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31. 发明授权

US07524971B2 1,5-diarylpyrrole derivatives, preparation method thereof and application of same in therapeutics 失效
标题翻译： 1,5-二芳基吡咯衍生物及其制备方法及其在治疗中的应用
公开(公告)号：US07524971B2
公开(公告)日：2009-04-28
申请号：US11832851
申请日：2007-08-02
申请人： Francis Barth , Christian Congy , Laurent Hortala , Murielle Rinaldi-Carmona
发明人： Francis Barth , Christian Congy , Laurent Hortala , Murielle Rinaldi-Carmona
IPC分类号： C07D207/30
CPC分类号： C07D207/323 , C07D207/335 , C07D403/12
摘要： The invention relates to compounds having formula (I): Wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also relates to a method of preparing said compounds and to die application thereof in therapeutics.
摘要翻译：本发明涉及具有式（I）的化合物：其中X，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义。本发明还涉及一种制备所述化合物并将其在治疗中应用的方法。

32. 发明授权

US07384960B2 Pyrazolecarboxylic acid tricyclic derivatives, preparation and pharmaceutical compositions containing same 有权
标题翻译：吡唑羧酸三环衍生物，制剂和含有它们的药物组合物
公开(公告)号：US07384960B2
公开(公告)日：2008-06-10
申请号：US11119074
申请日：2005-04-29
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31/454 , A61K31/416 , C07D231/54 , C07D295/28
CPC分类号： C07D231/56 , C07D231/54 , C07D495/04
摘要： The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.
摘要翻译：本发明的主题是下式的吡唑羧酸的三环衍生物：其中R 1代表C 3 -C 15羧基或 NR 2 R 3 N 3基团。本发明还涉及制备式（I）化合物的方法，含有它们的药物组合物。式（I）化合物在大麻素CB 1受体上是有活性的。

33. 发明授权

US07320978B2 Oxazole derivatives, preparation and therapeutic use thereof 失效
标题翻译：恶唑衍生物，其制备和治疗用途
公开(公告)号：US07320978B2
公开(公告)日：2008-01-22
申请号：US11461629
申请日：2006-08-01
申请人： Francis Barth , Joelle Arnaud-Taillades , Christian Congy , Murielle Rinaldi-Carmona
发明人： Francis Barth , Joelle Arnaud-Taillades , Christian Congy , Murielle Rinaldi-Carmona
IPC分类号： A61K31/422 , A61K31/445 , A61K31/496 , C07D413/02 , C07D263/30
CPC分类号： C07D263/34 , C07D413/06 , C07D491/10
摘要： This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.
摘要翻译：本发明涉及式（I）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7和R 8如本文所述。本发明还涉及其预防和治疗用途的方法。

34. 发明授权

US07294645B2 Derivatives of N′-(1,5-diphenyl-1H-pyrazol-3-yl) sulfonamide with CB1 receptor affinity 有权
标题翻译：具有CB1受体亲和力的N' - （1,5-二苯基-1H-吡唑-3-基）磺酰胺的衍生物
公开(公告)号：US07294645B2
公开(公告)日：2007-11-13
申请号：US11428928
申请日：2006-07-06
申请人： Francis Barth , Serge Martinez , Murielle Rinaldi-Carmona , Christian Congy
发明人： Francis Barth , Serge Martinez , Murielle Rinaldi-Carmona , Christian Congy
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D231/12 , C07D409/12 , C07D413/14
摘要： The invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 are as defined herein. The invention also relates to the preparation method thereof and to the use of same in therapeutics.
摘要翻译：本发明涉及式（I）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9，R 9， >如本文所定义。本发明还涉及其制备方法及其在治疗中的应用。

35. 发明授权

US07282516B2 4-cyanopyrazole-3-carboxamide derivatives, preparation, and application thereof 有权
标题翻译： 4-氰基吡唑-3-甲酰胺衍生物，其制备及应用
公开(公告)号：US07282516B2
公开(公告)日：2007-10-16
申请号：US11315774
申请日：2005-12-22
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona
IPC分类号： A61K31/4155 , A61K31/454 , C07D231/16
CPC分类号： C07D401/12 , C07D231/14
摘要： The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 are as described herein. Also disclosed and claimed are the method of preparation and therapeutic application of compound of formula (I).
摘要翻译：本发明涉及式（I）的4-氰基吡唑-3-甲酰胺衍生物：其中R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8是如本文所述。还公开并要求保护的是式（I）化合物的制备和治疗应用的方法。

36. 发明申请

US20060264470A1 Thiophene-2-carboxamide derivatives, preparation and therapeutic application thereof 失效
标题翻译：噻吩-2-甲酰胺衍生物，其制备和治疗应用
公开(公告)号：US20060264470A1
公开(公告)日：2006-11-23
申请号：US11400702
申请日：2006-04-07
申请人： Francis Barth , Jean-Philippe Ducoux , Murielle Rinaldi-Carmona , Christian Congy
发明人： Francis Barth , Jean-Philippe Ducoux , Murielle Rinaldi-Carmona , Christian Congy
IPC分类号： A61K31/453 , A61K31/405 , C07D409/02
CPC分类号： C07D333/38 , C07D409/12
摘要： The invention discloses and claims a compound of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R11 are as defined herein. Further embodiments of the invention include a method of preparation of a compound of formula (I), its pharmaceutical composition and a method of treatment of a disease using a compound of formula (I).
摘要翻译：本发明公开并要求具有式（I）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8和R 11， / SUB>如本文所定义。本发明的其它实施方案包括制备式（I）化合物的方法，其药物组合物和使用式（I）化合物治疗疾病的方法。

37. 发明授权

US5462960A Pyrazole-3-carboxamide derivatives, process for their preparation and pharmaceutical compositions in which they are present 失效
标题翻译：吡唑-3-甲酰胺衍生物，其制备方法及其存在的药物组合物
公开(公告)号：US5462960A
公开(公告)日：1995-10-31
申请号：US357880
申请日：1994-12-16
申请人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31/415 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/55 , A61P25/00 , A61P25/18 , A61P43/00 , C07D231/14 , C07D401/12 , C07D471/08
CPC分类号： C07D231/14
摘要： The present invention relates to novel pyrazole-3-carboxamide derivatives of the formula ##STR1## in which the substituents are as defined in the specification. The present invention further relates to a process for the preparation of these novel derivatives and to the pharmaceutical compositions in which they are present.
摘要翻译：本发明涉及式（I）的新的吡唑-3-甲酰胺衍生物，其中取代基如说明书中所定义。本发明还涉及制备这些新型衍生物的方法及其存在的药物组合物。

38. 发明授权

US07202268B2 Derivatives of indole-3-carboxamide, preparation method thereof and application of same in therapeutics 失效
标题翻译：吲哚-3-甲酰胺的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US07202268B2
公开(公告)日：2007-04-10
申请号：US11138843
申请日：2005-05-26
申请人： Francis Barth , Mireille Rinaldi-Carmona , Claude Vernhet
发明人： Francis Barth , Mireille Rinaldi-Carmona , Claude Vernhet
IPC分类号： A61K31/40 , A61K31/405 , C07D209/42 , C07D209/12 , C07D209/18
CPC分类号： C07D209/42
摘要： The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3–C10 alkyl, a C5–C10 carbocyclic radical that is unsubstituted or substituted one or more times with a methyl group; R2 represents a hydrogen atom or a (C1–C4)alkyl group; R3 represents a halogen atom or a (C1–C4)alkyl group; R4 represents a hydrogen or halogen atom or a (C1–C4)alkyl group; R5 represents a (C1–C4)alkyl group or a trifluoromethyl; X represents a sulfur atom, an —NHSO2— group or an —SO2— group; and n is equal to 2 or 3. The invention also relates to a method of preparing the aforementioned derivatives and to the application of same in therapeutics.
摘要翻译：本发明涉及具有通式（I）的吲哚-3-甲酰胺衍生物：

39. 发明申请

US20050288356A1 Derivatives of indole-3-carboxamide, preparation method thereof and application of same in therapeutics 失效
标题翻译：吲哚-3-甲酰胺的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US20050288356A1
公开(公告)日：2005-12-29
申请号：US11138843
申请日：2005-05-26
申请人： Francis Barth , Mireille Rinaldi-Carmona , Claude Vernhet
发明人： Francis Barth , Mireille Rinaldi-Carmona , Claude Vernhet
IPC分类号： A61P1/00 , A61P5/14 , A61P9/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P27/02 , A61P31/00 , A61P35/00 , A61P37/00 , C07D209/42 , A61K31/405
CPC分类号： C07D209/42
摘要： The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3-C10 alkyl, a C5-C10 carbocyclic radical that is unsubstituted or substituted one or more times with a methyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a halogen atom or a (C1-C4)alkyl group; R4 represents a hydrogen or halogen atom or a (C1-C4)alkyl group; R5 represents a (C1-C4)alkyl group or a trifluoromethyl; X represents a sulfur atom, an —NHSO2— group or an —SO2— group; and n is equal to 2 or 3. The invention also relates to a method of preparing the aforementioned derivatives and to the application of same in therapeutics.
摘要翻译：本发明涉及具有通式（I）的吲哚-3-甲酰胺的衍生物：其中：R 1表示C 3 -C 10烷基，烷基，未被取代或被甲基取代一次或多次的C 5 -C 10 -C 10碳环基团; R 2表示氢原子或（C 1 -C 4 -C 4）烷基; R 3表示卤素原子或（C 1 -C 4 -C 4）烷基; R 4表示氢或卤素原子或（C 1 -C 4 -C 4）烷基; R 5表示（C 1 -C 4 -C 4）烷基或三氟甲基; X表示硫原子，-NHSO 2 - 或-SO 2 - ; - 并且n等于2或3.本发明还涉及制备上述衍生物的方法及其在治疗中的应用。

40. 发明授权

US06794382B2 Benzimidazole derivatives, preparation and therapeutic use thereof 失效
标题翻译：苯并咪唑衍生物，其制备和治疗用途
公开(公告)号：US06794382B2
公开(公告)日：2004-09-21
申请号：US10343467
申请日：2003-01-30
申请人： Francis Barth , Daniel Bichon , Frank Bolkenius , Viviane Van Dorsselaer
发明人： Francis Barth , Daniel Bichon , Frank Bolkenius , Viviane Van Dorsselaer
IPC分类号： C07D47106
CPC分类号： C07D471/06 , C07D487/06
摘要： The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group. Preparation process and therapeutic application.
摘要翻译：本发明涉及X表示氮原子或碳原子的一般结构式的苯并咪唑衍生物，当X表示氮原子时：R 3表示氢原子或C 1 -C 4烷基，或不存在，得到式（I）包括仲胺或叔胺; R 4表示氢原子或C 1 -C 6烷基，C 3 -C 7环烷基，任选取代的C 3 -C 7杂环烷基， - （CH 2）p - 杂芳基，杂芳基 - 羰基，苯基羰基，（ C 1 -C 6）烷基羰基， - （CH 2）p COOR，任选取代的苯基磺酰基或任选取代的 - （CH 2）对苯基，并且当X表示碳原子时：R 3表示氢原子或-NR 5 R 6基，-N（ R5）3 +，-NHCOR7，-CONHR5，-COR7，-NHCONH2，-OH或-CH2OH，R4表示氢原子或任选取代的 - （CH 2）p - 苯基， - （CH 2）p - - （CH2）tNR7R8组。制备方法和治疗应用。

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