C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/309.1
C07D 275/04 (2006.01) C07D 417/06 (2006.01)
Patent
CA 1086747
ABSTRACT OF THE DISCLOSURE 6-Substituted-1,2-benzisothiazolin-3-ones of the formula (I) Image (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.
270309
Boshagen Horst
Horlein Ulrich
Meng Karl-August
Seuter Friedel
Aktiengesellschaft Bayer
Fetherstonhaugh & Co.
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