公开(公告)号：JP2002363157A

公开(公告)日：2002-12-18

申请号：JP2002132484

申请日：2002-05-08

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

Abstract: PROBLEM TO BE SOLVED: To provide a medicine having dipeptidyl peptidase IV-inhibiting characteristic and useful for treatment of glucose intolerance, hyperglycemia and related disorders. SOLUTION: This invention relates to a compound represented by formula (I) [wherein the ring A is a 5-membered nitrogen-containing heterocycle which may be substituted with cyano group; Ak is a straight-chain or branched (1-6C) alkylene chain; X is a single bond or the like; R1 and R2 are each hydrogen atom or the like; R3 is a straight-chain or branched chain (1-6C) alkyl or the like; Y represents CH-NO2 or the like], existing tautomer thereof, optical isomer thereof and addition salt of pharmaceutically acceptable acid thereof, a method for synthesizing the compound and, a pharmaceutical composition containing the compound.

公开(公告)号：JP2002363167A

公开(公告)日：2002-12-18

申请号：JP2002087792

申请日：2002-03-27

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

Abstract: PROBLEM TO BE SOLVED: To provide a medicine used as an inhibitor of dipeptidyl peptidase IV and usable for treatment of hyperglycemia and related disorders, prevention of transplanted piece refuse after transplantation, treatment of cancer and prevention of tumor metastasis, treatment of AIDS and paradentitis and recovery of intestine after resection. SOLUTION: This invention relates to a compound represented by the formula (I) [wherein the ring A represents a five-membered nitrogen-containing heterocycle which may be substituted by cyano group; R1 represents hydrogen atom or the like; Ak represents a straight or branched (1-6C)alkylene chain or the like; X represents a single bond or the like; R2 represents a straight-chain or a branched (1-6C)alkyl group or the like; Y represents a group of NR3 or the like (wherein R3 is hydrogen atom or the like)], its optical isomer and addition salt of its pharmaceutically acceptable acid, a method for producing the compound and a pharmaceutical composition containing the compound.

公开(公告)号：WO2006103342A9

公开(公告)日：2007-10-25

申请号：PCT/FR2006000673

申请日：2006-03-29

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

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

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

CPC classification number: C07D213/40 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D333/20

Abstract: The invention concerns a compound of formula (I), wherein: R 3 represents a hydrogen atom; and R 1 and R 2 form together, with the carbon atoms bearing them, a benzene, naphthalene or quinoline ring, each of said rings being optionally substituted, or R 1 represents a hydrogen atom, and R 2 and R 3 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-, -(CH 2 ) m -NR 4 -Ak-, - (CO)-NR 4 -Ak- and -(CH 2 ) m -NR 4 -(CO)-; m represents an integer between 1 and 6 inclusive; Ak represents an optionally substituted alkylene chain; and R 4 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.

Abstract translation: 本发明涉及式（I）化合物，其中：R 3表示氢原子; 和R 1和R 2 2一起形成带有它们的碳原子，苯，萘或喹啉环，每个所述环任选被取代，或R _{1 表示氢原子，并且R 2和R 3和它们的原子一起形成苯，萘或喹啉环，每个 所述环任选被取代; n表示1或2; -X-表示选自以下的基团： - （CH 2）m -O-Ak-， - （CH 2 CH 2）m -N > - > - （ - ）（CO）-NR 4 -A - 和 - （CH 2 CH 2）m -NR 4 - （CO） - ; m表示1〜6的整数， Ak表示任选取代的亚烷基链; R 4表示氢原子或烷基; Ar表示芳基或杂芳基; 其光学异构体，以及其药学上可接受的酸加成盐。 本发明适用于药物。}

公开(公告)号：WO2006103342A8

公开(公告)日：2007-12-21

申请号：PCT/FR2006000673

申请日：2006-03-29

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

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

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

CPC classification number: C07D213/40 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D333/20

Abstract: The invention concerns a compound of formula (I), wherein: R 3 represents a hydrogen atom; and R 1 and R 2 form together, with the carbon atoms bearing them, a benzene, naphthalene or quinoline ring, each of said rings being optionally substituted, or R 1 represents a hydrogen atom, and R 2 and R 3 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-, -(CH 2 ) m -NR 4 -Ak-, - (CO)-NR 4 -Ak- and -(CH 2 ) m -NR 4 -(CO)-; m represents an integer between 1 and 6 inclusive; Ak represents an optionally substituted alkylene chain; and R 4 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.

Abstract translation: 本发明涉及式（I）的化合物，其中：R 3代表氢原子; 和R SUB1和R SUB2与承载它们的碳原子一起形成苯环，萘环或喹啉环，每个所述环任选被取代，或R _{1表示氢原子，并且R 2和R 3与带有它们的原子一起形成苯环，萘环或喹啉环，每个 所述环任选被取代; n代表1或2; -X-表示选自 - （CH 2）m -O-Ak - ， - （CH 2 SUB）m -NR 4 - （CO） - ; m表示1和6之间的整数; Ak表示任选取代的亚烷基链; 并且R 4代表氢原子或烷基; Ar表示芳基或杂芳基; 其光学异构体，以及其药学上可接受的酸加成盐。 本发明适用于药物。}

公开(公告)号：WO2006103342A2

公开(公告)日：2006-10-05

申请号：PCT/FR2006000673

申请日：2006-03-29

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

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

IPC: C07D295/096 ,  A61K31/495 ,  A61P3/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D213/40 ,  C07D295/135 ,  C07D295/155 ,  C07D333/20

CPC classification number: C07D213/40 ,  C07D295/096 ,  C07D295/135 ,  C07D295/155 ,  C07D333/20

Abstract: The invention concerns a compound of formula (I), wherein: R 3 represents a hydrogen atom; and R 1 and R 2 form together, with the carbon atoms bearing them, a benzene, naphthalene or quinoline ring, each of said rings being optionally substituted, or R 1 represents a hydrogen atom, and R 2 and R 3 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-, -(CH 2 ) m -NR 4 -Ak-, - (CO)-NR 4 -Ak- and -(CH 2 ) m -NR 4 -(CO)-; m represents an integer between 1 and 6 inclusive; Ak represents an optionally substituted alkylene chain; and R 4 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：WO2009074733A3

公开(公告)日：2009-08-20

申请号：PCT/FR2008001311

申请日：2008-09-19

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

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

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

CPC classification number: C07D207/09 ,  C07D209/42 ,  C07D209/52 ,  C07D217/26 ,  C07D233/36 ,  C07D271/08 ,  C07D495/10

Abstract: The invention relates to compounds of the formula (I) in which A is an angiotensine-converting enzyme inhibitor including at least one salifiable basic function, B is a compound including at least one acidic sailifiable function and at least one NO-donor group, m is the number of acidic salified functions of B, and n is the number of basic salified functions of A, provided that the bond(s) between A and B are of the ionic type. The invention can be used in drugs.

Abstract translation: 本发明涉及式（I）化合物，其中A是包含至少一种可成碱性功能的血管紧张素转换酶抑制剂，B是包含至少一个酸性可释放功能的化合物和至少一个NO供体基团，m 是B的酸性盐化函数的数量，n是A的碱性盐化函数的数量，条件是A和B之间的键是离子型。 本发明可用于药物。

公开(公告)号：CY1110782T1

公开(公告)日：2015-06-10

申请号：CY101100834

申请日：2010-09-15

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

Abstract: Ενώσειςτουτύπου (I): (A)m · (B)n (I) στονοποίοτοΑ παριστάνειμιαένωσηαναστολέατουενζύμουμετατροπήςτηςαγγειοτασίνηςη οποίαπεριέχειμιατουλάχιστονβασικήομάδαπουμπορείνασχηματίζειάλας, τοΒ παριστάνειμιαένωσηη οποίαπεριέχειμιατουλάχιστονόξινηομάδαπουμπορείνασχηματίζειάλαςκαιτουλάχιστονμιαομάδαδότη NO, το m παριστάνειτοναριθμότωνόξινωνομάδωνπουέχουνσχηματίσειάλαςκαιτο n παριστάνειτοναριθμότωνβασικώνομάδωντουΑ πουέχουνσχηματίσειάλας, όπουεννοείταιότιο ήοιδεσμοίμεταξύΑ καιΒ είναιιοντικούτύπου. Φάρμακα.

公开(公告)号：CA2639700C

公开(公告)日：2012-08-28

申请号：CA2639700

申请日：2008-09-22

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: C07K5/062 ,  A61K31/4245 ,  A61K38/05 ,  A61P9/00 ,  A61P29/00 ,  A61P39/06 ,  C07D271/08 ,  C07D493/04 ,  C07F9/653

Abstract: La présent invention concerne des composés de formule (I) : A .cndot. B (I) dans laquelle A représente le périndopril ou le perindoprilate, B représente un composé comportant au moins une fonction acide salifiable et au moins un groupement donneur de NO, étant entendu que la ou les liaisons entre A et B sont de type ionique. L'invention s'étend au procédé de préparation de ces composés, leur utilisation et les compositions pharmaceutiques qui les contiennent.

公开(公告)号：AU2008217013B2

公开(公告)日：2012-08-16

申请号：AU2008217013

申请日：2008-09-15

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: C07D271/08 ,  A61K31/34 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4164 ,  A61K31/4245 ,  A61K31/435 ,  A61K31/5383 ,  A61K31/662 ,  A61P9/10 ,  A61P9/12 ,  A61P29/00 ,  A61P39/00 ,  C07D207/16 ,  C07D209/42 ,  C07D209/52 ,  C07D217/26 ,  C07D233/32 ,  C07D307/93 ,  C07D495/10 ,  C07F9/38

Abstract: -69 New addition salts of angiotensin-converting enzyme inhibitors with NO donor acids, a process for their preparation and pharmaceutical compositions containing them Compounds of formula (I) : 5 (A)m . (B). (I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound 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 10 functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicaments.

公开(公告)号：PL2039682T3

公开(公告)日：2010-10-29

申请号：PL08290885

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