公开(公告)号：WO2007144512A3

公开(公告)日：2008-03-20

申请号：PCT/FR2007000989

申请日：2007-06-14

Applicant: SERVIER LAB ,  CORDI ALEXIS ,  HABERKORN LAURE ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

Inventor： CORDI ALEXIS ,  HABERKORN LAURE ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

IPC: C07D257/04 ,  A61K31/41 ,  A61P9/00 ,  A61P9/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14

CPC classification number: C07D257/04 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14

Abstract: The invention relates to compounds of formula (I): in which: R 1 is an alkanoyl group, R 2 is an alkyl group substituted with a group G, or R 1 and R 2 form, together with the nitrogen atom which bears them, an imidazolyl or benzimidazolyl group, substituted with a group G, and G is a -(CH 2 ) n -A-(CH 2 ) m -(CR 4 R 5 ) P -(CH 2 ) O -R 3 group in which n, m, p, o, R 4 , R 5 and A are as defined in the description, and R 3 is a group of formula (II) or formula (III). The invention also relates to the use of said compounds as angiotensin receptor antagonists and as NO donors, in the fields of hypertension and cardiovascular pathologies.

Abstract translation: 本发明涉及式（I）的化合物：其中：R 1是烷酰基，R 2是被基团G取代的烷基， 与它们的氮原子一起形成与基团G取代的咪唑基或苯并咪唑基，并且G是 - （CH 2）n - 2 ）_{名词 -A-（CH 2 ）米 - （CR 4 - [R}

公开(公告)号：WO2009004164A9

公开(公告)日：2010-03-18

申请号：PCT/FR2008000731

申请日：2008-05-29

Applicant: SERVIER LAB ,  CORDI ALEXIS ,  HABERKORN LAURE ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

Inventor： CORDI ALEXIS ,  HABERKORN LAURE ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

IPC: C07D403/04 ,  A61K31/4184

CPC classification number: C07D403/04

Abstract: The invention relates to compounds of the general formula (I) G-(CH2)n-A-(CH2)m-(CR1R2)p-(CH2)o-R3 in which: n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; p is 1 or 0; o is 0, 1 or 2; R1 and R2 each represent a hydrogen atom or an alkyl group; one of the groups -CH2- or -CR1R2- can also be replaced with a phenylene, -PhC(O)- or -PhC(O)O- group; A and G are such as defined in the description; and R3 is a group (II) or (III). The invention can be used for drugs.

Abstract translation: 本发明涉及通式（I）G-（CH2）n -A-（CH2）m-（CR1R2）对 - （CH2）o-R3的化合物，其中：n为0,1,2或3; m为0,1,2或3; p为1或0; o为0,1或2; R1和R2各自表示氢原子或烷基; -CH 2 - 或-CR 1 R 2基团之一也可以被亚苯基-PhC（O） - 或-PhC（O）O-基团取代; A和G如描述中所定义; 并且R 3是（II）或（III）基团。 本发明可用于药物。

公开(公告)号：WO2009004164A3

公开(公告)日：2009-04-30

申请号：PCT/FR2008000731

申请日：2008-05-29

Applicant: SERVIER LAB ,  CORDI ALEXIS ,  HABERKORN LAURE ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

Inventor： CORDI ALEXIS ,  HABERKORN LAURE ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

IPC: C07D403/04 ,  A61K31/4184

CPC classification number: C07D403/04

Abstract: The invention relates to compounds of the general formula (I) G-(CH2)n-A-(CH2)m-(CR1R2)p-(CH2)o-R3 in which: n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; p is 1 or 0; o is 0, 1 or 2; R1 and R2 each represent a hydrogen atom or an alkyl group; one of the groups -CH2- or -CR1R2- can also be replaced with a phenylene, -PhC(O)- or -PhC(O)O- group; A and G are such as defined in the description; and R3 is a group (II) or (III). The invention can be used for drugs.

Abstract translation: 本发明涉及通式（I）G-（CH2）n -A-（CH2）m-（CR1R2）对 - （CH2）o-R3的化合物，其中：n为0,1,2或3; m为0,1,2或3; p为1或0; o为0,1或2; R1和R2各自表示氢原子或烷基; -CH 2 - 或-CR 1 R 2基团之一也可以被亚苯基-PhC（O） - 或-PhC（O）O-基团取代; A和G如描述中所定义; 并且R 3是（II）或（III）基团。 本发明可用于药物。

公开(公告)号：EP2144506A4

公开(公告)日：2010-05-05

申请号：EP07868093

申请日：2007-12-28

Applicant: CORTEX PHARMA INC ,  SERVIER LAB

Inventor： CORDI ALEXIS ,  ROGERS GARY ,  MUELLER RUDOLF

IPC: C07D498/04 ,  A61K31/53 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D498/04

公开(公告)号：ES2374995T3

公开(公告)日：2012-02-23

申请号：ES07868093

申请日：2007-12-28

Applicant: CORTEX PHARMA INC ,  SERVIER LAB ,  SERVIER LAB

Inventor： CORDI ALEXIS ,  ROGERS GARY ,  MUELLER RUDOLF

IPC: C07D498/04 ,  A61K31/53 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

Abstract: Compuesto de fórmula: **Fórmula** o una sal de adición farmacéuticamente aceptable de un ácido o una base del mismo.

公开(公告)号：BR112013005967A2

公开(公告)日：2016-05-03

申请号：BR112013005967

申请日：2011-09-15

Applicant: SERVIER LAB

Inventor： CORDI ALEXIS ,  DANOBER LAURENCE ,  DESOS PATRICE ,  LESTAGE PIERRE

IPC: C07D291/08 ,  A61K31/551 ,  A61P25/00

Abstract: derivados di-hidro benzoxa tiazepinas, o respectivo preparo, compoisções farmacêuticas e utilização como moduladores dos receptores ampa. a presente invenção refere-se aos compostos de fórmula (i); na qual r1 representa um átomo de hidrogênio, um grupamento heterocíclico, ciano, alcóxi carbonila, alquil sulfonil amino alquila, ou n-hidróxi carbóxi midamida; a respectiva utilização como moduladores dos receptores ampa.

公开(公告)号：CY1112493T1

公开(公告)日：2015-12-09

申请号：CY111101287

申请日：2011-12-28

Applicant: SERVIER LAB

Inventor： CORDI ALEXIS ,  ROGERS GARY ,  MUELLER RUDOLF

IPC: C07D498/04 ,  A61K31/53 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

Abstract: Αυτήη εφεύρεσηαναφέρεταιστηνπρόληψηκαιθεραπείατηςεγκεφαλικήςανεπάρκειας, συμπεριλαμβανομένηςτηςενίσχυσηςτηςλειτουργίαςτωνυποδοχέωνστιςσυνάψειςστοεγκεφαλικόδίκτυουπεύθυνεςγιασυμπεριφορέςυψηλότερηςτάξης. Αυτάταεγκεφαλικάδίκτυαεμπλέκονταισεγνωστικέςικανότητεςπουσχετίζονταιμεεξασθένησημνήμης, όπωςπαρατηρείταισεμιαποικιλίαανιών, καισεανισορροπίεςστηνευρωνικήδραστηριότηταμεταξύδιαφορετικώνπεριοχώντουεγκεφάλου, όπωςσυνιστάταισεδιαταραχέςόπωςη νόσοςτουΡarkinson, σχιζοφρένειακαισυναισθηματικέςδιαταραχές. Κατάμιασυγκεκριμένηάποψη, ηπαρούσαεφεύρεσησχετίζεταιμεμιαένωσηχρήσιμηγιατηθεραπείατέτοιωνπαθήσεων, καιμεμεθόδουςχρήσηςαυτήςτηςένωσηςγιαμιατέτοιαθεραπεία.

公开(公告)号：AP3050A

公开(公告)日：2014-11-30

申请号：AP2011005935

申请日：2010-03-18

Applicant: SERVIER LAB

Inventor： CORDI ALEXIS ,  DESOS PATRICE ,  LESTAGE PIERRE

IPC: A61K31/554 ,  A61P25/00 ,  C07D285/36

Abstract: Benzothiadiazepine derivatives (I) and their optical and positional isomers, or addition salts with an acid or base, are new. Benzothiadiazepine derivatives of formula (I) and their optical and positional isomers, or addition salts with an acid or base, are new. R 1>, R 2> : H, halo, or 1-6C alkyl (optionally substituted by one or more halo, 1-6C alkoxy, 1-6C alkylthio, 1-6C alkoxycarbonyl, carboxy group, 1-6C acyl, hydroxyl group, 1-6C hydroxyalkyl group, CN, nitro, amino group (substituted by an 1-6C acyl and optionally substituted by one or more 1-6C alkyl), aminocarbonyl group (optionally substituted by one or more 1-6C alkyl), aminosulfonyl group (optionally substituted by one or more 1-6C alkyl), alkyl(1-6C)sulfonylamino1-6C alkyl, N-hydroxycarboximidamide or benzyloxy); R 3> : H, 1-6C alkyl, 3-8C cycloalkyl, or 3-8C-cycloalkyl-1-6C alkyl; and R 4> : H or 1-6C alkyl (optionally substituted by one or more halo). Independent claims are included for: (1) the preparation of (I); and (2) 1,1-dioxo-2,3,4,5-tetrahydro-1H-benzo[f][1,2,5]thiadiazepin-8-ol (VI) as an intermediate for the synthesis of (I). [Image] ACTIVITY : Neuroprotective; Nootropic; Antiparkinsonian; Cerebroprotective; Anticonvulsant; Antialcoholic; Neuroleptic; Vasotropic; Antidepressant; Tranquilizer. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor modulator; N-methyl-D-aspartate (NMDA) receptor antagonist. The NMDA receptor antagonistic activity of (I) was tested in rats. The result showed that 8-phenoxy-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine-1,1-dioxide exhibited an IC 50value of 9 microM.

公开(公告)号：NZ595082A

公开(公告)日：2013-12-20

申请号：NZ59508210

申请日：2010-03-18

Applicant: SERVIER LAB

Inventor： DANOBER LAURENCE ,  CORDI ALEXIS ,  DESOS PATRICE ,  LESTAGE PIERRE

IPC: C07D285/36 ,  A61K31/554 ,  A61P25/00

Abstract: IP No. 595082 The present disclosure relates to new benzothiadiazepine compounds of formula (I), to a process for their preparation, to pharmaceutical compositions containing them, and also to the use thereof as positive allosteric modulators of AMPA receptors and antagonists of NMDA receptors. Preferred compounds include: 8-phenoxy-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine 1,1-dioxide; ethyl 3-[(1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy]-benzoate; 3-[(1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy]-N-methyl benzamide; { 3-[(1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy]phenyl} -methanol; 4-[(1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy]phenol; 4-[(5-methyl-1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy]phenol And; 4-[(1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy]aniline. Processes for their preparation are also disclosed along with the use of 2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-ol 1,1-dioxide (compound of formula VI) as an intermediate. Conditions which the compounds of the disclosure may be used in the treatment or prevention of include: progressive neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, Pick's disease, Huntington's chorea, Korsakoff's disease, schizophrenia, acute neurodegenerative diseases, frontal lobe and subcortical dementias, vascular dementias, epilepsy, cerebral vascular accidents and also depressive and anxious states.

公开(公告)号：MA34529B1

公开(公告)日：2013-09-02

申请号：MA35744

申请日：2013-03-14

Applicant: SERVIER LAB

Inventor： CORDI ALEXIS ,  DESOS PATRICE ,  LESTAGE PIERRE ,  DANOBER LAURENCE

IPC: C07D291/08 ,  A61K31/551 ,  A61P25/00

Abstract: Composés de formule (I) : dans laquelle R1 représente un atome d'hydrogène, un groupement hétérocyclique, cyano, alkoxycarbonyle, alkylsulfonylaminoalkyle, ou N-hydroxycarboximidamide; leur utilisation en tant que modulateurs des récepteurs AMPA.