TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES

• Main Authors: TEERHUIS, NEELTJE, MIRANDA, VEENEMAN, GERRIT, HERMAN, STOCK, HERMAN, THIJS
• Format: Patent
• Language: English
• Published: 25.01.2013
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; 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 disclosure relates to tetrahydronaphthalen-2-ol derivatives according to Formula 1 wherein R1 is (C1-C4 )alkyl, (C2-C4 )alkenyl or (C2-C4 )alkynyl, independently optionally substituted with one or more halogen, R1 having a cis-orientation in relation to both the exocyclic phenyl group at the 6-position and the benzyl group at the 8-position of the skeleton; R2-R13 are independently H, halogen, CN, OH, (C1-C4 )alkyl, optionally substituted with one or more halogen, or (C1-C2)alkyloxy; or a prodrug or an isotopically-labelled derivative thereof. Additionally the disclosure relates to the use of compounds of formula one and medicaments manufactured from them in the treatment of medical conditions of the prostate in particular and also for treating lower urinary tract symptoms, hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer. Examples of the compounds are: 4-( 4-fluorobenzyl)-6-methoxy-2-( 4-methoxyphenyl )-3-methyl-1,2-dihydronaphthalene, 4-(2,5-difIuorobenzyl )-6-methoxy-2-( 4-methoxyphenyl )-3-methyl-1,2-dihydronaphthalene, 4-(2,6-difIuorobenzyl )-6-methoxy-2-( 4-methoxyphenyl )-3-methyl-1,2-dihydronaphthalene.