DARGAZANLI, GIHAD,ESTENNE-BOUHTOU, GENEVIEVE,MAGAT, PASCALE,MARABOUT, BENOIT,ROGER, PIERRE
申请号：
HK10109250.4
公开号：
HK1142887B
申请日:
2007.05.03
申请国别(地区):
HK
年份:
2014
代理人:
摘要：
N-heterocyclylmethyl benzamide derivatives (I) and their acid addition salts, solvates and hydrates are new. - N-heterocyclylmethyl benzamide derivatives of formula (I) and their acid addition salts, solvates and hydrates are new. - R = H or vinyl - n = 0 or 1 - X = CH or N - R1 = phenyl or naphthyl optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy or CF3 or thienyl, pyridyl, oxazolyl, furyl, thiazolyl, quinolinyl or isoquinolinyl - R2 = H, halo, CF3, A, OA, thienyl, OAr, SH, SA, SO2NR4R5, SO2A, SO2Ar, CN, CONR4R5, COOR7, COA, COAr, NHCOR8, NHSO2A, NHSO2Ar or NHSO2NR4R5 - A = 1-6C alkyl optionally substituted by R3 - Ar = phenyl optionally substituted by R6 - R3 = halo, phenyl, 1-6C alkoxy or NR4R5 - R4, R5 = H or 1-6C alkyl or - NR4R5 = pyrrolidino, piperidino or morpholino - R6 = H, OH, SH, 1-6C alkyl or 1-6C alkoxy - R7 = H, A or Ar - R8 = A, 1-6C alkoxy or Ar and - provided that when R is vinyl, then n is 1 and X is CH. - ACTIVITY - Nootropic Neuroleptic Tranquilizer Antidepressant Antialcoholic Antimigraine Relaxant Analgesic Antiparkinsonian Anticonvulsant Neuroprotective. - MECHANISM OF ACTION - Glycine transporter inhibitor. - The most active compounds (unspecified) have IC50 values of 0.01-10 micro M against glycine uptake by SK-N-MC cells expressing native human glycine transporter glyt1.
