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21. 发明授权

US09192601B2 Methods for enhancing muscle performance and tone 有权
标题翻译：增强肌肉功能和调理的方法
公开(公告)号：US09192601B2
公开(公告)日：2015-11-24
申请号：US12810123
申请日：2008-12-29
申请人： Ronald M. Evans , Vihang A. Narkar , Reuben J. Shaw , Michael Downes , Ruth T. Yu
发明人： Ronald M. Evans , Vihang A. Narkar , Reuben J. Shaw , Michael Downes , Ruth T. Yu
IPC分类号： A61K31/4178 , A61K31/426 , A61K31/47 , C12Q1/68
CPC分类号： A61K31/426 , A61K31/4178 , A61K31/47 , C12Q1/6876 , C12Q2600/136 , C12Q2600/158
摘要： Provided herein are methods and compositions for improving muscle performance and increasing endurance. Agonists of AMP-activated protein kinase (AMPK) and agonists of peroxisome proliferator-activated receptor delta (PPARδ) can be used in such treatments.
摘要翻译：本文提供了用于改善肌肉性能和增加耐力的方法和组合物。 AMP活化蛋白激酶（AMPK）的激动剂和过氧化物酶体增殖物激活受体δ（PPARδ）的激动剂可用于此类治疗。

22. 发明申请

US20130116171A1 METHODS FOR TREATING METABOLIC DISORDERS USING FGF 审中-公开
公开(公告)号：US20130116171A1
公开(公告)日：2013-05-09
申请号：US13641451
申请日：2011-04-18
申请人： Johan W. Jonker , Michael Downes , Ronald M. Evans , Jaemyoung Suh
发明人： Johan W. Jonker , Michael Downes , Ronald M. Evans , Jaemyoung Suh
IPC分类号： A61K38/18 , A61K45/06
CPC分类号： A61K38/1825 , A61K9/0019 , A61K31/4439 , A61K45/06 , A61K47/60 , A61K47/61 , A61K2300/00
摘要： The method provides methods and compositions for treating metabolic disorders such as impaired glucose tolerance, elevated blood glucose, insulin resistance, dyslipidaemia, obesity, and fatty liver.

23. 发明申请

US20110263454A1 Methods of Identifying Functional Characteristics of Promoters, Transcription Modifying Proteins and Transcription Modulating Agents 审中-公开
标题翻译：鉴定启动子，转录修饰蛋白和转录调节剂功能特征的方法
公开(公告)号：US20110263454A1
公开(公告)日：2011-10-27
申请号：US13061500
申请日：2009-08-28
申请人： Johan W. Jonker , Michael Downes , Ronald M. Evans
发明人： Johan W. Jonker , Michael Downes , Ronald M. Evans
IPC分类号： C40B30/06 , C40B60/12
CPC分类号： C12Q1/6897 , C12N15/1086
摘要： Provided herein is, inter alia, methods and compositions useful in therapeutic interrogation of complex physiologic pathways by massively parallel and permissive transcriptional screening. Thus, methods and compositions are provided herein that are useful for high-throughput functional analysis of complex, transcriptionally regulated physiological pathways. While examples are provided relating to nuclear receptors, the methods and composition can be generalized and applied to any class of transcription factor or any class of gene product that can regulate the activity of transcription. For example, in addition to nuclear receptors, the methods and compositions provided herein are generally applicable to all known transcription factors and any gene encoded product that modulates said transcription factor activity. Moreover, data obtained through the methods provided herein are directly comparable thereby facilitating high-throughput functional analysis.
摘要翻译：本文提供了通过大规模平行和允许的转录筛选在治疗性询问复杂生理学途径中有用的方法和组合物。因此，本文提供了可用于复杂的转录调节生理学途径的高通量功能分析的方法和组合物。虽然提供了与核受体相关的实例，但是该方法和组成可以被推广并应用于可以调节转录活性的任何类型的转录因子或任何类型的基因产物。例如，除了核受体之外，本文提供的方法和组合物通常可应用于调节所述转录因子活性的所有已知转录因子和任何基因编码产物。此外，通过本文提供的方法获得的数据是直接可比的，因此有助于高通量功能分析。

24. 发明申请

US20110014126A1 USE OF VITAMIN D RECEPTOR AGONISTS AND PRECURSORS TO TREAT FIBROSIS 有权
标题翻译：维生素D受体激动剂和前列腺素治疗纤维化的使用
公开(公告)号：US20110014126A1
公开(公告)日：2011-01-20
申请号：US12772981
申请日：2010-05-03
申请人： Ronald M. Evans , Michael Downes , Christopher Liddle , Nanthakumar Subramaniam , Caroline Flora Samer
发明人： Ronald M. Evans , Michael Downes , Christopher Liddle , Nanthakumar Subramaniam , Caroline Flora Samer
IPC分类号： A61K31/59 , A61P1/16 , C12Q1/02 , A61K49/00 , C12N5/071
CPC分类号： A61K31/00 , A61K31/592 , A61K31/593 , G01N33/5067 , G01N33/82 , G01N2800/085
摘要： This application relates to methods of treating, preventing, and ameliorating fibrosis, such as fibrosis of the liver. In particular, the application relates to methods of using a vitamin D receptor agonist (such as vitamin D, vitamin D analogs, vitamin D precursors, and vitamin D receptor agonists precursors) for the treatment of liver fibrosis. Also disclosed are methods for screening for agents that treat, prevent, and ameliorate fibrosis.
摘要翻译：本申请涉及治疗，预防和改善纤维化（例如肝纤维化）的方法。特别地，本申请涉及使用维生素D受体激动剂（例如维生素D，维生素D类似物，维生素D前体和维生素D受体激动剂前体）用于治疗肝纤维化的方法。还公开了用于筛选治疗，预防和改善纤维化的药剂的方法。

25. 发明授权

US07647217B2 Structure of the farnesoid X receptor ligand binding domain and methods of use therefor 失效
标题翻译：法呢酯X受体配体结合域的结构及其用途
公开(公告)号：US07647217B2
公开(公告)日：2010-01-12
申请号：US10535042
申请日：2003-11-14
申请人： Michael R Downes , Mark A. Verdicia , Joseph P. Noel , Ronald M. Evans , Lindsey J. Bowman , Marianne Bowman
发明人： Michael R Downes , Mark A. Verdicia , Joseph P. Noel , Ronald M. Evans , Lindsey J. Bowman , Marianne Bowman
IPC分类号： G06G7/58 , C07K14/00
CPC分类号： C07K14/70567 , C07K2299/00 , G01N33/743 , G01N2500/00 , G06F19/16 , G06F19/706
摘要： The present invention provides compositions comprising the ligand binding domain (LBD) of a farnesoid X receptor (FXR) in crystalline form. In alternative embodiments, the LBD of FXR is complexed with a ligand therefor. There are provided high resolution structures of FXR complexed with a novel high affinity agonist, fexaramine. The discovered structure of a FXR LBD provides the first three-dimensional view of the structural basis for FXR ligand binding. The present invention further provides a computer for producing a three-dimensional representation of FXR or a complex thereof, and a computer for determining at least a portion of the structure coordinates of FXR or a complex thereof. The present invention further provides methods of using this structural information to predict molecules capable of binding to FXR; to identify compounds with agonist, antagonist or partial agonist activity for FXR; and to determine whether a test compound is capable of binding to the LBD of FXR. The present invention further provides compositions comprising compounds identified by such invention methods.
摘要翻译：本发明提供了包含结晶形式的法呢甾X受体（FXR）的配体结合结构域（LBD）的组合物。在替代实施方案中，FXR的LBD与其配体复合。提供了与新型高亲和力激动剂fexaramine复合的FXR的高分辨率结构。所发现的FXR LBD的结构提供了FXR配体结合的结构基础的第一个三维视图。本发明还提供一种用于产生FXR或其复数的三维表示的计算机，以及用于确定FXR的结构坐标的至少一部分或其复合体的计算机。本发明还提供使用该结构信息来预测能够结合FXR的分子的方法; 识别FXR激动剂，拮抗剂或部分激动剂活性的化合物; 并确定测试化合物是否能够结合FXR的LBD。本发明还提供包含通过本发明方法鉴定的化合物的组合物。

26. 发明授权

US07041498B2 Method for modulating processes mediated by farnesoid activated receptors 失效
公开(公告)号：US07041498B2
公开(公告)日：2006-05-09
申请号：US10155379
申请日：2002-05-24
申请人： Ronald M. Evans , Barry M. Forman , Cary A. Weinberger
发明人： Ronald M. Evans , Barry M. Forman , Cary A. Weinberger
IPC分类号： C12N5/00 , C12N15/24 , C07H17/00
CPC分类号： A61K31/045 , A61K31/202 , A61K31/22 , A61K31/336 , C07K14/70567 , G01N33/74 , G01N2333/70567
摘要： Farnesyl pyrophosphate, the metabolically active form of farnesol, is a key precursor in the synthesis of cholesterol, carotenoids, steroid hormones, bile acids and other molecules involved in cellular growth and metabolism. A nuclear receptor has been identified that is transcriptionally activated by farnesol and related molecules. This novel signaling pathway can be modulated by the use of key metabolic intermediates (or analogs and/or derivatives thereof) as transcriptional regulatory signals.

27. 发明授权

US06706762B1 Methods for the use of inhibitors of co-repressors for the treatment of neoplastic diseases 失效
标题翻译：联合抑制剂抑制剂治疗肿瘤性疾病的方法
公开(公告)号：US06706762B1
公开(公告)日：2004-03-16
申请号：US08966876
申请日：1997-11-10
申请人： Ronald M. Evans , Richard J. Lin , Laszlo Nagy
发明人： Ronald M. Evans , Richard J. Lin , Laszlo Nagy
IPC分类号： A61K3119
CPC分类号： C12Q1/6897 , A61K38/005 , C07K14/70567 , A61K2300/00
摘要： In accordance with the present invention, it has been discovered that histone deacetylase associates with hormone receptor complexes and contributes to the repression thereof. It has further been discovered that exposure of a repressed system to histone deacetylase inhibitors relieves this repression, and that in combination with a ligand for a member the steroid/thyroid superfamily of receptors, the differentiation effects of retinoids are enhanced. Thus, histone deacetylase inhibitors have been found to be useful for the activation of genes responsive to hormone receptors and to conteract the oncogenic functions of oncogenic proteins. In accordance with another aspect of the invention, formulations useful for modulation of hormone-mediated processes have been developed. In addition, assays have been developed for the identification of compounds useful to modulate the above-described processes as well as methods of employing such compounds for the treatment of neoplastic diseases.
摘要翻译：根据本发明，已经发现组蛋白脱乙酰酶与激素受体复合物缔合并有助于其抑制。进一步发现，抑制系统暴露于组蛋白脱乙酰酶抑制剂减轻了这种抑制作用，并且与受体的类固醇/甲状腺超家族成员的配体结合，维生素A的分化作用增强。因此，已经发现组蛋白脱乙酰酶抑制剂可用于激活对激素受体起反应的基因并且使致癌蛋白的致癌功能得以稳定。根据本发明的另一方面，已经开发了可用于调节激素介导的过程的制剂。此外，已经开发了用于鉴定可用于调节上述方法的化合物的测定法以及使用这些化合物治疗肿瘤性疾病的方法。

28. 发明授权

US06673587B1 Histone deacetylase, and uses therefor 有权
标题翻译：新组蛋白脱乙酰酶，并用于此
公开(公告)号：US06673587B1
公开(公告)日：2004-01-06
申请号：US09637145
申请日：2000-08-11
申请人： Ronald M. Evans , Hung-Ying Kao , Michael Downes , Peter Ordentlich
发明人： Ronald M. Evans , Hung-Ying Kao , Michael Downes , Peter Ordentlich
IPC分类号： C12N916
CPC分类号： C12N9/16
摘要： The present invention relates to the identification, isolation, sequencing and characterization of a new member of the histone deacetylase family, as well as its transcripts, gene products, associated sequence information, and related genes. The present invention also relates to methods for detecting and diagnosing carriers of normal and mutant alleles of these genes, methods for detecting and diagnosing diseases, methods of identifying genes and proteins related to or interacting with such genes and proteins, methods of screening for potential therapeutics for diseases, methods of treatment for diseases, and to cell lines and animal models useful in screening for and evaluating potentially useful therapies for diseases. In a particular aspect of the present invention, a novel family member, HDAC7, is described and its interaction with SMRT/N-CoR and mSin3A, its biochemical properties and subcellular localization are characterized. In addition, evidence is provided that the HDAC4, 5, and 7 deacetylases may mediate nuclear receptor repression. The findings described here indicate that two or more classes of histone deacetylases can collectively contribute to SMRT/N-CoR action and that at least some deacetylases may directly associate with SMRT/N-CoR in a mSin3A independent fashion.
摘要翻译：本发明涉及组蛋白脱乙酰酶家族的新成员以及其转录物，基因产物，相关序列信息和相关基因的鉴定，分离，测序和表征。本发明还涉及用于检测和诊断这些基因的正常和突变等位基因的载体的方法，用于检测和诊断疾病的方法，鉴定与这些基因和蛋白质相关或与之相互作用的基因和蛋白质的方法，筛选潜在治疗剂的方法用于疾病的治疗方法，以及用于筛选和评估潜在有用的疾病疗法的细胞系和动物模型。在本发明的特定方面，描述了新型家族成员HDAC7，并且与SMRT / N-CoR和mSin3A的相互作用，其生物化学性质和亚细胞定位被表征。此外，证据表明HDAC4,5和7脱乙酰酶可能介导核受体抑制。这里描述的发现表明，两种或更多类组蛋白脱乙酰酶可以共同促进SMRT / N-CoR作用，并且至少一些脱乙酰酶可以以独立于mSin3A的方式直接与SMRT / N-CoR相关联。

29. 发明授权

US06387673B1 Compounds useful for the modulation of processes mediated by nuclear hormone receptors, methods for the identification and use of such compounds 失效
标题翻译：可用于调节核激素受体介导的过程的化合物，用于鉴定和使用这些化合物的方法
公开(公告)号：US06387673B1
公开(公告)日：2002-05-14
申请号：US08846881
申请日：1997-05-01
申请人： Ronald M. Evans , Laszlo Nagy
发明人： Ronald M. Evans , Laszlo Nagy
IPC分类号： C12N999
CPC分类号： C12Q1/6897 , A61K38/005 , C07K14/70567 , A61K2300/00
摘要： In accordance with the present invention, it has been discovered that histone deacetylase associates with hormone receptor complexes and contributes to the repression thereof. It has further been discovered that exposure of a repressed system to histone deacetylase inhibitors relieves this repression. Thus, histone deacetylase inhibitors have been found to be useful for the activation of genes responsive to hormone receptors. In accordance with another aspect of the invention, formulations useful for modulation of hormone-mediated processes have been developed. In addition, assays have been developed for the identification of compounds useful to modulate the above-described processes.
摘要翻译：根据本发明，已经发现组蛋白脱乙酰酶与激素受体复合物缔合并有助于其抑制。进一步发现，抑制系统暴露于组蛋白脱乙酰酶抑制剂减轻了这种镇压作用。因此，已经发现组蛋白脱乙酰酶抑制剂可用于激活对激素受体有反应的基因。根据本发明的另一方面，已经开发了可用于调节激素介导的过程的制剂。此外，已经开发了用于鉴定可用于调节上述过程的化合物的测定。

30. 发明授权

US06278040B1 Receptor-deficient mice and cell lines derived therefrom, and uses thereof 失效
标题翻译：受体缺陷小鼠和由其衍生的细胞系及其用途
公开(公告)号：US06278040B1
公开(公告)日：2001-08-21
申请号：US08802468
申请日：1997-02-19
申请人： Henry M. Sucov , Ronald M. Evans , Kenneth R. Chien
发明人： Henry M. Sucov , Ronald M. Evans , Kenneth R. Chien
IPC分类号： C12N1509
CPC分类号： C12N15/8509 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/03 , A01K2267/0375 , A61K31/203 , A61K49/0008
摘要： In accordance with the present invention, there are provided targeted loss of function mutant mice which express less than endogenous levels of at least one member of the steroid/thyroid superfamily of receptors in at least one specific tissue type. For example, mutations in the RXR&agr; gene in mouse germlines are lethal in the embryonic stage between E13.5 and E16.5 when bred to homozygosity. The major defect responsible for this lethal effect is hypoplastic development of the ventricular chambers of the heart, which is manifest as a grossly thinned ventricular wall with concurrent defects in ventricular septation. This phenotype is identical to a subset of the effects of embryonic vitamin A deficiency, and therefore establishes RXR&agr; as a genetic component of the vitamin A signaling pathway in cardiac morphogenesis. The cardiac outflow tracts and associated vessels, which are populated by derivatives of the neural crest and which are also sensitive to vitamin A deficiency, are normal in homozygous embryos, indicating the genetic independence of ventricular chamber development. Hepatic differentiation was dramatically but transiently retarded, yet is histologically and morphologically normal. These results ascribe an essential function for the RXR&agr; gene in embryonic development, and provide the first evidence of a requirement for RXR in one of its predicted hormone response pathways.
摘要翻译：根据本发明，提供了在至少一种特定组织类型中表达低于受体的类固醇/甲状腺超家族的至少一种成员的内源水平的功能突变小鼠的靶向丧失。例如，当培育成纯合子时，E13.5和E16.5之间的胚胎阶段，小鼠种系中RXRalpha基因的突变是致命的。负责这种致死作用的主要缺陷是心脏心室的发育不良，这表现为心室隔膜同时缺陷的严重变薄的心室壁。这种表型与胚胎维生素A缺乏症的一个亚组相同，因此在心脏形态发生中建立了RXRalpha作为维生素A信号通路的遗传成分。由神经嵴的衍生物填充并且对维生素A缺乏敏感的心脏流出道和相关血管在纯合胚中是正常的，表明心室发育的遗传独立性。肝分化显着但短暂延迟，但组织学和形态学正常。这些结果归因于胚胎发育中RXRalpha基因的基本功能，并提供了其预测的激素反应途径之一的RXR要求的第一个证据。

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