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Summary
Novelty: Novel phenols and benzamides, and pharmaceutical compositions thereof, are disclosed. They have potential use for the prevention and treatment of Type I diabetes.
Biology: Two assays describing the activity of the compounds using non-obese diabetic (NOD) mice are described. In vitro, pancreatic islet cells from the female BALB/c mice were tested in a disease recurrence model. The survival times, compared with control, of mice administered with the test compound are reported in tabular form. In an inhibition of cyclophosphamide-induced diabetes assay, male NOD mice (Taconic Farm) were given a 250 mg/kg dose of cyclophosphamide ip. Mice given 4-[(dimethyl amino)-methyl]-2,6-bis(1,1-dimethyl-ethyl)phenol took 15.7 days to become diabetic (control, 12 days).
Chemistry: Fifty-seven compounds are disclosed; syntheses are not given. Eight examples of formulations containing the active compunds are detailed. Several methods of administration including capsules, tablets, aerosols and suppositories are detailed. A wide dose range of 0.1-50mg/kg/day (adult human) is reported. Two compounds are specifically claimed including 4-[(dimethylamino)-methyl]-2,6-bis(1,1-dimethyl-ethyl) phenol.
Structure: 