Patent number: 8048893
Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
Type:
Grant
Filed:
February 27, 2009
Date of Patent:
November 1, 2011
Assignee:
Aventis Pharma SA
Inventors:
Arielle Genevois-Borella, Jean-Luc Malleron, Jean Bouquerel, Gilles Doerflinger, Andrees Bohme, Gaetan Touyer, Jean-Francois Sabuco, Corrine Terrier, Serge Mignani, Michel Evers, Youssef El-Ahmad
Publication number: 20090170833
Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
Type:
Application
Filed:
February 27, 2009
Publication date:
July 2, 2009
Applicant:
Aventis Pharma S.A.
Inventors:
Arielle GENEVOIS-BORELLA, Jean-Luc MALLERON, Jean BOUQUEREL, Gilles DOERFLINGER, Andrees BOHME, Gaetan TOUYER, Jean-Francois SABUCO, Corrine TERRIER, Serge MIGNANI, Michel EVERS, Youssef EL-AHMAD
Patent number: 7524838
Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
Type:
Grant
Filed:
November 24, 2004
Date of Patent:
April 28, 2009
Assignee:
Aventis Pharma S.A.
Inventors:
Arielle Genevois-Borella, Jean-Luc Malleron, Jean Bouquerel, Gilles Doerflinger, Andrees Bohme, Gaetan Touyer, Jean-Francois Sabuco, Corrine Terrier, Serge Mignani, Michel Evers, Youssef El-Ahmad
Patent number: 7232834
Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them.
Type:
Grant
Filed:
September 10, 2003
Date of Patent:
June 19, 2007
Assignee:
Novexel SA
Inventors:
Eric Bacque, Antony Bigot, Youssef El Ahmad, Jean-Luc Malleron, Serge Mignani, Baptiste Ronan, Michel Tabart, Fabrice Viviani
Patent number: 7232833
Abstract: The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 is C—R?1, to C—R?5 respectively, or alternatively at most one represents N, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH2 or Z is O, S, SO, SO2 and, in this case, n is equal to 2, R2 is —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CH2OH or —CH2—CH2OH, wherein R is as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.
Type:
Grant
Filed:
March 26, 2004
Date of Patent:
June 19, 2007
Assignee:
Novexel
Inventors:
Antony Bigot, Youssef El-Ahmad, Jean-Luc Malleron, Jean-Paul Martin, Serge Mignani, Guy Pantel, Baptiste Ronan, Michel Tabart, Michel Cheve, Fabrice Viviani
Publication number: 20050165005
Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
Type:
Application
Filed:
November 24, 2004
Publication date:
July 28, 2005
Applicant:
Aventis Pharma S.A.
Inventors:
Arielle Genevois-Borella, Jean-Luc Malleron, Jean Bouquerel, Gilles Doerflinger, Andrees Bohme, Gaetan Touyer, Jean-Francois Sabuco, Corrine Terrier, Serge Mignani, Michel Evers, Youssef El-Ahmad
Patent number: 6841562
Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their p
Type:
Grant
Filed:
September 10, 2003
Date of Patent:
January 11, 2005
Assignee:
Aventis Pharma S.A.
Inventors:
Eric Bacqué, Antony Bigot, Youssef El Ahmad, Jean-Luc Malleron, Serge Mignani, Baptiste Ronan, Michel Tabart, Fabrice Viviani