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21. 发明专利

ZA200408154B Derivatives of N-Äphenyl(piperidin-2-YL)methylÜbenzamide, the preparation method thereof and application of same in therapeutics. 未知
公开(公告)号：ZA200408154B
公开(公告)日：2005-10-10
申请号：ZA200408154
申请日：2004-10-08
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 , C07D , A61K , A61P
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.

22. 发明专利

AU780711B2 Novel branched substituted amino derivatives of 3-amino-1-phenyl-H(1,2,4)triazol, methods for producing them and pharmaceutical compositions containing them 未知
公开(公告)号：AU780711B2
公开(公告)日：2005-04-14
申请号：AU2525901
申请日：2000-12-14
申请人： SANOFI AVENTIS
发明人： GESLIN MICHEL , GULLY DANIELLE , MAFFRAND JEAN-PIERRE , ROGER PIERRE
IPC分类号： A61K31/4196 , A61P1/14 , A61P15/10 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , B29C44/12 , C07D249/14 , C07D405/12
摘要： The present invention relates to novel branched substituted amino derivatives of 3-amino-1-phenyl-1H-[1,2,4]triazole, processes for their preparation and pharmaceutical compositions comprising them.

23. 发明专利

HRP20040977A2 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：HRP20040977A2
公开(公告)日：2004-12-31
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： 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： 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.

24. 发明专利

CA2481461A1 DERIVES DE N-[PHENYL(PIPERIDIN-2-YL)METHYL] BENZAMIDE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 未知
公开(公告)号：CA2481461A1
公开(公告)日：2003-10-30
申请号：CA2481461
申请日：2003-04-17
申请人： SANOFI AVENTIS
发明人： MARABOUT BENOIT , MEDAISKO FLORENCE , SEVRIN MIREILLE , ROGER PIERRE , VERONIQUE CORINNE , DARGAZANLI GIHAD , MAGAT PASCALE , ESTENNE-BOUHTOU GENEVIEVE
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： Composés de formule générale (I) dans laquelle A représente soit un groupe d e formule N-R1 dans laquelle R1 représente un atome d'hydrogène, un groupe alkyle, un groupe cycloalkyle, un groupe phénylalkyle, un groupe alcényle ou un groupe alcynyle, soit un groupe de formule N+ (O-) R1 dans laquelle R1 es t tel que défini ci-dessus, soit encore un groupe de formule N+ (R') R1 dans laquelle R' représente un groupe alkyle et R1 est tel que défini ci-dessus, X représente un atome d'hydrogène ou un ou plusieurs substituants choisis parm i les atomes d'halogènes et les groupes trifluorométhyle, alkyle et alcoxy, R2 représente un atome d'hydrogène, un ou plusieurs substituants choisis parmi les atomes d'halogènes et les groupes trifluorométhyle, alkyles, alcoxy, ami no de formule NR3R4 dans laquelle R3 et R4 représentant chacun un atome d'hydrogène ou un groupe alkyle, ou forment avec l'atome d'azote qui les por te un cycle pyrrolidine, pipéridine ou morpholine, soit un groupe phényle éventuellement substitué. Application en thérapeutique.

25. 发明专利

CO5251379A1 NUEVOS DERIVADOS AMINOSUBSTITUIDOS RAMIFICADOS DE 3- AMINO-1-FENIL-1H[1,2,4] TRIAZOL, PROCEDIMIENTOS PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知
公开(公告)号：CO5251379A1
公开(公告)日：2003-02-28
申请号：CO00095200
申请日：2000-12-14
申请人： SANOFI AVENTIS
发明人： GESLIN MICHAEL , GULLY DANIELLE , MAFFRAND JEAN PIERRE , ROGER PIERRE
IPC分类号： A61K31/4196 , A61P1/14 , A61P15/10 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , B29C44/12 , C07D249/14 , C07D405/12
摘要： Compuestos de fórmula: en la cual:- R1 y R2 representan, cada uno independientemente del otro, un átomo de halógeno; un (C1-C5)alquilo; un (C1- C5) alcoxi; un grupo nitro, trifluorometilo o ciano; un grupo amino NRaRb en el cual Ra y Rb representan cada uno independientemente del otro, un hidrógeno, un (C1 -C3) alquilo, un CO (C1 -C3) alquilo, o bien en el cual Ra y Rb constituyen con el átomo de nitrógeno al que están enlazados, un heterociclo de 5 a 7 eslabones; un grupo S-R en el cual R representa un átomo de hidrógeno o un (C1 -C5) alquilo, pudiendo el átomo de azufre ser monooxidado o dioxidado; - R3 representa hidrógeno o es tal como se lo ha definido anteriormente para R1 ;- R4 representa hidrógeno; un halógeno; un (C1 - C5) alquilo; un (C3-C5)cicloalquilo; un (C3-C5)cicloalquil(C1 -C2)alquilo; un grupo Rc-X-(C1-C2)alquilo en el cual Rc representa hidrógeno o un (C1 -C3)alquilo y X representa O, S, SO, S02; - R5 representa un (C1 -C5)alquilo, un alquinilo de 3 a 5 átomos de carbono, un alquenilo de 3 a 5 átomos de carbono; un (C3-C5)cicloalquil(C1 -C3)alquilo; un (C1 -C3)alquil-X(Co-C3)alquilo en el cual X representa O, S, SO, SO2 ; - R6 representa un grupo fenilo substituido por uno o varios radicales Z de los cuales al menos uno está en posición 2 y Z representa un halógeno, un grupo nitro, trifluorometilo o ciano; un (C1 -C5) alquilo; un (C1 - C5) alquil-X- o (C1 -C3) alquil-X- (C1 -C2) alquilo en los cuales X representa O, S, SO o SO2; un hidroxi(C1 - C3)alquilo; un CORd O COORd donde Rd representa un (C1 - C3) alquilo o un (C3-C5) cicloalquilo ; - 2 - - o bien R6 representa -CHR7R8 en el cual - R7 representa un (C3-C5) cicloalquilo; un grupo fenilo que puede ser substituido en posición 3, 4 y 5 por uno o varios radicales ZAND#39, con ZAND#39 que representa un halógeno, un grupo nitro, trifluorometilo o ciano; un (C1 -C5) alquilo; un (C1 -C5) alquil-X- o (C1 -C3) alquil-X-(C1 -C2) alquilo donde X representa O, S, SO o SO2; un hidroxi(C1 -C3) alquilo; un CORd O COORd en los cuales Rd es tal como se ha definido anteriormente; un metilendioxi, un etilendioxi; o bien un grupo piridilo eventualmente substituido por un grupo amino NRaRb tal como se ha definido precedentemente o por un radical ZAND#39 tal como se ha definido anteriormente; - R8 representa un (C1 -C6)alquilo; (C3-C5) cicloalquilo; un (C3-C5) cicloalquil (C1 -C3) alquilo; (C1 -C3) alquil-X- (C1-C3) alquilo donde X representa O, S, SO o SO2; un (C3-C5) cicloalquil (C1 -C2) alquil-X- (C1 -C3) alquilo donde X representa O, S, SO, SO2;así como sus sales de adición farmacéuticamente aceptables, sus hidratos y/o solvatos.

26. 发明专利

AU2525901A Novel branched substituted amino derivatives of 3-amino-1-phenyl-H(1,2,4)triazol, methods for producing them and pharmaceutical compositions containing them 未知
公开(公告)号：AU2525901A
公开(公告)日：2001-06-25
申请号：AU2525901
申请日：2000-12-14
申请人： SANOFI AVENTIS
发明人： GESLIN MICHEL , GULLY DANIELLE , MAFFRAND JEAN-PIERRE , ROGER PIERRE
IPC分类号： A61K31/4196 , A61P1/14 , A61P15/10 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , B29C44/12 , C07D249/14 , C07D405/12
摘要： The present invention relates to novel branched substituted amino derivatives of 3-amino-1-phenyl-1H-[1,2,4]triazole, processes for their preparation and pharmaceutical compositions comprising them.

27. 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.

28. 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.

29. 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.

30. 发明专利

SK287069B6 Aminothiazole derivates, preparation method thereof and pharmaceutical compositions comprising the same 未知
公开(公告)号：SK287069B6
公开(公告)日：2009-11-05
申请号：SK382002
申请日：2000-07-11
申请人： SANOFI AVENTIS
发明人： FONTAINE EVELYNE , GESLIN MICHEL , GULLY DANIELLE , PRADINES ANTOINE , ROGER PIERRE
IPC分类号： C07D277/00 , C07D277/20 , A61K31/00 , A61K31/426 , A61K31/427 , A61P1/00 , A61P1/12 , A61P3/04 , A61P3/10 , A61P5/04 , A61P9/00 , A61P9/14 , A61P15/00 , A61P15/06 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07B53/00 , C07D277/42 , C07D417/00 , C07D417/12
摘要： It is described compounds of formula (I.2) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined in Claim 1. Said compounds have an affinity for CRF receptors. It is described the method of preparation and pharmaceutical compositions too.

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