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1. 发明授权

US08338451B2 Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof 有权
标题翻译： 2-杂芳基-6-苯基咪唑并[1,2-a]吡啶的多取代衍生物及其制备和治疗用途
公开(公告)号：US08338451B2
公开(公告)日：2012-12-25
申请号：US12881815
申请日：2010-09-14
申请人： Danielle De Peretti , Yannick Evanno , Patrick Lardenois , David Machnik , Nathalie Rakotoarisoa , Antonio Almario Garcia
发明人： Danielle De Peretti , Yannick Evanno , Patrick Lardenois , David Machnik , Nathalie Rakotoarisoa , Antonio Almario Garcia
IPC分类号： A61K31/44 , C07D513/02
CPC分类号： C07D471/04 , C07D213/73 , C07F7/1804
摘要： Compounds of formula (I): wherein R, R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
摘要翻译：式（I）的化合物：其中R，R 1，R 2，R 3，R 4和X如本公开内容所定义，或其酸加成盐，及其合成用途及其合成方法。

2. 发明授权

US07462621B2 Use of substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a] pyrimidin-5(1H)one derivatives as therapeutic agents 失效
标题翻译：取代的2-吡啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-吡啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H ）一种衍生物作为治疗剂
公开(公告)号：US07462621B2
公开(公告)日：2008-12-09
申请号：US11696982
申请日：2007-04-05
申请人： Thierry Gallet , Patrick Lardenois , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Thierry Gallet , Patrick Lardenois , Alistair Lochead , Severine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61K31/55
CPC分类号： A01N43/90 , C07D213/50 , C07D213/60 , C07D487/04
摘要： The invention relates to an use of pyrimidone derivative represented by formula (I) or a salt thereof: wherein m, n, p, X, Y, R1, R2, R3, R4 and R5 are as defined herein for treating a variety of disease states. More specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β or GSK3β and cdk5/p25, such as Alzheimer's disease.
摘要翻译：本发明涉及由式（I）表示的嘧啶酮衍生物或其盐的用途：其中m，n，p，X，Y，R 1，R 2，R 3，R 4和R 5如本文所定义，用于治疗各种疾病状态。更具体地，本发明涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β或GSK3β和cdk5 / p25的异常活性引起的神经变性疾病的预防和/或治疗，例如阿尔茨海默氏病。

3. 发明授权

US07214682B2 Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo{1,2-a}pyrimidin-5(1h)one derivatives 失效
公开(公告)号：US07214682B2
公开(公告)日：2007-05-08
申请号：US10490135
申请日：2002-09-19
申请人： Thierry Gallet , Patrick Lardenois , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Thierry Gallet , Patrick Lardenois , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： A01N43/90 , A61K31/519 , A01N43/62 , A61K31/55 , C07D471/00 , C07D487/00
CPC分类号： A01N43/90 , C07D213/50 , C07D213/60 , C07D487/04
摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C1-6 alkyl group optionally; a C3-6 cycloalkyl group, a C1-4 alkythio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, each independently, a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; with the proviso that when R3 and R4 represent each a hydrogen atom then R5 is not a hydrogen atom. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β or GSK3β, and cdk5/p25, such as Alzheimer disease

4. 发明申请

US20050182062A1 1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof 有权
标题翻译： 1,4-二氮杂双环[3.2.2]壬烷甲酰胺衍生物，其制备和治疗用途
公开(公告)号：US20050182062A1
公开(公告)日：2005-08-18
申请号：US11098670
申请日：2005-04-04
申请人： Frederic Galli , Patrick Lardenois , Odile Leclerc , Alistair Lochead
发明人： Frederic Galli , Patrick Lardenois , Odile Leclerc , Alistair Lochead
IPC分类号： A61K31/498 , A61K31/519 , C07D487/04 , C07D487/08 , C07D519/00
CPC分类号： C07D487/08
摘要： The present invention discloses and claims compounds of general formula in which X represents a nitrogen atom or a group of formula C—R2, P represents a group of formula C—R3, Q represents a group of formula C—R4, R represents a group of formula C—R5, W represents a group of formula C—R6, or one of the symbols P, Q, R and W represents a nitrogen atom, R1 represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or an alkyl group, R3, R4, R5 and R6 each represent a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano or amino group or other functional groups. The compounds of the invention are useful in a variety of therapeutic applications.
摘要翻译：本发明公开并要求通式的化合物，其中X表示氮原子或式CR 2的基团，P表示式CR 3的基团，Q表示式CR 4的基团，R表示式CR 5的基团，W表示式CR 6的基团，或其中之一符号P，Q，R和W表示氮原子，R 1表示氢原子或烷基，R 2表示氢原子或烷基，R R 3，R 4，R 5和R 6各自表示氢或卤素原子，或烷基，烷氧基，硝基，氨基，三氟甲基，氰基或氨基或其它官能团。本发明的化合物可用于各种治疗应用。

5. 发明授权

US5922739A 5-Naphthalen-1-yl-1,3-dioxane derivatives, preparation and therapeutical use thereof 失效
标题翻译： 5-萘-1-基-1,3-二恶烷衍生物，其制备和治疗用途
公开(公告)号：US5922739A
公开(公告)日：1999-07-13
申请号：US77710
申请日：1998-06-08
申请人： Gihad Dargazanli , Yannick Evanno , Jonathan Frost , Patrick Lardenois , Mireille Sevrin , Pascal George
发明人： Gihad Dargazanli , Yannick Evanno , Jonathan Frost , Patrick Lardenois , Mireille Sevrin , Pascal George
IPC分类号： A61K31/00 , A61K31/335 , A61K31/357 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P9/00 , A61P25/00 , C07D319/06 , C07D405/12 , A01N43/32 , A01N43/40 , C07D401/00
CPC分类号： C07D319/06
摘要： Compounds of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkylmethyl or phenyl-(C.sub.1 -C.sub.3)alkyl group optionally substituted on the phenyl ring with one or more atoms or groups chosen from halogens and methyl, trifluoromethyl, methoxy and cyano groups, R.sub.2 represents a hydroxyl or alkoxy group or a group of general formula NR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 each represent a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylmethyl group, a phenyl group, a phenylmethyl group or a pyridyl group, or alternatively R.sub.3 and R.sub.4 form, together with the nitrogen atom, a pyrrolidine or piptzidine ring, and n represents the number 1, 2 or 3.Application in therapy.
摘要翻译： PCT No.PCT / FR96 / 01926 Sec。 371日期1998年6月8日第 102（e）1998年6月8日PCT 1996年12月4日PCT PCT。出版物WO97 / 20836 日期：1997年6月12日通式（I）的化合物，其中R 1表示氢原子或（C 1 -C 4）烷基，（C 3 -C 6）环烷基甲基或苯基 - （C 1 -C 3）烷基，具有一个或多个选自卤素和甲基，三氟甲基，甲氧基和氰基的原子或基团，R 2表示羟基或烷氧基或通式NR 3 R 4的基团，其中R 3和R 4各自表示氢原子，烷基，环烷基，环烷基甲基，苯基，苯甲基或吡啶基，或者R3和R4与氮原子一起形成吡咯烷或吡啶环，n表示数字1,2或3.应用在治疗。

6. 发明授权

US08507520B2 Polysubstituted 2-aryl-6-phenylimidazo[1,2-A]pyridine derivatives, and preparation and therapeutic use thereof 有权
标题翻译：多取代2-芳基-6-苯基咪唑并[1,2-A]吡啶衍生物及其制备和治疗用途
公开(公告)号：US08507520B2
公开(公告)日：2013-08-13
申请号：US12881827
申请日：2010-09-14
申请人： Danielle De Peretti , Yannick Evanno , Patrick Lardenois , Nathalie Rakotoarisoa , Antonio Almario Garcia , André Malanda
发明人： Danielle De Peretti , Yannick Evanno , Patrick Lardenois , Nathalie Rakotoarisoa , Antonio Almario Garcia , André Malanda
IPC分类号： C07D491/02 , C07D498/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04 , C07D213/73 , C07F7/1804
摘要： Compounds of formula (I): wherein R, R1, R2, R3, R4, and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
摘要翻译：式（I）化合物：其中R，R 1，R 2，R 3，R 4和X如本公开内容所定义，或其酸加成盐，及其合成方法及其应用。

7. 发明授权

US07915284B2 2-aryl-6-phenylimidazo[1,2-a]pyridine derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译： 2-芳基-6-苯基咪唑并[1,2-a]吡啶衍生物，其制备及其治疗用途
公开(公告)号：US07915284B2
公开(公告)日：2011-03-29
申请号：US12407449
申请日：2009-03-19
申请人： Antonio Almario Garcia , Patrick Lardenois , Anne Olivier
发明人： Antonio Almario Garcia , Patrick Lardenois , Anne Olivier
IPC分类号： A61K31/437 , C07D471/04 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention is related to a compound of formula (I) wherein R1, R2, R3 and R4 are as defined herein, or an addition salt of an acid thereof, the pharmaceutical composition and preparation thereof, and the therapeutic use thereof in the treatment or the prevention of diseases involving Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.
摘要翻译：本发明涉及其中R 1，R 2，R 3和R 4如本文所定义的式（I）化合物或其酸的加成盐，其药物组合物及其制备及其在治疗中的治疗用途或预防涉及Nurr-1核受体，也称为NR4A2，NOT，TINUR，RNR-1和HZF3的疾病。

8. 发明申请

US20090054416A1 1,4-Diazabicyclo[3.2.2]nonanecarboxamide Derivatives, Preparation and Therapeutic Use Thereof 有权
标题翻译： 1,4-二氮杂双环[3.2.2]壬烷甲酰胺衍生物，其制备和治疗用途
公开(公告)号：US20090054416A1
公开(公告)日：2009-02-26
申请号：US12258483
申请日：2008-10-27
申请人： Frederic GALLI , Patrick LARDENOIS , Odile LECLERC , Alistair LOCHEAD
发明人： Frederic GALLI , Patrick LARDENOIS , Odile LECLERC , Alistair LOCHEAD
IPC分类号： A61K31/551 , C07D243/10 , A61P25/00
CPC分类号： C07D487/08
摘要： The present invention discloses and claims compounds of general formula in which X, R1, P, Q, R and W are as described herein. The compounds of the invention are useful in a variety of therapeutic applications.
摘要翻译：本发明公开并要求其中X，R 1，P，Q，R和W如本文所述的通式的化合物。本发明的化合物可用于各种治疗应用。

9. 发明授权

US07388005B2 Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders 失效
标题翻译：取代的2-嘧啶基-6,7,8,9-四氢嘧啶并[1,2-a]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑并[1,2-a]嘧啶-5（1H）神经变性疾病的衍生物
公开(公告)号：US07388005B2
公开(公告)日：2008-06-17
申请号：US10490136
申请日：2002-09-19
申请人： Thierry Gallet , Patrick Lardenois , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Thierry Gallet , Patrick Lardenois , Alistair Lochead , Séverine Marguerie , Alain Nedelec , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： A61K31/551 , A61K31/519 , C07D487/04 , A61P25/28
CPC分类号： A61K31/519 , A61K31/551 , C07D487/04
摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β3 or GSK3β3 and cdk5/p25, such as Alzheimer disease.
摘要翻译：本发明涉及由式（I）表示的嘧啶酮衍生物或其盐，其中：X表示两个氢原子，硫原子，氧原子或C 1-12烷基和氢原子; y表示键，亚乙烯基，亚乙炔基，氧原子，硫原子，磺酰基，亚砜基，羰基，任选的氮原子; 或任选取代的亚甲基; R1表示任选取代的嘧啶基团; R 2可以表示任选被C 6,10芳氧基或C 6,10芳基氨基取代的C 1-6烷基; C 3-6环烷基，C 1-4烷硫基，C 1-4烷氧基，C 1 -C 4烷氧基， 1-2个全卤代烷基，C 1-3卤代烷基，苯硫基，苄基，苯环，茚满环，5,6,7， 8-四氢萘环，萘环，吡啶环，吡咯环，噻吩环，呋喃环或咪唑环; R 3和R 4各自独立地表示氢原子，C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R5表示氢原子，C 1-6烷基或卤素原子。本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β3或GSK3β3和cdk5 / p25的异常活性引起的神经变性疾病，例如阿尔茨海默病。

10. 发明申请

US20070021405A1 ARYL- AND HETEROARYLPIPERIDINECARBOXYLATE-DERIVATIVES METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开
标题翻译： ARYL-和异二氢吡啶羧酸酯衍生物的制备方法及其作为脂肪酸氨基水解酶酶抑制剂的用途
公开(公告)号：US20070021405A1
公开(公告)日：2007-01-25
申请号：US11465238
申请日：2006-08-17
申请人： Ahmed ABOUABDELLAH , Antonio ALMARIO GARCIA , Christian HOORNAERT , Patrick LARDENOIS , Frank MARGUET
发明人： Ahmed ABOUABDELLAH , Antonio ALMARIO GARCIA , Christian HOORNAERT , Patrick LARDENOIS , Frank MARGUET
IPC分类号： C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D471/04 , C07D207/06 , C07D211/16 , C07D211/52 , C07D401/04 , C07D401/06
摘要： The present invention comprises compounds corresponding to the general formula (I): in which m, n=1 to 3 and m+n=2 to 5; p=1 to 7; A=single bond or X, Y and/or Z; X=optionally substituted methylene; Y=C2-alkenylene, which is optionally substituted, or C2-alkynylene; Z=C3-7-cycloalkyl; R1 represents a group of aryl or heteroaryl type; R2 represents a hydrogen or fluorine atom or a hydroxyl, C1-6-alkoxy or NR8R9 group; R3 represents a hydrogen atom or a C1-6-alkyl group; R4 represents a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-3-alkyl group; in the base form or in the form of an addition salt with an acid, of a hydrate or of a solvate. The compounds are useful in the treatment of a number of diseases and/or pathological conditions such as chronic pain, dizziness, vomiting, nausea, eating disorders, neurological and psychiatric pathologies, acute or chronic neurodegenerative diseases, epilepsy, sleep disorders, cardiovascular diseases, renal ischaemia, cancers, disorders of the immune system, allergic diseases, parasitic, viral or bacterial infectious diseases, inflammatory diseases, osteoporosis, eye conditions, pulmonary conditions, gastrointestinal diseases or urinary incontinence.
摘要翻译：本发明包括对应于通式（I）的化合物：其中m，n = 1至3，m + n = 2至5; p = 1〜7; A =单键或X，Y和/或Z; X =任选取代的亚甲基; Y = C 2 - 亚烯基，其任选被取代，或C 2 - 亚炔基; Z = C 3-7 - 环烷基; R 1表示芳基或杂芳基的基团; R 2表示氢或氟原子或羟基，C 1-6 - 烷氧基或NR 8 R 9 >组 R 3表示氢原子或C 1-6 - 烷基; R 4表示氢原子或C 1-6 - 烷基，C 3-7 - 环烷基或C 3-7 环烷基-C 1-3 - 烷基; 以碱的形式或与酸的加成盐，水合物或溶剂化物的形式。这些化合物可用于治疗许多疾病和/或病理状况，例如慢性疼痛，头晕，呕吐，恶心，进食障碍，神经和精神病理学，急性或慢性神经变性疾病，癫痫症，睡眠障碍，心血管疾病，肾缺血，癌症，免疫系统疾病，过敏性疾病，寄生虫，病毒或细菌感染性疾病，炎性疾病，骨质疏松症，眼睛条件，肺部疾病，胃肠道疾病或尿失禁。

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