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公开(公告)号：US09446044B2
公开(公告)日：2016-09-20
申请号：US14238925
申请日：2012-08-17
IPC分类号： A61K31/5377 , C07D513/04 , A61K31/519 , C07C271/28 , C07D277/68 , C07C219/04 , C07D277/64
CPC分类号： A61K31/519 , A61K31/5377 , C07C219/04 , C07C271/28 , C07D277/64 , C07D277/68 , C07D513/04
摘要： The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.
摘要翻译： 本发明涉及新颖的噻唑并[5,4-f]喹唑啉化合物和可用于改善，治疗或控制唐氏综合征或早期阿尔茨海默氏病或改善，治疗或控制癌症尤其是实体瘤的方法。 更具体地说，本发明涉及DYRK1A和/或DYRK1B抑制剂及其制备方法。
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公开(公告)号：US20140275064A1
公开(公告)日：2014-09-18
申请号：US14238925
申请日：2012-08-17
IPC分类号： C07D513/04 , C07D277/64 , A61K31/519 , A61K31/5377 , C07C219/04
CPC分类号： A61K31/519 , A61K31/5377 , C07C219/04 , C07C271/28 , C07D277/64 , C07D277/68 , C07D513/04
摘要： The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.
摘要翻译： 本发明涉及新颖的噻唑并[5,4-f]喹唑啉化合物和可用于改善，治疗或控制唐氏综合征或早期阿尔茨海默氏病或改善，治疗或控制癌症尤其是实体瘤的方法。 更具体地说，本发明涉及DYRK1A和/或DYRK1B抑制剂及其制备方法。
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13.发明申请SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS 审中-公开取代的异喹啉及其作为管状体聚合抑制剂的用途公开(公告)号：US20130131018A1
公开(公告)日：2013-05-23
申请号：US13701917
申请日：2011-06-01
申请人： Bertrand Leblond , Thierry Taverne , Eric Beausoleil , Cédric Chauvignac , Anne-Sophie Casagrande , Laurent Desire
发明人： Bertrand Leblond , Thierry Taverne , Eric Beausoleil , Cédric Chauvignac , Anne-Sophie Casagrande , Laurent Desire
IPC分类号： C07D217/20 , A61K31/437 , A61K31/472 , A61K45/06 , C07D498/04 , C07D401/10 , C07D405/10 , A61K31/4725 , A61K31/675 , C07F9/62
CPC分类号： C07D217/20 , A61K31/437 , A61K31/472 , A61K31/4725 , A61K31/675 , A61K45/06 , C07D401/10 , C07D405/10 , C07D407/06 , C07D498/04 , C07F9/62
摘要： The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
摘要翻译： 本发明一般涉及取代的异喹啉及其作为微管蛋白聚合抑制剂的用途。 特别地，本发明涉及具有有用治疗活性的取代的异喹啉，这些化合物在治疗方法中的用途以及制备药物以及含有这些化合物的组合物。
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14.发明申请公开(公告)号：US20070142277A1
公开(公告)日：2007-06-21
申请号：US10578493
申请日：2004-11-05
申请人： Laurent Desire
发明人： Laurent Desire
CPC分类号： C12N9/6421 , A61K38/00
摘要： The present invention relates generally to the fields of genetics, biochemistry, medicinal chemistry and medicine. The present invention more particularly discloses the identification of a human gene variant involved in neuropathological conditions, and methods for the diagnosis, prevention and treatment of such diseases and related disorders, as well as for the screening of therapeutically active drugs. The present invention relates to catalytically active beta-secretase (Memapsin2, BACE) variants, and nucleic acids encoding them. The invention is useful in the identification of agents that inhibit the activity of a particular BACE isoform and thus agents and therapies affecting the genesis, development or progression of neuropathological conditions, including Alzheimer's disease and dementia.
摘要翻译： 本发明一般涉及遗传学，生物化学，药物化学和医学领域。 本发明更具体地公开了鉴定涉及神经病理学病症的人基因变体，以及用于诊断，预防和治疗这些疾病和相关疾病以及用于筛选治疗活性药物的方法。 本发明涉及催化活性β-分泌酶（Memapsin2，BACE）变体和编码它们的核酸。 本发明可用于鉴定抑制特定BACE同种型的活性的药剂，因此可用于影响神经病理学病症（包括阿尔茨海默病和痴呆）的发生，发展或进展的药剂和疗法。
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