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62. 发明专利

NO324352B1 未知
公开(公告)号：NO324352B1
公开(公告)日：2007-09-24
申请号：NO20020155
申请日：2002-01-11
申请人： SANOFI AVENTIS
发明人： GULLY DANIELLE , ROGER PIERRE , PRADINES ANTOINE , FONTAINE EVELYNE , GESLIN MICHEL
IPC分类号： C07D277/20 , C07D277/42 , 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 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07B53/00 , C07D417/12
摘要： Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotrophin releasing factor (CRF) antagonists.

63. 发明专利

HK1098465A1 USE OF TRICYCLIC COMPOUNDS AS GLYCINE TRANSPORT INHIBITORS 未知
公开(公告)号：HK1098465A1
公开(公告)日：2007-07-20
申请号：HK07104714
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： A61K20060101 , A61P20060101 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D20060101 , 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.

64. 发明专利

AT361279T 未知
公开(公告)号：AT361279T
公开(公告)日：2007-05-15
申请号：AT03740634
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： 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.

65. 发明专利

EA007225B1 ПРОИЗВОДНЫЕ N-[ФЕНИЛ(ПИПЕРИДИН-2-ИЛ)МЕТИЛ]БЕНЗАМИДА И ИХ ПРИМЕНЕНИЕ В ТЕРАПИИ 未知
公开(公告)号：EA007225B1
公开(公告)日：2006-08-25
申请号：EA200401172
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 , VERONIGUE 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： Данноеизобретениеотноситсяк соединениям, имеющимобщуюформулу (I), гдеА представляетсобойгруппуформулы N-R, где Rпредставляетсобойатомводорода, алкильнуюгруппу, циклоалкильнуюгруппу, фенилалкильнуюгруппу, алкенильнуюгруппуилиалкинильнуюгруппу; илигруппуформулы N(O)R, где Rявляетсятаким, какопределеновыше; илигруппуформулы N(R')R, где R' представляетсобойалкильнуюгруппуи Rтакой, какопределеновыше. Хпредставляетсобойатомводородаилиодинилиболеечемодинзаместитель, выбранныйизатомовгалогенаи трифторметильной, алкильныхи алкоксигрупп. Rпредставляетсобойатомводородаилиодинилиболеечемодинзаместитель, выбранныйизатомовгалогенаи трифторметила, алкильных, алкокси, аминогруппформулы NRR, где Rи R, каждыйпредставляетсобойатомводородаилиалкильнуюгруппу, илиобразуетвместес несущимихатомомазотапирролидиновое, пиперидиновоеилиморфолиновоекольцоиливозможнозамещеннуюфенильнуюгруппу. Данноеизобретениепригоднодляпримененияв терапии.

66. 发明专利

NO20062030L 未知
公开(公告)号：NO20062030L
公开(公告)日：2006-07-07
申请号：NO20062030
申请日：2006-05-05
申请人： SANOFI AVENTIS
发明人： ROGER PIERRE , MAGAT PASCALE , DARGAZANLI GIHAD , MARABOUT BENOIT , ESTENNE-BOUHTOU GENEVIEVE
IPC分类号： A61P25/04 , C07D471/08 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , 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.

67. 发明专利

PL373195A1 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：PL373195A1
公开(公告)日：2005-08-22
申请号：PL37319503
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： 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.

68. 发明专利

DE60010126T2 未知
公开(公告)号：DE60010126T2
公开(公告)日：2005-04-28
申请号：DE60010126
申请日：2000-12-14
申请人： SANOFI AVENTIS SA
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.

69. 发明专利

AU2004281217A1 Use of tricyclic compounds as glycine transport inhibitors 未知
公开(公告)号：AU2004281217A1
公开(公告)日：2005-04-28
申请号：AU2004281217
申请日：2004-10-15
申请人： SANOFI AVENTIS
发明人： ESTENNE-BOUHTOU GENEVIEVE , ROGER PIERRE , MARABOUT BENOIT , DARGAZANLI GIHAD , MAGAT PASCALE
IPC分类号： C07D471/08 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , 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.

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