemistry.
SUBSTANCE: present invention relates to compounds which are oestrogen receptor modulators. Disclosed is a compound of formula I', in which: B is nitrogen or carbon; D is carbon; A is a condensed ring system selected from a group consisting of: , , , and ; each Re is independently selected from hydrogen, OH or where two adjacent Re together form: ; each Rh is hydrogen; Rg is hydrogen, C1-C3-alkyl, C1-C3-fluoroalkyl, fluorine, chlorine or bromine; each Ra is independently selected from: H, C1-C3-alkyl, C1-C3-fluoroalkyl, phenyl (optionally substituted with 1 to 3 groups selected from fluorine, chlorine, C1-C3-alkyl, CN, C1-C3-alkyl, OH), OC1-3 alkyl, fluorine and chlorine; X is O, CH2 or a bond when B is carbon, or CH2 or a bond when B is nitrogen; Y and Z are each CRf; U and V are each CRa; each Rf is H; and W is -CHR'-CHR'-NH-C1-C4-alkyl, -CHR'-CHR'-NH-C1-C4-fluoroalkyl, -CHR'-CHR'-NH-C3-C6-cycloalkyl, -CHR'-CHR'-NH-C1-C4-alkyl-C3-C6-cycloalkyl, alkyl or fluoroalkyl; where each R' independently represents H or C1-C3-alkyl; or a pharmaceutically acceptable salt thereof. Also disclosed is a pharmaceutical composition which contains the compounds described herein, and the use of such oestrogen receptor modulators for treating diseases or conditions, particularly cancer, which are mediated or dependent on oestrogen receptors.
EFFECT: disclosed compounds modify the effects of endogenous oestrogens acting through the ER, and/or trigger ER degradation, and are applicable as agents for treating or preventing diseases or conditions, in which the actions of oestrogens and/or oestrogen receptors are involved in the aetiology or pathology of the disease or condition or contribute to at least one symptom of the disease or condition, and where such actions of oestrogen and/or oestrogen receptors are undesirable.
30 cl, 1 tbl
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Authors
Dates
2024-09-16—Published
2019-01-22—Filed