NOVEL BENZYLPIPERAZINE DERIVATIVE AND DRUG COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT

    公开(公告)号:JPS6219577A

    公开(公告)日:1987-01-28

    申请号:JP15730085

    申请日:1985-07-16

    申请人: KANEBO LTD

    摘要: NEW MATERIAL:1-(4-Chlorobenzyl)-4-(2,4-dichlorocinnamyl)piperazine shown by the formula I and its acid addition salt. USE:A drug and a remedy for hyperlipemia having strong and sure cholesterol lowering action, no side effects and high safety, being applied to human preferably by oral administration. PREPARATION:For example, N-(4-chlorobenzyl)piperazine shown by the formula II or its salt is reacted with a 2,4-dichlorocinnamyl halide shown by the formula III (X is halogen) in a solvent such as benzene, etc., in the presence of a base such as triethylamine, etc., under heating at 50 deg.C- the boiling temperature of the solvent for 1-10hr to give the compound shown by the formula I. This compound is dissolved in a solvent such as ethanol, etc., and treated with an acid such as conc. hydrochloric acid, etc., to give an acid addition salt of the compound shown by the formula I.

    NOVEL PERFLUOROCARBOXYLIC ACID FLUORIDE AND PRODUCTION THEREOF

    公开(公告)号:JPS61260047A

    公开(公告)日:1986-11-18

    申请号:JP10304285

    申请日:1985-05-15

    摘要: NEW MATERIAL:The perfluoro(2-dialkylaminopropionyl fluoride) of formula I (R1 and R2 are 1-5C perfluoroalkyl or bonded together directly or via O or N to form a heterocyclic 5- or 6-membered ring together with N atom bonded to both groups). EXAMPLE:Perfluoro[2-(N,N-dimethylamino)propionyl fluoride]. USE:A synthetic intermediate for fluorine-containing product such as surfactant, agricultural chemical, pharmaceutical, etc., or a monomer of a fluorine- containing polymer. PREPARATION:The compound of formula I can be produced by the electrolysis of 2-dialkylaminopropionic acid derivative of formula II (R1' and R2' are 1-5C alkyl or bonded together directly or via O or N to form a 5- or 6-membered heterocyclic group; X is Cl, alkoxy or dialkylamino) in liquid hydrogen fluoride.

    STABILIZED LIQUID COMPOSITION OF MECLIZINE HYDROCHLORIDE

    公开(公告)号:JPS60204712A

    公开(公告)日:1985-10-16

    申请号:JP6151684

    申请日:1984-03-29

    摘要: PURPOSE:The titled composition suitably used as an antidinic that is obtained by adding a specific solubilizer such as nonionic ether-type surfactant or saccharide to meclizine hydrochloride, thus being storable for a long period of time, because solubility does not decrease, even when it is stored at low temperature as well as at elevated temperature. CONSTITUTION:Meclizine hydrochloride which is antihistamic agent inhibiting excitement in labyrinthus and vomitting center and developing curative effect on vomitting and dizziness with duration is combined with, as a solubilizer, 15- 35W/V% of saccharide such as sucrose or glucose, 0.01-0.1W/V% of nonionic ether type surfactant, preferably of 10-17 HLB, 0.01-0.5W/V% of cyclodextrin, 0.1-10W/V% of dextrin, preferably malto dextrin obtained by enzymatic treatment, 0.5-10W/V% of glycerol or propylene glycol or 0.005-2wt% of polyvinyl pyrrolidone.