Medicaments for treating mycobacterial diseases, especially tuberculosis or leprosy, contain new or known canthin-6-one compounds

摘要

The use of canthin-6-one compounds (I) for the treatment of disorders associated with or caused by mycobacteria is new. (I) include the new compound benzo(e)canthin-6-one N-oxide (I'). The use of canthin-6-one compounds of formula (I) is claimed for the production of medicaments for the treatment of disorders associated with or caused by mycobacteria. B' : N, N +>-O ->, N +>-R or N +>-R.X ->; R : Q (optionally substituted (os), e.g. by one or more halo); X ->mineral or organic anion; R 1- R 8H, Q (os by halo), halo, OH, NO 2, CN, SH, COOH, CONH 2, NH 2, OQ, COOQ, NHCOQ, N(COQ) 2, NHQ, NQ 2, SQ, Het, SO 2NQ 2or NQSO 2Q; or adjacent groups R 1>- R 8>(or B plus R 2>or R 3>) : group completing a ring, specifically a 5-30C ring optionally containing O, N and/or S heteroatom(s) (e.g. benzene, naphthalene, pyridine, pyrrole, thiophene, furan or pyrazine), os by Q (os by halo), halo, OH, NO 2, CN, SH, COOH, CONH 2, NH 2, OQ, COOQ, NHCOQ, N(COQ) 2, NHQ, NQ 2, SQ, Het, SO 2NQ 2or NQSO 2Q; Q : 1-12C (preferably 1-6C) saturated or unsaturated, linear, branched or cyclic alkyl; Het : heterocyclyl (containing 2-6C and 1-4 of S, N or O). An independent claim is included for benzo(e)canthin-6-one N-oxide (I') as a new compound. [Image] ACTIVITY : Antibacterial; Antitubercular; Tuberculostatic; Antileprotic; Antiinflammatory; Neuroprotective; Antiulcer; Osteopathic. Canthin-6-one (Ia) and its derivatives showed activity (comparable with isoniazid in many (unspecified) cases) against Mycobacterium bovisBCG in mice when administered at a dose of 20 mg/kg i.p. per day for 5 days, starting 5 days after inoculation with BCG; no quantitative results are given. (Ia) had minimum inhibitory concentration 7.5 mu g/ml in vitro against Mycobacterium bovisBCG. MECHANISM OF ACTION : None given.