163437-01-2

Upstream product

• 64840-90-0 eperisone 
• 110-89-4 piperidine 
• 50-00-0 formaldehyd 
• 27465-51-6 1-(4-ethylphenyl)-1-propanone 
• 56839-43-1 eperisone hydrochloride 

Relevant academic research and scientific papers

Enantioselective separation and simultaneous determination of tolperisone and eperisone in rat plasma by LC-MS/MS

Tolperisone and eperisone used as muscle relaxants possess one chiral center each and exist as two optical isomers for each drug. Therefore, enantioselective assays to measure each enantiomer in biological matrices are of great importance. In the present study a simple and complete reverse-phase liquid chromatography tandem mass spectrometric method for separation and enantioselective determination of tolperisone and eperisone in rat plasma was developed. The analytes were extracted from rat plasma by a simple protein precipitation method with acetonitrile as the extraction solvent. The enantioselective separation of analytes was achieved on a Cellulose Tris (4-chloro-3-methylphenylcarbamate) chiral column with a mobile phase of acetonitrile: 10 mM ammonium acetate in an isocratic mode of elution and mass spectrometric detection. The calibration curve for each enantiomer was found to be linear over 0.2 to 20 ng/mL for each enantiomer. The proposed method exhibited good intra- and interday precision (% CV) ranged between 0.95-6.05% and 1.11-8.21%, respectively. The intra- and interday accuracy for the proposed assay method ranged between 94.0-100.5% and 92.7-102.1%, respectively. The proposed method was validated as per regulatory guidelines. Chirality 25:622-627, 2013. 2013 Wiley Periodicals, Inc.

TOLPERISONE ANALOGS AND METHODS OF USE

The present invention is, in part, directed to tolperisone analogs (e.g., compounds of formula (I), (I-a), (I-b), (II), (Il-a), (III), (Ill-a), (ΙΙΙ-b), (III-c), (IV), (IV-a), (V), or (V-a)) and methods of use thereof for the treatment of various conditions including elevated muscle tone and tension (e.g., spasticity, muscle spasm). In one aspect, the tolperisone analogs disclosed herein have an additional substituent at the α-position, which blocks the generation of a β- elimination product.

NOVEL FORMS OF EPERISONE

The invention relates to novel crystalline forms of (2RS)-1 -(4-ethylphenyl)-2-methyl-3- piperidin-1-yl-propan-1-one. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotonic conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.

Propiophenone derivatives in the treatment of pathological muscular conditions

New propiophenone derivatives prepared by the reaction of propiophenone, formaldehyde and piperidine, as well as pharmacologically acceptable acid-addition salts thereof are provided, which possess improved pharmacological activities such as anti-tremorine and anti-nicotine activities superior to those of the known analogous compound. The new compounds are useful for the therapeutic treatment of human patient suffering from pathological muscular contracture, spastic paralysis due to cerebral apoplexy, spinal and cerebral palsies and the like.