Substituted imidazole derivatives and their preparation and use

• Main Authors: JARMO SAKARI SALONEN, ARJA LEENA KARJALAINEN, HANNU TAPANI SIPILA, ARTO JOHANNES KARJALAINEN, RAIMO EINARI VIRTANEN, MAIRE MARJATTA ELORANTA, ANTTI SAKARI HAAPALINNA
• Format: Patent
• Language: English
• Published: 23.11.1995
• Edition: 5
• Subjects: 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

PCT No. PCT/FI92/00349 Sec. 371 Date Sep. 19, 1994 Sec. 102(e) Date Sep. 19, 1994 PCT Filed Dec. 18, 1992 PCT Pub. No. WO93/13074 PCT Pub. Date Jul. 8, 1993.The invention provides compounds of the formula I wherein Y is -CH2- or -CO-; R1 is F, Cl or OH; R2 is H, F or Cl; and R3 is H, CH3 or CH2CH3, excluding 4-(5-chloro-2,3-dihydro-1H-inden-2-yl)-1H-imidazole and 4-(4-chloro-2,3-dihydro-1H-inden-2-yl)-1H-imidazole; and their non-toxic acid addition salts and mixtures thereof. Processes for the preparation of these compounds are described, as are pharmaceutical compositions comprising at least one of the compounds or its salt. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are highly selective and long acting antagonists at alpha 2-adrenoceptors. Their peroral bioavailability is good. The compounds are especially useful in the treatment of cognitive disorders.