New pyrazolopyridazinone derivatives are cannabinoid receptor antagonists useful to prevent/treat psychiatric disorders, cognitive disorders, neurodegenerative diseases, metabolic disorders, dyslipidemia, pain, ulcer and tobacco weaning

摘要

Pyrazolopyridazinone compounds (I), and their addition salts, hydrates and solvates are new. Pyrazolopyridazinone compounds of formula (I), and their addition salts, hydrates and solvates are new. R 11-12C alkyl (optionally substituted by F), non-aromatic 3-12C carbocyclic (optionally substituted by 1-4C alkyl, 1-4C alkoxy, F, OH, CF 3, OCF 3 or 1-4C alkylthio), phenyl (optionally substituted by halo, OH, Alk, -OAlk, methylenedioxy, -CH 2-NHAlk, -CH 2N(Alk) 2, CN, NO 2, S(O) nAlk, OS(O) nAlk, 1-4C alkylcarbonyl, 1-4C alkoxycarbonyl or phenyl, phenoxy, pyrrolyl, imidazolyl, pyridyl, pyrazolyl, oxazolyl, thiazolyl, triazolyl or thiadiazolyl, optionally substituted by 1-4C alkyl), benzyl (optionally substituted on phenyl by halo, Alk, OH, OAlk, methylenedioxy, S(O) nAlk or -OS(O) nAlk), phenethyl (optionally substituted on phenyl by halo, 1-4C alkyl, 1-4C alkoxy, CF 3 or OCF 3), benzhydryl, benzhydrylmethyl, heterocyclic aromatic comprising pyrrolyl, imidazolyl, furyl, thienyl, pyrazolyl, oxazolyl, pyridyl, indolyl, benzothienyl or thieno[3,2-b]thienyl, optionally substituted by halo, Alk, OAlk, CN, NO 2 or -S(O) nAlk; R 2phenyl (optionally substituted by halo, OH, Alk, OAlk, -S(O) nAlk or -OS(O) nAlk); R 3phenyl (optionally substituted by halo, OH, Alk, OAlk, -S(O) nAlk or OS(O) nAlk); R 4H, 1-4C alkyl, 1-4C alkoxy or OH; n : 0-2; and Alk : 1-4C alkyl (optionally substituted by F). Independent claims are included for: (1) the preparation of (I); and (2) pyrazolopyridazinone compound of formula (II). ACTIVITY : Neuroleptic; Nootropic; Tranquilizer; Neuroprotective; Metabolic; Anorectic; Antidiabetic; Analgesic; Antianginal; Antilipemic; Gastrointestinal-Gen; Antiemetic; Antidiarrheic; Antiulcer; Hepatotropic; Immunomodulator; Antiarthritic; Antirheumatic; Antiinflammatory; Antiparkinsonian; Antismoking; Antidepressant; Hypnotic; Antialcoholic; Antimigraine; Anticonvulsant; Muscular-Gen.; Inotropic; Vasotropic; Cerebroprotective; Antiaddictive; Eating-Disorders-Gen; Cardiovascular-Gen; Uropathic; Virucide; Endocrine-Gen; Hypertensive; Antiarteriosclerotic; Antibacterial; Immunosuppressive; Antiasthmatic; Respiratory-Gen; Ophthalmological; Antiinfertility; Gynecological; CNS-Gen; Osteopathic. MECHANISM OF ACTION : Cannabinoid CB 1 receptor antagonist.