New N-((4,5-diphenyl-3-alkyl-2-thienyl)methyl)methyl amine derivatives are cannabinoids receptor inhibitor useful to treat or prevent e.g. gastro-intestinal disorders, inflammatory phenomena and diseases of the immune system

摘要

N-[(4,5-Diphenyl-3-alkyl-2-thienyl)methyl]methyl amine derivatives (I) and their hydrates and solvates are new. N-[(4,5-Diphenyl-3-alkyl-2-thienyl)methyl]methyl amine derivatives of formula (I) and their hydrates and solvates are new. X : C(O), SO 2, C(O)N(R 6) or CO; R 11-7C alkyl, 3-7C cycloalkyl(methyl) (optionally substituted by 1-3C alkyl), phenyl (optionally mono, di- or - trisubstituted by halo, 1-4C alkyl, 1-4C alkoxy, CN, CF 3, OCF 3, S(O) n-Alk, 1-4C alkylcarbonyl or phenyl), benzyl (optionally substituted by halo, 1-4C alkyl, 1-4C alkoxy or CF 3) or indolyl; R 2H or 1-3C alkyl; R 31-5C alkyl or 3-7C cycloalkyl; R 4, R 5phenyl (optionally mono, di- or - trisubstituted by halo, 1-4C alkyl, 1-4C alkoxy, CN, CF 3 or S(O) n-Alk); R 6H or 1-3C alkyl; n : 0-2; and Alk : 1-4C alkyl. An INDPENDENT CLAIM is also included for the preparation of (I). [Image] ACTIVITY : Gastrointestinal-Gen.; Antiinflammatory; Immunomodulator; Neuroleptic; Antialcoholic; Antismoking; Anorectic; Eating-Disorders-Gen.; Antidiabetic; Antilipemic; Analgesic; Antianginal; Antidiarrheic; Antiulcer; Antiemetic; Uropathic; Endocrine-Gen.; Cardiovascular-Gen.; Hypertensive; Hemostatic; Immunosuppressive; Antibacterial; Hepatotropic; Antiasthmatic; Vasotropic; Ophthalmological; Antiinfertility; Antiarthritic; Antirheumatic; Neuroprotective; Virucide; Cerebroprotective; CNS-Gen.; Osteopathic; Nootropic; Tranquilizer. MECHANISM OF ACTION : Cannabinoids receptor inhibitor. The antagonistic activity of (I) against cannabinoids receptor was tested. The results showed that (I) exhibited a median inhibitory concentration =5x10 -7.