Non-steroidal, tetracylic compounds for estrogen-related treatments

• Main Authors: MESTRES JORDI, LOOZEN HUBERT JAN JOZEF, VEENEMAN GERRIT HERMAN, DE ZWART EDUARD WILLEM
• Format: Patent
• Language: English
• Published: 03.02.2004
• 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 non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of R or R is 'R; R and 'R are OH, optionally independently etherified or esterified; X is N or -C(R )-, wherein R is H1 halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or -C(R )-, with the proviso that X and Y are not both N, wherein R has the same meaning as defined for R ; Z is C(R ,'R )- or -C(R ,∝R )-C(R ,'R )-, wherein R , 'R , R , 'R , R , and 'R , independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens. These compounds are useful for estrogen-receptor related treatments in view of a desirable profile of activity for estrogen alpha and estrogen beta receptors.