New oxaphenanthrene derivatives useful as cannabinoid receptor inhibitors, e.g. for treating psychoses, anxiety, depression, aprosexia, memory and cognitive disorders, appetite loss, obesity

摘要

Oxaphenanthrene derivatives (I) are new. Oxaphenanthrene derivatives of formula (I) and their salts, solvates and isomers are new. A : a 6-membered saturated, unsaturated or aromatic carbocylic or heterocyclic ring, where the saturated ring can have CH 2 groups replaced by CO; R 1>-R 4>H, halo, or 1-12C alkyl in which H atoms can be replaced by F, CH 2 groups can be replaced by C=C, ethynylene, CO, O, S, NH, NR 1> or optionally substituted phenylene, and CH 3 groups can be replaced by 4-R 5>-piperidino, thiomorpholino, morpholino or 4-R 5>-1-piperazinyl; R 5>H or alkyl. Independent claims are also included for two processes for preparing (I). [Image] ACTIVITY : Neuroleptic; Tranquilizer; Antidepressant; Nootropic; Anorectic; Antiaddictive; Neuroprotective; Analgesic; Antiinflammatory; Antibacterial; Ophthalmological; Cytostatic; Antidiabetic; Antiemetic; Antiasthmatic; Antiulcer; Antidiarrheic; Cardiant; Vasotropic. MECHANISM OF ACTION : Cannabinoid receptor inhibitor. 6,6-Difluoro-3-pentyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-1-ol had an IC50 of 1.4 mu M in a competitive binding assay on human CB2 cannabinoid receptor.