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41. 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.

42. 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.

43. 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.

44. 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.

45. 发明专利

ECSP045369A DERIVADOS DE N-[FENIL(PIPERIDIN-2-IL)METIL]BENZAMIDA, SU PREPARACION Y SU APLICACION EN TERAPEUTICA 未知
公开(公告)号：ECSP045369A
公开(公告)日：2005-03-10
申请号：ECSP045369
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 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： Compuestos de fórmula general (I): en la cual:A representa o bien un grupo de fórmula general N-R1 en la cual R1 representa un átomo de hidrógeno, un grupo alquilo, un grupo cicloalquilo, un grupo fenilalquilo, un grupo alquenilo o un grupo alquinilo,o bien un grupo de fórmula N+ (O-)R1 en la cual R1 es tal como se ha definido anteriormente, o también un grupo de fórmula N+(R=)R1 en la cual R= representa un grupo alquilo y R1 es tal como se ha definido anteriormente, X representa un átomo de hidrógeno o uno o varios substituyentes elegidos entre los átomos de halógenos y los grupos trifluorometilo, alquilo y alcoxi, R2 representa un átomo de hidrógeno, o uno o varios substituyentes elegidos entre los átomos de halógenos y los grupos trifluorometilo, alquilos, alcoxi, amino de fórmula general NR3R4 en la cual R3 y R4 representan cada uno, un átomo de hidrógeno o un grupo alquilo, o forman con el átomo de nitrógeno que los lleva, un ciclo pirrolidino, piperidino o morfolino, o bien un grupo fenilo eventualmente substituido.Aplicación en terapéutica.

46. 发明专利

CY1108925T1 ΤΡΙΚΥΚΛΙΚΕΣ ΕΝΩΣΕΙΣ ΩΣ ΑΝΑΣΤΟΛΕΙΣ ΤΗΣ ΜΕΤΑΦΟΡΑΣ ΓΛΥΚΙΝΗΣ 未知
公开(公告)号：CY1108925T1
公开(公告)日：2014-07-02
申请号：CY081100494
申请日：2008-05-12
申请人： SANOFI AVENTIS
发明人： DARGAZANLI GIHAD , ESTENNE-BOUHTOU GENEVIEVE , MAGAT PASCALE , MARABOUT BENOÎT , ROGER PIERRE
IPC分类号： C07D471/08 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , C07D487/08
摘要： Μιαένωσητηςγενικήςφόρμουλας (I) σύμφωναμετηνοποίατο R αναπαριστάέναάτομουδρογόνουή μιαομάδαβινύλιο, το n αναπαριστά 0 ή 1 ή 2 τοΧ αναπαριστάμιαομάδατηςφόρμουλας CH ήέναάτομοαζώτουτο R1 αναπαριστάείτεμιαομάδαφαινύλιοή ναφθύλιοείτεμιαομάδακυκλοεξύλιο, είτεμιαομάδαετεροαρύλιο, το R2 αναπαριστάείτεέναάτομουδρογόνου, είτεέναή περισσότεραυποκατάσταταπουεπιλέγονταιανάμεσασταάτομααλογόνουκαιτιςομάδεςτριφθορομεθύλιο, αλκύλιο, αλκοξύ, θειενύλιο, φαινυλοξύ, υδροξύ, μέρκαπτο, θειοαλκύλιο, κύανοή μιαομάδατηςφόρμουλας -NR4 R5 , SΟ2NR4R5 , -SΟ2 -αλκύλιο, - SO2-φαινύλιο, -CONR4R5, -COOR7, -CO-αλκύλιο, -CO-φαινύλιο, -NHCOR8 , -ΝΗSO2-αλκύλιο, -ΝΗSO2-φαινύλιοκαι -NHSO2 NR4 R5 ήμιαδισθενήομάδατηςφόρμουλας -OCF2O-, τα R4 και R5 σχηματίζουνμετοάτομοαζώτουπουταφέρειένακυκλοπυρρολιδίνιο, ένακυκλοπιπεριδίνιοή ένακυκλομορφολίνη. Οιενώσειςτηςφόρμουλας (I) παρουσιάζουνμιασυγκεκριμένηδράσηωςσυγκεκριμένοιαναστολείςτωνμεταφορέων glyt1 ή/και glyt2.

47. 发明专利

AU2004281217B2 Use of tricyclic compounds as glycine transport inhibitors 未知
公开(公告)号：AU2004281217B2
公开(公告)日：2010-07-22
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： 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.

48. 发明专利

AU2003262420B2 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：AU2003262420B2
公开(公告)日：2009-02-19
申请号：AU2003262420
申请日：2003-04-17
申请人： SANOFI AVENTIS
发明人： MAGAT PASCALE , ESTENNE-BOUHTOU GENEVIEVE , VERONIQUE CORINNE , ROGER PIERRE , MARABOUT BENOIT , DARGAZANLI GIHAD , MEDAISKO FLORENCE , SEVRIN MIREILLE
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.

49. 发明专利

DE602004011806D1 未知
公开(公告)号：DE602004011806D1
公开(公告)日：2008-03-27
申请号：DE602004011806
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 , 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.

50. 发明专利

DE60313602T2 未知
公开(公告)号：DE60313602T2
公开(公告)日：2008-01-10
申请号：DE60313602
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： 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.

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