摘要 |
<p>6-Substituted-1,2-benzisothiazolin-3-ones of the formula (I) (I) and the pharmaceutically acceptable acid addition salts thereof wherein R1 when taken independently of R2 is chloro, bromo, fluoro, nitro, alkyl of 1 to 4 carbon atoms alkoxy of 1 to 4 carbon atoms or an aromatic substituent selected from the group consisting of phenoxy, benzyloxy and phenylthio which aromatic substituent is unsubstituted or substituted with halo or alkyl of 1 to 4 carbon atoms; R2 when taken independently of RI is hydrogen alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms R1 and R2 taken together are trimethylene tetramethylene or pentamethylene R3 is hydrogen, halo, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms each of R4 and R5 is alkyl of 1 to 4 carbon atoms; and A is alkylene of 2 to 5 carbon atoms, alkylenoxyalkyl of 4 to 8 carbon atoms or alkylenethioalkyl of 4 to 8 carbon atoms are antichrombotic agents. The compounds, of which 2-(2-di-ethylamino-ethyl)-4,5-dimethyl-1,2-benzisothiazolin-3-one is a representative embodiment can be prepared by cyclization of an appropriately substituted bis-¢2-(amino-alkylcarbamyl)phenyl!disulfide, or by other disclosed methods.</p> |