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1. 发明授权

US07476668B2 Thiadiazine derivatives and use thereof as positive AMPA receptor modulators 失效
标题翻译：噻二嗪衍生物及其作为阳性AMPA受体调节剂的用途
公开(公告)号：US07476668B2
公开(公告)日：2009-01-13
申请号：US10555743
申请日：2004-05-04
申请人： Emmanuel Graindorge , Pierre Francotte , Stéphane Boverie , Pascal De Tullio , Bernard Pirotte , Pierre Lestage , Laurence Danober , Pierre Renard , Daniel-Henri Caignard
发明人： Emmanuel Graindorge , Pierre Francotte , Stéphane Boverie , Pascal De Tullio , Bernard Pirotte , Pierre Lestage , Laurence Danober , Pierre Renard , Daniel-Henri Caignard
IPC分类号： C07D513/04 , A61K31/542
CPC分类号： C07D513/04
摘要： Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR′ and SO2NHR′ wherein R′ represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.
摘要翻译：式（I）的化合物：其中：A表示噻吩基，呋喃基，吡咯基，氧硫杂环戊烷，噻唑，异噻唑，恶唑或咪唑，其中：=“3.13mm”wi =“6.35mm” file =“US07476668-20090113-P00001.TIF”alt =“custom character”img-content =“character”img-format =“tif”/>表示单键或双键，R1表示氢，直链或支链（任选被一个或多个选自卤素或（C 1 -C 6）烷氧基 - （C 1 -C 6）烷基的基团取代的C 1 -C 6烷基，R 2表示氢或任选被一个或多个（C 1 -C 6）烷氧基取代的直链或支链卤素，R3表示氢或选自直链或支链（C1-C6）烷基，CONHR'和SO2NHR'的基团，其中R'表示直链或支链（C1-C6）烷基，其对映异构体和非对映异构体，以及其加成盐与药学上可接受的酸或碱。含有该药物的药物，可用作AMPA抑制剂。

2. 发明授权

US07268129B2 Fluorinated benzothiadiazine compounds 失效
标题翻译：氟化苯并噻二嗪化合物
公开(公告)号：US07268129B2
公开(公告)日：2007-09-11
申请号：US11041495
申请日：2005-01-24
申请人： Pierre Francotte , Pierre Fraikin , Pascal De Tullio , Bernard Pirotte , Pierre Lestage , Laurence Danober , Daniel-Henri Caignard , Pierre Renard
发明人： Pierre Francotte , Pierre Fraikin , Pascal De Tullio , Bernard Pirotte , Pierre Lestage , Laurence Danober , Daniel-Henri Caignard , Pierre Renard
IPC分类号： C07D285/22 , A61K31/5415 , A61P25/24
CPC分类号： C07D285/24
摘要： Compounds of formula (I): wherein: RF represents monofluoro- or polyfluoro-alkyl or monofluoro- or polyfluoro-cycloalkylalkyl, R1 represents hydrogen or a group selected from alkylaminocarbonyl and optionally substituted alkyl, R2 represents hydrogen, halogen or a group selected from cycloalkyl and optionally substituted alkyl, R3 to R6, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, nitro, cyano, alkylsulphonyl, hydroxy, alkoxy, optionally substituted alkyl and optionally substituted amino, its optical isomers when they exist, and also their addition salts with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as AMPA modulators.
摘要翻译：式（I）化合物：其中：R F表示单氟或多氟 - 烷基或单氟或多氟环烷基烷基，R 1表示氢或选自烷基氨基羰基和任选取代的烷基，R 2表示氢，卤素或选自环烷基和任选取代的烷基，R 3至R 6的基团，其中可以相同或不同，各自表示选自氢，卤素，硝基，氰基，烷基磺酰基，羟基，烷氧基，任选取代的烷基和任选取代的氨基的原子或基团，当它们存在时的光学异构体，以及它们与药学上可接受的酸或碱。含有与AMPA调节剂有用的药用产品。

3. 发明授权

US07741320B2 Cycloalkylated benzothiadiazines, a process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：环烷基化苯并噻二嗪，其制备方法和含有它们的药物组合物
公开(公告)号：US07741320B2
公开(公告)日：2010-06-22
申请号：US12459844
申请日：2009-07-09
申请人： Pierre Francotte , Pascal De Tullio , Bernard Pirotte , Laurence Danober , Pierre Lestage , Daniel-Henri Caignard
发明人： Pierre Francotte , Pascal De Tullio , Bernard Pirotte , Laurence Danober , Pierre Lestage , Daniel-Henri Caignard
IPC分类号： C07D285/22 , A61K31/5415 , A61P25/24
CPC分类号： C07D285/28
摘要： Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.
摘要翻译：式（I）化合物：其中：RCy表示未取代或取代的环烷基或环烷基烷基，可以相同或不同的R 1，R 2，R 3和R 4各自表示氢或卤素原子或硝基; 氰基; 羟基; 烷氧基烷基; 未取代或取代的氨基; 羧基; 烷氧基羰基; 芳氧基羰基; 未取代或取代的氨基羰基。含有该药物的药物可用于治疗或预防由AMPA受体调节剂治疗的病症。

4. 发明申请

US20100009974A1 Cycloalkylated benzothiadiazines, a process for their preparation and pharmaceutical compostions containing them 失效
标题翻译：环烷基化苯并噻二嗪，其制备方法和含有它们的药物组合物
公开(公告)号：US20100009974A1
公开(公告)日：2010-01-14
申请号：US12459844
申请日：2009-07-09
申请人： Pierre FRANCOTTE , Pascal De Tullio , Bernard Pirotte , Laurence Danober , Pierre Lestage , Daniel-Henri Caignard
发明人： Pierre FRANCOTTE , Pascal De Tullio , Bernard Pirotte , Laurence Danober , Pierre Lestage , Daniel-Henri Caignard
IPC分类号： A61K31/5415 , C07D285/24 , A61P25/28
CPC分类号： C07D285/28
摘要： Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.
摘要翻译：式（I）化合物：其中：RCy表示未取代或取代的环烷基或环烷基烷基，可以相同或不同的R 1，R 2，R 3和R 4各自表示氢或卤素原子或硝基; 氰基; 羟基; 烷氧基烷基; 未取代或取代的氨基; 羧基; 烷氧基羰基; 芳氧基羰基; 未取代或取代的氨基羰基。含有该药物的药物可用于治疗或预防由AMPA受体调节剂治疗的病症。

5. 发明申请

US20070004709A1 Thiadiazine derivatives and use thereof as positive ampa receptor modulators 失效
标题翻译：噻二嗪衍生物及其作为正安培受体调节剂的用途
公开(公告)号：US20070004709A1
公开(公告)日：2007-01-04
申请号：US10555743
申请日：2004-05-04
申请人： Pierre Francotte , Stephane Boverie , Pascal De Tullio , Bernard Pirotte , Pierre Lestage , Laurence Danober , Pierre Renard , Daniel-Henri Caignard
发明人： Pierre Francotte , Stephane Boverie , Pascal De Tullio , Bernard Pirotte , Pierre Lestage , Laurence Danober , Pierre Renard , Daniel-Henri Caignard
IPC分类号： A61K31/549 , C07D498/02
CPC分类号： C07D513/04
摘要： Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR′ and SO2NHR′ wherein R′ represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.
摘要翻译：式（I）化合物：其中：A表示噻吩基，呋喃基，吡咯基，氧硫杂环戊烷，噻唑，异噻唑，恶唑或咪唑，表示单键或双键，R <1 表示任选被一个或多个选自卤素或（C 1 -C 6）烷基的基团取代的直链或支链（C 1 -C 6 -C 6）烷基， -C 6 -C 6烷氧基 - （C 1 -C 6 -C 6）烷基，R 2表示氢或直链或任选被一个或多个卤素取代的支链（C 1 -C 6 -C 6）烷基，R 3 3表示氢或选自直链或支链（C 1 -C 6 -C 6）烷基，CONHR'和SO 2 NHR'，其中R'表示直链或支链（C 1 -C 6） 1 -C 6烷基，其对映体和非对映异构体及其加成盐w 具有药学上可接受的酸或碱。含有该药物的药物，可用作AMPA抑制剂。

6. 发明申请

US20070112063A1 Benzopyran derivatives, method of production and use thereof 失效
公开(公告)号：US20070112063A1
公开(公告)日：2007-05-17
申请号：US10588265
申请日：2005-01-21
申请人： Sophie Sebille , Bernard Piroite , Stephane Boverie , Pascal De Tullio , Philippe Lebrun , Marie-Helene Antoine
发明人： Sophie Sebille , Bernard Piroite , Stephane Boverie , Pascal De Tullio , Philippe Lebrun , Marie-Helene Antoine
IPC分类号： A61K31/353
CPC分类号： C07D311/68 , C07D405/12 , C07D409/12
摘要： The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof. wherein: R1, R2, R3 and R4 are independently hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, nitro, amino, cyano, cyanomethyl, perhalomethyl, C1-6-monoalkyl- or dialkylamino, sulfamoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkylsulfinyl, formyl, C1-6-alkylcarbonylamino, R8arylthio, R8arylsulfinyl, R8arylsulfonyl, C1-6-alkoxycarbonyl, C1-6-alkoxycarbonyl-C1-6-alkyl, carbamoyl, carbamoylmethyl, C1-6-monoalkyl- or dialkylaminocarbonyl, C1-6-monoalkyl- or dialkylaminothiocarbonyl, ureido, C1-6-monoalkyl- or dialkylaminocarbonylamino, thioureido, C1-6-monoalkyl- or dialkylaminothiocarbonylamino, C1-6-monoalkyl- or dialkylaminosulfonyl, carboxy, carboxy-C1-6-alkyl, acyl, R8aryl, R8aryl-C1-6-alkyl, R8aryloxy; R5 and R6 are each independently hydrogen, C1-6-alkyl or, R5 and R6 taken together with the carbon atom to which they are attached form a 3- to 6-membered carbocyclic ring; R7 is 2-, 3- or 4-pyridyl optionally mono- or polysubstituted by R1; R7 is 2- or 3-thienyl optionally mono- or polysubstituted substituted by R1 or R7 is phenyl optionally mono- or polysubstituted by R1 with the exception of or R7 representing C6H5; R8 is hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, nitro, amino, cyano, cyanomethyl, perhalomethyl; or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, including a racemic mixture or any polymorphic and tautomeric form.

7. 发明授权

US06242443B1 1,2,4-benzothiadiazine derivatives, their preparation and use 失效
标题翻译： 1,2,4-苯并噻二嗪衍生物，其制备和用途
公开(公告)号：US06242443B1
公开(公告)日：2001-06-05
申请号：US08877456
申请日：1997-06-17
申请人： Bernard Pirotte , Philippe Lebrun , Pascal De Tullio , Fabian Somers , Jacques Delarge , John Bondo Hansen , Flemming Elmelund Nielsen , Holger Claus Hansen , John Patrick Mogensen , Tina Møller-Tagmose
发明人： Bernard Pirotte , Philippe Lebrun , Pascal De Tullio , Fabian Somers , Jacques Delarge , John Bondo Hansen , Flemming Elmelund Nielsen , Holger Claus Hansen , John Patrick Mogensen , Tina Møller-Tagmose
IPC分类号： C07D28524
CPC分类号： A61K31/541 , A61K31/5415 , C07D285/24 , C07D453/02 , C07D453/06
摘要： 1,2,4-Benzothiadiazine derivatives represented by formula wherein D, R1, R2, R3, R4, R5, R12, R13, R14, R15 are defined in the description, composition thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.
摘要翻译：所述化合物的制备方法及其制备方法在本说明书中进行了说明，其中，式（Ⅳ）所示的1,2,4-苯并噻二嗪衍生物由式Ⅵ所示，D，R 1，R 2，R 3，R 4，R 5，R 12，R 13，R 14，可用于治疗中枢神经系统疾病，心血管系统，肺系统，胃肠系统和内分泌系统。

8. 发明授权

US5792764A Pyrido-1,2,4-thiadiazine and pyrido-1,4-thiazine derivatives, their preparation and use 失效
标题翻译：吡啶-1,2,4-噻二嗪和吡啶-1,4-噻嗪衍生物，其制备和用途
公开(公告)号：US5792764A
公开(公告)日：1998-08-11
申请号：US785435
申请日：1997-01-17
申请人： Bernard Pirotte , Philippe Lebrun , Pascal De Tullio , Fabian Somers , Jacques Delarge , Holger Claus Hansen , Flemming Elmelund Nielsen , John Bondo Hansen
发明人： Bernard Pirotte , Philippe Lebrun , Pascal De Tullio , Fabian Somers , Jacques Delarge , Holger Claus Hansen , Flemming Elmelund Nielsen , John Bondo Hansen
IPC分类号： A61K31/00 , A61K31/54 , A61K31/542 , A61K31/549 , A61P1/00 , A61P3/00 , A61P3/10 , A61P5/48 , A61P5/50 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P17/14 , A61P25/06 , A61P25/08 , A61P25/28 , C07D513/04
CPC分类号： C07D513/04
摘要： Pyrido-1,2,4-thiadiazine and pyrido-1,4-thiazine derivatives represented by the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, pulmonary system, the gastrointestinal system and the endocrinologic system.
摘要翻译：其中A，B，D，R 1，R 2，R 3和R 4表示的吡咯并-1,2,4-噻二嗪和吡啶并-1,4-噻嗪衍生物在其描述中的定义，其组成和方法描述了制备化合物。该化合物可用于治疗中枢神经系统疾病，心血管系统，肺系统，胃肠系统和内分泌系统。

9. 发明授权

US07507761B2 Benzopyran derivatives, method of production and use thereof 失效
标题翻译：苯并吡喃衍生物，其制备方法和用途
公开(公告)号：US07507761B2
公开(公告)日：2009-03-24
申请号：US10588265
申请日：2005-01-21
申请人： Sophie Sebille , Bernard Pirotte , Stéphane Boverie , Pascal De Tullio , Philippe Lebrun , Marie-Hélène Antoine
发明人： Sophie Sebille , Bernard Pirotte , Stéphane Boverie , Pascal De Tullio , Philippe Lebrun , Marie-Hélène Antoine
IPC分类号： A61K31/353 , C07D311/68 , C07D311/70
CPC分类号： C07D311/68 , C07D405/12 , C07D409/12
摘要： The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof. wherein: R1, R2, R3 and R4 are independently hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, nitro, amino, cyano, cyanomethyl, perhalomethyl, C1-6-monoalkyl- or dialkylamino, sulfamoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkylsulfinyl, formyl, C1-6-alkylcarbonylamino, R8arylthio, R8arylsulfinyl, R8arylsulfonyl, C1-6-alkoxycarbonyl, C1-6-alkoxycarbonyl-C1-6-alkyl, carbamoyl, carbamoylmethyl, C1-6-monoalkyl- or dialkylaminocarbonyl, C1-6-monoalkyl- or dialkylaminothiocarbonyl, ureido, C1-6-monoalkyl- or dialkylaminocarbonylamino, thioureido, C1-6-monoalkyl- or dialkylaminothiocarbonylamino, C1-6-monoalkyl- or dialkylaminosulfonyl, carboxy, carboxy-C1-6-alkyl, acyl, R8aryl, R8aryl-C1-6-alkyl, R8aryloxy; R5 and R6 are each independently hydrogen, C1-6-alkyl or, R5 and R6 taken together with the carbon atom to which they are attached form a 3- to 6-membered carbocyclic ring; R7 is 2-, 3- or 4-pyridyl optionally mono- or polysubstituted by R1; R7 is 2- or 3-thienyl optionally mono- or polysubstituted substituted by R1 or R7 is phenyl optionally mono- or polysubstituted by R1 with the exception of or R7 representing C6H5; R8 is hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, nitro, amino, cyano, cyanomethyl, perhalomethyl; or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, including a racemic mixture or any polymorphic and tautomeric form.
摘要翻译：本发明涉及式I的新型苯并吡喃衍生物，其制备方法，包含衍生物的组合物及其用途。其中：R 1，R 2，R 3和R 4独立地是氢，卤素，C 1-6 - 烷基，C 3-8 - 环烷基，羟基，C 1-6 - 烷氧基，C 1-6 - 烷氧基-C 1-6 - 烷基，硝基，氨基氰基，氰基甲基，全卤代甲基，C 1-6 - 单烷基 - 或二烷基氨基，氨磺酰基，C 1-6 - 烷硫基，C 1-6 - 烷基磺酰基，C 1-6 - 烷基亚磺酰基，甲酰基，C 1-6 - 烷基羰基氨基，R 8芳硫基，R 8芳基亚磺酰基， C 1-6 - 烷氧基羰基-C 1-6 - 烷基，氨基甲酰基，氨基甲酰基甲基，C 1-6 - 单烷基 - 或二烷基氨基羰基，C 1-6 - 单烷基 - 或二烷基氨基硫代羰基，脲基，C 1-6 - 单烷基 - 或二烷基氨基羰基氨基羧基-C 1-6 - 烷基，酰基，R 8芳基，R 8芳基-C 1-6 - 烷基，R 8芳氧基，C 1-6 - 烷基 - 或二烷基氨基硫代羰基氨基， R 5和R 6各自独立地为氢，C 1-6 - 烷基或者R 5和R 6与它们所连接的碳原子一起形成3-至6-元碳环; R7是任选被R1单取代或多取代的2-，3-或4-吡啶基; R 7是任选被R 1或R 7取代的单或多取代的2-或3-噻吩基，R 3是任选被R1单取代或多取代的苯基，或者R 7代表C 6 H 5; R 8为氢，卤素，C 1-6 - 烷基，C 3-8 - 环烷基，羟基，C 1-6 - 烷氧基，硝基，氨基，氰基，氰基甲基，全卤代甲基。或其盐与药学上可接受的酸或碱，或任何光学异构体或光学异构体的混合物，包括外消旋混合物或任何多晶型和互变异构形式。

10. 发明授权

US06894043B1 Benzothiadiazine derivatives, preparation method and pharmaceutical compositions containing same 失效
标题翻译：苯并噻二嗪衍生物，制备方法和含有它们的药物组合物
公开(公告)号：US06894043B1
公开(公告)日：2005-05-17
申请号：US10148257
申请日：2000-11-28
申请人： Bernard Pirotte , Pascal De Tullio , Stéphane Boverie , Isabelle Kempen , Pierre Lestage
发明人： Bernard Pirotte , Pascal De Tullio , Stéphane Boverie , Isabelle Kempen , Pierre Lestage
IPC分类号： A61K31/549 , A61P25/18 , A61P25/28 , A61P43/00 , C07D285/24 , A61K31/5415
CPC分类号： C07D285/24 , Y02P20/55
摘要： Compound selected from those of formula (I): wherein: X represents flourine, bromine, iodine or methyl, each of R1 and R2, which may be identical or different, represents hydrogen or alkyl, its isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid Medicinal products containing the same which are useful as AMPA modulators.
摘要翻译：选自式（I）的化合物的化合物：其中：X表示氟，溴，碘或甲基，R 1和R 2各自可以相同或不同表示氢或烷基，其存在时的异构体，以及其与药学上可接受的酸的加成盐，其含有该药物的药物可用作AMPA调节剂。

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