10-aryl-11-hbenzo [b]fluorene derivatives and analogs for...

C - Chemistry – Metallurgy – 07 – C

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C07C 321/28 (2006.01) A61K 31/05 (2006.01) A61K 31/085 (2006.01) A61K 31/136 (2006.01) A61K 31/40 (2006.01) A61K 31/4453 (2006.01) A61P 5/30 (2006.01) C07C 39/17 (2006.01) C07C 39/21 (2006.01) C07C 39/24 (2006.01) C07C 39/42 (2006.01) C07C 43/215 (2006.01) C07C 43/225 (2006.01) C07C 43/23 (2006.01) C07C 217/16 (2006.01) C07C 217/20 (2006.01) C07C 323/18 (2006.01) C07D 211/70 (2006.01) C07D 239/42 (2006.01) C07D 277/66 (2006.01) C07D 295/08 (2006.01) C07D 295/092 (2006.01) C07D 317/54 (2006.01)

Patent

CA 2420289

The invention provides for a non-steroidal compound having the formula [I], wherein Re and 'Re are OH, optionally independently etherified or esterified; Z is -CH2- or -CH2CH2-; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, -CF3, -OCF3, (1C-8C)Alkyl, hydroxy, (1C- 8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, -O(CH2)mX, wherein X is halogen or phenyl and m = 2-4; -O(CH2)mNRaRb, -S(CH2)mNRaRb or - (CH2)mNRaRb, wherein m = 2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C- 8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, - CF3, -OCF3, -CN, -NO2, -OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C- 8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C- 8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, -CF3, -OCF3, -CN, -NO2, hydroxy, hydroxy(1C- 4C)alkyl, (1C-8C)alkoxy, aryloxy, (1C-8C)alkylthio, carboxyl, carboxylate, (1C- 8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl. The compounds can be used for the preparation of a medicine, in particular for use in estrogen-receptor- related treatments.

L'invention concerne un composé non stéroïdique ayant la formule [I], où R?e¿ et 'R?e¿ représentent OH, éventuellement indépendamment éthérifiés ou estérifiés; Z représente -CH¿2?- ou -CH¿2?CH¿2?-; R?1¿ représente H, halogène, CF¿3?, ou (1C-4C)alkyle; R?2¿, R?3¿ et R?4¿ représentent indépendamment H, halogène, -CF¿3?, -OCF¿3?, (1C-8C)alkyle, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyle, halo(1C-8C)alkyle, -O(CH¿2?)¿m?X, X représentant un halogène ou phényle et m valant 2-4; -O(CH¿2?)¿m?NR¿a?R¿b?, -S(CH¿2?)¿m?NR¿a?R¿b? ou -(CH¿2?)¿m?NR¿a?R¿b?, m valant 2-4 et R¿a?, R¿b? représentant indépendamment (1C-8C)alkyle, (2C-8C)alcényle, (2C-8C)alkynyle, ou aryle, éventuellement substitué par un halogène, -CF¿3?, -OCF¿3?, -CN, -NO¿2?, -OH, (1C-8C)alcoxy, aryloxy, carboxyle, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyle, aryle, aryl(1C-8C)alkyle, halo(1C-8C)alkyle ou R¿a? et R¿b? forment une structure cycle à 3-8 chaînons, éventuellement substitués par un halogène, -CF¿3?, -OCF¿3?, -CN, -NO¿2?, hydroxy, hydroxy(1C-4C)alkyle, (1C-8C)alcoxy, aryloxy, (1C-8C)alkylthio, carboxyle, carboxylate, (1C-8C)alkyle, aryle, aryl(1C-8C)alkyle, halo(1C-8C)alkyle. Les composés peuvent être utilisés pour préparer un médicament destiné à être utilisé notamment dans des traitements liés au récepteur des oestrogènes.

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