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1. 发明授权

US07402682B2 3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-B]吲哚-1-甲酰胺衍生物，其制备和治疗用途
公开(公告)号：US07402682B2
公开(公告)日：2008-07-22
申请号：US11427508
申请日：2006-06-29
申请人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： C07D487/02 , C07D209/42 , A61K31/503
CPC分类号： C07D487/04 , C07D209/42
摘要： A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.
摘要翻译：本发明的主题是通式（I）的化合物，其中X表示氢或卤素原子; R 1表示氢原子或（C 1 -C 4 -C 4）烷基; R 2和R 3各自独立地表示氢原子或（C 1 -C 4）烷基，或者R 2和R 3形式，与携带它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，杂芳基可以携带一个或多个卤素原子和/或一个或多个（C 1 C 1 -C 4烷基或（C 1 -C 4 -C 4）烷氧基; 以碱的形式，与酸，溶剂合物或水合物的加成盐，包含它们的药物组合物，其制备方法和合成中间体。

2. 发明申请

US20080249098A1 3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide Derivatives, Their Preparation and Therapeutic Use 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-B]吲哚-1-甲酰胺衍生物及其制备和治疗用途
公开(公告)号：US20080249098A1
公开(公告)日：2008-10-09
申请号：US12140608
申请日：2008-06-17
申请人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： A61K31/5025 , A61P25/00
CPC分类号： C07D487/04 , C07D209/42
摘要： A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4) alkyl or (C1-C4) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.
摘要翻译：本发明的主题是通式（I）的化合物，其中X表示氢或卤素原子; R 1表示氢原子或（C 1 -C 4 -C 4）烷基; R 2和R 3各自独立地表示氢原子或（C 1 -C 4）烷基，或者R 2和R 3形式，与携带它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，杂芳基可以携带一个或多个卤素原子和/或一个或多个（C 1 C 1 -C 4烷基或（C 1 -C 4 -C 4）烷氧基; 以碱的形式，与酸，溶剂合物或水合物的加成盐，包含它们的药物组合物，其制备方法和合成中间体。

3. 发明授权

US07323467B2 3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺衍生物，其制备及其在治疗中的应用
公开(公告)号：US07323467B2
公开(公告)日：2008-01-29
申请号：US11749342
申请日：2007-05-16
申请人： Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： A61K31/5025 , A61P25/02 , A61P25/16
CPC分类号： C07D209/42 , C07D487/04
摘要： The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for preparing them, and novel intermediates therefor.
摘要翻译：本发明公开并要求通式（I）化合物的治疗用途，其中X，R 1，R 2和R 3是如上所述这里。本发明还公开了制备它们的方法及其新颖的中间体。

4. 发明授权

US07569567B2 3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-b]吲哚-1-甲酰胺衍生物，其制备和治疗用途
公开(公告)号：US07569567B2
公开(公告)日：2009-08-04
申请号：US12140608
申请日：2008-06-17
申请人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： A61K31/503 , C07D487/02
CPC分类号： C07D487/04 , C07D209/42
摘要： A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4) alkyl or (C1-C4) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.
摘要翻译：本发明的主题是通式（I）的化合物，其中X表示氢或卤素原子; R1表示氢原子或（C1-C4）烷基; R2和R3各自独立地表示氢原子或（C1-C4）烷基，或者R2和R3与携带它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，杂芳基可以携带一个或多个卤素原子和/或一个或多个（C 1 -C 4）烷基或（C 1 -C 4）烷氧基; 以碱的形式，与酸，溶剂合物或水合物的加成盐，包含它们的药物组合物，其制备方法和合成中间体。

5. 发明授权

US07405306B2 3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics 有权
公开(公告)号：US07405306B2
公开(公告)日：2008-07-29
申请号：US11867366
申请日：2007-10-04
申请人： Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： C07D487/02 , C07D209/42 , A61K31/503
CPC分类号： C07D209/42 , C07D487/04
摘要： The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for preparing them, and novel intermediates therefor.

6. 发明申请

US20050124615A1 3-heteroarly-3,5-dihydro-4-oxo-4h-pyridazino[4,5-b] indole-1-acetamide derivatives, preparation and use thereof in medicaments 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺衍生物，其药物的制备和用途
公开(公告)号：US20050124615A1
公开(公告)日：2005-06-09
申请号：US10509695
申请日：2003-04-02
申请人： Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： A61K31/5025 , A61K31/503 , A61K31/5377 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , C07D20060101 , C07D209/00 , C07D209/18 , C07D209/42 , C07D241/00 , C07D487/02 , C07D487/04
CPC分类号： C07D209/42 , C07D487/04
摘要： The invention provides compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each independently of one another represent a hydrogen atom or a (C1-C4)alkyl group, or else R2 and R3, together with the nitrogen atom bearing them, form a pyrrolidinyl, piperidinyl, morpholinyl or 4-(C1-C4)alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type which may carry one or more halogen atoms and/or one or more (C1-C4)alkyl and/or (C1-C4)alkoxy groups; in the form of bases, addition salts with acids, solvates or hydrates; the pharmaceutical compositions comprising them, processes for preparing them, and synthesis intermediates.
摘要翻译：本发明提供通式（I）的化合物，其中X表示氢或卤素原子; R 1表示氢原子或（C 1 -C 4 -C 4）烷基; R 2和R 3各自独立地表示氢原子或（C 1 -C 4）烷基，）烷基，或者R 2和R 3 3与带有它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-（C 1 C 4 -C 4烷基哌嗪基; 并且Het表示可携带一个或多个卤素原子和/或一个或多个（C 1 -C 4）烷基的吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，（C 1 -C 4）烷基和/或（C 1 -C 4 -C 4）烷氧基; 碱的形式，与酸，溶剂合物或水合物的加成盐; 包含它们的药物组合物，其制备方法和合成中间体。

7. 发明申请

US20050096321A1 3-heteroaryl-3, 5-dihydro-4-oxo-4H-pyridazino[4, 5-b]indole-1-carboxamide derivatives their preparations and therapeutic use 有权
标题翻译： 3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-b]吲哚-1-甲酰胺衍生物的制备和治疗用途
公开(公告)号：US20050096321A1
公开(公告)日：2005-05-05
申请号：US10499725
申请日：2002-11-20
申请人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
发明人： Philippe Burnier , Jacques Froissant , Benoit Marabout , Frank Marguet , Frederic Puech
IPC分类号： A61K31/50 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/02 , C07D209/42 , C07D487/04 , C07D487/02 , A61K31/503
CPC分类号： C07D487/04 , C07D209/42
摘要： The invention concerns compounds of general formula (I), wherein: X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3, represent each, independently of each other, a hydrogen atom or a (C1-C4)alkyl group, or R2 and R3 form, with the atom which bears them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl, pyridazinyl type, the heteroaromatic group may represent one or several halogen atoms and/or one or several (C1-C4)alkyl, (C1-C4)alkoxyl groups; in the form of bases, addition salts to acids, solvates or hydrates. The invention also concerns pharmaceutical compositions containing same, methods for preparing same and synthesis intermediates.
摘要翻译：本发明涉及通式（I）的化合物，其中：X表示氢或卤素原子; R 1表示氢原子或（C 1 -C 4 -C 4）烷基; R 2和R 3各自独立地表示氢原子或（C 1 -C 4）烷基，或者R 2和R 3形式，其中带有它们的原子，吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基，哒嗪基类的杂芳族基团，杂芳基可以表示一个或多个卤素原子和/或一个或多个（C 1 H 3） -C 1-4烷基，（C 1 -C 4 -C 4）烷氧基; 以碱的形式，与酸，溶剂化物或水合物的加成盐。本发明还涉及含有其的药物组合物，其制备方法和合成中间体。

8. 发明授权

US07547706B2 1H-pyrimido[4,5-b]indole derivatives, their preparation and therapeutic use 失效
标题翻译： 1H-嘧啶并[4,5-b]吲哚衍生物，其制备和治疗用途
公开(公告)号：US07547706B2
公开(公告)日：2009-06-16
申请号：US11873789
申请日：2007-10-17
申请人： Jacques Froissant , Frank Marguet , Anne Olivier-Bandini , Frederic Puech
发明人： Jacques Froissant , Frank Marguet , Anne Olivier-Bandini , Frederic Puech
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D487/04 , C07D209/12
摘要： The invention concerns compounds of general formula (I): Wherein n, X, Y, R1 and R2 are as defined herein. The invention also concerns a method for preparing the compounds and their therapeutic use.
摘要翻译：本发明涉及通式（I）的化合物：其中n，X，Y，R 1和R 2如本文所定义。本发明还涉及一种制备化合物及其治疗用途的方法。

9. 发明申请

US20080125410A1 1H-Pyrimido[4,5-b]indole derivatives, their preparation and therapeutic use 失效
标题翻译： 1H-嘧啶并[4,5-b]吲哚衍生物，其制备和治疗用途
公开(公告)号：US20080125410A1
公开(公告)日：2008-05-29
申请号：US11873789
申请日：2007-10-17
申请人： Jacques Froissant , Frank Marguet , Anne Olivier-Bandini , Frederic Puech
发明人： Jacques Froissant , Frank Marguet , Anne Olivier-Bandini , Frederic Puech
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , C07D209/12
摘要： The invention concerns compounds of general formula (I): Wherein n, X, Y, R1 and R2 are as defined herein. The invention also concerns a method for preparing the compounds and their therapeutic use.
摘要翻译：本发明涉及通式（I）的化合物：其中n，X，Y，R 1和R 2 2如本文所定义。本发明还涉及一种制备化合物及其治疗用途的方法。

10. 发明授权

US08546395B2 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译：（1H-吡咯并[2,3-b]吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物及其治疗用途
公开(公告)号：US08546395B2
公开(公告)日：2013-10-01
申请号：US13128998
申请日：2009-11-30
申请人： Christophe Pacaud , Frederic Puech
发明人： Christophe Pacaud , Frederic Puech
IPC分类号： A01N43/58 , A61K31/50 , C07D487/00
CPC分类号： C07D519/00 , C07D401/12
摘要： The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R2 represents an aryl group optionally substituted with one or more halogen atoms or C1-6-alkyl, C1-6-alkyloxy, C1-6-alkylthio, C1-6-fluoroalkyl, C1-6-fluoroalkyloxy and —CN groups or R2 represents a group chosen from C1-6-alkyl, C1-6-fluoroalkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkyl groups; A represents a C1-7-alkylene group; B represents a C1-7-alkylene group; L represents either a nitrogen atom optionally substituted with an Rc or Rd group, or a carbon atom substituted with an Re1 group and an Rd group or two Re2 groups; the carbon atoms of A and of B being optionally substituted with one or more Rf groups, which may be identical to or different from one another. Preparation process and therapeutic use.
摘要翻译：本发明涉及对应于通式（I）的6-环氨基-3-（1H-吡咯并[2,3-b]吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物，其中R 2表示任选被一个或多个卤素原子或C 1-6 - 烷基，C 1-6 - 烷氧基，C 1-6 - 烷硫基，C 1-6 - 氟烷基，C 1-6 - 氟烷氧基和-CN基团取代的芳基，或者R 2表示选自 C 1-6 - 烷基，C 1-6 - 氟烷基，C 3-7 - 环烷基或C 3-7 - 环烷基-C 1-6 - 烷基; A表示C 1-7 - 亚烷基; B表示C 1-7 - 亚烷基; L表示任选被Rc或Rd基团取代的氮原子或被Re 1基团和Rd基团或两个Re 2基团取代的碳原子; A和B的碳原子任选被一个或多个可以彼此相同或不同的R f基团取代。制备过程和治疗用途。

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