公开(公告)号：EP1912988B1

公开(公告)日：2014-04-16

申请号：EP06794254.0

申请日：2006-08-01

申请人： Aventis Pharma S.A.

发明人： BJERGARDE, Kirsten ,  NAIR, Anil ,  PATEK, Marcel ,  DODSON, Mark ,  ACKERMAN-BERRIER, Martha ,  SMRCINA, Martin ,  LEROY, Vincent ,  BACQUE, Eric ,  TABART, Michel ,  RONAN, Baptiste ,  VIVIANI, Fabrice ,  SOUAILLE, Catherine

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  C07D213/85

CPC分类号： C07D471/04

公开(公告)号：EP1912988A1

公开(公告)日：2008-04-23

申请号：EP06794254.0

申请日：2006-08-01

申请人： Aventis Pharma S.A.

发明人： BJERGARDE, Kirsten ,  NAIR, Anil ,  PATEK, Marcel ,  DODSON, Mark ,  ACKERMAN-BERRIER, Martha ,  SMRCINA, Martin ,  LEROY, Vincent ,  BACQUE, Eric ,  TABART, Michel ,  RONAN, Baptiste ,  VIVIANI, Fabrice ,  SOUAILLE, Catherine

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  C07D213/85

CPC分类号： C07D471/04

摘要： The invention relates to specific novel 7-aza-indazoles having formula (I), which modulate the activity of proteins, particularly kinases, compositions containing same and the use thereof as a medicament, in particular as anticancer agents.

公开(公告)号：EP1599464B1

公开(公告)日：2010-09-22

申请号：EP04705838.3

申请日：2004-01-28

申请人： Aventis Pharma S.A.

发明人： PATEK, Marcel ,  NAIR, Anil ,  HITTINGER, Augustin ,  NEMECEK, Conception ,  BOND, Daniel ,  HARLOW, Greg ,  BOUCHARD, Hervé ,  MAUGER, Jacques ,  MALLERON, Jean-Luc ,  PALERMO, Mark ,  AL-OBEIDI, Fahad ,  FAITG, Thomas ,  STROBEL, Hartmut ,  RUF, Sven ,  RITTER, Kurt ,  EL-AHMAD, Youssef ,  LESUISSE, Dominique ,  BENARD, Didier

IPC分类号： C07D401/06 ,  A61K31/14 ,  A61K31/41 ,  C07D409/14 ,  C07D401/14 ,  C07D401/04 ,  C07D417/14 ,  C07D521/00 ,  C07D413/06 ,  C07D417/06 ,  C07D405/06 ,  C07D403/06

CPC分类号： C07D401/06 ,  C07D401/14

摘要： The invention relates to novel products having formula (I), wherein: p denotes 0 to 2; R and R1 denote O or NH; R2 and R3 denote hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, or R2 and R3, together with the carbon atom to which they are bound, form a carbocyclic or heterocyclic radical, all of said radicals being optionally substituted; A1 denotes a single bond, alkyl, allyl and propynyl; Y and Y1 denote H, OCF3, S(O)nCF3, S(O)nAlk, SO2CHF2, SO2CF2CF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, SF5 and SO2NR5R6, whereby R5 and R6 are selected from among hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl and heteroaryl, which are optionally substituted, or R5 and R6, together with N to which they are bound, form a heterocyclic radical; A2 denotes Al, CO and SO2; B2 denotes a heterocyclic radical which is optionally substituted with one or more substituents which are selected from the values of Y2; Y2 denotes hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -O-alkenyl, -O-alkynyl, O-cycloalkyl, S(O)n-alkyl, -S(O)n-alkenyl, -S(O)n-alkynyl, S(O)n-cycloalkyl, -COOR13,-OCOR13, NR5R6, CONR5R6, S(O)n-NR5R6,-NR10-CO-R13, -NR10-SO2-R13, -NH-SO2-NR5R6, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13, all of said radicals being optionally substituted; and n denotes an integer of between 0 and 2. The aforementioned products are in all the isomeric forms and the salts thereof for use as medicaments.

公开(公告)号：EP1599464A2

公开(公告)日：2005-11-30

申请号：EP04705838.3

申请日：2004-01-28

申请人： Aventis Pharma S.A.

发明人： PATEK, Marcel ,  NAIR, Anil ,  HITTINGER, Augustin ,  NEMECEK, Conception ,  BOND, Daniel ,  HARLOW, Greg ,  BOUCHARD, Hervé ,  MAUGER, Jacques ,  MALLERON, Jean-Luc ,  PALERMO, Mark ,  AL-OBEIDI, Fahad ,  FAITG, Thomas ,  STROBEL, Hartmut ,  RUF, Sven ,  RITTER, Kurt ,  EL-AHMAD, Youssef ,  LESUISSE, Dominique ,  BENARD, Didier

IPC分类号： C07D401/06 ,  A61K31/14 ,  A61K31/41 ,  C07D409/14 ,  C07D401/14 ,  C07D401/04 ,  C07D417/14 ,  C07D521/00 ,  C07D413/06 ,  C07D417/06 ,  C07D405/06 ,  C07D403/06

CPC分类号： C07D401/06 ,  C07D401/14

摘要： The invention relates to novel products having formula (I), wherein: p denotes 0 to 2; R and R1 denote O or NH; R2 and R3 denote hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, or R2 and R3, together with the carbon atom to which they are bound, form a carbocyclic or heterocyclic radical, all of said radicals being optionally substituted; A1 denotes a single bond, alkyl, allyl and propynyl; Y and Y1 denote H, OCF3, S(O)nCF3, S(O)nAlk, SO2CHF2, SO2CF2CF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, SF5 and SO2NR5R6, whereby R5 and R6 are selected from among hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl and heteroaryl, which are optionally substituted, or R5 and R6, together with N to which they are bound, form a heterocyclic radical; A2 denotes Al, CO and SO2; B2 denotes a heterocyclic radical which is optionally substituted with one or more substituents which are selected from the values of Y2; Y2 denotes hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -O-alkenyl, -O-alkynyl, O-cycloalkyl, S(O)n-alkyl, -S(O)n-alkenyl, -S(O)n-alkynyl, S(O)n-cycloalkyl, -COOR13,-OCOR13, NR5R6, CONR5R6, S(O)n-NR5R6,-NR10-CO-R13, -NR10-SO2-R13, -NH-SO2-NR5R6, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13, all of said radicals being optionally substituted; and n denotes an integer of between 0 and 2. The aforementioned products are in all the isomeric forms and the salts thereof for use as medicaments.

公开(公告)号：EP1358171A2

公开(公告)日：2003-11-05

申请号：EP02700386.2

申请日：2002-01-23

申请人： Aventis Pharma S.A.

发明人： DEPREZ, Pierre ,  PATEK, Marcel

IPC分类号： C07D295/12 ,  C07D295/20 ,  C07C275/34 ,  C07C275/42 ,  C07C275/30 ,  C07D407/12 ,  C07C275/28

CPC分类号： C07D295/13 ,  C07C275/24 ,  C07C275/34 ,  C07D407/12 ,  Y02P20/55

摘要： The invention concerns novel products of formula (I) wherein: Y represents oxygen or sulphur; Z represents C=CH2, CH-CH3 or CH2; R1 represents hydrogen, morpholinyl or the radical (II) wherein the two nitrogen atoms are linear or form a cyclic radical; X represents carbonyl, alkylene or alkenylene, linear or branched containing not more than 6 carbon atoms optionally oxygen- or sulphur-interrupted; R4, R5 and R6 represent hydrogen, a nitrogen-protecting, alkyl, cycloalkyl, aryl and arylalkyl group optionally substituted; R2 represents alkyl optionally substituted by aryl, heteroaryl or -NR4R5; R3 represents alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl optionally substituted. Said products are all in the form of isomers and the salts as medicines.