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1. 发明申请

WO2005037783A3 USE OF TRICYCLIC COMPOUNDS AS GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：作为甘油运输抑制剂的三氯化合物的使用
公开(公告)号：WO2005037783A3
公开(公告)日：2005-07-07
申请号：PCT/FR2004002643
申请日：2004-10-15
申请人： SANOFI AVENTIS , DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
IPC分类号： A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D471/08 , C07D487/08 , A61K31/4748 , A61P25/00
CPC分类号： C07D471/08 , C07D487/08
摘要： The invention relates to a compound having general formula (I), wherein: R represents a hydrogen atom or a vinyl group; n represents 0, 1 or 2; X represents a groups having formula CH or a nitrogen atom; R1 represents a phenyl or naphthyl group, or a cyclohexyl group, or a heteroaryl group; R2 represents a hydrogen atom, or one or more substituents selected from among the halogen atoms and the trifluoromethyl, alkyl, alkoxy, thienyl, phenyloxy, hydroxy, mercapto, thioalkyl, cyano groups or a group having general formula -NR4R5, SO2NR4R5, -SO2-alkyl, -SO2-phenyl, -CONR4R5, -COOR7, -CO-alkyl, -CO-phenyl, -NHCOR8, -NHSO2-alkyl, -NHSO2-phenyl and -NHSO2NR4R5 or a divalent group having formula -OCF2O-; and R4 and R5 each represent a hydrogen atom or an alkyl group or R4 and R5, together with the nitrogen atom bearing same, form a pyrrolidine, piperidine or morpholine ring. Compounds having formula (I) have a unique activity as specific inhibitors of glyt1 and/or glyt2 transporters.
摘要翻译：本发明涉及具有通式（I）的化合物，其中：R表示氢原子或乙烯基; n表示0,1或2; X表示具有式CH或氮原子的基团; R1表示苯基或萘基，或环己基或杂芳基; R 2表示氢原子或选自卤素原子和三氟甲基，烷基，烷氧基，噻吩基，苯氧基，羟基，巯基，硫代烷基，氰基或具有通式-NR4R5，SO2NR4R5，-SO2的基团的一个或多个取代基 - 烷基，-SO 2 - 苯基，-CONR 4 R 5，-COOR 7，-CO-烷基，-CO-苯基，-NHCOR 8，-NHSO 2 - 烷基，-NHSO 2 - 苯基和-NHSO 2 NR 4 R 5或具有式-OCF 2 O - 并且R 4和R 5各自表示氢原子或烷基，或者R 4和R 5与含有它们的氮原子一起形成吡咯烷，哌啶或吗啉环。具有式（I）的化合物作为glyt1和/或glyt2转运蛋白的特异性抑制剂具有独特的活性。

2. 发明专利

HK1142887A1 USE OF TRICYCLIC COMPOUNDS AS GLYCINE TRANSPORT INHIBITORS 未知
公开(公告)号：HK1142887A1
公开(公告)日：2010-12-17
申请号：HK10109250
申请日：2007-05-03
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
IPC分类号： C07D20060101 , A61P20060101 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D471/08 , C07D487/08
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. [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.

3. 发明专利

NO329065B1 未知
公开(公告)号：NO329065B1
公开(公告)日：2010-08-09
申请号：NO20044388
申请日：2004-10-15
申请人： SANOFI AVENTIS
发明人： MAGAT PASCALE , DARGAZANLI GIHAD , MARABOUT BENOIT , ESTENNE-BOUHTOU GENEVIEVE , MEDAISKO FLORENCE , ROGER PIERRE , SEVRIN MIREILLE , VERONIQUE CORINNE
IPC分类号： C07D211/26 , A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/32 , C07D211/94
摘要： N-((Piperidin-2-yl)-phenylmethyl)-trifluoromethyl-benzamides (I) are new. Piperidine derivatives of formula (I), in the form of the pure (1R,2R) or (1S,2S) optical isomer or the threo-diastereomer, and their acid addition salts are new. A = N-R1, N+(R1)-O- or N+(R')R1; R1 = H, 1-7C alkyl (optionally substituted by one or more F), (3-7C) cycloalkyl-(1-3C) alkyl, phenyl-(1-3C) alkyl (optionally substituted by 1 or 2 of OH or OMe), 2-4C alkenyl or 2-4C alkynyl; R' = 1-7C alkyl; X = H or one or more of halo, CF3, 1-4C alkyl and/or 1-4C alkoxy; R2 = H or one or more of halo, CF3, 1-4C alkyl, 1-4C alkoxy, NR3R4 or phenyl (optionally substituted by X); R3, R4 = H or 1-4C alkyl; or NR3R4 = pyrrolidino, piperidino or morpholino.

4. 发明专利

MEP12208A USE OF TRICYCLIC COMPOUNDS AS GLYCINE TRANSPORT INHIBITORS 未知
公开(公告)号：MEP12208A
公开(公告)日：2010-06-10
申请号：MEP12208
申请日：2004-10-15
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
IPC分类号： A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D471/08 , C07D487/08
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. [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.

5. 发明专利

HRP20040977B1 DERIVATIVES OF N-[PHENYL(PIPERIDIN-2-YL)METHYL]BENZAMIDE, THE PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS 未知
公开(公告)号：HRP20040977B1
公开(公告)日：2008-04-30
申请号：HRP20040977
申请日：2004-10-18
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , MEDAISKO FLORENCE , ROGER PIERRE , SEVRIN MIREILLE , VERONIQUE CORINNE
IPC分类号： C07D211/26 , A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/32 , C07D211/94
摘要： N-((Piperidin-2-yl)-phenylmethyl)-trifluoromethyl-benzamides (I) are new. Piperidine derivatives of formula (I), in the form of the pure (1R,2R) or (1S,2S) optical isomer or the threo-diastereomer, and their acid addition salts are new. A = N-R1, N+(R1)-O- or N+(R')R1; R1 = H, 1-7C alkyl (optionally substituted by one or more F), (3-7C) cycloalkyl-(1-3C) alkyl, phenyl-(1-3C) alkyl (optionally substituted by 1 or 2 of OH or OMe), 2-4C alkenyl or 2-4C alkynyl; R' = 1-7C alkyl; X = H or one or more of halo, CF3, 1-4C alkyl and/or 1-4C alkoxy; R2 = H or one or more of halo, CF3, 1-4C alkyl, 1-4C alkoxy, NR3R4 or phenyl (optionally substituted by X); R3, R4 = H or 1-4C alkyl; or NR3R4 = pyrrolidino, piperidino or morpholino.

6. 发明专利

RS91404A N-(FENIL(PIPERIDIN-2-IL)METIL)BENZAMIDNI DERIVATI, NJIHOVO DOBIJANJE I NJIHOVA PRIMENA U TERAPIJI 未知
公开(公告)号：RS91404A
公开(公告)日：2007-02-05
申请号：YUP91404
申请日：2003-04-17
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , MEDIASKO FLORENCE , ROGER PIERRE , SEVRIN MIREILLE , VERONIQUE CORINNE
IPC分类号： C07D211/26 , A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/32 , C07D211/94
摘要： Pronalazak se odnosi na jedinjenja opšte formule (I) pri čemu A - predstavlja grupu formule N-R1 gde R1 označava vodonikov atom, alkil grupu, cikloalkil grupu, fenilalkil grupu, alkenil grupu ili neku alkinil grupu; ili grupu formule N+(O-)R1, pri čemu je R1 definisan gore iznad; ili grupu formule N+(R)R1, gde R predstavlja alkil grupu, a R1 je definisan gore iznad. X predstavlja vodonikov atom ili jedan ili više supstituenata odabranih od atoma halogena i trifluormetil, alkil i alkoksi grupa. R2 predstavlja vodonikov atom, jedan ili više supstituenata odabranih od atoma halogena i trifluormetil, alkil i alkoksi grupa, amino grupe formule NR3R4 gde R3 i R4 pojedinacno predstavljaju vodonikov atom ili alkil grupu, ili, zajedno sa azotovim atomom za koji su vezani čine pirolidinski, piperidinski ili morfolinski prsten, ili opciono supstituisanu fenil grupu. Sadašnji pronalazak je pogodan za upotrebu u terapeutskim sredstvima.

7. 发明专利

BRPI0415489A 未知
公开(公告)号：BRPI0415489A
公开(公告)日：2006-12-26
申请号：BRPI0415489
申请日：2004-10-15
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
IPC分类号： A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D471/08 , C07D487/08 , A61K31/4748 , A61P25/00
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. [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.

8. 发明专利

NZ536015A N-[phenyl(piperidin-2-yl)methyl]benzamide derivatives, the preparation and their application in therapy 未知
公开(公告)号：NZ536015A
公开(公告)日：2006-11-30
申请号：NZ53601503
申请日：2003-04-17
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , MEDAISKO FLORENCE , ROGER PIERRE , SEVRIN MIREILLE , VERONIQUE CORINNE
IPC分类号： A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/26 , C07D211/32 , C07D211/94
摘要： Compound in the form of a pure optical isomer (1R,2R) or (1S,2S) or in the form of a threo diastereoisomer, corresponding to general formula (I) are disclosed, wherein: A denotes: a group with formula N-R1 in which R1 denotes a hydrogen atom, an alkyl group, a cycloalkyl group, a phenylalkyl group, an alkenyl group or an alkynyl group; or a group with formula N+(O-)R1 in which R1 is as defined above; or a group with formula N+(R')R1 in which R' denotes an alkyl group and R1 is as defined above; X denotes a hydrogen atom or one or more substituents selected from the halogen atoms and the trifluoromethyl, alkyl and alkoxy groups; R2 denotes a hydrogen atom, one or more substituents selected from the halogen atoms and the trifluoromethyl, alkyl, alkoxy, amino groups with formula NR3R4 in which R3 and R4 each denote a hydrogen atom or an alkyl group or, together with the nitrogen atom bearing same, form a pyrrolidine, piperidine or morpholine ring, or an optionally substituted phenyl group. The compound of formula (I) is suitable for use in therapeutics, particularly for the treatment of behavioural disorders associated with dementia, psychoses, schizophrenia (deficient form and productive form), for the treatment of various forms of anxiety, for the treatment of various forms of depression, including psychotic depression, for the treatment of disorders due to alcohol abuse or to withdrawal from alcohol, sexual behaviour disorders, food intake disorders, and for the treatment of migraine, for the treatment of intense and/or chronic pain, for the treatment of Parkinson's, for the treatment of epilepsy and other epileptic syndromes as a supplement to another antiepileptic treatment.

9. 发明专利

CA2542647A1 COMPOSES TRICYCLIQUES COMME INHIBITEURS DE TRANSPORT DE GLYCINE 未知
公开(公告)号：CA2542647A1
公开(公告)日：2005-04-28
申请号：CA2542647
申请日：2004-10-15
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , ROGER PIERRE
IPC分类号： C07D471/08 , A61K31/4748 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D487/08

10. 发明专利

AR039413A1 DERIVADOS DE N-(FENIL(PIPERIDIN-2-IL)METIL)BENZAMIDA, SU PREPARACION Y SU APLICACION EN TERAPEUTICA 未知
公开(公告)号：AR039413A1
公开(公告)日：2005-02-16
申请号：ARP030101310
申请日：2003-04-15
申请人： SANOFI AVENTIS
发明人： ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOIT , MEDAISKO FLORENCE , DARGAZANLI GIHAD , ROGER PIERRE , SEVRIN MIREILLE , VERONIQUE CORINNE
IPC分类号： A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/26 , C07D211/32 , C07D211/94 , A61P25/08 , A61P25/20 , A61P23/00
摘要： Reivindicación 1: compuesto en forma de isómero óptico puro (1R, 2R) ó (1S, 2S) ó en forma de diastereoisómero treo, caracterizado porque responde a la fórmula general (1): en la cuaL: A representa o bien un grupo de fórmula general N-R1 en la cual R1 representa, o bien un átomo de hidrógeno, o bien un grupo alquilo (C1-7) lineal o ramificado eventualmente sustituido por uno o varios átomos de flúor, o bien un grupo cicloalquilo (C4-7), o bien un grupo cicloalquilo(C3-7)-alquilo(C1-3), o bien un grupo fenilalquilo (C1-3) eventualmente sustituido por uno o dos grupos hidroxi o metoxi, o bien un grupo alquenilo (C2-4), o bien un grupo alquinilo (C2-4), o bien un grupo de fórmula general N+(O-)R1 en la cual R1 es tal como se ha definido anteriormente, o bien un grupo de fórmula general N+(R')R1 en la cual R' representa un grupo alquilo (C1-7) lineal o ramificado y r1 es tal como se ha definido anteriormente; X representa un átomo de hidrógeno o uno o varios sustituyentes elegidos entre los átomos de halógeno y los grupos trifluorometilo, alquilo (C1-4) lineal o ramificada y alcoxi (C1-4); R2 representa o bien un átomo de hidrógeno bien uno o varios sustituyentes elegidos entre los átomos de halógenos y los grupos trifluorometilo, alquilo (C1-4), alcoxi (C1-4), amino de fórmula general NR3R4 en la cual R3 y R4 representan cada uno, independientemente del otro, un átomo de hidrógeno o un grupo alquilo (C1-4), o forman con el átomo de nitrógeno que los lleva, un ciclo pirrolidino piperidino o morfolino, o bien un grupo fenilo eventualmente sustituido por un átomo o un grupo tal como se han definido para el símbolo X anteriormente, en estado de base libre o de sal de adición con un ácido.

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