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31. 发明授权

US07741368B2 Approach to antimicrobial host defense with molecular shields with EPA and DHA analogs 有权
标题翻译：用EPA和DHA类似物进行分子屏蔽的抗微生物宿主防御方法
公开(公告)号：US07741368B2
公开(公告)日：2010-06-22
申请号：US11353436
申请日：2006-02-14
申请人： Charles N. Serhan , Sean P. Colgan
发明人： Charles N. Serhan , Sean P. Colgan
IPC分类号： A61K31/20 , A61K31/205 , A61K31/22
CPC分类号： A61K31/202 , A61K31/232
摘要： Methods to cause tissue, such as mucosal cells, to express increased amounts of bactericidal permeability increasing protein (BPI) are described. Various BPI inducing agents include icosapentanoic acid (EPA) analogs and docosahexaenoic acid (DHA) analogs.
摘要翻译：描述了引起组织如粘膜细胞表达增加量的杀菌通透性增加蛋白（BPI）的方法。各种BPI诱导剂包括二十碳五烯酸（EPA）类似物和二十二碳六烯酸（DHA）类似物。

32. 发明申请

US20100105773A1 USE OF RESOLVINS AND DOCOSATRIENES AND ANALOGUES THEREOF FOR THE TREATMENT OF ANGIOGENESIS AND OCULAR NEOVASCULARIZATION 审中-公开
标题翻译：用于治疗血液发生和血管新生血管的解决方案和文献综述及其类似物的使用
公开(公告)号：US20100105773A1
公开(公告)日：2010-04-29
申请号：US12514156
申请日：2007-11-09
申请人： Lois Smith , Kip Connor , Charles N. Serhan
发明人： Lois Smith , Kip Connor , Charles N. Serhan
IPC分类号： A61K31/202 , A61P19/02 , A61P17/02 , A61P17/06
CPC分类号： A61K31/202
摘要： The present invention relates to methods and compositions for the treatment of, or prevention of angiogenesis in a subject. In particular, the present invention relates to methods to treat a subject with, or at risk of developing angiogenesis by administering a pharmaceutical composition comprising a resolvin or resolvin analogue or precursor, and/or a protectin or protectin analogue. In another embodiment, the present invention relates to the use of resolvins and protectins to treat pathologies associated with angiogenesis.
摘要翻译：本发明涉及用于治疗或预防受试者血管发生的方法和组合物。特别地，本发明涉及通过施用包含阿维生素或解决方案类似物或前体，和/或保护素或保护素类似物的药物组合物来治疗患有或有风险发生血管生成的受试者的方法。在另一个实施方案中，本发明涉及抗凝血酶和保护素用于治疗与血管生成相关的病理学的用途。

33. 发明授权

US07700650B2 Lipoxin analogs and method for the treatment of periodontal disease 有权
标题翻译：脂氧素类似物和治疗牙周病的方法
公开(公告)号：US07700650B2
公开(公告)日：2010-04-20
申请号：US10239444
申请日：2001-03-20
申请人： Thomas E. Van Dyke , Nicos A. Petasis , Charles N. Serhan
发明人： Thomas E. Van Dyke , Nicos A. Petasis , Charles N. Serhan
IPC分类号： A01N37/06
CPC分类号： A61K31/202 , A61K31/22 , A61K31/365 , C07B2200/07 , C07C69/732 , C07C69/736 , C07C229/30 , C07C235/28 , C07C259/06 , C07C2601/16 , A61K2300/00
摘要： This invention provides new lipoxin analogs, compositions containing these analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond theoral cavity that are related to periodontal disease using the compositions containing lipoxin analogs, COX-2 inhibitors, or both.
摘要翻译：本发明提供新的脂氧素类似物，含有这些类似物的组合物，以及使用这些化合物和组合物治疗和预防口腔炎症的方法，包括牙龈炎，牙周炎和其它形式的牙周病。本发明还提供了含有COX-2抑制剂的组合物治疗和预防口腔炎症的方法，包括牙龈炎，牙周炎和其他形式的牙周病。此外，本发明提供了使用含有脂氧素类似物，COX-2抑制剂或两者的组合物来预防与口腔疾病相关的全腔外疾病的方法。

34. 发明申请

US20090270498A1 Lipoxin Compounds and Their use in Treating Cell Proliferative Disorders 失效
标题翻译： Lipoxin化合物及其在治疗细胞增殖性疾病中的应用
公开(公告)号：US20090270498A1
公开(公告)日：2009-10-29
申请号：US11837824
申请日：2007-08-13
申请人： Charles N. Serhan
发明人： Charles N. Serhan
IPC分类号： A61K31/336 , A61K31/202 , C07C57/03 , A61P7/00 , C07D303/12
CPC分类号： C07C69/736 , A61K31/202 , A61K31/232 , A61K31/557 , A61K31/60 , C07C59/42 , C07C69/587 , C07C69/732 , C07C69/734 , A61K2300/00
摘要： Compounds having the active site of natural lipoxins, but a longer tissue half-life are disclosed. In particular, 15-epi-lipoxins and their use in ameliorating undesired cell proliferation, which characterizes diseases such as cancer, are also disclosed.
摘要翻译：公开了具有天然脂氧素活性位点但具有较长组织半衰期的化合物。特别地，还公开了15表面脂蛋白及其在改善诸如癌症等疾病特征的不想要的细胞增殖中的用途。

35. 发明授权

US07585856B2 Resolvins: Biotemplates for novel therapeutic interventions 有权
标题翻译： Resolvins：用于新型治疗干预的生物模型
公开(公告)号：US07585856B2
公开(公告)日：2009-09-08
申请号：US10639714
申请日：2003-08-12
申请人： Charles N. Serhan
发明人： Charles N. Serhan
IPC分类号： A01N43/62
CPC分类号： A61K31/202 , C07C59/42 , C07C59/48 , C07C69/732 , C07F7/1804
摘要： The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.
摘要翻译：本发明一般涉及由膳食ω-3多不饱和脂肪酸（PUFA）如二十碳五烯酸（EPA）或二十二碳六烯酸（DHA），环氧合酶II（COX）之间的相互作用产生的新型分离的治疗剂，称为溶血素 -2）和止痛剂，例如阿司匹林（ASA）。令人惊讶的是，在合适的环境中仔细分离由组分组合产生的化合物，提供了具有独特结构和生理特性的二羟基EPA或DHA化合物。因此，本发明提供了例如减少，预防或消除炎症或PMN迁移的许多新的有用的EPA或DHA（resolvins）治疗二 - 或三羟基衍生物。本发明还提供了用于本说明书中公开的化合物的药物用途，制备方法和包装药物的方法。

36. 发明申请

US20090149538A1 Aspirin-Triggered Lipid Mediators 有权
标题翻译：阿司匹林触发脂质介质
公开(公告)号：US20090149538A1
公开(公告)日：2009-06-11
申请号：US12338240
申请日：2008-12-18
申请人： Charles N. Serhan , Clary B. Clish
发明人： Charles N. Serhan , Clary B. Clish
IPC分类号： A61K31/202 , C07C59/42 , A61P29/00 , A61P9/00
CPC分类号： C07C59/58 , C07B2200/07 , C07C59/42 , C07C69/732 , C12P7/6427 , C12P7/6436 , C12P7/6472 , Y02P20/55
摘要： Aspirin triggered lipid mediators (ATLMs) are disclosed which are useful for the treatment of prevention of inflammation associated with various diseases, including ischemia.
摘要翻译：公开了阿司匹林引发的脂质介质（ATLM），其可用于治疗与各种疾病（包括缺血）相关的炎症的预防。

37. 发明申请

US20080312323A1 Inhibition of TNF-alpha-Initiated Response 审中-公开
标题翻译：抑制TNF-α启动的反应
公开(公告)号：US20080312323A1
公开(公告)日：2008-12-18
申请号：US11531921
申请日：2006-09-14
申请人： Charles N. Serhan
发明人： Charles N. Serhan
IPC分类号： A61K31/202 , A61P29/00
CPC分类号： A61K31/232 , A61K31/216 , A61K31/23 , A61K31/557
摘要： The impact of lipoxin A4 (LXA4) and aspirin-triggered-lipoxins (ATL) was investigated in tumor necrosis factor (TNFα)-initiated neutrophil (PMN) responses in vitro and in vivo using metabolically stable LX analogs. At concentrations as low as 1-10 nM, the LXA4 and ATL analogs each inhibited TNFα-stimulated superoxide anion generation and IL-1β release by human PMN.
摘要翻译：在体外和体内使用代谢稳定的LX类似物在肿瘤坏死因子（TNFalpha）诱导的嗜中性粒细胞（PMN）反应中研究了脂氧素A4（LXA4）和阿司匹林引发的脂氧素（ATL）的影响。在低至1-10nM的浓度下，LXA4和ATL类似物各自抑制TNFα刺激的超氧化物阴离子产生和人PMN释放的IL-1beta。

38. 发明授权

US07341840B2 Methods for identification and uses of anti-inflammatory receptors for eicosapentaenoic acid analogs 有权
标题翻译：用于二十碳五烯酸类似物的抗炎症受体的鉴定和使用方法
公开(公告)号：US07341840B2
公开(公告)日：2008-03-11
申请号：US11218281
申请日：2005-09-01
申请人： Charles N. Serhan , Makoto Arita
发明人： Charles N. Serhan , Makoto Arita
IPC分类号： G01N33/53 , G01N33/567
CPC分类号： G01N33/5047 , G01N33/5023 , G01N33/5032 , G01N33/5041 , G01N33/505 , G01N33/566 , G01N2333/4703 , G01N2333/715 , G01N2333/726 , G01N2500/04
摘要： The present invention is directed to methods for the identification and uses of receptors that interact with anti-inflammatory compounds derived from eicosapentaenoic acid (EPA). The receptors are of the G-protein coupled receptor (GPCR) family, and are useful to screen candidate substances for anti-inflammatory activity, especially substances that are analogs of EPA. Such analogs are termed “resolvins”; and are typically di- and tri-hydroxy EPA analogs. One analog herein denoted Resolvin E1 was identified in humans and prepared by total synthesis. In nanomolar range Resolvin E1 reduces dermal inflammation, peritonitis, dendritic cells (DCs) migration and IL-12 production. Also described herein is a receptor denoted Reso ER1 that interacts with Resolvin E1 to attenuate cytokine induced activation of inflammatory pathways mediated by transcription factor (NF)-kB. Treatment of DCs with small-interfering RNA specific for ResoE1 eliminated the ligand's ability to regulate IL-12. Assays of anti-inflammatory activity based on these discoveries are also described.
摘要翻译：本发明涉及鉴定和使用与二十碳五烯酸（EPA）衍生的抗炎化合物相互作用的受体的方法。受体是G蛋白偶联受体（GPCR）家族，可用于筛选候选物质的抗炎活性，特别是类似于EPA的物质。这样的类似物被称为“溶解素”; 并且通常是二羟基和三羟基EPA类似物。在人类中鉴定了一种在本文中称为Resolvin E1的类似物，并通过全合成制备。在纳摩尔范围内，Resolvin E1可减少皮肤炎症，腹膜炎，树突细胞（DCs）迁移和IL-12的产生。本文还描述了称为Reso ER1的受体，其与Resolvin E1相互作用以减弱由转录因子（NF）-kB介导的炎症途径的细胞因子诱导的活化。用特异于ResoE1的小干扰RNA处理DC消除了配体调节IL-12的能力。还描述了基于这些发现的抗炎活性测定。

39. 发明授权

US06960674B2 Prevention of neutrophil recruitment 失效
公开(公告)号：US06960674B2
公开(公告)日：2005-11-01
申请号：US10366194
申请日：2003-02-13
申请人： Charles N. Serhan
发明人： Charles N. Serhan
IPC分类号： A61P1/04 , A61K31/047 , A61P9/10 , A61P17/06 , A61P19/02 , A61P29/00 , C07C59/68 , C07C69/734 , C07C69/736 , C07C59/00
CPC分类号： A61K31/22 , C07C59/68 , C07C69/736
摘要： Aspirin (ASA) triggers a switch in the biosynthesis of lipid mediators, inhibiting prostanoid production and initiating 15-epi-lipoxin generation, through the acetylation of cyclooxygenase II.

40. 发明授权

US06864288B2 Regulation of phospholipase D activity 失效
公开(公告)号：US06864288B2
公开(公告)日：2005-03-08
申请号：US10004155
申请日：2001-10-19
申请人： Charles N. Serhan
发明人： Charles N. Serhan
IPC分类号： A61P9/00 , A61K31/00 , A61K31/035 , A61K31/216 , A61K31/232 , A61P29/00 , A61P43/00 , A61K31/23 , A61K31/20
CPC分类号： A61K31/661 , A61K31/00 , A61K31/035 , A61K31/20 , A61K31/216 , A61K31/232 , A61K31/6615
摘要： Novel inhibitors of polyisoprenyl phosphate signaling regulates phopholipase D activity.

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