公开(公告)号：EP2089374A2

公开(公告)日：2009-08-19

申请号：EP07870250.3

申请日：2007-11-06

申请人： Pierre Fabre Medicament

发明人： VACHER, Bernard ,  BRUNEL, Yves ,  MAUREL, Jean-Louis

IPC分类号： C07D327/02 ,  C07C323/20

CPC分类号： C07D327/02 ,  C07B2200/07 ,  C07C319/20 ,  C07C323/20

摘要： The invention relates to a new method for preparing N- [3- [ (2-methoxyphényl) sulfanyl] -2-methylpropyl] -3,4- dihydro-2H-1, 5-benzoxathiepin-3-amine.

公开(公告)号：EP1313737B1

公开(公告)日：2009-06-03

申请号：EP01956555.5

申请日：2001-07-23

申请人： Aventis Pharma Deutschland GmbH ,  Genentech, Inc.

发明人： PEYMAN, Anushirwan ,  WILL, David ,  GADEK, Thomas, R. ,  McDOWELL, Robert ,  GOURVEST, Jean-François ,  RUXER, Jean-Marie ,  KNOLLE, Jochen

IPC分类号： C07D473/34 ,  C07D487/04 ,  A61K31/52 ,  A61P19/10

CPC分类号： C07D473/00 ,  C07D487/04

摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R?1, R2, R3¿, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them.

公开(公告)号：EP1996570A1

公开(公告)日：2008-12-03

申请号：EP07731168.6

申请日：2007-03-08

申请人： Pierre Fabre Médicament S.A.

发明人： VACHER, Bernard ,  CUISIAT, Stéphane ,  ROQUES, Nicolas

IPC分类号： C07D307/86 ,  C07D307/94 ,  C07D317/20 ,  C07C47/548

CPC分类号： C07C47/548 ,  C07C45/59 ,  C07D307/86 ,  C07D307/94 ,  C07D317/20

摘要： ABSTRACT. PROCESS FOR PREPARING [2-(2,3-DIHYDROBENZOFURAN- OR BENZOFURAN-7-YLOXY)ETHYL]-(3-CYCLOPENT-1-YLBENZYL)AMINE DERIVATIVES AND SYNTHESIS INTERMEDIATE The invention relates to a process for preparing compounds of general formula (see “abstract” paper version) in which: - (a) is a single or double bond; - W is a CH, CH2, CHCH3, CCH3 or C(CH3)2 group or a C(CH2)2 group (i.e. a carbon atom bearing two methylene groups linked to one another so as to form a spirocyclopropane unit), with the proviso, however, that, when (a) is a double bond, then W is exclusively a CH or CCH3 group and that, when (a) is a single bond, then W is exclusively a CH2, CHCH3, C(CH3)2 or C(CH2)2 group.

公开(公告)号：EP1965749A1

公开(公告)日：2008-09-10

申请号：EP06847141.6

申请日：2006-12-26

申请人： PIERRE FABRE MEDICAMENT

发明人： SOURNAC, Michel ,  BOUGARET, Joel

IPC分类号： A61J1/00 ,  B65D81/26 ,  A61K31/568

CPC分类号： A61K9/7023 ,  A61K31/568

摘要： The invention relates to chemically stabilising testosterone contained in self-adhesive transdermal devices by associating a desiccant agent with the device in a sealed package. The use of said desiccant agent makes it possible to limit the testosterone chemical degradation into androstenedione and other impurities, thereby enabling said device to be preserved during thirty six months.

公开(公告)号：EP1651677A2

公开(公告)日：2006-05-03

申请号：EP04785991.3

申请日：2004-07-22

申请人： Aventis Pharma S.A.

发明人： LAUX, Volker ,  MOURIER, Pierre ,  VISKOV, Christian

IPC分类号： C08B37/10 ,  A61K31/727

CPC分类号： C08B37/0078 ,  A61K31/727

摘要： The present invention relates to heparin-derived oligosaccharide mixtures, having an average molecular weight from 1,800 to 2,400 daltons and characterized by a high aXa activity and by the absence of aIIa activity. Said invention also relates to the preparation method thereof and to the pharmaceutical compositions containing said mixtures.

公开(公告)号：EP1587500A2

公开(公告)日：2005-10-26

申请号：EP03799644.4

申请日：2003-12-19

申请人： Aventis Pharma S.A.

发明人： CHACORNAC, Isabelle ,  PROBECK, Patricia

IPC分类号： A61K9/16 ,  B01J2/00

CPC分类号： B01J2/04 ,  A61K9/1617 ,  A61K9/1694

摘要： The invention relates to a compound for oral dosage of active substances having a bitter taste which comprises from 15 to 30 % of an active substance mixed with 60 to 80 % of glycerol ester or fat acid, eventually added with wax, and added with a surface active agent and is produced by a spray-cooling method making it possible to obtain granulometry of less than 350 νm.

公开(公告)号：EP1582531A1

公开(公告)日：2005-10-05

申请号：EP04290791.5

申请日：2004-03-24

申请人： Aventis Pharma S.A.

发明人： Mourier, Pierre ,  Viskov, Christian

IPC分类号： C08B37/10 ,  C07H3/06 ,  C12Q1/527

CPC分类号： C08B37/0078 ,  Y10T436/143333

摘要： The invention provides a process for preparing heparin products with a reduced content of glycoserine. A method for detecting glycoserine in preparations of heparin is also provided.

公开(公告)号：EP1578714A1

公开(公告)日：2005-09-28

申请号：EP03799643.6

申请日：2003-12-19

申请人： Aventis Pharma S.A.

发明人： CROCQ-STUERGA, Véronique ,  ROUSSEL, Patrick

IPC分类号： C07C55/08

CPC分类号： C12P7/40 ,  C07B2200/07 ,  C07C51/09 ,  C07C53/19 ,  C07C59/01 ,  C07C69/34 ,  C07C69/63 ,  C12P7/62

摘要： The invention relates to a chiral compound of a formula (I), wherein R1 is hydroxyl or a carboxy activator group and R2 is alkyl eventually substituted by halogen or benzyl. The preparation and the use of the inventive compound for synthesis of 2-bromomethyl-2-ethyl hexanoic chiral acid and the novel intermediate chemicals are also disclosed.

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).