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1. 发明授权

EP0662971B1 DERIVES DE 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效
标题翻译： 5H，10H - 咪唑并[1,2-α] [1,2-e]吡嗪将-4-酮衍生物，生产和YOU含药物
公开(公告)号：EP0662971B1
公开(公告)日：1998-05-13
申请号：EP93920940.9
申请日：1993-09-28
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge
IPC分类号： C07D487/04 , A61K31/495
CPC分类号： C07D487/04
摘要： Compounds having the formula (I) wherein R and R1, similar or different, represent a hydrogen or halogen atom or a radical alkyl, alkoxy, amino, acylamino, phenylureido, -N=CH-N(R2)R3, nitro, imidazolyl, phenyl, SO3H or cyano; R2 and R3 which may be similar or different, represent each an alkyle radical; the invention also relates to the salts of such compounds, their preparation, intermediates for preparing them and drugs containing them.

2. 发明公开

EP0752988A1 DERIVES DE 5H-INDENO[1,2-b]PYRAZINE-2,3-DIONE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效转让
标题翻译： 5H茚并[1,2-B]吡嗪-2,3-二酮衍生物，生产和药物含有它们
公开(公告)号：EP0752988A1
公开(公告)日：1997-01-15
申请号：EP95914405.0
申请日：1995-03-23
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MAGNANI, Serge , RIBEILL, Yves
IPC分类号： C07D241 , A61K31 , A61P3 , A61P9 , A61P25 , A61P29 , A61P39 , C07D487
CPC分类号： C07D241/38 , C07D487/04
摘要： Compounds of formula (I), wherein R, R1, R2 and R3 are as defined in the description, salts thereof, the preparation thereof and drugs containing same, 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.

3. 发明公开

EP0726900A1 7H-IMIDAZO(1,2-a)PYRAZINE-8-ONE ANTAGONISTES DU RECEPTEUR NMDA 失效
标题翻译： 7H-IMIDIZO-¬1,2-吡嗪-8-酮衍生物作为NMDA受体拮抗剂
公开(公告)号：EP0726900A1
公开(公告)日：1996-08-21
申请号：EP95900182.0
申请日：1994-11-02
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge
IPC分类号： A61K31 , A61P9 , C07D487
CPC分类号： C07D487/04
摘要： Drugs containing as the active ingredient at least one compound of formula (I), wherein R1 represents a hydrogen atom or an alkyl or phenyl radical, R2 represents (a) a phenyl radical, (b) a phenyl radical substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, phenyl, nitro or cyano radicals, (c) a naphthyl radical, (d) a naphthyl radical substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, phenyl, nitro or cyano radicals, (e) a 2-,3- or 4-pyridyl radical, (f) a 2-, 3- or 4-pyridiyl radical substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, phenyl, nitro or cyano radicals, (g) a 2- or 3-furyl radical, (h) a 2- or 3-furyl radical substituted by one or several substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, polyfluoroalkoxy, phenyl, nitro or cyano radicals or a salt of such a compound. The invention concerns the novel compounds of formula (I) and their preparation.

4. 发明授权

EP0752988B1 DERIVES DE 5H-INDENO[1,2-b]PYRAZINE-2,3-DIONE ANTAGONISTES DES RECEPTEURS AMPA ET NMDA 失效转让
标题翻译： -5H-茚并[1,2-B]的AMPA和NMDA受体的吡嗪-2,3-二酮衍生物拮抗剂
公开(公告)号：EP0752988B1
公开(公告)日：1999-05-26
申请号：EP95914405.6
申请日：1995-03-23
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MAGNANI, Serge , RIBEILL, Yves
IPC分类号： C07D241/38 , C07D487/04 , A61K31/495
CPC分类号： C07D241/38 , C07D487/04
摘要： Compounds of formula (I), wherein R, R1, R2 and R3 are as defined in the description, salts thereof, the preparation thereof and drugs containing same, 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.

5. 发明公开

EP0880522A1 DERIVES DE 5H,10H-IMIDAZO(1,2-a)INDENO(1,2-e)PYRAZINE-4-ONE, LEUR PREPARATION, LEURS INTERMEDIAIRES ET LES MEDICAMENTS LES CO NTENANT 失效
标题翻译： 5H，10H咪唑并（1,2-A）茚并（1,2-e）中吡嗪-4-酮衍生物，它们的生产和中间体及其药用Dieze ENTHATENDE
公开(公告)号：EP0880522A1
公开(公告)日：1998-12-02
申请号：EP97900236.0
申请日：1997-01-06
申请人： RHONE-POULENC RORER 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： A61K31 , A61P1 , A61P25 , A61P29 , A61P43 , C07D233 , C07D235 , C07D487 , C07F9
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.

6. 发明公开

EP0772615A1 DERIVES D'ACIDE IMIDAZO 1,2-a]INDENO 1,2-e]PYRAZINE-2-CARBOXYLIQUE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效转让
标题翻译：咪唑并[1,2-α]茚并[1,2-E]吡嗪-2-羧酸衍生物，它们的生产和药物含有它们
公开(公告)号：EP0772615A1
公开(公告)日：1997-05-14
申请号：EP95925891.0
申请日：1995-07-17
申请人： RHONE-POULENC RORER 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： A61K31 , A61P9 , A61P25 , A61P29 , A61P31 , A61P39 , A61P43 , C07D487
CPC分类号： C07D487/04
摘要： Compounds of formula (I), wherein R, R1, R2 and R3 are as defined in the description, salts thereof, preparation thereof and drugs containing said compounds.

7. 发明公开

EP0789699A1 SPIRO HETEROCYCLE-IMIDAZO(1,2-a]INDENO(1,2-e]PYRAZINE]-4'-ONES, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效转让
标题翻译：螺[HETEROZYCLISCHE咪唑并[1,2-α]茚并[1,2-e]吡嗪将）-4'- ONE，它们的生产和药物含有它们
公开(公告)号：EP0789699A1
公开(公告)日：1997-08-20
申请号：EP95936624.0
申请日：1995-10-30
申请人： RHONE-POULENC RORER 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 , A61K31 , A61P9 , A61P11 , A61P25 , A61P43 , C07D471
CPC分类号： C07D471/20 , C07D487/20
摘要： Compounds of formula (I), wherein R3 and R4, taken together with the carbon atom to which they are attached, form (a) a 2- or 3-pyrrolidine ring, a 2- or 4-piperidine ring or a 2-azacycloheptane ring, said rings being optionally substituted at the nitrogen atom by an alkyl radical, -CHO, -COOR11, -CO-alk-COOR6, -CO-alk-NR6R12, -CO-alk-CONR6R8, -CO-COOR6, -CO-CH2-O-CH2-COOR6, -CO-CH2-S-CH2-COOR6, -CO-CH=CH-COOR6, -CO-alk, -CO-Ar'. -CO-alk-Ar', -CO-NH-Ar', -CO-NH-alk-Ar', -CO-Het, -CO-alk-Het, -CO-NH-Het, -CO-NH-alk-Het, -CO-NH2, -CO-NH-alk, -CO-N(alk)alk', -CS-NH2, -CS-NH-alk, -CS-NH-Ar', -CS-NH-Het, -alk-Het, -alk-NR6R8, -alk-COOR6, -alk-CO-NR6R8, -alk-Ar', -SO2-alk, -SO2-Ar or -CO-cycloalkyl, where the cycloalkyl is optionally 2-substituted by a carboxy radical; or (b) a 2-pyrrolidine-5-one ring. The compounds of formula (I) have useful pharmacological properties and are α-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 especially NMDA receptor glycine modulation site ligands.

8. 发明公开

EP0708774A1 DERIVES D'IMIDAZO [1,2-a]PYRAZIN-4-ONE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效
标题翻译：咪唑并[1,2-α]吡嗪-4-酮衍生物，生产和THIS ENTHATENDE DRUGS
公开(公告)号：EP0708774A1
公开(公告)日：1996-05-01
申请号：EP94922904.0
申请日：1994-07-11
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
IPC分类号： A61K31 , A61P3 , A61P9 , A61P25 , A61P29 , C07D487
CPC分类号： C07D487/04
摘要： Compounds of formula (I), wherein either R is C=R3, C(R4)R5 or CH-R6, R1 and R2 are hydrogen, halogen, alkyl, alkoxy, amino, acylamino, -NH-CO-NH-Ar, -N=CH-N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO3H, R3 is oxygen, NOH, NO-alk-COOK or CH-R7, R4 is alkyl, -alk-Het or alk-Ar, R5 is alkyl, -alk-Het or -alk-Ar, or C(R4)R5 is cycloalkyl, R6 is hydroxy, alkyl, NR8R9, -alk-OH,-alk-NR8R9, -alk-Ar or -alk-Het, R7 is hydroxy, alkyl, phenyl, -alk-Ar, -alk-Het, NR10R11 or a heterocyclic ring, R8 and R9 are alkyl, or R8 is hydrogen and R9 is hydrogen or alkyl, -COR12, -CSR30 or -SO2R13, R10 and R11 are alkyl or cycloalkyl, R12 is alkyl, cycloalkyl, phenyl, -COO-alk, -CH2-COOX, -CH2-NH2, -NH-alk, -NH-Ar, -NH2 or -NH-Het, R13 is alkyl or phenyl, R30 is -NH-alk, -NH-Ar, -NH2 or -NH-Het; or R is a 2-imidazolylmethyl radical and each of R1 and R2 is a hydrogen atom. The compounds of formula (I) are α-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 especially NMDA receptor glycine modulation site ligands.

9. 发明公开

EP0662971A1 DERIVES DE 5H,10H-IMIDAZO 1,2-a]INDENO 1,2-e]PYRAZINE-4-ONE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效
标题翻译： 5H，10H咪唑并（1,2-A）茚并（1,2-D）吡嗪-4-酮衍生物，生产和YOU含药物。
公开(公告)号：EP0662971A1
公开(公告)日：1995-07-19
申请号：EP93920940.0
申请日：1993-09-28
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge
IPC分类号： A61K31 , A61P9 , A61P25 , C07D487
CPC分类号： C07D487/04
摘要： Compounds having the formula (I) wherein R and R1, similar or different, represent a hydrogen or halogen atom or a radical alkyl, alkoxy, amino, acylamino, phenylureido, -N=CH-N(R2)R3, nitro, imidazolyl, phenyl, SO3H or cyano; R2 and R3 which may be similar or different, represent each an alkyle radical; the invention also relates to the salts of such compounds, their preparation, intermediates for preparing them and drugs containing them.

10. 发明公开

EP0636124A1 DERIVES D'ACIDE 3,4-DIHYDRO-2H-1,2,4-BENZOTHIADIAZINE 1,1-DIOXYDE-3-CARBOXYLIQUE, LEUR PREPARATION ET LES MEDICAMENTS LES CONTENANT 失效
标题翻译： 3,4-二氢-2H-1,2,4-苯并噻二嗪1,1-二氧化物-3- CARBO酸衍生物，及其制备方法和含有coorperation。
公开(公告)号：EP0636124A1
公开(公告)日：1995-02-01
申请号：EP93909013.0
申请日：1993-04-09
申请人： RHONE-POULENC RORER S.A.
发明人： ALOUP, Jean-Claude , AUDIAU, François , DAMOUR, Dominique , JIMONET, Patrick , MIGNANI, Serge
IPC分类号： A61K31 , A61P1 , A61P3 , A61P9 , A61P21 , A61P25 , A61P31 , A61P43 , C07D285 , C07D417 , C07D513
CPC分类号： C07D417/04 , C07D285/24 , C07D417/06 , C07D513/06
摘要： Compounds of formula (I), wherein R is (a) a hydrogen atom, (b) an alkyl radical, (c) an allyl radical, (d) a phenyl radical, (e) a 2-or-3-pyridyl alkyl radical, (f) a 2-quinolylalkyl radical, (g) a naphthylalkyl radical, (h) a cycloalkylalkyl radical, (i) a 2H-3-naphtho[1,8-cd]isothiazol-2-yl-1,1-dioxide)alkyl radical, (j) a (5,6-dihydro 1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolyl-2,2-dioxide)alkyl, (k) an -alk-CO-R5 radical, (l) an -alk-R6-R7 radical, (m) a 4-phenylpirerazinyl-alkyl radical wherein the phenyl nucleus is optionally substituted by one or more substituents selected from halogen atoms and alkyl or alkoxy radicals, (n) a 10-phenothiazinylalkyl radical (o) a (10-alkyl-2-phenothiazinyl)alkyl radical, (p) a 3-indolylalkyl radical, (q) a phenylalkyloxy radical, (r) a 1-phenylalkyl-4-piperidyl radical, (s) a 2-thienylalkyl radical, or (t) a phenylalkyl radical wherein the phenyl is unsubstituted or substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy, polyfluoroalkyl, amino, nitro, cyano, phenyl, vinyl, polyfluoroalkoxy, alkoxycarbonyl, carboxy, phenylalkyloxy, phenylalkyl, benzoylamino, phenylcarbonyl and phenoxy radicals in which the phenyl nucleus is optionally substituted by one or more substituents selected from halogen atoms and alkyl, alkoxy or polyfluoroalkyl radicals; R1 is a carboxy, alkoxycarbonyl, tetrazolyl, -CO-NH2, -CO-NH-alk, -CO-N(alk)2, -CO-NHOH, -CO-N(alk)OH, -CO-NH-O-R8, -CO-N(alk)-OR8 or a group which is convertible in vivo into a carboxy radical; each of R2, R3 and R4, which are the same or different, is a hydrogen or halogen atom or an alkyl or alkoxy radical; R5 is a hydroxy, alkoxy, phenyl or -NR9R10 radical; R6 is an oxygen, sulphur or nitrogen atom or a SO, SO2 or -N-alk radical, R7 is an alkyl, phenylalkyl or phenyl radical optionally substituted by one or more hydrogen atoms; R8 is an alkyl or phenylalkyl radical; each of R9 and R10, which are the same or different, is a hydrogen atom or an alkyl or phenyl radical; and alk is an alkyl or alkylene radical, salts thereof; preparation thereof; and drugs containing same.

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