公开(公告)号：MY144927A

公开(公告)日：2011-11-30

申请号：MYPI20083604

申请日：2008-09-16

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN-GILLES ,  BENOIST ALAIN ,  RUPIN ALAIN ,  VERBEUREN TONY ,  COURCHAY CHRISTINE ,  SIMONET SERGE

IPC: C07D207/09

Abstract: COMPOUNDS OF FORMULA (I) : WHEREIN A REPRESENTS AN ANGIOTENSIN-CONVERTING ENZYME INHIBITOR COMPOUND CONTAINING AT LEAST ONE SALT-FORMING BASIC FUNCTION, B REPRESENTS A COMPOUDD CONTAINING AT LEAST ONE SALT- FORMING ACID FUNCTION AND AT LEAST ONE NO DONOR GROUP, M REPRESENTS THE NUMBER OF ACID FUNCTIONS OF B THAT HAVE BEEN CONVERTED TO A SALT AND N REPRESENTS THE NUMBER OF BASIC FUNCTIONS OF A THAT HAVE BEEN CONVERTED TO A SALT, THE BOND OR BONDS BETWEEN A AND B BEING OF THE IONIC TYPE.

公开(公告)号：DK2039682T3

公开(公告)日：2010-11-08

申请号：DK08290885

申请日：2008-09-19

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  PARMENTIER JEAN-GILLES ,  BENOIST ALAIN ,  VERBEUREN TONY ,  RUPIN ALAIN ,  COURCHAY CHRISTINE ,  SIMONET SERGE ,  GLOANEC PHILIPPE

IPC: A61K31/385 ,  C07D207/09 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4245 ,  A61K31/472 ,  C07D209/42 ,  C07D209/52 ,  C07D217/26 ,  C07D233/36 ,  C07D271/08 ,  C07D495/10

公开(公告)号：SI2039682T1

公开(公告)日：2010-10-29

申请号：SI200830064

申请日：2008-09-19

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN-GILLES ,  BENOIST ALAIN ,  VERBEUREN TONY ,  RUPIN ALAIN ,  COURCHAY CHRISTINE ,  SIMONET SERGE

IPC: A61K31/385 ,  C07D207/00 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4245 ,  A61K31/472 ,  C07D209/00 ,  C07D217/00 ,  C07D233/00 ,  C07D271/00 ,  C07D495/00

公开(公告)号：SV2010003511A

公开(公告)日：2010-07-29

申请号：SV2010003511

申请日：2010-03-18

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN-GILLES ,  BENOIST ALAIN ,  VERBEUREN TONY ,  RUPIN ALAIN ,  COURCHAY CHRISTINE ,  SIMONET SERGE

IPC: A61K31/34 ,  A61K31/40 ,  A61K31/404 ,  A61K31/407 ,  A61K31/421 ,  A61K31/472 ,  A61P9/00 ,  C07D207/08 ,  C07D207/12 ,  C07D209/08 ,  C07D209/42 ,  C07D209/52 ,  C07D215/48 ,  C07D271/04 ,  C07D339/06 ,  C07D495/10 ,  C07F9/38

Abstract: COMPUESTOS DE FORMULA (I): (A)M. (B)N (I) EN LA QUE A REPRESENTA UN COMPUESTO INHIBIDOR DE LA ENZIMA DE CONVERSIÓN DE LA ANGIOTENSINA QUE CONLLEVA AL MENOS UNA FUNCIÓN BÁSICA SALIFICABLE, B REPRESENTA UN 10 COMPUESTO QUE CONLLEVA AL MENOS UNA FUNCIÓN ACIDA SALIFICABLE Y AL MENOS UN GRUPO DONADOR DE NO, M REPRESENTA EL NUMERO DE FUNCIONES ACIDAS SALIFICADA DE B Y N REPRESENTA EL NUMERO DE FUNCIONES BÁSICA SALIFICADAS DE A, DEBIENDO ENTENDERSE QUE EL O LOS ENLACES ENTRE A Y B SON DE TIPO IÓNICO

公开(公告)号：TNSN07357A1

公开(公告)日：2008-12-31

申请号：TNSN07357

申请日：2007-09-18

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  MILLAN MARK ,  ORTUNO JEAN-CLAUDE ,  MANNOURY LA COUR CLOTILDE ,  GOBERT ALAIN

IPC: A61K31/495 ,  A61P1/08 ,  A61P3/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D213/40 ,  C07D295/08 ,  C07D295/12 ,  C07D295/14 ,  C07D333/20

Abstract: The invention concerns a compound of formula (I), wherein: R3 represents a hydrogen atom; and R1 and R2 form together, with the carbon atoms bearing them, a benzene, naphthalene or quinoline ring, each of said rings being optionally substituted, or R1 represents a hydrogen atom, and R2 and R3 form together, with the atoms bearing them, a benzene, naphthalene or quinoline ring, each of said rings being optionally substituted; n represents 1 or 2; -X- represents a group selected among -(CH2)m-O-Ak-, -(CH2)m-NR4-Ak-, - (CO)-NR4-Ak- and -(CH2)m-NR4-(CO)-; m represents an integer between 1 and 6 inclusive; Ak represents an optionally substituted alkylene chain; and R4 represents a hydrogen atom or an alkyl group; Ar represents an aryl or heteroaryl group; its optical isomers, as well as a pharmaceutically acceptable acid-addition salt thereof. The invention is applicable to medicines.

公开(公告)号：FR2883876B1

公开(公告)日：2007-05-04

申请号：FR0503071

申请日：2005-03-30

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  MILLAN MARK ,  ORTUNO JEAN CLAUDE ,  MANNOURY LA COUR CLOTILDE ,  GOBERT ALAIN

IPC: C07D295/10 ,  A61K31/495 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00

Abstract: Indanyl-piperazine derivatives (I) are new. Indanyl-piperazine derivatives of formula (I) and their optical isomers, salts, enantiomers or diastereoisomers are new. R 3 = H and R 1+R 2 = benzene, naphthalene or quinoline (optionally substituted by H, halo or 1-6C alkyl (optionally substituted by halo)); or R 1 = H; and R 2+R 3 = benzene, naphthalene or quinoline (optionally substituted by H, halo or 1-6C alkyl (optionally substituted by halo)); n = 1-2; X = (CH 2) m-OT, (CH 2) m-NR 4T, C(O)NR 4T or (CH 2) mNR 4C(O); m = 1-6; T = 1-6C alkyl optionally substituted by OH; R 4 = H or 1-6C alkyl; A = (hetero)aryl; aryl = phenyl, biphenyl or naphthyl (optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, CN or 1-6C trihaloalkyl); and heteroaryl = 5-12 membered aromatic mono- or bicyclic rings containing O, N or S heteroatoms and optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH or 1-6C trihaloalkyl. An independent claim is also included for preparation of (I). [Image] ACTIVITY : Antidepressant; Tranquilizer; Anorectic; Analgesic; Antiinflammatory; Neuroleptic; Antiemetic; Gastrointestinal-Gen. MECHANISM OF ACTION : Serotonin receptor inhibitor; Neurokinin-1 antagonist. The ability of (1RS)-1-[1-(3,5-difluorobenzyloxymethyl)indan-1-yl]piperazine dihydrochloride to inhibit serotonin receptor in rats was tested using biological assays. The result showed that (1RS)-1-[1-(3,5-difluoro-benzyloxymethyl)-indan-1-yl]-piperazine dichlorhydrate exhibits a pK i (negative log of inhibitory constant) value of 8.49.

公开(公告)号：NO322569B1

公开(公告)日：2006-10-30

申请号：NO20022285

申请日：2002-05-14

Applicant: SERVIER LAB

Inventor： BOULANGER MICHELLE ,  NANTEUIL GUILLAUME DE ,  PORTEVIN BERNARD ,  LEVENS NIGEL ,  BENOIST ALAIN ,  NOSJEAN OLIVIER ,  HUSSON-ROBERT BERNADETTE

IPC: C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D295/185 ,  C07K5/02

Abstract: Alpha amino acid derivatives (I), their optical isomers and addition salts, are new. Alpha amino acid derivatives of formula (I), their optical isomers and addition salts, are new: A = five-membered heterocycle, optionally substituted by a cyano group; Ak = 1-6C alkylene; X = single bond or phenylene; R1, R2, R4 = H or 1-6C alkyl; Y = NR4 or CH-NO2; R3 = NO2 or CN; and provided that: (i) when Y is CH-NO2, then R3 may further be 1-6C alkyl; and (ii) when A is unsubstituted, then Ak is propylene, X is a bond, Y is NH and R3 is NO2, are excluded.

公开(公告)号：FR2824825B1

公开(公告)日：2005-05-06

申请号：FR0106375

申请日：2001-05-15

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON ROBERT BERNADETTE ,  BOULANGER MICHELLE

IPC: C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D295/185 ,  C07K5/02 ,  C07D207/42

Abstract: Alpha amino acid derivatives (I), their optical isomers and addition salts, are new. Alpha amino acid derivatives of formula (I), their optical isomers and addition salts, are new: A = five-membered heterocycle, optionally substituted by a cyano group; Ak = 1-6C alkylene; X = single bond or phenylene; R1, R2, R4 = H or 1-6C alkyl; Y = NR4 or CH-NO2; R3 = NO2 or CN; and provided that: (i) when Y is CH-NO2, then R3 may further be 1-6C alkyl; and (ii) when A is unsubstituted, then Ak is propylene, X is a bond, Y is NH and R3 is NO2, are excluded.

公开(公告)号：DE69816004T2

公开(公告)日：2004-04-29

申请号：DE69816004

申请日：1998-11-25

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BONNET JACQUELINE ,  TORDJMAN CHARLES

IPC: A61K31/00 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61P19/00 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D209/44 ,  C07D209/52 ,  C07D209/72 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D487/04 ,  C07D491/16

Abstract: Compounds of formula (I): wherein: R represents hydrogen, alkyl, optionally-substituted amino, or linear or branched (C1-C6)-acyl, R1 and R2, which may be identical or different, each represents independently of the other aryl, heteroaryl, or (C5-C7)-cycloalkyl, or one of those groups optionally substituted, A, together with the atoms in common with the pyrrole, represents saturated or unsaturated, monocyclic or bicyclic (C3-C12)-cycloalkyl, or a saturated heterocycle having 5 to 7 ring members and containing one or two nitrogen, or 7-oxabicyclo[2.2.1]heptane, or one of those groups optionally substituted, their isomers, and also addition salts thereof with a pharmaceutically-acceptable acid or base, pharmaceutical compositions thereof, and use thereof as medicaments.

公开(公告)号：AR033735A1

公开(公告)日：2004-01-07

申请号：ARP020101750

申请日：2002-05-14

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON-ROBERT BERNADETTE ,  BOULANGER MICHELLE

IPC: C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D295/185 ,  C07K5/02 ,  C07D295/18 ,  A61K31/33

Abstract: Compuesto de fórmula (1), en la cual fórmula (2) representa un heterociclo que contiene nitrógeno de 5 miembros; Ak representa una cadena alquileno; X representa un enlace simple o un grupo fenileno; R1 y R2, que pueden ser idénticos o diferentes, cada uno representa un átomo de hidrógeno o un grupo alquilo; R3 representa un grupo alquilo, nitro o ciano, cuando Y es CH-NO2; o nitro y ciano cuando Y representa NR4; Y representa NR4 o CH-NO2; R4 representa un átomo de hidrógeno o un grupo alquilo; sus tautómeros cuando estos existen, sus isómeros ópticos y sales de adición de los mismos con un ácido farmacéuticamente aceptable, con exclusión de los compuestos en los cuales, simultáneamente, fórmula (2) representa un heterociclo que contiene nitrógeno de 5 miembros no sustituido; Ak representa el grupo -(CH2)3-; X representa un enlace simple; Y representa NH y R3 representa el grupo nitro. Medicamentos para la intolerancia de glucosa y trastornos asociados a hiperglucemia.