4-(CONDENSED CYCLICMETHYL)-IMIDAZOLE-2-THIONES ACTING AS ALPHA2 ADRENERGIC AGONISTS

• Main Authors: KEN CHOW, DANIEL W. GIL, LARRY A. WHEELER, PHONG X. NGUYEN, MICHAEL E. GARST, JOHN E. DONELLO, TODD M. HEIDELBAUGH
• Format: Patent
• Language: English; Spanish
• Published: 07.06.2007
• 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

Compounds of Formula 1 (I) where the variables have the meaning defined in the specificationare agonists of alpha2 adrenergic receptors. Several compounds ofthe disclosure are specific or selective to alpha2B and/or alpha2Cadrenergic receptors in preference over alpha2A adrenergic receptors.Additionally some of the claimed compounds have no or only minimal cardivascularand/or sedatory activity. The compounds of Formula 1 are useful as medicamentsin mammals, including humans, for treatment of diseases and or alleviationsof conditions which are responsive to treatment by agonists of alpha2adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascularand/or sedatory activity are useful for treating pain and other conditions withminimal side effects. Se describen compuestos de la formula (I) en donde las variables tienen el significado definido en la descripcion, los cuales son agonistas de receptores adrenergicos alfa2. varios compuestos de la descripcion son especificos o selectivos para receptores adrenergicos alfa2B y/o alfa2c en preferencia sobre los receptores adrenergicos alfa2A. Ademas, algunos de los compuestos reclamados no tienen o solo tienen una actividad cardiovascular y/o sedante minima. Los compuestos de la formula I son utiles como medicamentos en mamiferos, incluyendo humanos, para el tratamiento de enfermedades y/o alivio de condiciones que respondan a tratamiento por agonistas de receptores adrenergicos alfa2. los compuestos de la formula que no tienen una actividad cardiovascular y/o sedante son utiles para tratar dolor y otras condiciones con minimos efectos secundarios.