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公开(公告)号：EP2516441B1
公开(公告)日：2015-01-21
申请号：EP10798439.5
申请日：2010-12-21
发明人： GALEMMO, Robert, A., Jr. , ARTIS, Dean Richard , YE, Xiaocong Michael , AUBELE, Danielle, L. , TRUONG, Anh, P. , BOWERS, Simeon , HOM, Roy, K. , ZHU, Yong-Liang , NEITZ, R., Jeffrey , SEALY, Jennifer , ADLER, Marc , BEROZA, Paul , ANDERSON, John, P.
IPC分类号： C07D475/04 , C07D475/12 , A61K31/4985 , A61P25/00
CPC分类号： C07D475/00 , A61K31/519 , A61K31/5377 , A61K31/5383 , C07D475/04 , C07D475/12 , C07D487/14 , C07D498/14 , C07D519/00
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公开(公告)号：EP1881982B1
公开(公告)日：2013-11-20
申请号：EP06770821.4
申请日：2006-05-22
发明人： STAPPENBECK, Frank , KONRADI, Andrei , JAGODZINSKI, Jacek , SEMKO, Christopher, M. , XU, Ying-zi , SMITH, Jenifer, L. , ROSSITER, Kassandra
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/506 , A61P29/00
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
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公开(公告)号：EP2424841A1
公开(公告)日：2012-03-07
申请号：EP10719684.2
申请日：2010-04-27
发明人： XU, Ying-Zi , YUAN, Shendong , WONE, David , KONRADI, Andrei
IPC分类号： C07D213/02 , C07D401/12 , A61K31/4412 , A61P37/00
CPC分类号： C07D213/82 , C07D401/14 , C07D405/14 , G01N33/68
摘要： The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula (I) or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R
1 , R
2 , R
3 , R
4 , R
5 and R
6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.摘要翻译： 本发明提供了具有根据下式（I）的结构的α4整联蛋白拮抗剂或其互变异构体，互变异构体混合物，盐或溶剂化物的化合物，其中Cy，环A，m，n，p，R 1，R 2，R 3，R 4，R 5和R 6在说明书中定义。 本发明进一步提供了包含本发明化合物的药物组合物以及制备和使用本发明化合物和组合物的方法，例如用于治疗和预防各种病症和病症，如克罗恩氏病和溃疡性结肠炎。
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公开(公告)号：EP2374792A1
公开(公告)日：2011-10-12
申请号：EP10189143.0
申请日：2005-03-11
发明人： Neitzel, Martin , Marugg, Jennifer
IPC分类号： C07C311/15 , C07C317/32 , A61K31/34 , A61P25/28
CPC分类号： C07D277/24 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/51 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07D209/14 , C07D211/58 , C07D231/06 , C07D307/52 , C07D307/81
摘要： The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).
摘要翻译： 本发明提供用于治疗或预防认知障碍（例如阿尔茨海默病）的N-取代苯磺酰胺。 特别感兴趣的化合物由式（I）定义，其中R 1，R 2，R 3，R 4和R 3如说明书中所述。 本发明还包括包含式（I）化合物的药物组合物以及使用式（I）化合物治疗认知障碍（包括阿尔茨海默氏病）的方法。
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5.发明公开Truncated fragments of alpha-synuclein in Lewy body disease 有权在路易 - 科弗尔克兰凯特的VerkürzteAlpha-Synuklein-Fragmente
公开(公告)号：EP2361928A1
公开(公告)日：2011-08-31
申请号：EP10189868.2
申请日：2004-05-19
CPC分类号： A01K67/027 , C07K14/47 , C12N15/10 , C12N15/1096 , C12Q1/68
摘要： The application identifies novel fragments of alpha-synuclein in patients with Lewy Body Disease (LBD) and transgenic animal models thereof. These diseases are characterized by aggregations of alpha-synuclein. The fragments have a truncated C-terminus relative to full-length alpha-synuclein. Some fragments are characterized by a molecular weight of about 12 kDa as determined by SDS gel electrophoresis in trycine buffer and a truncation of at least ten contiguous amino acids from the C-terminus of natural alpha-synuclein. The site of cleavage preferably occurs after residue (117) and before residue (126) of natural alpha-synuclein. The identification of these novel fragments of alpha-synuclein has a number of application in for example, drug discovery, diagnostics, therapeutics, and transgenic animals.
摘要翻译： 该应用鉴定了路易体病（LBD）患者和其转基因动物模型中的α-突触核蛋白的新片段。 这些疾病的特征在于α-突触核蛋白的聚集。 片段相对于全长α-突触核蛋白具有截短的C-末端。 一些片段的特征在于通过在trycine缓冲液中的SDS凝胶电泳测定的约12kDa的分子量和从天然α-突触核蛋白的C末端截断至少十个相邻氨基酸。 切割位点优选在天然α-突触核蛋白的残基（117）和残基（126）之前发生。 这些新型α-突触核蛋白片段的鉴定在药物发现，诊断，治疗和转基因动物中有许多应用。
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6.发明公开Prevention and treatment of synucleinopathic disease 审中-公开Präventionund Behandlung von synucleinopathischer Erkrankung
公开(公告)号：EP2361629A1
公开(公告)日：2011-08-31
申请号：EP11164647.7
申请日：2003-10-31
发明人： Schenk, Dale B. , Masliah, Eliezer
CPC分类号： A61K39/0007 , A61K38/1709 , A61K45/06 , A61K51/1078 , A61K2039/55566
摘要： The invention provides improved agents and methods for treatment of diseases associated with synucleinopathic diseases, including Lewy bodies of alpha-synuclein in the brain of a patient. Such methods entail administering agents that induce a beneficial immunogenic response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease.
摘要翻译： 本发明提供用于治疗与突触核蛋白病相关疾病（包括患者脑中的α-突触核蛋白的路易体）的改进剂和方法。 这样的方法需要对路易体诱导有益的免疫原性应答的给药剂。 该方法对帕金森病的预防和治疗治疗特别有用。
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公开(公告)号：EP2360185A2
公开(公告)日：2011-08-24
申请号：EP10012871.9
申请日：2003-02-25
发明人： Taylor, Julie , Yednock, Ted A.
IPC分类号： C07K16/28 , A61K39/395 , G01N33/533 , G01N33/53 , A61P1/04 , A61P37/02 , A61P25/02
CPC分类号： C07K16/2839 , A61K39/3955 , A61K45/06 , A61K2039/505 , A61K2039/507 , A61K2039/545 , C07K16/2842 , C07K2317/24 , C07K2317/76 , G01N33/56966 , G01N2333/4737 , G01N2333/7055
摘要： A method of chronically reducing a patient's pathological inflammation via the administration of an agent that specifically binds to an alpha-4 integrin or a dimer comprising an alpha-4 integrin is disclosed. The agent provided must have a binding affinity such that administration is sufficient to suppress pathological inflammation, and the agent is administered chronically to provide long-term suppression of pathological inflammation.
摘要翻译： 公开了通过施用特异性结合α-4整联蛋白或包含α-4整联蛋白的二聚体的试剂来长期减少患者的病理性炎症的方法。 提供的试剂必须具有结合亲和力，以便施用足以抑制病理性炎症，并且该试剂长期施用以提供对病理性炎症的长期抑制。
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公开(公告)号：EP2360142A1
公开(公告)日：2011-08-24
申请号：EP10189144.8
申请日：2005-03-11
发明人： Neitzel, Martin , Marugg, Jennifer
IPC分类号： C07C311/15 , C07C317/32 , C07D209/14 , C07D211/58 , C07D231/06 , C07D277/24 , C07D307/52 , C07D307/81 , A61K31/18 , A61K31/34 , A61K31/435 , A61P25/28
CPC分类号： C07D277/24 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/51 , C07C317/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07D209/14 , C07D211/58 , C07D231/06 , C07D307/52 , C07D307/81
摘要： The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).
摘要翻译： 本发明提供了用于治疗或预防认知障碍如阿尔茨海默病的N-取代苯磺酰胺。 特别感兴趣的化合物由式（I）定义，其中R 1，R 2，R 3，R 4和R 3如说明书中所述。 本发明还包括包含式（I）化合物的药物组合物以及使用式（I）化合物治疗认知障碍，包括阿尔茨海默病的方法。
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9.发明授权PYRIMIDINYL AMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 有权PYRIMIDINYLAMIDVERBINDUNGEN由VLA-4介导的白细胞粘着INHIBIT
公开(公告)号：EP1940826B1
公开(公告)日：2010-12-29
申请号：EP06804253.0
申请日：2006-09-28
发明人： SEMKO, Christopher, Michael , XU, Ying-zi , STAPPENBECK, Frank , SMITH, Jenifer, Lea , ROSSITER, Kassandra, Inez , FUKUDA, Juri, Y. , KONRADI, Andrei, W.
IPC分类号： C07D405/12 , C07D409/12 , C07D417/12 , C07D239/50 , C07D401/12 , A61K31/506 , A61P29/00
CPC分类号： C07D403/02 , C07D239/50 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis (Formula I).
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公开(公告)号：EP2258400A2
公开(公告)日：2010-12-08
申请号：EP10180274.2
申请日：2005-07-08
发明人： Konradi, Andrei, W. , Pleiss, Michael, A. , Semko, Christopher, M. , Yednock, Theodore , Smith, Jenifer, L.
CPC分类号： A61K45/06 , A61K31/785 , A61K47/60 , A61Q5/00
摘要： Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g ., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
摘要翻译： 公开了结合VLA-4的缀合物。 这些缀合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的缀合物可用于治疗哺乳动物患者（例如人，例如哮喘，阿尔茨海默病，动脉粥样硬化，AIDS痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血）中的炎性疾病。 也可以给予缀合物用于治疗诸如多发性硬化症的炎性脑疾病。
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