New 1,5-diphenyl-3-sulfonamidomethyl-1H-pyrazole derivatives are cannabinoid receptor antagonists used for treating e.g. eating disorders, gastrointestinal disorders, inflammation and immunological disorders

摘要

1,5-Diphenyl-3-sulfonamidomethyl-1H-pyrazole derivatives (I), are new. 1,5-Diphenyl-3-sulfonamidomethyl-1H-pyrazole derivatives of formula (I) and their acid addition salts, hydrates and solvates are new. R 11-6C alkyl, 3-7C cycloalkyl (optionally substituted by at least 1 1-3C alkyl), 3-7C cycloalkylmethyl (optionally ring-substituted by at least 1 1-3C alkyl), phenyl (optionally substituted by 1-3 halo, 1-4C alkyl, 1-3C alkoxy, CN, CF 3, OCF 3, SO 2Me, 1-3C alkylcarbonyl or phenyl), benzyl (optionally substituted by 1 or 2 halo, 1-3C alkyl or 1-3C alkoxy) or CF 3; R 2, R 3H or 1-3C alkyl, and R 4-R 9H, halo, 1-7C alkyl, 1-5C alkoxy or CF 3. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antiinflammatory; Neuroleptic; Antialcoholic; Antismoking; Tranquilizer; Antidepressant; Antimigraine; Anticonvulsant; Antiparkinsonian; Neuroprotective; Nootropic; Vasotropic; Analgesic; Anorectic; Antidiabetic; Antidiarrheic; Antiulcer; Antiemetic; Urotropic; Antibacterial; Immunosuppressive; Hepatotropic; Antiasthmatic; Ophthalmological; Antirheumatic; Antiarthritic; Virucide; Cerebroprotective; Cytostatic. MECHANISM OF ACTION : CB 1 cannabinoid receptor antagonist. In a CB 1 receptor affinity assay described in FEBS Letters, 350, 240 (1994), results showed that (I) exhibited IC 50 values of 0.5 mu M or less.