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1.发明授权DERIVES DE 2-AMINOTHIAZOLINE ET LEUR UTILISATION COMME INHIBITEURS DE NO-SYNTHASE 有权2 AMINOTHIAZOLINDERIVATE及其作为NO合酶抑制剂
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.
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2.发明授权DERIVES DE 4,5-DIHYDRO-THIAZOL-2-YLAMINE ET LEUR UTILISATION COMME INHIBITEURS DE NO SYNTHASE 有权4,5-二氢-2- THIAZOLYLAMINDERIVATE及其作为NO合酶抑制剂
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).
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3.发明公开DERIVES DE 2-AMINOTHIAZOLINE ET LEUR UTILISATION COMME INHIBITEURS DE NO-SYNTHASE 有权2 AMINOTHIAZOLINDERIVATE及其作为NO合酶抑制剂
公开(公告)号：EP1299365A1
公开(公告)日：2003-04-09
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.
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公开(公告)号：EP1487803A1
公开(公告)日：2004-12-22
申请号：EP03744395.9
申请日：2003-03-07
申请人： Aventis Pharma S.A.
发明人： DAMOUR, Dominique , CARRY, Jean-Christophe , NEMECEK, Patrick , TERRIER, Corinne , NARDI, Frederico , FILOCHE, Bruno , CHERRIER, Marie-Pierre , BEZARD, Daniel
IPC分类号： C07D231/56 , A61K31/416 , A61P35/00 , C07D409/04 , C07D405/04 , C07D401/04 , C07D471/04 , C07D403/12 , C07D403/04 , C07D401/12 , C07D409/12 , C07D413/12 , C07D413/14
CPC分类号： C07D231/56
摘要： Disclosed are substituted indazoles, compositions containing said substituted indazoles, a production method, and the use thereof. The invention particularly relates to novel specific substituted indazoles having a kinase-inhibiting activity and a therapeutic activity, especially in oncology.
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5.发明授权DERIVES DE 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE ANTAGONISTES DES RECEPTEURS AMPA ET NMDA, LEUR PREPARATION, LEURS INTERMEDIAIRES ET LES MEDICAMENTS LES CONTENANT 失效5H，10H - 咪唑并[1,2-α]茚并[1,2-e]吡嗪将-4-酮衍生物及其NMDA AMPA受体拮抗剂，它们的制备及中间体和药物含有它们
公开(公告)号：EP0880522B1
公开(公告)日：2001-09-19
申请号：EP97900236.7
申请日：1997-01-06
申请人： Aventis Pharma S.A.
发明人： ALOUP, Jean-Claude , BOUQUEREL, Jean , DAMOUR, Dominique , HARDY, Jean-Claude , JIMONET, Patrick , MANFRE, Franco , MIGNANI, Serge , NEMECEK, Patrick
IPC分类号： C07D487/04 , C07D233/90 , A61K31/495 , C07F9/6561 , C07F9/6506
CPC分类号： C07D487/04 , C07F9/6561
摘要： Compounds of formula (I), wherein R is a hydrogen atom or a -COOH, -alk-COOH, -PO3H2, -CH2-PO3H2, or -CH=CH-COOH radical, or a phenyl radical substituted by a carboxy radical, R1 is an alk-CN, -alk-COOH, -alk-Het, alk-PO3H2 or -alk-CO-NH-SO2R2 radical, R2 is an alkyl or phenyl radical, alk is an alkyl radical, Het is a saturated or unsaturated mono- or polycyclic heterocyclic ring containing 1-9 carbon atoms and one or more heteroatoms selected from O, S and N, said heterocyclic ring optionally being substituted by one or more alkyl, phenyl or phenylalkyl radicals, with the proviso that when R is a hydrogen atom or a -COOH or -PO3H2 radical, R1 cannot be -alk-COOH, isomers, racemic mixtures, enantiomers and diastereoisomers thereof, salts thereof, the preparation thereof, intermediates thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites.
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6.发明授权DERIVES DE 5H, 10H-IMIDAZO [1,2-a] INDENO [1,2-e] PYRAZIN-4-ONE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效5H，10H - 咪唑并[1,2-α] [1,2-e]吡嗪将-4-酮衍生物的生产和药物含有它们
公开(公告)号：EP0820455B1
公开(公告)日：2001-10-31
申请号：EP96911018.8
申请日：1996-04-02
申请人： Aventis Pharma S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , HARDY, Jean-Claude , JIMONET, Patrick , MANFRE, Franco , MIGNANI, Serge , NEMECEK, Patrick , RIBEILL, Yves
IPC分类号： C07D487/04 , A61K31/495 , C07D233/90 , C07F9/6561 , C07F9/6506 , A61K31/675
CPC分类号： C07D487/04 , C07D233/90 , C07F9/65066 , C07F9/6561
摘要： Compounds of formula (I), wherein R is a hydrogen atom or a carboxy, alkoxycarbonyl, -CO-NR4R5, -PO3H2 or -CH2OH radical, and R1 is an -alk-NH2, -alk-NH-CO-R3, -alk-COOR4, -alk-CO-NR5R6 or -CO-NH-R7 radical. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
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7.发明公开DERIVES DE 4,5-DIHYDRO-THIAZOL-2-YLAMINE ET LEUR UTILISATION COMME INHIBITEURS DE NO SYNTHASE 有权4,5-二氢-2- THIAZOLYLAMINDERIVATE及其作为NO合酶抑制剂
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).
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8.发明授权DERIVES D'IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZIN-4-ONE ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT 失效咪唑并[1,2-α]茚并[1,2-e]吡嗪将-4-酮衍生物和药物制剂含有它们
公开(公告)号：EP0752992B1
公开(公告)日：2001-05-30
申请号：EP95914404.9
申请日：1995-03-23
申请人： Aventis Pharma S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
IPC分类号： C07D487/04 , A61K31/495
CPC分类号： C07D487/04
摘要： Pharmaceutical compositions containing, as the active principle, compounds of formula (I), wherein R, R1 and R2 are as defined in the description, or salts thereof, the novel compounds of formula (I), and the preparation thereof, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.
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