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1. 发明授权

US06448241B1 Thiazolobenzoheterocycles, their preparation and medicaments containing them 失效
标题翻译：噻唑环杂环，它们的制备和含有它们的药物
公开(公告)号：US06448241B1
公开(公告)日：2002-09-10
申请号：US09863403
申请日：2001-05-24
申请人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
发明人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
IPC分类号： C07D49806
CPC分类号： C07D513/06 , C07D517/06 , C07D517/08
摘要： Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.
摘要翻译：讨论式（I）化合物：其外消旋物，对映体，非对映异构体和无机酸盐及其有机酸盐，其制备方法和含有它们的药物。

2. 发明授权

US06100264A 5H, 10H-imidazo [1,2-A] indeno [1,2-E] pyrazin-4-one derivatives, their preparation, their intermediates and medicaments containing them 失效
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，其中间体和含有它们的药物
公开(公告)号：US06100264A
公开(公告)日：2000-08-08
申请号：US352216
申请日：1999-07-13
申请人： Jean-Claude Aloup , Jean Bouquerel , Dominique Damour , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek
发明人： Jean-Claude Aloup , Jean Bouquerel , Dominique Damour , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4985 , A61K31/675 , A61P1/00 , A61P1/14 , A61P25/00 , A61P29/00 , A61P43/00 , C07D233/90 , C07D235/00 , C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： A compound of the formula ##STR1## in which Ra represents an -alk-COOalk' radical, a --CH.sub.2 --PO(Oalk).sub.2 radical, a --CH.dbd.CH--COOalk' radical or a phenyl radical substituted with an alkoxycarbonyl radical.
摘要翻译：下式的化合物，其中Ra表示-alk-COOalk'基，-CH2-PO（Oalk）2基，-CH = CH-COOalk'基或被烷氧基羰基取代的苯基。

3. 发明授权

US6057454A 1-oxo-1H-inden-2-yl-1H-imidazole-2-carboxylic acid intermediates 失效
标题翻译： 1-氧代-1H-茚-2-基-1H-咪唑-2-羧酸中间体
公开(公告)号：US6057454A
公开(公告)日：2000-05-02
申请号：US205689
申请日：1998-12-04
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
IPC分类号： A61K31/495 , A61P1/14 , A61P3/00 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00 , C07D233/90 , C07D487/04 , C07F9/6506 , C07F9/6561 , C07D401/10 , C07D413/10 , C07D403/10
CPC分类号： C07D487/04 , C07D233/90 , C07F9/65066 , C07F9/6561
摘要： A compound of formula (II): ##STR1## in which R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (II) can be used to prepare compounds of formula (I): ##STR2## in which R and R.sub.1 have the same meanings as above. 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. The compounds of formula (I) are also 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（II）的化合物：其中R是氢原子或羧基，烷氧基羰基，-CO-NR4R5，-PO3H2或-CH2OH基团，R1是-alk-NH2，-alk-NH-CO-R3 ，-alk-COOR 4，-alk-CO-NR 5 R 6或-CO-NH-R 7基团。式（II）化合物可用于制备式（I）的化合物：其中R和R 1具有与上述相同的含义。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）受体的拮抗剂，也称为quisqualate受体。式（I）化合物也是N-甲基-D-天冬氨酸（NMDA）受体的非竞争性拮抗剂，更具体地是NMDA受体甘氨酸调节位点的配体。

4. 发明授权

US5990108A 5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives, preparation thereof, intermediates thereof and drugs containing the same 失效
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，其中间体和含有它们的药物
公开(公告)号：US5990108A
公开(公告)日：1999-11-23
申请号：US101428
申请日：1998-07-09
申请人： Jean-Claude Aloup , Jean Bouquerel , Dominique Damour , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek
发明人： Jean-Claude Aloup , Jean Bouquerel , Dominique Damour , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4985 , A61K31/675 , A61P1/00 , A61P1/14 , A61P25/00 , A61P29/00 , A61P43/00 , C07D233/90 , C07D235/00 , C07D487/04 , C07F9/6561
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, --PO.sub.3 H.sub.2, --CH.sub.2 --PO.sub.3 H.sub.2, or --CH.dbd.CH--COOH radical, or a phenyl radical substituted by a carboxy radical, R.sub.1 is an alk-CN, -alk-COOH, -alk-Het, alk-PO.sub.3 H.sub.2 or -alk-CO--NH--SO.sub.2 R.sub.2 radical, R.sub.2 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 --PO.sub.3 H.sub.2 radical, R.sub.1 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. ##STR1##
摘要翻译： PCT No.PCT / FR97 / 00019 Sec。 371日期：1998年7月9日 102（e）日期1998年7月9日PCT 1997年1月6日PCT PCT。出版物WO97 / 25328 日期：1997年7月17日式（I）化合物其中R为氢原子或-COOH，-alk-COOH，-PO3H2，-CH2-PO3H2或-CH = CH-COOH基，或苯基取代通过羧基，R 1是烷基-C CN，-alk-COOH，-alk-Het，alk-PO 3 H 2或-alk -CO-NH-SO 2 R 2基团，R 2是烷基或苯基， Het是含有1-9个碳原子和一个或多个选自O，S和N的杂原子的饱和或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，其中条件是当R是氢原子或-COOH或-PO 3 H 2基团时，R 1不能是-alk COOH，其异构体，外消旋混合物，对映异构体和非对映异构体，其盐，其制备，其中间体和含有所述化合物的药物，被披露。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。

5. 发明授权

US4994470A Benzopyran derivatives and pharmaceutical compositions containing them 失效
标题翻译：苯并吡喃衍生物和含有它们的药物组合物
公开(公告)号：US4994470A
公开(公告)日：1991-02-19
申请号：US465448
申请日：1990-01-16
申请人： Michel Barreau , Jean-Claude Hardy , Christian Renault
发明人： Michel Barreau , Jean-Claude Hardy , Christian Renault
IPC分类号： A61K31/443 , A61K31/445 , A61P9/06 , C07D405/06 , C07D405/14
CPC分类号： C07D405/06
摘要： New benzopyran derivatives of general formula (I) in which:R.sub.1 denotes a hydrogen or halogen atom or a hydroxy, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, or acylamino radical,R denotes a radical of general formula: ##STR1## in which A denotes a single bond or a methylene radical and R.sub.2 and R.sub.3 which may be identical or different, denote a hydrogen or halogen atom or a hydroxy, alkyl, alkyloxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano radical, or form together, when they are adjacent, a methylenedioxy or ethylenedioxy radical, or alternatively R denotes a 2-oxo-2H-benzimidazolyl radical,and R' and R" are identical and denote hydrogen atoms or alkyl radicals, their isomeric forms and their preparation.These new products are useful as antiarrhythmic and antifibrillating agents. ##STR2##
摘要翻译：新的通式（I）的苯并吡喃衍生物，其中：R1表示氢或卤素原子或羟基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基或酰基氨基，R表示通式的基团： IMAGE>其中A表示单键或亚甲基，R 2和R 3可以相同或不同，表示氢或卤素原子或羟基，烷基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基，酰基氨基，氨磺酰基或氰基，或者当它们相邻时一起形成亚甲二氧基或亚乙二氧基，或者R表示2-氧代-2H-苯并咪唑基，R'和R“相同且表示氢原子或烷基，它们的异构形式及其制备方法。这些新产品可用作抗心律不齐和抗纤颤剂。（一）

6. 发明授权

US4977166A Benzopyran derivatives and pharmaceutical compositions containing them 失效
标题翻译：苯并吡喃衍生物和含有它们的药物组合物
公开(公告)号：US4977166A
公开(公告)日：1990-12-11
申请号：US327093
申请日：1989-03-22
申请人： Jean-Claude Hardy , Christian Renault
发明人： Jean-Claude Hardy , Christian Renault
IPC分类号： A61K31/35 , A61K31/352 , A61K31/443 , A61K31/445 , A61K31/495 , A61P9/06 , C07D311/58 , C07D401/06 , C07D405/06 , C07D407/12
CPC分类号： C07D401/06 , C07D311/58 , C07D407/12
摘要： New benzopyran derivatives of formula: ##STR1## in which R.sub.1 is hydrogen, halogen, hydroxy, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl) amino or acylamino,X is nitrogen or a >CH-radicalR is a radical of formula: ##STR2## in which A denotes a single bond or methylene or, when X is nitrogen, A may denote carbonyl, and R.sub.2 and R.sub.3, which are identical or different, are hydrogen, halogen, hydroxy, alkyl, alkoxy, nitro, amino, alkylsulphonamido, bis(alkylsulphonyl)amino, acylamino, sulphamoyl or cyano, or, when they are adjacent, together form a methylenedioxy or ethylenedioxy radical, or elseR is pyridyl or 2(2H)-benzimidazolonyl if X denotes >CH--, andR' and R" are identical and are hydrogen or alkyl, their isomeric forms and mixtures thereof, and their acid addition salts, can be used as antiarrhythmic and antifibrillation agents.
摘要翻译：新的苯并吡喃衍生物，其中R 1是氢，卤素，羟基，烷氧基，硝基，氨基，烷基磺酰胺基，双（烷基磺酰基）氨基或酰基氨基，X是氮或者CH-基R是式式中：A表示单键或亚甲基的基团，或当X为氮时，A可以表示羰基，并且相同或不同的R 2和R 3为氢，卤素，羟基，烷基，烷氧基，硝基，氨基，烷基磺酰氨基，双（烷基磺酰基）氨基，酰氨基，氨磺酰基或氰基，或当它们相邻时一起形成亚甲二氧基或亚乙二氧基，或者如果X表示> CH，则R是吡啶基或2（2H） - 和R'和R“相同，为氢或烷基，它们的异构形式及其混合物及其酸加成盐可用作抗心律失常药和抗颤剂。

7. 发明授权

US06423715B1 Thiazolobenzoheterocycles, their preparation and medicaments containing them 失效
公开(公告)号：US06423715B1
公开(公告)日：2002-07-23
申请号：US09987648
申请日：2001-11-15
申请人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
发明人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
IPC分类号： C07D51306
CPC分类号： C07D513/06 , C07D517/06 , C07D517/08
摘要： Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.

8. 发明授权

US06288075B1 Thiazolo[5,4,3-ij]quinolines, preparation and medicines containing the same 失效
标题翻译：噻唑并[5,4,3-ij]喹啉，制剂及含有它们的药物
公开(公告)号：US06288075B1
公开(公告)日：2001-09-11
申请号：US09384237
申请日：1999-08-27
申请人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
发明人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
IPC分类号： C07D51306
CPC分类号： C07D513/06 , C07D517/06 , C07D517/08
摘要： Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.
摘要翻译：讨论式（I）化合物：其外消旋物，对映体，非对映异构体和无机酸盐及其有机酸盐，其制备方法和含有它们的药物。

9. 发明授权

US06369221B1 Thiazolobenzoheterocycles, preparation and medicines containing same 失效
标题翻译：噻唑环杂环，制备物和含有它们的药物
公开(公告)号：US06369221B1
公开(公告)日：2002-04-09
申请号：US09484836
申请日：2000-01-18
申请人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-François Peyronel
发明人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-François Peyronel
IPC分类号： C07D49800
CPC分类号： C07D513/06
摘要： Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them. Also disclosed are novel intermediates for preparing the foregoing compounds, these intermediates having the formula
摘要翻译：公开了通式的噻唑并苯并杂环，包括它们的异构体，外消旋体，对映体和其盐，以及制备这些化合物的方法和含有它们的药物。还公开了用于制备前述化合物的新型中间体，这些具有下式的中间体

10. 发明授权

US5902803A 5H,10H-imidazo�1,2-a!indeno�1,2-e!pyrazin-4-one derivatives, preparation thereof, and drugs containing said derivatives 失效
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：US5902803A
公开(公告)日：1999-05-11
申请号：US930967
申请日：1997-10-03
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Jean-Claude Hardy , Patrick Jimonet , Franco Manfre , Serge Mignani , Patrick Nemecek , Yves Ribeill
IPC分类号： A61K31/495 , A61P1/14 , A61P3/00 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P31/04 , A61P31/12 , A61P43/00 , C07D233/90 , C07D487/04 , C07F9/6506 , C07F9/6561
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--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 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-aspartame (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.
摘要翻译： PCT No.PCT / FR96 / 00496 Sec。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年4月2日PCT PCT。出版物WO96 / 31511 PCT 日期：10月10日，式（I）的化合物，其中R为氢原子或羧基，烷氧基羰基，-CO-NR4R5，-PO3H2或-CH2OH基，R1为-alk-NH2，-alk-NH- CO-R3，-alk-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-阿斯巴甜（NMDA）受体的非竞争性拮抗剂，更具体地是NMDA受体甘氨酸调节剂位点的配体。

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