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1. 发明申请

US20110065727A1 POLYSUBSTITUTED DERIVATIVES OF 2-HETEROARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF 有权
标题翻译： 2-异丙基-6-苯基咪唑并[1,2-a]吡啶的多取代衍生物及其制备及其治疗用途
公开(公告)号：US20110065727A1
公开(公告)日：2011-03-17
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： A61K31/444 , C07D471/04 , A61K31/4709 , A61K31/4725 , A61K31/506 , C07F7/18 , C07F5/04 , C07D213/73 , A61P25/00 , A61P25/30 , A61P25/18 , A61P25/24 , A61P35/00 , A61P19/10 , A61P29/00 , A61P25/28 , A61P25/16
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如本发明所定义，或其酸加成盐，以及其合成用途和方法。

2. 发明申请

US20110065745A1 POLYSUBSTITUTED 2-ARYL-6-PHENYLIMIDAZO[1,2-A]PYRIDINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF 有权
标题翻译：多取代的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：US20110065745A1
公开(公告)日：2011-03-17
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 , Andre MALANDA
发明人： Danielle DE PERETTI , Yannick EVANNO , Patrick LARDENOIS , Nathalie RAKOTOARISOA , Antonio ALMARIO GARCIA , Andre MALANDA
IPC分类号： A61K31/437 , C07D471/04 , A61P25/08 , A61P29/00 , A61P35/00 , A61P19/10 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/16 , A61P25/18 , C07D213/73 , C07F7/18
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。

3. 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。

4. 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。

5. 发明申请

US20070167461A1 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-6,7,8,9-四氢吡啶并[1,2-a]嘧啶-4-酮和7-吡啶-2,3-二氢吲哚并[1,2-a]吡啶-5（1H，）一种衍生物作为治疗剂
公开(公告)号：US20070167461A1
公开(公告)日：2007-07-19
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： A61K31/519
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。

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