公开(公告)号：EP2170833B1

公开(公告)日：2011-06-01

申请号：EP08759156.6

申请日：2008-06-11

申请人： Sanofi-Aventis

发明人： HALLAND, Nis ,  NAZARÉ, Marc ,  LINDENSCHMIDT, Andreas ,  ALONSO, Jorge ,  R'KYEK, Omar ,  URMANN, Matthias

IPC分类号： C07D231/56

CPC分类号： C07D231/56

摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

公开(公告)号：EP2240474A1

公开(公告)日：2010-10-20

申请号：EP08864630.2

申请日：2008-12-12

申请人： Sanofi-Aventis

发明人： SCHOENAFINGER, Karl ,  KEIL, Stefanie ,  URMANN, Matthias ,  MATTER, Hans ,  GLIEN, Maike ,  WENDLER, Wolfgang

IPC分类号： C07D417/12 ,  A61K31/4439 ,  A61P3/10 ,  A61P5/50 ,  A61P25/28

CPC分类号： C07D417/12

摘要： The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What is described are compounds of the Formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

公开(公告)号：EP2120923A1

公开(公告)日：2009-11-25

申请号：EP08700981.7

申请日：2008-01-04

申请人： Sanofi-Aventis

发明人： BRUMMERHOP, Harm ,  STENGELIN, Siegfried ,  HEUER, Hubert ,  KILP, Susanne ,  HERLING, Andreas ,  KLABUNDE, Thomas ,  KADEREIT, Dieter ,  URMANN, Matthias

IPC分类号： A61K31/351 ,  A61P3/00

CPC分类号： A61K31/351

摘要： The invention relates to the use of substituted pyranone acid derivatives and their physiologically acceptable salts for producing medicaments for the treatment of metabolic syndrome. The invention also relates to the use of compounds of formula (I), in which the radicals are defined as cited in the description, and their physiologically acceptable salts for producing a medicament for the treatment of metabolic syndrome.

公开(公告)号：EP2044033A1

公开(公告)日：2009-04-08

申请号：EP07764976.2

申请日：2007-06-30

申请人： Sanofi-Aventis

发明人： ALONSO, Jorge ,  LINDENSCHMIDT, Andreas ,  NAZARÉ, Marc ,  HALLAND, Nis ,  RKYEK, Omar ,  URMANN, Matthias

IPC分类号： C07D235/10 ,  C07D235/12 ,  C07D235/08 ,  C07D235/02 ,  C07D487/04

CPC分类号： C07D235/10 ,  C07D235/08 ,  C07D235/16 ,  C07D401/04 ,  C07D471/04

摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein RO; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo-nitroarenes and Λ/-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricitdes and arthropodicides.

公开(公告)号：EP1888567A1

公开(公告)日：2008-02-20

申请号：EP06753510.4

申请日：2006-05-06

申请人： Sanofi-Aventis

发明人： WAGNER, Michael ,  URMANN, Matthias ,  WEHNER, Volkmar ,  LORENZ, Martin ,  BAUER, Armin ,  NAZARÉ, Marc ,  MATTER, Hans

IPC分类号： C07D409/12 ,  A61K31/4535 ,  A61P7/02 ,  C07D409/14 ,  C07D333/38 ,  C07D405/12 ,  C07D211/58 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14

CPC分类号： C07D211/58 ,  C07D333/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14

摘要： The present invention relates to compounds of the Formula (I), in which R1; R2; R3; V; G1 and G2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa, and can in general be applied in conditions in which an undesired activity of factor Xa is present or for the cure or prevention of which an inhibition of factor Xa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

公开(公告)号：EP2288607B1

公开(公告)日：2014-09-24

申请号：EP09772053.6

申请日：2009-05-22

申请人： SANOFI

发明人： KEIL, Stefanie ,  URMANN, Matthias ,  WENDLER, Wolfgang ,  GLIEN, Maike ,  MATTER, Hans ,  MUNSON, Harry, Randall, Jr.

IPC分类号： C07D413/14 ,  A61K31/4439 ,  A61K31/404 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D413/14

公开(公告)号：EP2173716B1

公开(公告)日：2014-03-19

申请号：EP08801470.9

申请日：2008-06-19

申请人： SANOFI

发明人： R'KYEK, Omar ,  NAZARÈ, Marc ,  LINDENSCHMIDT, Andreas ,  ALONSO, Jorge ,  URMANN, Matthias ,  HALLAND, Nis

IPC分类号： C07D213/127 ,  C07D213/26 ,  C07D213/30 ,  C07D215/12 ,  C07D215/14 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D333/24 ,  C07D471/04 ,  C07D333/38 ,  C07D409/06

CPC分类号： C07D231/12 ,  C07D213/127 ,  C07D213/26 ,  C07D213/30 ,  C07D215/12 ,  C07D215/14 ,  C07D231/56 ,  C07D239/26 ,  C07D333/38 ,  C07D409/06 ,  C07D471/04

公开(公告)号：EP2288604A1

公开(公告)日：2011-03-02

申请号：EP09761383.0

申请日：2009-05-22

申请人： Sanofi-Aventis

发明人： KEIL, Stefanie ,  URMANN, Matthias ,  WENDLER, Wolfgang ,  GLIEN, Maike ,  MATTER, Hans ,  FALK, Eugen

IPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04 ,  A61K31/4709 ,  A61K31/4706 ,  A61K31/5365 ,  A61K31/5383 ,  A61K31/436 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

摘要： Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

公开(公告)号：EP2102198A1

公开(公告)日：2009-09-23

申请号：EP07846915.2

申请日：2007-11-30

申请人： Sanofi-Aventis

发明人： KEIL, Stefanie ,  URMANN, Matthias ,  SCHOENAFINGER, Karl ,  WENDLER, Wolfgang ,  GLIEN, Maike ,  SCHAEFER, Hans-Ludwig ,  FALK, Eugen

IPC分类号： C07D413/12 ,  A61K31/4245 ,  A61K31/4725 ,  A61P3/06

CPC分类号： C07D413/12

摘要： The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

公开(公告)号：EP1628972B1

公开(公告)日：2009-04-22

申请号：EP04731155.0

申请日：2004-05-05

申请人： Sanofi-Aventis Deutschland GmbH

发明人： NAZARE, Marc ,  WEHNER, Volkmar ,  LAUX, Volker ,  URMANN, Matthias ,  BAUER, Armin ,  MATTER, Hans

IPC分类号： C07D413/14 ,  C07D401/14 ,  C07D401/12 ,  C07D413/04 ,  A61K31/416 ,  A61P7/02

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14

摘要： The present invention relates to compounds of the formulae (I) and (Ib) wherein R0; R1 ;R2 ;Q; V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae (I) and (Ib), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.