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公开(公告)号：US20090233943A9
公开(公告)日：2009-09-17
申请号：US12120608
申请日：2008-05-14
申请人： Jeremy Nicholas Burrows , Sven Hellberg , Katharina Hogdin , Sofia Karlstrom , Karin Kolmodin , Johan Lindstrom , Can Slivo
发明人： Jeremy Nicholas Burrows , Sven Hellberg , Katharina Hogdin , Sofia Karlstrom , Karin Kolmodin , Johan Lindstrom , Can Slivo
IPC分类号： A61K31/497 , C07D233/90 , A61K31/4168 , C07D403/10 , A61K31/506 , C07D401/10 , A61K31/4439
CPC分类号： C07D401/10 , C07D233/86 , C07D233/88 , C07D403/10 , C07D417/10
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译： 本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。 这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。
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公开(公告)号：US06552225B1
公开(公告)日：2003-04-22
申请号：US10069880
申请日：2002-06-17
申请人： Roger John Butlin , Janet Elizabeth Pease , Michael Howard Block , Thorsten Nowak , Jeremy Nicholas Burrows
发明人： Roger John Butlin , Janet Elizabeth Pease , Michael Howard Block , Thorsten Nowak , Jeremy Nicholas Burrows
IPC分类号： A61K3140
CPC分类号： C07D213/76 , C07C311/46 , C07C323/67 , C07C2601/14 , C07D207/12 , C07D211/46 , C07D295/26
摘要： A compound of formula (I) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
摘要翻译： 式（I）的化合物，其中：R 1，R 2，R 3，R 4，R 5，R 6和R 7如所定义; 或其药学上可接受的盐或体内可水解的酯。 还描述了在温血动物如人中产生式（I）化合物在产生PDH活性升高中的用途。 详细描述了制备式（I）化合物的药物组合物，方法和方法。
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公开(公告)号：US20100267723A1
公开(公告)日：2010-10-21
申请号：US12759869
申请日：2010-04-14
IPC分类号： A61K31/5377 , C07D413/14 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/24
CPC分类号： C07D405/14 , A61K31/5377 , C07D413/14
摘要： A compound of formula (I) wherein R1 is hydrogen or fluoro; R2 and R3 are independently selected from hydrogen or methyl, or a pharmaceutically acceptable salt thereof; pharmaceutical formulations containing said compound; the use of said compound in therapy; the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as methods of treatment of said disorders, comprising administering to subjects in need of such treatment, a therapeutically effective amount of said compound.
摘要翻译： 式（I）的化合物，其中R 1是氢或氟; R2和R3独立地选自氢或甲基，或其药学上可接受的盐; 含有所述化合物的药物制剂; 所述化合物在治疗中的用途; 用于治疗与糖原合酶激酶-3相关病症（例如阿尔茨海默病）相关的病症的用途以及治疗所述病症的方法，包括向需要这种治疗的受试者施用治疗有效量的所述化合物。
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公开(公告)号：US08178529B2
公开(公告)日：2012-05-15
申请号：US12759869
申请日：2010-04-14
IPC分类号： A61K31/506 , C07D413/14
CPC分类号： C07D405/14 , A61K31/5377 , C07D413/14
摘要： Imidazole substituted pyrimidines and pharmaceutically acceptable salts thereof; pharmaceutical formulations containing such pyrimidines; the use of such compounds in therapy; the use of such compounds for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as methods of treatment of such disorders comprising administering to subjects in need of such treatment therapeutically effective amounts of such compounds.
摘要翻译： 咪唑取代嘧啶及其药学上可接受的盐; 含有此类嘧啶的药物制剂; 这种化合物在治疗中的应用; 使用这些化合物来治疗与糖原合酶激酶-3相关疾病（例如阿尔茨海默氏病）相关的病症，以及治疗这种病症的方法，包括向需要这种治疗的受试者施用治疗有效量的这些化合物。
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5.发明申请Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease 审中-公开用于治疗糖原合酶激酶-3相关疾病如阿尔茨海默病的咪唑取代嘧啶公开(公告)号：US20120077813A1
公开(公告)日：2012-03-29
申请号：US13264529
申请日：2010-04-14
IPC分类号： A61K31/5377 , A61P25/24 , A61P25/28 , A61P25/18 , A61P31/14 , A61P25/16 , A61P3/00 , A61P31/00 , C07D413/14 , A61P25/00
CPC分类号： C07D405/14 , A61K31/5377 , C07D413/14
摘要： The present invention relates to a new compound of formula (I) wherein R1 is hydrogen or fluoro; R2 and R3 are independently selected from hydrogen or methyl; or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, to the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as for the method of treatment of said disorders, comprising administering to a mammal, including human in need of such treatment, a therapeutically effective amount of said compound.
摘要翻译： 本发明涉及新的式（I）化合物，其中R 1是氢或氟; R2和R3独立地选自氢或甲基; 或其药学上可接受的盐，含有所述化合物的药物制剂，以使用所述活性化合物在治疗中，用于治疗与糖原合酶激酶3相关病症如阿尔茨海默病相关的病症的用途，以及 治疗所述疾病的方法，包括向需要这种治疗的哺乳动物，包括给予治疗有效量的所述化合物施用。
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公开(公告)号：US20080287460A1
公开(公告)日：2008-11-20
申请号：US12120608
申请日：2008-05-14
申请人： Jeremy Nicholas Burrows , Sven Hellberg , Katharina Hogdin , Sofia Karlstrom , Karin Kolmodin , Johan Lindstrom , Can Slivo
发明人： Jeremy Nicholas Burrows , Sven Hellberg , Katharina Hogdin , Sofia Karlstrom , Karin Kolmodin , Johan Lindstrom , Can Slivo
IPC分类号： A61K31/497 , C07D233/90 , A61K31/4168 , C07D403/10 , A61K31/506 , C07D401/10 , A61K31/4439
CPC分类号： C07D401/10 , C07D233/86 , C07D233/88 , C07D403/10 , C07D417/10
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译： 本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。 这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。
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公开(公告)号：US06878712B1
公开(公告)日：2005-04-12
申请号：US10069995
申请日：2000-08-30
申请人： Roger John Butlin , Janet Elizabeth Pease , Michael Howard Block , Thorsten Nowak , Jeremy Nicholas Burrows , David Stephen Clarke
发明人： Roger John Butlin , Janet Elizabeth Pease , Michael Howard Block , Thorsten Nowak , Jeremy Nicholas Burrows , David Stephen Clarke
IPC分类号： C07D295/18 , A61K31/404 , A61K31/4468 , A61K31/495 , A61P3/06 , A61P3/10 , A61P9/10 , C07D209/08 , C07D211/32 , C07D211/58 , C07D241/04 , C07D295/185 , C07D295/192 , C07D295/22 , C07D295/26 , A61K31/496 , C07D295/16 , C07D409/12
CPC分类号： C07D295/185 , C07D209/08 , C07D211/32 , C07D211/58 , C07D295/192 , C07D295/26
摘要： A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independently C1-3alkyl optionally substituted by fluoro or chloro; or R1 and R2 together with the carbon atom to which they are attached, form a C3-5cycloalkyl ring optionally substituted by fluoro; R3 is defined within; and n is 0-5; wherein the values of R3 may be the same or different; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
摘要翻译： 式（I）化合物：其中：环A是如在其中所定义的氮连接的单环或双环杂环; R 1和R 2独立地是任选被氟或氯取代的C 1-3烷基;或R 1 >和R 2与它们所连接的碳原子一起形成任选被氟取代的C 3-5环烷基环; R 3定义在其中; andn是0-5; 其中R 3的值可以相同或不同;或其药学上可接受的盐或其体内可水解的酯。 还描述了在温血动物如人中产生式（I）化合物在产生PDH活性升高中的用途。 详细描述了制备式（I）化合物的药物组合物，方法和方法。
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8.发明授权Substituted N-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity 失效提取丙酮酸脱氢酶活性的取代的N-苯基2-羟基-2-甲基-3,3,3-三氟丙酰胺衍生物公开(公告)号：US06689909B1
公开(公告)日：2004-02-10
申请号：US10069994
申请日：2002-06-17
申请人： Roger John Butlin , Janet Elizabeth Pease , Michael Howard Block , Thorsten Nowak , Jeremy Nicholas Burrows
发明人： Roger John Butlin , Janet Elizabeth Pease , Michael Howard Block , Thorsten Nowak , Jeremy Nicholas Burrows
IPC分类号： C07C23305
CPC分类号： C07D295/185 , C07C317/42 , C07C317/44 , C07C317/50 , C07C323/65 , C07D295/135
摘要： A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
摘要翻译： 式（I）的化合物，其中：n为1或2; R 1是氯，氟，溴，甲基或甲氧基; R 2定义如下： R 3如上所定义; 和R 4是氢或氟; 或其药学上可接受的盐或体内可水解的酯。 还描述了在温血动物如人中产生式（I）化合物在产生PDH活性升高中的用途。 详细描述了制备式（I）化合物的药物组合物，方法和方法。
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