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1. 发明申请

WO1995002601A1 IMIDAZO[1,2-a]PYRAZINE-4-ONE, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译：咪唑并[1,2-a]吡嗪-4-酮，其制备方法和含有其的药物
公开(公告)号：WO1995002601A1
公开(公告)日：1995-01-26
申请号：PCT/FR1994000866
申请日：1994-07-11
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEIL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
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 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 especially NMDA receptor glycine modulation site ligands.
摘要翻译：式（I）化合物，其中R为C = R3，C（R4）R5或CH-R6，R1和R2为氢，卤素，烷基，烷氧基，氨基，酰氨基，-NH-CO-NH-Ar， -N = CH-N（烷基）烷基，硝基，氰基，苯基，咪唑基或SO3H，R3是氧，NOH，NO-烷基-OCOK或CH-R7，R4是烷基，-alk-Het或alk-Ar R5是烷基，-alk-Het或-alk-Ar，或C（R4）R5是环烷基，R6是羟基，烷基，NR8R9，-alk-OH，-alk-NR8R9，-alk-Ar或 - Het中，R 7为羟基，烷基，苯基，-alk-Ar，-alk-Het，NR 10 R 11或杂环，R 8和R 9为烷基，或R 8为氢，R 9为氢或烷基，-COR 12，-CSR 30或 - SO2R13，R10和R11是烷基或环烷基，R12是烷基，环烷基，苯基，-COO-烷基，-CH2-COOX，-CH2-NH2，-NH-alk，-NH-Ar，-NH2或-NH-Het R 13是烷基或苯基，R 30是-NH-alk，-NH-Ar，-NH 2或-NH-Het; 或R为2-咪唑基甲基，R 1和R 2各自为氢原子。式（I）化合物是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，所述受体也称为quisqualate受体。此外，式（I）化合物是非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体。

2. 发明申请

WO1997025328A1 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE DERIVATIVES, PREPARATION THEREOF, INTERMEDIATES THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译： 5H，10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮衍生物，其制备方法，其中间体和包含其的药物
公开(公告)号：WO1997025328A1
公开(公告)日：1997-07-17
申请号：PCT/FR1997000019
申请日：1997-01-06
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , BOUQUEREL, Jean , DAMOUR, Dominique , HARDY, Jean-Claude , JIMONET, Patrick , MANFRE, Marco , MIGNANI, Serge , NEMECEK, Patrick
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
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 alpha -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.
摘要翻译：式（I）的化合物，其中R为氢原子或-COOH，-alk-COOH，-PO3H2，-CH2-PO3H2或-CH = CH-COOH基，或被羧基取代的苯基， R 1是烷基或烷基，烷基或苯基，烷基是烷基，烷基是烷基，烷基或烷基，烷基或苯基，烷基或烷基，烷基或烷基，含有1-9个碳原子和一个或多个选自O，S和N的杂原子的不饱和单环或多环杂环，所述杂环任选被一个或多个烷基，苯基或苯基烷基取代，条件是当R为公开了氢原子或-COOH或-PO 3 H 2基团，R 1不能为-alk COOH，异构体，外消旋混合物，对映体和非对映异构体，其盐，其制备，其中间体和含有所述化合物的药物。式（I）化合物具有有价值的药理学性质，也是也称为quisqualate受体的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体的拮抗剂。此外，式（I）化合物是N-甲基-D-天冬氨酸（NMDA）受体的非竞争性拮抗剂，特别是NMDA受体甘氨酸调节剂位点的配体。

3. 发明申请

WO1995026351A1 1,2,4-TRIAZOLO[4,3-a]PYRAZINE-4-ONE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译： 1,2,4-三唑[4,3-a]吡嗪-4-酮衍生物，其制备方法和含有其的药物
公开(公告)号：WO1995026351A1
公开(公告)日：1995-10-05
申请号：PCT/FR1995000360
申请日：1995-03-23
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
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 same.
摘要翻译：式（I）化合物，其中R，R 1，R 2和R 3如说明书中所定义，其盐，其制备方法和含有其的药物。

4. 发明申请

WO1995026350A1 IMIDAZO(1,2-A)INDENO(1,2-E)PYRAZINE-4-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：咪唑（1,2-A）茚（1,2-E）吡嗪-4-酮衍生物和含有其的药物组合物
公开(公告)号：WO1995026350A1
公开(公告)日：1995-10-05
申请号：PCT/FR1995000358
申请日：1995-03-23
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
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.
摘要翻译：公开了作为活性成分的含有式（I）化合物或其盐，其中R，R 1和R 2如说明书中所定义的式（I）化合物及其制备方法的药物组合物。式（I）化合物具有有价值的药理学性质，并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，所述受体也称为quisqualate受体。此外，式（I）化合物是非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体。

5. 发明申请

WO1996014318A1 SPIRO[HETEROCYCLE-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE]-4'-ONES, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译：螺[咪唑并[咪唑并[1,2-a]茚并[1,2-e]吡嗪] -4'-ONES，其制备方法和含有其的药物
公开(公告)号：WO1996014318A1
公开(公告)日：1996-05-17
申请号：PCT/FR1995001430
申请日：1995-10-30
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/20
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 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 especially NMDA receptor glycine modulation site ligands.
摘要翻译：式（I）化合物，其中R 3和R 4与它们所连接的碳原子一起形成（a）2-或3-吡咯烷环，2-或4-哌啶环或2-氮杂环庚烷所述环任选在氮原子上被烷基取代，-CHO，-COOR11，-CO-alk-COOR6，-CO-alk-NR6R12，-CO-alk-CONR6R8，-CO-COOR6，-CO -CH 2 -O-CH 2 -COOR 6，-CO-CH 2 -S-CH 2 -COOR 6，-CO-CH = CH-COOR 6，-CO-alk，-CO-Ar“-CO-alk-Ar”， - -NH-Ar“，-CO-NH-alk-Ar”，-CO-Het，-CO-烷基-Het，-CO-NH-Het，-CO-NH-烷基-Het，-CO-NH 2， 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或-CO-环烷基，其中环烷基任选被羧基任意地2-取代; 或（b）2-吡咯烷-5-酮环。式（I）化合物具有有用的药理学性质，并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，所述受体也称为quisqualate受体。此外，式（I）化合物是非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体。

6. 发明申请

WO1996002544A1 IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-2-CARBOXYLIC ACID DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译：咪唑并[1,2-a]茚并[1,2-e]吡嗪-2-羧酸衍生物，其制备方法和含有其的药物
公开(公告)号：WO1996002544A1
公开(公告)日：1996-02-01
申请号：PCT/FR1995000951
申请日：1995-07-17
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MIGNANI, Serge , RIBEILL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
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.
摘要翻译：式（I）化合物，其中R，R 1，R 2和R 3如说明书中所定义，其盐，其制备方法和含有所述化合物的药物。

7. 发明申请

WO1995026342A1 5H-INDENO[1,2-b]PYRAZINE-2,3-DIONE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译： 5H-INDENO [1,2-b]吡嗪-2,3-二酮衍生物，其制备方法和含有其的药物
公开(公告)号：WO1995026342A1
公开(公告)日：1995-10-05
申请号：PCT/FR1995000359
申请日：1995-03-23
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , AUDIAU, François , BARREAU, Michel , DAMOUR, Dominique , GENEVOIS-BORELLA, Arielle , JIMONET, Patrick , MAGNANI, Serge , RIBEILL, Yves
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D241/38
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.
摘要翻译：公开了式（I）化合物，其中R，R 1，R 2和R 3如说明书中所定义，其盐，其制备方法和含有其的药物。式（I）化合物具有有价值的药理学性质，并且是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，所述受体也称为quisqualate受体。此外，式（I）化合物是非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体。

8. 发明申请

WO1995002602A1 IMIDAZO(1,2-A)PYRAZIN-4-ONE DERIVATIVES FOR USE AS AMPA AND NMDA RECEPTOR ANTAGONISTS 审中-公开
标题翻译：用作AMPA和NMDA受体拮抗剂的咪达佐（1,2-A）吡嗪-4-酮衍生物
公开(公告)号：WO1995002602A1
公开(公告)日：1995-01-26
申请号：PCT/FR1994000865
申请日：1994-07-11
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , MIGNANI, Serge
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D491/14
CPC分类号： C07D487/14 , C07D491/14 , C07D495/14
摘要： Compounds of formula (I), wherein R is an oxygen or sulphur atom or an NH or N-alk radical, and each of R1 and R2, which are the same or different, is a hydrogen or halogen atom or an alkyl, alkoxy, amino, acylamino, -NH-CO-NH-Ar,-N=CH-N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO3H radical, the preparation thereof, and drugs containing such compounds, are disclosed.
摘要翻译：式（I）的化合物，其中R是氧或硫原子或NH或N-烷基，R 1和R 2各自相同或不同，为氢或卤素原子或烷基，烷氧基，氨基，酰氨基，-NH-CO-NH-Ar，-N = CH-N（alk）alk'，硝基，氰基，苯基，咪唑基或SO3H基，其制备方法和含有这些化合物的药物。

9. 发明申请

WO1997025326A1 2-SUBSTITUTED 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONES, PREPARATION THEREOF AND DRUGS CONTAINING SAME 审中-公开
标题翻译： 2-取代的5H，10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮，其制备方法和含有其的药物
公开(公告)号：WO1997025326A1
公开(公告)日：1997-07-17
申请号：PCT/FR1997000017
申请日：1997-01-06
申请人： RHONE-POULENC RORER S.A. , ALOUP, Jean-Claude , BOUQUEREL, Jean , DAMOUR, Dominique , HARDY, Jean-Claude , MIGNANI, Serge
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07F9/6561
摘要： Compounds of formula (I), wherein R is a -CO-CH2-PO3H2, -CO-NH-tetrazole-5-yl, -CO-NHOH, -CO-NH-NH2, -alk-COOH, -alk-COOalk', -CH2-PO3H2, -CO-NH-SO2-R1 or -CH=CH-COOH radical, or a phenyl radical substituted by a carboxy radical, alk and alk' are an alkyl radical and R1 is an alkyl, trifluoromethyl or phenyl radical optionally substituted by a carboxy or alkoxycarbonyl radical, racemic mixtures, isomers, enantiomers and diastereoisomers thereof, salts thereof, the preparation thereof and drugs containing said compounds, are disclosed.
摘要翻译：式（I）化合物，其中R是-CO-CH 2 -PO 3 H 2，-CO-NH-四唑-5-基，-CO-NHOH，-CO-NH-NH 2，-alk-COOH，-alk COO 或者被羧基取代的苯基，烷基和烷基是烷基，R 1是烷基，三氟甲基或三氟甲基，公开了任选被羧基或烷氧基羰基取代的苯基，其外消旋混合物，异构体，对映体和非对映异构体，其盐，其制备物和含有所述化合物的药物。

10. 发明申请

WO1996031511A1 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZIN-4-ONE DERIVATIVES, PREPARATION THEREOF, AND DRUGS CONTAINING SAID DERIVATIVES 审中-公开
标题翻译： 5H，10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮衍生物，其制备方法和含有所述衍生物的药物
公开(公告)号：WO1996031511A1
公开(公告)日：1996-10-10
申请号：PCT/FR1996000496
申请日：1996-04-02
申请人： RHONE-POULENC RORER S.A. , 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
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D233/90 , C07F9/6506 , 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 alpha -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.
摘要翻译：式（I）的化合物，其中R是氢原子或羧基，烷氧基羰基，-CO-NR4R5，-PO3H2或-CH2OH基，R1是-alk-NH2，-alk-NH-CO-R3，烷基-COOR4，-alk-CO-NR5R6或-CO-NH-R7基团。式（I）化合物具有有价值的药理学性质，也是也称为quisqualate受体的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体的拮抗剂。此外，式（I）化合物是N-甲基-D-天冬氨酸（NMDA）受体的非竞争性拮抗剂，更特别地是NMDA受体甘氨酸调节位点的配体。

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