27-03-2014 дата публикации
Номер: US20140088091A1
The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuromuscular blocker or skeletal muscle relaxant. 2. The compound according to claim 1 , wherein Ris hydrogen claim 1 , mercapto or C-C-alkyl.3. The compound according to claim 2 , wherein Ris hydrogen or is taken together with Rto form an alicyclic claim 2 , aryl or heteroaryl ring system claim 2 , which is optionally substituted by halogen claim 2 , amino claim 2 , C-C-alkyl claim 2 , C-C-haloalkyl claim 2 , C-C-alkoxy claim 2 , C-C-haloalkoxy claim 2 , mercapto claim 2 , alkylthio claim 2 , alkylamino claim 2 , arylthio claim 2 , heteroarylthio claim 2 , arylamino or heteroarylamino.4. The compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare independently selected from aryl or heteroaryl.5. The compound according to claim 4 , wherein the compound is an addition salt of hydrochloride claim 4 , hydrobromide claim 4 , phosphate claim 4 , nitrate claim 4 , acetate claim 4 , malate claim 4 , succinate claim 4 , fumarate claim 4 , tartrate claim 4 , salicylate claim 4 , sorbate claim 4 , lactate claim 4 , p-toluene sulphate claim 4 , or naphthalene-1 claim 4 ,5-disulfonate.7. The method according to claim 6 , wherein the reaction of compound 2 and compound 3 is in the presence of a solvent.8. The method according to claim 7 , wherein the reaction of compound 4 is a cyclization reaction with diethyl amine claim 7 , pyrrolidine claim 7 , morpholine claim 7 , piperidine claim 7 , N-methylpiperazine claim 7 , in toluene claim 7 , ethylbenzane claim 7 , o-xylene claim 7 , m-xylene claim 7 , p-xylene claim 7 , or isopropylbenzene.9. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier or excipient.10. Use of the compound of as a neuromuscular blocker or skeletal muscle relaxant.11. The compound of claim 3 , wherein the ...
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