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公开(公告)号：US20060211730A1
公开(公告)日：2006-09-21
申请号：US11377886
申请日：2006-03-16
申请人： Jeremy Levin , Zhong Li , George Diamantidis , Frank Lovering , Weiheng Wang , Jeffrey Condon , Yang-I Lin , Jerauld Skotnicki , Kaapjoo Park
发明人： Jeremy Levin , Zhong Li , George Diamantidis , Frank Lovering , Weiheng Wang , Jeffrey Condon , Yang-I Lin , Jerauld Skotnicki , Kaapjoo Park
IPC分类号： A61K31/4709 , C07D403/02 , C07D405/02
CPC分类号： C07D215/04 , C07D235/12 , C07D249/18 , C07D271/12 , C07D401/12 , C07D405/12
摘要： This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-α, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.
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2.发明授权Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders 失效雷帕霉素类似物及其在治疗神经，增殖和炎性疾病中的用途公开(公告)号：US07560457B2
公开(公告)日：2009-07-14
申请号：US11698504
申请日：2007-01-26
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18 , C07D491/14 , C07D498/22
摘要： The present invention provides compounds of the following structure, wherein R1, R2, R4, R4′, R6, R7, and R15 are defined above: These compounds are useful in treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders. The compounds are therefore useful as neuroprotective and neuroregenerative, anti-proliferative, and anti-inflammatory agents.
摘要翻译： 本发明提供以下结构的化合物，其中R 1，R 2，R 4，R 4'，R 6，R 7和R 15如上所定义：这些化合物可用于治疗由卒中或头部损伤引起的神经系统疾病或并发症; 良性或恶性肿瘤性疾病，癌和腺癌; 增生性疾病; 和炎症性疾病。 因此，这些化合物可用作神经保护和神经再生，抗增殖和抗炎剂。
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3.发明申请Rapamycin derivatives and the uses thereof in the treatment of neurological disorders 失效雷帕霉素衍生物及其用于治疗神经障碍的用途公开(公告)号：US20060135550A1
公开(公告)日：2006-06-22
申请号：US11300941
申请日：2005-12-15
申请人： Edmund Graziani , Kevin Pong , Jerauld Skotnicki
发明人： Edmund Graziani , Kevin Pong , Jerauld Skotnicki
IPC分类号： C07D491/14 , A61K31/4745
CPC分类号： C07D498/18
摘要： The present invention provides compounds of the following structure, wherein R1-R9, R15, and n are defined herein. These compounds are useful in treating neurological disorders or complications due to stroke or head injury, and as neuroprotective and neuroregenerative agents.
摘要翻译： 本发明提供下列结构的化合物，其中R 1 -R 9，R 15和n如本文所定义。 这些化合物可用于治疗由于中风或头部损伤引起的神经系统疾病或并发症，以及作为神经保护和神经再生剂。
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4.发明授权Rapamycin analogues and uses thereof in the treatment of neurological disorders 失效雷帕霉素类似物及其在神经障碍治疗中的用途公开(公告)号：US07276498B2
公开(公告)日：2007-10-02
申请号：US11300839
申请日：2005-12-15
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18 , C07D491/14 , C07D498/22
摘要： The present invention provides compounds of the following structure, wherein R1, R2, R4, R4′, R6, R7, and R15 are defined above: These compounds are useful in treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders. The compounds are therefore useful as neuroprotective and neuroregenerative, anti-proliferative, and anti-inflammatory agents.
摘要翻译： 本发明提供下列结构的化合物，其中R 1，R 2，R 4，R 4'，或 >，R 6，R 7和R 15定义如上：这些化合物可用于治疗由于中风或神经系统疾病引起的神经障碍或并发症 头部受伤; 良性或恶性肿瘤性疾病，癌和腺癌; 增生性疾病; 和炎症性疾病。 因此，这些化合物可用作神经保护和神经再生，抗增殖和抗炎剂。
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5.发明授权Rapamycin derivatives and the uses thereof in the treatment of neurological disorders 失效雷帕霉素衍生物及其用于治疗神经障碍的用途公开(公告)号：US07273874B2
公开(公告)日：2007-09-25
申请号：US11300941
申请日：2005-12-15
IPC分类号： C07D498/18 , A61K31/435
CPC分类号： C07D498/18
摘要： The present invention provides compounds of the following structure, wherein R1-R9, R15, and n are defined herein. These compounds are useful in treating neurological disorders or complications due to stroke or head injury, and as neuroprotective and neuroregenerative agents.
摘要翻译： 本发明提供下列结构的化合物，其中R 1 -R 9，R 15和n如本文所定义。 这些化合物可用于治疗由于中风或头部损伤引起的神经系统疾病或并发症，以及作为神经保护和神经再生剂。
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6.发明授权Rapamycin derivatives and the uses thereof in the treatment of neurological disorders 失效雷帕霉素衍生物及其用于治疗神经障碍的用途公开(公告)号：US07476678B2
公开(公告)日：2009-01-13
申请号：US11891879
申请日：2007-08-14
IPC分类号： A61K31/435
CPC分类号： C07D498/18
摘要： Pharmaceutical composition containing compounds of the following structure, wherein R1-R9, R15, and n are defined herein, are provided. These compositions are useful in treating neurological disorders or complications due to stroke or head injury, and as neuroprotective and neuroregenerative agents.
摘要翻译： 提供含有下列结构的化合物的药物组合物，其中R1-R9，R15和n在本文中定义。 这些组合物可用于治疗由于卒中或头部损伤引起的神经障碍或并发症，以及作为神经保护和神经再生剂。
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7.发明申请公开(公告)号：US20080097093A1
公开(公告)日：2008-04-24
申请号：US11974831
申请日：2007-10-16
申请人： Jerauld Skotnicki
发明人： Jerauld Skotnicki
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： Processes for preparing individual diastereomers of mono-pegylated rapamycin 42 ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) are provided.
摘要翻译： 提供了用3-羟基-2-（羟甲基）-2-甲基丙酸（CCI-779）制备单聚乙二醇化雷帕霉素42酯的单独非对映异构体的方法。
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8.发明申请Rapamycin derivatives and the uses thereof in the treatment of neurological disorders 失效雷帕霉素衍生物及其用于治疗神经障碍的用途公开(公告)号：US20080027089A1
公开(公告)日：2008-01-31
申请号：US11891879
申请日：2007-08-14
申请人： Edmund Graziani , Kevin Pong , Jerauld Skotnicki
发明人： Edmund Graziani , Kevin Pong , Jerauld Skotnicki
IPC分类号： A61K31/4353 , A61P25/28
CPC分类号： C07D498/18
摘要： Pharmaceutical composition containing compounds of the following structure, wherein R1-R9, R15, and n are defined herein, are provided. These compositions are useful in treating neurological disorders or complications due to stroke or head injury, and as neuroprotective and neuroregenerative agents.
摘要翻译： 提供含有下列结构的化合物的药物组合物，其中R 1〜R 9，R 15和n如本文所定义。 这些组合物可用于治疗由于卒中或头部损伤引起的神经障碍或并发症，以及作为神经保护和神经再生剂。
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9.发明申请Rapamycin Analogues and the Uses Thereof in the Treatment of Neurological, Proliferative, and Inflammatory Disorders 失效雷帕霉素类似物及其在治疗神经，增生和炎症疾病中的应用公开(公告)号：US20090239855A1
公开(公告)日：2009-09-24
申请号：US12481211
申请日：2009-06-09
IPC分类号： A61K31/5383 , C07D491/22 , A61P25/00
CPC分类号： C07D498/18 , C07D491/14 , C07D498/22
摘要： The present invention provides for methods of treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders using compounds of the following structure: The compounds are therefore useful as neuroprotective and neuroregenerative, anti-proliferative, and anti-inflammatory agents.
摘要翻译： 本发明提供治疗由于卒中或头部损伤引起的神经障碍或并发症的方法; 良性或恶性肿瘤性疾病，癌和腺癌; 增生性疾病; 和炎症性疾病，使用以下结构的化合物：因此，化合物可用作神经保护和神经再生，抗增殖和抗炎剂。
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10.发明申请Rapamycin Analogues and the Uses Thereof in the Treatment of Neurological Disorders 审中-公开雷帕霉素类似物及其在神经障碍治疗中的应用公开(公告)号：US20090203682A1
公开(公告)日：2009-08-13
申请号：US12276668
申请日：2008-11-24
IPC分类号： A61K31/5365 , A61P25/00
CPC分类号： C07D498/18 , C07D491/14 , C07D498/22
摘要： Method of treatment of neurological disorders or complications due to stroke or head injury through the administration of a pharmaceutical composition including a pharmaceutically acceptable excipient or carrier and a compound of formula I are provided:
摘要翻译： 提供了通过施用包含药学上可接受的赋形剂或载体和式I化合物的药物组合物治疗由中风或头部损伤导致的神经障碍或并发症的方法：
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