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51. 发明申请

US20060025431A1 Substituted 8'-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one derivatives 失效
标题翻译：取代的8'-吡啶基 - 二氢螺 - [环烷基] - 嘧啶并[1,2-a]嘧啶-6-酮和8'-嘧啶基 - 二氢螺 - [环烷基] - 嘧啶并[1,2-a]嘧啶-6-酮衍生品
公开(公告)号：US20060025431A1
公开(公告)日：2006-02-02
申请号：US11220999
申请日：2005-09-07
申请人： Pascal George , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
发明人： Pascal George , Alistair Lochead , Mourad Saady , Franck Slowinski , Philippe Yaiche
IPC分类号： A61K31/519 , C07D487/10
CPC分类号： C07D487/10
摘要： The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. 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, such as Alzheimer disease.
摘要翻译：本发明涉及由式（I）表示的二氢螺环 - [环烷基] - 嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，m，n，p和q如本文所述。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，所述活性成分用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

52. 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。

53. 发明授权

US4914092A Benzothiazepin-4-one derivatives, their preparation and their application in therapy 失效
标题翻译：苯并硫氮杂-4-酮衍生物，其制备及其在治疗中的应用
公开(公告)号：US4914092A
公开(公告)日：1990-04-03
申请号：US339978
申请日：1989-04-18
申请人： Alistair Lochead , Jean C. Muller , Colombe Denys , Andre Dumas
发明人： Alistair Lochead , Jean C. Muller , Colombe Denys , Andre Dumas
IPC分类号： A61K31/55 , A61K31/554 , A61P3/00 , A61P3/14 , A61P9/08 , A61P25/02 , C07D281/10 , C07D417/12
CPC分类号： C07D417/12 , C07D281/10
摘要： A compound, in the form of a pure diastereoisomer or mixture thereof, which is a benzothiazepin-4-one derivative of formula (I): ##STR1## in which: R1 is hydrogen or a C.sub.2 -C.sub.4 alkanoyl group;R2 and R3 independently each is hydrogen, a linear or branched C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.5 cycloalkyl group, a phenyl group, a benzyl group or a phenethyl group, or R2 and R3 together form, with the nitrogen atom to which they are attached, a pyrrolidinyl, 2,2-dimethylpyrrolidinyl, piperidyl, 4-phenylpiperidyl, 4-(3-methoxyphenyl)piperidyl, 4-(4-fluorobenzoyl)piperidyl, 1,2,3,6-tetrahydropyridyl, perhydroazepinyl, perhydroazocinyl, 1,3-thiazolidinyl, thiomorpholinyl, morpholinyl, 2,3-dihydroindolyl, 1,2,3,4-tetrahydroisoquinolyl, 6-methoxy-1,2,3,4-tetrahydroisoquinolyl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolyl or 2,3,4,5-tetrahydro-1H-benz[b]azepinyl group; andX is hydrogen or chlorine;or a pharmacologically acceptable acid addition salt thereof.
摘要翻译：化合物，其为纯的非对映异构体或其混合物，其为式（I）的苯并硫氮杂-4-酮衍生物：其中：R 1为氢或C 2 -C 4烷酰基; R 2和R 3各自独立地为氢，直链或支链C 1 -C 4烷基，C 3 -C 5环烷基，苯基，苄基或苯乙基，或R 2和R 3一起与其中的氮原子一起形成吡咯烷基，2,2-二甲基吡咯烷基，哌啶基，4-苯基哌啶基，4-（3-甲氧基苯基）哌啶基，4-（4-氟苯甲酰基）哌啶基，1,2,3,6-四氢吡啶基，全氢化吖嗪基，，1,3-噻唑烷二基，硫代吗啉基，吗啉基，2,3-二氢吲哚基，1,2,3,4-四氢异喹啉，6-甲氧基-1,2,3,4-四氢异喹啉，6,7-二甲氧基-1,2 3,4-四氢异喹啉基或2,3,4,5-四氢-1H-苯并[b]吖庚因基; X为氢或氯; 或其药理学上可接受的酸加成盐。

54. 发明授权

US09073914B2 Substituted alkyl pyrimidin-4-one derivatives 有权
标题翻译：取代的烷基嘧啶-4-酮衍生物
公开(公告)号：US09073914B2
公开(公告)日：2015-07-07
申请号：US12968868
申请日：2010-12-15
申请人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
发明人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00 , C07D239/70 , C07D471/04 , A61K31/517 , C07D487/04
CPC分类号： C07D471/04 , A61K31/517 , A61K31/519 , C07D487/04 , Y02A50/411
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物：其中X，R 1，R 2，R 3，R 4和m如本公开所定义。还公开了制备式（I）化合物，其中间体及其在治疗中的用途的方法。

55. 发明授权

US08598187B2 Arylamide pyrimidone compounds 有权
标题翻译：芳酰胺嘧啶酮化合物
公开(公告)号：US08598187B2
公开(公告)日：2013-12-03
申请号：US12606662
申请日：2009-10-27
申请人： Alistair Lochead , Mourad Saady , Corinne Veronique , Philippe Yaiche
发明人： Alistair Lochead , Mourad Saady , Corinne Veronique , Philippe Yaiche
IPC分类号： C07D403/04 , A61K31/495
CPC分类号： C07D403/04 , A61K9/0019 , A61K9/2018 , A61K9/4858 , C07D413/14 , Y02A50/411
摘要： The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
摘要翻译：本发明公开了一系列由式（I）表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中X，Z，R1，R2，R3，R4，R5，R6，R7，n和 m如本文所定义。本文还公开了制备式（I）化合物，其中间体及其在治疗各种疾病状况中的用途的方法。

56. 发明授权

US08592580B2 Substituted triazinone derivatives 有权
标题翻译：取代的三嗪酮衍生物
公开(公告)号：US08592580B2
公开(公告)日：2013-11-26
申请号：US12968935
申请日：2010-12-15
申请人： Alistair Lochead , Mourad Saady , Philippe Yaiche
发明人： Alistair Lochead , Mourad Saady , Philippe Yaiche
IPC分类号： C07D401/04 , C07D487/04 , A61K31/53 , A61P3/04 , A61P3/10 , A61P25/18 , A61P25/28
CPC分类号： C07D401/04 , C07D487/04
摘要： Triazinone derivatives represented by formula (I) wherein: Z, R1, R2, R3, R4, and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
摘要翻译：由式（I）表示的三嗪酮衍生物其中：Z，R1，R2，R3，R4和n如本公开所定义。还公开了制备式（I）化合物及其在治疗中的用途的方法。

57. 发明授权

US08507475B2 Substituted heteroarylamide diazepinopyrimidone derivatives 有权
标题翻译：取代的杂芳基酰胺二氮杂吡啶并吡啶酮衍生物
公开(公告)号：US08507475B2
公开(公告)日：2013-08-13
申请号：US12844273
申请日：2010-07-27
申请人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
发明人： Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
IPC分类号： A61P3/00 , A61P25/00 , A61P35/00 , A61K31/551 , C07D487/02
CPC分类号： C07D487/04 , C07D519/00
摘要： The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
摘要翻译：本发明涉及由式（I）表示的一系列嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中：Y，Z，R 1，R 2，R 3，R 4，R 5和n如披露还公开了制备式（I）化合物，其中间体及其在治疗各种疾病状况中的用途的方法。

58. 发明授权

US08211903B2 Substituted pyrimido isoquinoline derivatives 有权
标题翻译：取代的嘧啶异喹啉衍生物
公开(公告)号：US08211903B2
公开(公告)日：2012-07-03
申请号：US12968950
申请日：2010-12-15
申请人： Alistair Lochead , Mourad Saady , Philippe Yaiche
发明人： Alistair Lochead , Mourad Saady , Philippe Yaiche
IPC分类号： A01N43/54 , A61K31/505 , C07D239/70 , C07D471/00
CPC分类号： A01N43/54 , C07D471/04
摘要： Pyrimido isoquinoline derivatives represented by formula (I): wherein: R1, R2, R3, R4, R7, R8, R9, R10, and are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
摘要翻译：由式（I）表示的嘧啶异喹啉衍生物：其中：R1，R2，R3，R4，R7，R8，R9，R10，如本公开中所定义。还公开了制备式（I）化合物及其在治疗中的用途的方法。

59. 发明授权

US08198287B2 Substituted heteroaryl pyridopyrimidone derivatives 有权
标题翻译：取代的杂芳基吡啶并嘧啶衍生物
公开(公告)号：US08198287B2
公开(公告)日：2012-06-12
申请号：US12487270
申请日：2009-06-18
申请人： Aude Fayol , Thierry Gallet , Alistair Lochead , Mourad Saady , Corinne Veronique , Philippe Yaiche
发明人： Aude Fayol , Thierry Gallet , Alistair Lochead , Mourad Saady , Corinne Veronique , Philippe Yaiche
IPC分类号： A01N43/90 , A61K31/519 , C07D239/70
CPC分类号： A01N43/90 , C07D239/70
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). 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, such as Alzheimer disease.
摘要翻译：公开并要求保护由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物。其中m，n，o，Y，Z，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。还公开了式（I）化合物的盐。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GSK3和bgr的异常活性如阿尔茨海默病引起的神经退行性疾病。

60. 发明申请

US20110319381A1 DERIVATIVES OF AZASPIRANYL-ALKYLCARBAMATES OF 5-MEMBER HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 有权
标题翻译： 5-甲基杂环化合物的AZASPIRANYL-ALKYLCARBAMATES的衍生物，其制备方法及其治疗用途
公开(公告)号：US20110319381A1
公开(公告)日：2011-12-29
申请号：US13145926
申请日：2010-02-04
申请人： Ahmed Abouabdellah , Nathalie Chereze , Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
发明人： Ahmed Abouabdellah , Nathalie Chereze , Aude Fayol , Alistair Lochead , Mourad Saady , Julien Vache , Philippe Yaiche
IPC分类号： A61K31/4439 , C07D413/14 , A61K31/4709 , A61K31/444 , A61K31/506 , A61K31/497 , A61P29/00 , A61P1/08 , A61P25/00 , A61P25/28 , A61P37/00 , A61P1/00 , A61P35/00 , A61P31/00 , A61P33/00 , A61P9/10 , C07D417/14
CPC分类号： C07D417/14 , C07D413/14
摘要： The invention relates to a compound of the general formula (I) in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, NR8R9 group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-member heterocyclic compound; the compound being in the form of a base or acid addition salt. The invention also relates to the therapeutic use thereof.
摘要翻译：本发明涉及其中R 2为氢或氟原子或羟基，氰基，三氟甲基，C 1-6 - 烷基，C 1-6 - 烷氧基，NR 8 R 9基团的通式（I）的化合物; m，n，o和p独立地为等于0,1,2或3的整数; A是共价键或C 1-8亚烷基; R1是任选取代的芳基或杂芳基; R3是氢或氟原子或C1-6烷基或三氟甲基; R4是任选取代的5元杂环化合物; 该化合物为碱或酸加成盐的形式。本发明还涉及其治疗用途。

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