2-imino-3-alkylbenzothiazoline derivatives bearing a heterocyclic
申请人:Rhone Poulenc Rorer, S.A.
公开号:US05260297A1
公开(公告)日:1993-11-09
Compounds of formula: ##STR1## in which R.sub.1 represents a substituted 1-piperazinyl, substituted 1,2,3,6-tetrahydro-1-pyridyl or substituted piperidino radical, R.sub.2 represents a polyfluoroalkoxy or a polyfluoroalkyl radical and n is equal to 2 or 3, the salts of these compounds with an acid, processes for preparing them and medicinal products containing them.
Benzothiazole derivatives and medicinal products containing them
申请人:Rhone-Poulenc Rorer S.A.
公开号:US05340824A1
公开(公告)日:1994-08-23
##STR1## Compounds of formula (I), in which R.sub.1 is a polyfluoralkoxy, R.sub.2 is a sulphur or nitrogen atom substituted by an alkyl radical or a sulfonyl or sulfinyl radical, R.sub.3 is a phenyl, benzoyl, --NR.sub.4 R.sub.5 or piperidinyl-4radical substituted in position 1 by a phenylalkyl radical, R.sub.4 is an alkyl radical, R.sub.5 is a phenylalkyl radical, n is equal to 1, 2 or 3, m is equal to 0, 1, 2 or 3. The present invention also relates to the salts of said compounds, processes for the preparation of the latter and drugs containing them.
2-iminobenzothiazoline derivatives, their preparation and pharmaceutical
申请人:Rhone-Poulenc Sante
公开号:US05008280A1
公开(公告)日:1991-04-16
Compounds of the formula: ##STR1## in which - R.sub.1 denotes a polyfluoroalkoxy or polyfluoroalkyl radical, and - R.sub.2 denotes either a chain --CH.sub.2 --(CH(R.sub.4)).sub.n --R.sub.3, in which R.sub.3 denotes a dialkylamino, piperidino, 1-pyrrolidinyl, mercapto, acylthio, alkylthio, alkylsulphinyl or alkylsulphonyl radical, R.sub.4 denotes a hydrogen atom or an alkyl radical and n is equal to 0 or 1, or a residue of formula: ##STR2## the said alkyl and alkoxy radicals and portions containing 1 to 4 carbon atoms each in a straight or branched chain and said the acyl portions containing 2 to 4 carbon atoms each, and the salts of these compounds, are useful in the treatment of diseases in which glutamate is implicated.
3,4-Dihydro-8-trifluoromethoxy-1,2,4-thiadiazino [3,4-b]benzothiazole (2) was prepared in five steps from 6-trifluoromethoxy-2-benzothiazolamine (riluzole, 1). The key final step consisted of an original N-S bond forming reaction between unsubstituted imine and thiol groups, using chloramine-T as reagent (75% yield).