10-ARYL-11H-BENZO[B]FLUORENE DERIVATIVES AND ANALOGS FOR MEDICINAL USE

• Main Authors: MESTRES JORDI, LOOZEN HUBERT JANJOZEF, VEENEMAN GERRIT HERMAN, DE ZWART EDUARD WILLEM
• Format: Patent
• Language: English
• Published: 25.03.2004
• Edition: 7
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention provides for a non-steroidal compound having the formula wherein R and 'R are OH, optionally independently etherified or esterified; Z is -CH2- or -CH2CH2-; R is H, halogen, CF3, or (1C-4C)alkyl; R , R and R 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.