公开(公告)号：JP2002212184A

公开(公告)日：2002-07-31

申请号：JP2001378235

申请日：2001-12-12

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  GLOANEC PHILIPPE ,  VERBEUREN TONY ,  RUPIN ALAIN ,  VALLEZ MARIE ODILE

IPC: C07D487/04 ,  A61K31/4985 ,  A61K31/536 ,  A61K38/00 ,  A61P7/02 ,  A61P9/10 ,  A61P43/00 ,  C07D471/04 ,  C07K5/078

Abstract: PROBLEM TO BE SOLVED: To obtain a new inhibitor of serine proteases such as thrombin having improved effects and selectivity. SOLUTION: This compound is represented by formula (I) [wherein, R1 represents hydrogen atom or a linear or a branched 1-6C alkyl group which is optionally substituted; a group represented by formula (II) represents a saturated ring having 4 to 7 ring members that may contain, in addition to nitrogen atom, one or two heteroatoms selected from O, S and N; n represents an integer of 1

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：HRP20190193T1

公开(公告)日：2019-04-05

申请号：HRP20190193

申请日：2019-01-30

Applicant: SERVIER LAB

Inventor： GLOANEC PHILIPPE ,  SCHAFFNER ARNAUD-PIERRE ,  SANSILVESTRI-MOREL PATRICIA ,  RUPIN ALAIN ,  MENNECIER PHILIPPE ,  VALLEZ MARIE-ODILE

IPC: A61K31/66 ,  A61K9/00 ,  A61K31/675 ,  A61K45/06 ,  C07F9/6568 ,  C07F9/6584

公开(公告)号：MD3271368T2

公开(公告)日：2019-03-31

申请号：MDE20180097

申请日：2017-01-13

Applicant: SERVIER LAB

Inventor： GLOANEC PHILIPPE ,  SCHAFFNER ARNAUD-PIERRE ,  SANSILVESTRI-MOREL PATRICIA ,  RUPIN ALAIN ,  MENNECIER PHILIPPE ,  VALLEZ MARIE-ODILE

IPC: A61K31/66 ,  A61K9/00 ,  A61K31/675 ,  A61K45/06 ,  C07F9/6568 ,  C07F9/6584

Abstract: Compuşii cu formula (I) în care: Ak1 reprezintă o catenă alchil, X reprezintă - (CH2) m-, -CH (R) -, -N (R) R, -CH2- sau -CH2-N (R) -CH2-, m şi R sunt definiţi ca în descriere, R1 şi R2 reprezintă fiecare H atunci când X reprezintă - (CH2) m-, -CH (R) -N (R) - sau -N (R) -CH2- sau într-adevăr împreună formează o legătură atunci când X reprezintă -CH2-N (R) -CH2-, R3 reprezintă NH2, -NH2, Cy-Ak3-NH2 sau piperidin-4-il, Cy şi Ak3 sunt definiţi ca în descriere, R4 şi R5, identici sau diferiţi, reprezintă fiecare H sau F, izomerii optici ai acestuia şi acidul acceptabil farmaceutic săruri de adiţie ale acestora. Invenţia se referă de asemenea la medicamente care conţin aceleaşi substanţe.

公开(公告)号：PH12018501373A1

公开(公告)日：2019-02-27

申请号：PH12018501373

申请日：2018-06-26

Applicant: SERVIER LAB

Inventor： GLOANEC PHILIPPE ,  SCHAFFNER ARNAUD-PIERRE ,  SANSILVESTRI-MOREL PATRICIA ,  RUPIN ALAIN ,  MENNECIER PHILIPPE ,  VALLEZ MARIE-ODILE

IPC: A61K31/675 ,  A61P9/00 ,  C07F9/6584

Abstract: Compounds of formula (I) in which: Ak1 represents an alkyl chain, X represents -(CH2)m-, -CH(R)-, -N(R)-,-CH2-N(R)-, -N(R)-CH2- or -CH2-N(R)-CH2-, m and R are as defined in the description, R1 and R2 each represent H when X represents -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)- or -N(R)-CH2-, or indeed together form a bond when X represents -CH2-N(R)-CH2-, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yle, Cy and Ak3 are as defined in the description, R4 and R5, identical or different, each represent H or F, the optical isomers of same, and the pharmaceutically acceptable acid addition salts thereof. The invention also relates to drugs containing same.

公开(公告)号：SG11201805757WA

公开(公告)日：2018-08-30

申请号：SG11201805757W

申请日：2017-01-13

Applicant: SERVIER LAB

Inventor： GLOANEC PHILIPPE ,  SCHAFFNER ARNAUD-PIERRE ,  SANSILVESTRI-MOREL PATRICIA ,  RUPIN ALAIN ,  MENNECIER PHILIPPE ,  VALLEZ MARIE-ODILE

IPC: C07F9/6584 ,  A61K31/675 ,  A61P9/00

Abstract: Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.

公开(公告)号：CA3011184A1

公开(公告)日：2017-07-20

申请号：CA3011184

申请日：2017-01-13

Applicant: SERVIER LAB

Inventor： GLOANEC PHILIPPE ,  SCHAFFNER ARNAUD-PIERRE ,  SANSILVESTRI-MOREL PATRICIA ,  RUPIN ALAIN ,  MENNECIER PHILIPPE ,  VALLEZ MARIE-ODILE

IPC: C07F9/6584 ,  A61K31/675 ,  A61P9/00

Abstract: Composés de formule (I) dans laquelle : Ak1 représente une chaîne alkyle, X représente -(CH2)m-, -CH(R)-, -N(R)-,-CH2-N(R)-, N(R)-CH2-ou -CH2-N(R)-CH2-, m et R sont tels que définis dans la description, R1 et R2 représentent chacun H lorsque X représente -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)- ou N(R)-CH2-, ou bien forment ensemble une liaison lorsque X représente -CH2-N(R)-CH2-, R3 représente NH2, Cy-NH2, Cy-Ak3-NH2 ou pipéridin-4-yle, Cy et Ak3 sont tels que définis dans la description, R4 et R5, identiques ou différents, représentent chacun H ou F, leurs isomères optiques, ainsi que leurs sels d'addition à un acide pharmaceutiquement acceptable. Médicaments.