SUBSTITUTED 2,5-DFFLYDRO-3H-PYRAZOLO[4,3-C]PYRIDAZIN-3-ONE DERIVATIVES, PREPARATION THEREOF AND USE OF SAME AS CANNABINOID CB1 RECEPTOR LIGANDS

• Main Authors: VAN BROECK, DIDIER, CONGY, CHRISTIAN, RINALDI-CARMONA, MURIELLE, ROUQUETTE, ARNAUD, DOS SANTOS, VICTOR
• Format: Patent
• Language: English; French; German
• Published: 02.09.2009
• 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

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.