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    • 6. 发明专利
      NZ547163A Derivatives of N-heterocyclylmethylbenzamides, preparation method thereof and application of therapeutics as glycine transport inhibitors 未知
    • Derivatives of N-heterocyclylmethylbenzamides, preparation method thereof and application of therapeutics as glycine transport inhibitors
    • NZ547163A
    • 2010-01-29
    • NZ54716304
    • 2004-10-15
    • SANOFI AVENTIS
    • DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
    • C07D471/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D487/08
    • Disclosed is a compound corresponding to general formula (I) in which R represents a hydrogen atom or a vinyl group; n represents 0 or 1 or 2 when R represents a hydrogen atom and n represents 1 when R represents a vinyl group; X represents a group of formula CH or a nitrogen atom when R represents a hydrogen atom and X represents a group of formula CH when R represents a vinyl group; R1 represents either a phenyl or naphthyl group optionally substituted with one or more substituents chosen from halogen atoms, linear or branched (C1-C6) alkyl, hydroxyl and (C1-C6)alkoxy groups, the trifluoromethyl group, or a cyclohexyl group, or a heteroaryl group chosen from the thienyl, pyridinyl, oxazolyl, furanyl, thiazolyl, quinolinyl, and isoquinolinyl groups; R2 represents either a hydrogen atom, or one or more substituents chosen from halogen atoms and the trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, thienyl, phenyloxy, hydroxyl, mercapto, thio (C1-C6) alkyl and cyano groups or a group of general formula -NR4R5 SO2NR4R5, ûSO2 (C1-C6) alkyl, -SO2-phenyl, -CONR4R5 , -COOR7, -CO- (C1-C6) alkyl, -CO-phenyl, -NHCOR8 , -NHSO2- (C1-C6)alkyl, -NHSO2-phenyl and -NHSO2NR4R5 or a group of formula -OCF2O- attached at the 2- and 3-positions of the phenyl group; the groups (C1-C6) alkyl, (C1-C6) alkoxy, -SO2- (C1-C6) alkyl, -CO-(C1-C6)alkyl and -NHSO2-(C1-C6)alkyl being optionally substituted with one or more groups R3; the groups phenyl, -SO2-phenyl, -CO-phenyl and ûNHSO2 phenyl being optionally substituted with a group R6; R3 represents a halogen atom, or a phenyl, (C1-C6) alkoxy or -NR4R5 group; R4 and R5 represent, independently of each other, a hydrogen atom or a (C1-C6) alkyl group or R4 and R5 form with the nitrogen atom bearing them a pyrrolidine ring, a piperidine ring or a morpholine ring; R6 represents a hydrogen atom, a halogen atom, a trifluoromethyl group, a cyano group, a hydroxyl group, a mercapto group, a (C1-C6)alkyl or (C1-C6)alkoxy group; R7 represents a hydrogen atom or a (C1-C6) alkyl group optionally substituted with one or more groups R3, or a phenyl group optionally substituted with a group R6; R8 represents a (C1-C6) alkyl group optionally substituted with one or more groups R3, or a (C1-C6) alkoxy group, or a phenyl group optionally substituted with a group R6, in the form of a free base or of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed is the use of a compound of formula (I) for the preparation of a medicament intended for the treatment of contractures, of pain, of Parkinson's disease and of Parkinsonian symptoms, of epilepsy, of mixed forms and other epileptic syndromes as a supplement to another antiepileptic treatment, or in monotherapy, of sleep apnea, and for neuroprotection. Also disclosed is the use of a compound of formula (I) for the preparation of a medicament intended for the treatment of behavioural disorders associated with dementia, psychoses, various forms of anxiety, panic attacks, phobias, obsessive-compulsive disorders, various forms of depression, of disorders due to alcohol abuse or to withdrawal from alcohol, sexual behaviour disorders, food intake disorders, and migraine.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明专利
      DE602004011806T2  未知
    • DE602004011806T2
    • 2009-02-05
    • DE602004011806
    • 2004-10-15
    • SANOFI AVENTIS
    • DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
    • C07D471/08 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D487/08
    • 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. [Image] R : H or vinyl; n : 0 or 1; X : CH or N; R 1 : phenyl or naphthyl optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy or CF 3; or thienyl, pyridyl, oxazolyl, furyl, thiazolyl, quinolinyl or isoquinolinyl; R 2 : H, halo, CF 3, A, OA, thienyl, OAr, SH, SA, SO 2NR 4R 5, SO 2A, SO 2Ar, CN, CONR 4R 5, COOR 7, COA, COAr, NHCOR 8, NHSO 2A, NHSO 2Ar or NHSO 2NR 4R 5; A : 1-6C alkyl optionally substituted by R 3; Ar : phenyl optionally substituted by R 6; R 3 : halo, phenyl, 1-6C alkoxy or NR 4R 5; R 4, R 5 : H or 1-6C alkyl; or NR 4R 5 : pyrrolidino, piperidino or morpholino; R 6 : H, OH, SH, 1-6C alkyl or 1-6C alkoxy; R 7 : H, A or Ar; R 8 : 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 MicroM against glycine uptake by SK-N-MC cells expressing native human glycine transporter glyt1.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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