公开(公告)号：EP1446402B1

公开(公告)日：2005-11-02

申请号：EP02793211.0

申请日：2002-11-07

申请人： Aventis Pharma S.A.

发明人： BACQUE, Eric ,  BIGOT, Antony ,  CARRY, Jean-Christophe ,  MIGNANI, Serge

IPC分类号： C07D417/06 ,  C07D277/28 ,  A61K31/427 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/16 ,  C07D333/20 ,  C07D413/06

CPC分类号： C07D239/26 ,  C07D277/28 ,  C07D333/20 ,  C07D413/06 ,  C07D417/06

摘要： The invention concerns the use of 2-amino-4-heteroarylethyl thiazoline derivatives of formula (I), wherein: Het represents a thienyl, pyrimidyl, pyridyl or thiazolyl radical or their pharmaceutically acceptable salts and their use inhibitors of inducible no-synthase

公开(公告)号：EP1824859A1

公开(公告)日：2007-08-29

申请号：EP05822880.0

申请日：2005-11-25

申请人： Aventis Pharma S.A.

发明人： CARRY, Jean-Christophe ,  DOERFLINGER, Gilles, Résidence Les Millepertuis ,  BIGOT, Antony ,  BARBALAT-DAMOUR, Dominique ,  CLERC, François ,  JANIN, Yves ,  BARBERIS, Claude ,  GENEVOIS-BORELLA, Arielle ,  RONAN, Baptiste ,  MINOUX, Hervé

IPC分类号： C07D495/04 ,  A61K31/4162

CPC分类号： C07D495/04

摘要： Products of formula (I), wherein R1 represents R2, NHCO(R2), CH=CH-(R2) and NH-R4 with R2 represents alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkylene, aryl, heteroaryl, arylalkyl and heteroarylalkyl; R3 represents alkyl, alkyl-aryl, alkyl-heteroaryl, -aryl, -heteroaryl; R4 represents aryl, heteroaryl,cycloalkyl, heterocycloalkyl, all of which are optionally substituted; said products being in all forms isomeric and the salts thereof; the preparation thereof; as medicaments acting as inhibitors for kinase proteins; the preparation of hydroxamates that are substituted by condensed heterocycles, a method for the preparation thereof, compositions containing them, and the use thereof as a medicament, particularly as anti canceral agents

公开(公告)号：EP1446393B1

公开(公告)日：2006-03-08

申请号：EP02796839.5

申请日：2002-11-07

申请人： Aventis Pharma S.A.

发明人： BIGOT, Antony ,  CARRY, Jean-Christophe ,  MIGNANI, Serge

IPC分类号： C07D277/18 ,  C07D417/12 ,  C07D417/06 ,  C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/497 ,  A61P25/16 ,  C07D295/13 ,  C07D295/15

CPC分类号： C07D295/13 ,  C07D241/04 ,  C07D277/18 ,  C07D295/15 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The invention concerns the use of 2-amino-thiazoline derivatives of formula (I), wherein: Y is a (CH2) methylene and X is selected among the following groups: O, NH, C1-C4 N-alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a (C=O) carboxy and X is selected among the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, or their pharmaceutically acceptable salts as inhibitors of inducible NO-synthase.

公开(公告)号：EP1450750B1

公开(公告)日：2009-10-21

申请号：EP02793210.2

申请日：2002-11-07

申请人： Aventis Pharma S.A.

发明人： BACQUE, Eric ,  BIGOT, Antony ,  CARRY, Jean-Christophe ,  MIGNANI, Serge ,  RONAN, Baptiste ,  TABART, Michel

IPC分类号： C07D417/06 ,  A61K31/4178

CPC分类号： C07D213/40 ,  C07D213/55 ,  C07D213/64 ,  C07D213/89 ,  C07D417/06 ,  C07F7/1856

摘要： The invention concerns the use of 2-amino-4-pyridylmethyl-thiazoline derivatives of formula (I), wherein: either R1 = R2 = Cl, or C1-C4 alkyl, or hydroxy; or C1-C4 alkoxy or at least one of the two R1 and R2 is hydrogen and the other a C1-C4 alkyl radical, a hydroxy, a C1-C4 alkoxy or a chlorine or their pharmaceutically acceptable salts as inhibitors of inducible NO-synthase.

公开(公告)号：EP1539734A1

公开(公告)日：2005-06-15

申请号：EP03769606.9

申请日：2003-09-10

申请人： Aventis Pharma S.A.

发明人： BACQUE, Eric ,  BIGOT, Antony ,  EL AHMAD, Youssef ,  MALLERON, Jean-Luc ,  MIGNANI, Serge ,  RONAN, Baptiste ,  TABART, Michel ,  VIVIANI, Fabrice

IPC分类号： C07D401/06 ,  A61K31/4709 ,  A61P31/04 ,  C07D409/14 ,  C07D211/60

CPC分类号： C07D401/06 ,  C07D211/60 ,  C07D409/14 ,  Y02P20/55

摘要： The invention concerns piperidine quinolyl derivatives of general formula (I)) wherein: R1a is hydrogen, halogen, hydroxy, amino, alkylamino, dialkylamino, hydroxyamino, alkyloxyamino or alkyl alkyloxy amino and R1b is hydrogen, or R1a and R1b form an oxo; R2 is carboxy, carboxymethyl or hydroxymethyl; R3 is alkyl substituted either by phenylthio optionally substituted by halogen, hydroxy, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxy, alkyloxycarbonyl, cyano or amino, or by cycloalkylthio (3 to 7 members) optionally substituted by halogen or trifluoromethyl, or by heteroarylthio (5 to 6 members and 1 to 4 heteroatoms selected among N, O and S), optionally substituted par halogen, hydroxy, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxy, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl, or heteroaryl such as defined above; R4 is alkyl, alkenyl-CH2- or alkynyl-CH2-, cycloalkyl or cycloalkyl alkyl, in their various separated or mixed isomeric forms, as well as their salts. Said novel derivatives are potent antibacterial agents

公开(公告)号：EP1299103A1

公开(公告)日：2003-04-09

申请号：EP01943579.1

申请日：2001-06-07

申请人： Aventis Pharma S.A.

发明人： CARRY, Jean-Christophe ,  DAMOUR, Dominique ,  GUYON, Claude ,  MIGNANI, Serge ,  BACQUE, Eric ,  BIGOT, Antony

IPC分类号： A61K31/426 ,  A61P25/00 ,  C07D277/18

CPC分类号： C07D277/18

摘要： The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2-ylamine of formula (I) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (I) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved abnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2).

公开(公告)号：EP1611127A2

公开(公告)日：2006-01-04

申请号：EP04742385.0

申请日：2004-03-29

申请人： Aventis Pharma S.A.

发明人： BIGOT, Antony ,  CHEVE, Michel ,  EL AHMAD, Youssef ,  MALLERON, Jean-Luc ,  MARTIN, Jean-Paul ,  MIGNANI, Serge ,  PANTEL, Guy ,  RONAN, Baptiste ,  TABART, Michel ,  VIVIANI, Fabrice

IPC分类号： C07D409/14 ,  C07D401/06 ,  C07D413/06

CPC分类号： C07D401/06 ,  C07D409/14 ,  C07D413/06

摘要： The invention concerns 4-substituted quinoline derivatives active as antimicrobial agents, of general formula (I), wherein: X1, X2, X3, X4 and X5 respectively represent >C-R'1 to >C-R'5, or not more than one represents N; Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being hydrogen or alkyl; m is 1, 2, or 3 and n is 0, 1 or 2; Z is CH2 or Z represents O, S, SO, SO2 and, in that case, n is equal to 2; R2 represents -CO2R, -CH2CO2R, -CH2-CH2CO2R, -CH2OH or -CH2-CH2OH, R being as defined above; R3 represents phenyl, heteroaryl or alk-R°3, wherein alk is an alkyl and R°3 represents various groups, optionally oxygenated, sulphured or aminated, in their enantiomeric or diastereoisomeric forms or mixtures thereof, and optionally in their syn or anti forms or mixtures thereof, as well as their salts.

公开(公告)号：EP1299365B1

公开(公告)日：2005-09-28

申请号：EP01943580.9

申请日：2001-06-07

申请人： Aventis Pharma S.A.

发明人： CARRY, Jean-Christophe ,  DAMOUR, Dominique ,  GUYON, Claude ,  MIGNANI, Serge ,  BIGOT, Antony ,  BACQUE, Eric ,  TABART, Michel

IPC分类号： C07D277/18 ,  C07D417/06 ,  C07D417/12 ,  C07D277/28 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61P25/00 ,  C07D213/38 ,  C07D213/40 ,  C07D333/20 ,  C07D241/12 ,  C07D213/70 ,  C07D213/89 ,  C07C335/06 ,  C07C215/00 ,  C07C229/00 ,  C07C233/00 ,  C07C271/00 ,  C07C333/00

CPC分类号： C07D417/06 ,  A61K31/426 ,  A61K31/4439 ,  C07D277/18 ,  Y02P20/55

摘要： The invention concerns 2-aminithiazoline derivatives of formula (I) wherein: either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, -CH-R3, -CH2-S-R4 or phenyl radical substituted by a nitro or NH-C(=NH)CH3 radical; or R1 is an alkyl radical and R2 is a hydrogen atom; R3 is a cycloalkyl (3-6C), pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl, phenyl or phenyl radical substituted by a nitro, hydroxy or carboxy radical; R4 represents a pyridyl or pyridyl N-oxide radical; alk represents an alkylene radical or their pharmaceutically acceptable salts excluding some known compounds, and the use of said derivatives as inducible NO-synthase inhibitors.

公开(公告)号：EP1299103B1

公开(公告)日：2005-09-28

申请号：EP01943579.1

申请日：2001-06-07

申请人： Aventis Pharma S.A.

发明人： CARRY, Jean-Christophe ,  DAMOUR, Dominique ,  GUYON, Claude ,  MIGNANI, Serge ,  BACQUE, Eric ,  BIGOT, Antony

IPC分类号： A61K31/426 ,  A61P25/00 ,  C07D277/18

CPC分类号： C07D277/18

摘要： The invention concerns pharmaceutical compositions containing as active principle a 4,5-dihydro-1,3-thiazol-2-ylamine of formula (I) wherein: R represents an -alk-S-alk-Ar, phenyl or phenyl radical substituted by alkoxy or halogen or one of its pharmaceutically acceptable salts, the novel derivatives of formula (I) and their preparation. Said compounds are useful for preventing and treating diseases wherein is involved abnormal production of nitrogen monoxide (NO) by induction of inducible NO-synthase (NOS-2).

公开(公告)号：EP1450750A2

公开(公告)日：2004-09-01

申请号：EP02793210.2

申请日：2002-11-07

申请人： Aventis Pharma S.A.

发明人： BACQUE, Eric ,  BIGOT, Antony ,  CARRY, Jean-Christophe ,  MIGNANI, Serge ,  RONAN, Baptiste ,  TABART, Michel

IPC分类号： A61K6/00

CPC分类号： C07D213/40 ,  C07D213/55 ,  C07D213/64 ,  C07D213/89 ,  C07D417/06 ,  C07F7/1856

摘要： The invention concerns the use of 2-amino-4-pyridylmethyl-thiazoline derivatives of formula (I), wherein: either R1 = R2 = Cl, or C1-C4 alkyl, or hydroxy; or C1-C4 alkoxy or at least one of the two R1 and R2 is hydrogen and the other a C1-C4 alkyl radical, a hydroxy, a C1-C4 alkoxy or a chlorine or their pharmaceutically acceptable salts as inhibitors of inducible NO-synthase.