公开(公告)号：CZ20022646A3

公开(公告)日：2002-11-13

申请号：CZ20022646

申请日：2001-02-01

Applicant: SERVIER LAB

Inventor： LESIEUR DANIEL ,  BLANC-DELMAS ELODIE ,  YOUS SAID ,  DEPREUX PATRICK ,  GUILLAUMET GERALD ,  DACQUET CATHERINE ,  LEVENS NIGEL ,  BOUTIN JEAN ALBERT ,  BENNEJEAN CAROLINE ,  RENARD PIERRE

IPC: A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61P1/00 ,  A61P1/04 ,  A61P1/14 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P13/00 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/00 ,  A61P21/04 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07D263/58 ,  C07D277/68 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04 ,  A61K31/4353

Abstract: Compounds of formula (I): wherein: X represents an oxygen or a sulphur or CH 2 or R 1 and R 2 represent a hydrogen atom, or a group as defined in the description, A represents an alkylene chain as described in the description, B is as defined in the description, R 3 and R 4 represent a hydrogen atom or a group as defined in the description, D represents an optionally substituted benzene, optionally substituted pyrazine, optionally substituted pyrimidine or optionally substituted pyridazine and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.

公开(公告)号：PL353084A1

公开(公告)日：2002-10-07

申请号：PL35308402

申请日：2002-03-28

Applicant: SERVIER LAB

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

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097 ,  C07D207/08 ,  A61K31/401

Abstract: Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. ring A = a 5 membered nitrogen heterocycle that may be substituted by cyano; R1 = H, 1-6C alkyl or acyl, prolyl, alanyl, histidylprolyl, or phenylalanylprolyl; Ak = 1-6C alkylene or heteroalkylene; X = a bond or phenylene optionally substituted by one or more groups selected from halogens, 1-6C alkyl, alkoxy or polyhaloalkyl, or OH; R2 = 1-6C alkyl (optionally substituted by one or more groups selected from aryl, 1-6C alkylsulfonyl, 3-7C cycloalkylsulfonyl, 3-7C cycloalkyl, and halogen), 3-10C cycloalkyl, or a group -NR2aR2b; R2a and R2b = H, 1-6C alkyl, or together with the N atom they form a nitrogen heterocycle; Y = -NR3, -NH-CH=N-, -C(=NH)-NH-, or -NR4-C(=NR5)-NR6-; R3 = H, 1-6C alkyl, 3-7C cycloalkyl, or aryl; R4, R5, R6 = H, 1-6C alkyl; or R4 and R6 together, or R5 and R6 together = imidazolidine or dihydrobenzimidazole in which the term nitrogen heterocycle encompasses a monocyclic saturated ring of 5 - 7 members having 1 - 3 heteroatoms at least one of which is N and others may be N, O or S, and the term 1-6c alkylene encompasses a group that may be straight or branched and one methylene group may be replaced by an atom or O or S.

公开(公告)号：NO20021542L

公开(公告)日：2002-09-30

申请号：NO20021542

申请日：2002-03-27

Applicant: SERVIER LAB

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

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097 ,  C07D

Abstract: Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. ring A = a 5 membered nitrogen heterocycle that may be substituted by cyano; R1 = H, 1-6C alkyl or acyl, prolyl, alanyl, histidylprolyl, or phenylalanylprolyl; Ak = 1-6C alkylene or heteroalkylene; X = a bond or phenylene optionally substituted by one or more groups selected from halogens, 1-6C alkyl, alkoxy or polyhaloalkyl, or OH; R2 = 1-6C alkyl (optionally substituted by one or more groups selected from aryl, 1-6C alkylsulfonyl, 3-7C cycloalkylsulfonyl, 3-7C cycloalkyl, and halogen), 3-10C cycloalkyl, or a group -NR2aR2b; R2a and R2b = H, 1-6C alkyl, or together with the N atom they form a nitrogen heterocycle; Y = -NR3, -NH-CH=N-, -C(=NH)-NH-, or -NR4-C(=NR5)-NR6-; R3 = H, 1-6C alkyl, 3-7C cycloalkyl, or aryl; R4, R5, R6 = H, 1-6C alkyl; or R4 and R6 together, or R5 and R6 together = imidazolidine or dihydrobenzimidazole in which the term nitrogen heterocycle encompasses a monocyclic saturated ring of 5 - 7 members having 1 - 3 heteroatoms at least one of which is N and others may be N, O or S, and the term 1-6c alkylene encompasses a group that may be straight or branched and one methylene group may be replaced by an atom or O or S.

公开(公告)号：CA2379197A1

公开(公告)日：2002-09-28

申请号：CA2379197

申请日：2002-03-28

Applicant: SERVIER LAB

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

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097 ,  C07D207/08

Abstract: L'invention concerne de nouveaux composés répondant à la formule (I) (Voir formule I) dans laquelle (Voir formule II) représente un hétérocycle azoté à 5 chaînons éventuellement substitué ; R1 représente un atome d'hydrogène ou un groupement alkyle, acyl e, prolyle, alanyle, histidylprolyle ou phénylalanylprolyle ; Ak représente une chaîne alkylène ou hétéroalkylène ; X représente une liaison simple ou un groupement phénylène éventuellement substitué ; R2 représente un groupement alkyle éventuellement substitué, cycloalkyle en C3- C10 ou -NR2a R2b dans lequel R2a et R2b, identiques ou différents, représentent chacun un atome d'hydrogène ou un groupement alkyle, ou bien forment ensemble, avec l'atome d'azote qui les porte, un hétérocycle azoté ; et Y représente un groupement (Voir formule III, IV ou V) dans lesquels R3 représente un atome d'hydrogène ou un groupement alkyle, cycloalkyle en C3-C7 ou aryle, et R4, R5 et R6, identiques ou différents, représentent chacun un atome d'hydrogène ou un groupement alkyle, ou bien R4 et R6, ou R5 et R6 forment ensemble, avec les atomes qui les portent, un cycle imidazolidine ou dihydrobenzimidazole. L'invention vise également les isomères optiques des composés de formule (I), ainsi que leurs sels d'addition à un acide pharmaceutiquement acceptable. Les composés selon l'invention sont utiles en tant qu'inhibiteurs de dipeptidyl- peptidase IV.

公开(公告)号：NO20023662L

公开(公告)日：2002-09-27

申请号：NO20023662

申请日：2002-08-01

Applicant: SERVIER LAB

Inventor： LESIEUR DANIEL ,  BLANC-DELMAS ELODIE ,  YOUS SAID ,  DEPREUX PATRICK ,  GUILLAUMET GERALD ,  DACQUET CATHERINE ,  LEVENS NIGEL ,  BOUTIN JEAN ALBERT ,  BENNEJEAN CAROLINE ,  RENARD PIERRE

IPC: A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61P1/00 ,  A61P1/04 ,  A61P1/14 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P13/00 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/00 ,  A61P21/04 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07D263/58 ,  C07D277/68 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04

Abstract: Compounds of formula (I): wherein: X represents an oxygen or a sulphur or CH 2 or R 1 and R 2 represent a hydrogen atom, or a group as defined in the description, A represents an alkylene chain as described in the description, B is as defined in the description, R 3 and R 4 represent a hydrogen atom or a group as defined in the description, D represents an optionally substituted benzene, optionally substituted pyrazine, optionally substituted pyrimidine or optionally substituted pyridazine and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.

公开(公告)号：NO20023662A

公开(公告)日：2002-09-27

申请号：NO20023662

申请日：2002-08-01

Applicant: SERVIER LAB

Inventor： LESIEUR DANIEL ,  BLANC-DELMAS ELODIE ,  YOUS SAID ,  DEPREUX PATRICK ,  GUILLAUMET GERALD ,  DACQUET CATHERINE ,  LEVENS NIGEL ,  BOUTIN JEAN ALBERT ,  BENNEJEAN CAROLINE ,  RENARD PIERRE

IPC: A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61P1/00 ,  A61P1/04 ,  A61P1/14 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P13/00 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/00 ,  A61P21/04 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07D263/58 ,  C07D277/68 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04

CPC classification number: C07D263/58 ,  C07D277/68 ,  C07D471/04

公开(公告)号：CA2424802A1

公开(公告)日：2002-04-18

申请号：CA2424802

申请日：2001-10-11

Applicant: SERVIER LAB

Inventor： BOUTIN JEAN ALBERT ,  FAUCHERE JEAN-LUC ,  ORTUNO JEAN-CLAUDE ,  LEVENS NIGEL ,  CHAMORRO SUSANA

IPC: C07D249/14 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/55 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P15/10 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

Abstract: Composé de formule (I), dans laquelle: R3 représente un atome d'hydrogène ou un groupement alkyle, alkényle, alkynyle, aryle, hétéroaryle, cycloalkyle ou hétérocycloalkyle; R4 représente un groupement de formule (II), dans laquell e B représente un groupement mono ou polycyclique, aromatique ou non, contenan t 3 à 10 sommets, pouvant contenir de 1 à 3 hétéroatomes, R5 représente un ato me d'hydrogène ou un groupement alkyle, A représente un groupement choisi parmi - A2-, -A1-A2, -A2-A1- ou -A1-A2-A1-; V représente une liaison ou un groupemen t - CH2-, -CO-, -CS-, -CH2-NH- ou -CH=N-, ou V et R3 forment ensemble avec les groupements -A- et -N-R4 qui les portent un groupement -A-CH=N-R4, et leur utilisation dans le traitement des pathologies liées au neuropeptide Y (NPY) .

公开(公告)号：NO20021542D0

公开(公告)日：2002-03-27

申请号：NO20021542

申请日：2002-03-27

Applicant: SERVIER LAB

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

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097 ,  C07D

Abstract: Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. ring A = a 5 membered nitrogen heterocycle that may be substituted by cyano; R1 = H, 1-6C alkyl or acyl, prolyl, alanyl, histidylprolyl, or phenylalanylprolyl; Ak = 1-6C alkylene or heteroalkylene; X = a bond or phenylene optionally substituted by one or more groups selected from halogens, 1-6C alkyl, alkoxy or polyhaloalkyl, or OH; R2 = 1-6C alkyl (optionally substituted by one or more groups selected from aryl, 1-6C alkylsulfonyl, 3-7C cycloalkylsulfonyl, 3-7C cycloalkyl, and halogen), 3-10C cycloalkyl, or a group -NR2aR2b; R2a and R2b = H, 1-6C alkyl, or together with the N atom they form a nitrogen heterocycle; Y = -NR3, -NH-CH=N-, -C(=NH)-NH-, or -NR4-C(=NR5)-NR6-; R3 = H, 1-6C alkyl, 3-7C cycloalkyl, or aryl; R4, R5, R6 = H, 1-6C alkyl; or R4 and R6 together, or R5 and R6 together = imidazolidine or dihydrobenzimidazole in which the term nitrogen heterocycle encompasses a monocyclic saturated ring of 5 - 7 members having 1 - 3 heteroatoms at least one of which is N and others may be N, O or S, and the term 1-6c alkylene encompasses a group that may be straight or branched and one methylene group may be replaced by an atom or O or S.

公开(公告)号：AU2003226860B8

公开(公告)日：2008-07-10

申请号：AU2003226860

申请日：2003-02-04

Applicant: SERVIER LAB

Inventor： RENARD PIERRE ,  BAUT GUILLAUME LE ,  DUFLOS MURIEL ,  HUSSON-ROBERT BERNADETTE ,  DASSONVILLE ALEXANDRA ,  PFEIFFER BRUNO ,  LEVENS NIGEL ,  BRETECHE ANNE

IPC: C07C50/28 ,  A61K31/122 ,  A61K31/222 ,  A61K31/4402 ,  A61P3/10 ,  C07C45/00 ,  C07C45/28 ,  C07C46/00 ,  C07C46/10 ,  C07C50/30 ,  C07D213/50

Abstract: Compound of formula (I): wherein: R 1 and R 2 , which may be identical or different, each represents hydrogen, acyl or alkyl, Ar represents aryl or heteroaryl, A represents a group selected from: R 4 represents hydrogen or alkyl, R 5 represents hydrogen, alkyl, aryl or heteroaryl, R 3 represents aryl, heteroaryl, dicyclopropylmethyl or benzhydryl, or A-R 3 represents an optionally substituted naphthyl group, with the exclusion of 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-phenylethenyl)-1,4-benzoquinone, 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-naphthyl)-1,4-benzoquinone and 2,5-dihydroxy-3-(2-naphthyl)-6-phenyl-1,4-benzoquinone. Medicinal products containing the same which are useful in the treatment of diseases associated with a deregulation of glycaemia.

公开(公告)号：DE60212759T2

公开(公告)日：2007-08-02

申请号：DE60212759

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: C07D207/16 ,  C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D277/04 ,  C07D277/06 ,  C07D295/18 ,  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.