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1. 发明申请

US20120264796A1 METHODS FOR MODULATING CIRCADIAN RHYTHMS 审中-公开
标题翻译：调整CIRCADIAN RHYTHMS的方法
公开(公告)号：US20120264796A1
公开(公告)日：2012-10-18
申请号：US13257745
申请日：2010-03-22
申请人： Ronald Evans , Katja A. Lamia , Reuben J. Shaw , Luciano Ditacchio , Satchidananda Panda
发明人： Ronald Evans , Katja A. Lamia , Reuben J. Shaw , Luciano Ditacchio , Satchidananda Panda
IPC分类号： A61K31/4164 , G01N33/573
CPC分类号： C12Q1/485 , A61K31/155 , A61K31/7056 , A61K38/2264 , A61K45/06 , G01N2500/04 , G01N2800/2864
摘要： This disclosure described the role of AMPK in circadian rhythms and methods of screening for agents that modulate such rhythms, compositions that are useful for modulating such rhythms and uses thereof.
摘要翻译：本公开描述了AMPK在昼夜节律中的作用以及筛选调节这种节律的药剂的方法，可用于调节这种节律的组合物及其用途。

2. 发明申请

US20120134985A1 METHODS FOR MODULATING METABOLIC AND CIRCADIAN RHYTHMS 审中-公开
标题翻译：调节代谢和血液循环的方法
公开(公告)号：US20120134985A1
公开(公告)日：2012-05-31
申请号：US13257758
申请日：2010-03-22
申请人： Ronald Evans , Katja A. Lamia , Reuben J. Shaw
发明人： Ronald Evans , Katja A. Lamia , Reuben J. Shaw
IPC分类号： A61K39/395 , A61P25/00 , C07K16/42 , A61P3/00 , G01N33/566 , C12Q1/48
CPC分类号： A61K31/00 , A61K31/155 , A61K31/341 , A61K31/417 , A61K31/7056 , A61K38/2264 , A61K45/06 , C12N9/1205 , C12Q1/485 , G01N2333/9121 , G01N2500/04 , G01N2800/2864 , A61K2300/00
摘要： The role of AMPK in arcadian rhythms and methods of screening for agents that modulate such rhythms are disclosed. Compositions that are useful for modulating such rhythms and uses thereof are also disclosed.
摘要翻译：公开了AMPK在阿arc法节律中的作用和筛选调节这种节律的药剂的方法。还公开了可用于调节这种节律及其用途的组合物。

3. 发明申请

US20060211768A1 Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor 审中-公开
公开(公告)号：US20060211768A1
公开(公告)日：2006-09-21
申请号：US11256501
申请日：2005-10-21
申请人： Ronald Evans , David Mangelsdorf , Richard Heyman , Marcus Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald Evans , David Mangelsdorf , Richard Heyman , Marcus Boehm , Gregor Eichele , Christina Thaller
IPC分类号： A61K31/203
CPC分类号： C12P7/04 , A61K31/07 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/23 , A61K31/232 , C07K14/70567
摘要： In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.

4. 发明申请

US20060194949A1 Structure of the farnesoid x receptor ligand binding domain and methods of use therefor 失效
标题翻译：法呢基x受体配体结合域的结构及其使用方法
公开(公告)号：US20060194949A1
公开(公告)日：2006-08-31
申请号：US10535042
申请日：2003-11-14
申请人： Michael Downes , Mark Verdicia , Joseph Noel , Ronald Evans , Lindsey Bowman , Marianne Bowman
发明人： Michael Downes , Mark Verdicia , Joseph Noel , Ronald Evans , Lindsey Bowman , Marianne Bowman
IPC分类号： G06F19/00 , C07K14/705
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。

5. 发明申请

US20060292633A1 Method for modulating process mediated by farnesoid activated receptors 失效
公开(公告)号：US20060292633A1
公开(公告)日：2006-12-28
申请号：US11413604
申请日：2006-04-28
申请人： Ronald Evans , Barry Forman , Cary Weinberger
发明人： Ronald Evans , Barry Forman , Cary Weinberger
IPC分类号： G01N33/53 , A61K31/336 , A61K31/045 , A61K31/202 , A61K31/22
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.

6. 发明申请

US20070026445A1 Novel steroid-activated nuclear receptors and uses therefor 有权
标题翻译：新型类固醇激活的核受体及其用途
公开(公告)号：US20070026445A1
公开(公告)日：2007-02-01
申请号：US11495263
申请日：2006-07-27
申请人： Ronald Evans , Bruce Blumberg
发明人： Ronald Evans , Bruce Blumberg
IPC分类号： C12Q1/68 , G01N33/567 , G01N33/53
CPC分类号： A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/03 , A61K38/00 , C07K14/70567 , C07K2319/71 , C12N15/8509 , C12N2830/008 , C12Q1/6897 , G01N33/743 , G01N2333/90245 , G01N2500/00
摘要： A novel nuclear receptor, termed the steroid and xenobiotic receptor (SXR), a broad-specificity sensing receptor that is a novel branch of the nuclear receptor superfamily, has been discovered. SXR forms a heterodimer with RXR that can bind to and induce transcription from response elements present in steroid-inducible cytochrome P450 genes in response to hundreds of natural and synthetic compounds with biological activity, including therapeutic steroids as well as dietary steroids and lipids. Instead of hundreds of receptors, one for each inducing compound, the invention SXR receptors monitor aggregate levels of inducers to trigger production of metabolizing enzymes in a coordinated metabolic pathway. Agonists and antagonists of SXR are administered to subjects to achieve a variety of therapeutic goals dependent upon modulating metabolism of one or more endogenous steroids or xenobiotics to establish homeostasis. An assay is provided for identifying steroid drugs that are likely to cause drug interaction if administered to a subject in therapeutic amounts. Transgenic animals are also provided which express human SXR, thereby serving as useful models for human response to various agents which potentially impact P450-dependent metabolic processes.
摘要翻译：已经发现了一种称为类固醇和异种生物受体（SXR）的新型核受体，作为核受体超家族的新分支的广泛特异性感受器受体。 SXR与RXR形成异源二聚体，其可以结合并诱导存在于类固醇诱导细胞色素P450基因中的响应元件的转录，以响应数百种具有生物活性的天然和合成化合物，包括治疗类固醇以及膳食类固醇和脂质。代替数百个受体，每个诱导化合物一个，本发明SXR受体监测诱导剂的总体水平以引发协同代谢途径中代谢酶的产生。 SXR的激动剂和拮抗剂被施用于受试者以实现依赖于调节一种或多种内源性类固醇或异种生物的代谢以建立体内平衡的多种治疗目标。提供了用于鉴定如果以治疗量施用给受试者的可能引起药物相互作用的类固醇药物的测定。还提供了表达人SXR的转基因动物，从而作为人类对各种可能影响P450依赖性代谢过程的药物的反应的有用模型。

7. 发明申请

US20050143449A1 Non-steroidal farnesoid X receptor modulators and methods for the use thereof 审中-公开
标题翻译：非甾体法尼醇X受体调节剂及其使用方法
公开(公告)号：US20050143449A1
公开(公告)日：2005-06-30
申请号：US10658115
申请日：2003-09-08
申请人： Michael Downes , Ronald Evans , Robert Hughes , Kyriacos Nicolaou , Anthony Roecker
发明人： Michael Downes , Ronald Evans , Robert Hughes , Kyriacos Nicolaou , Anthony Roecker
IPC分类号： A61K20060101 , A61K31/16 , A61K31/21 , A61K31/215 , A61K31/33 , A61K31/35 , A61K31/353 , C07C20060101 , C07D311/04 , C07D311/74
CPC分类号： C07D311/94 , A61K31/16 , A61K31/353 , A61K31/44 , A61K31/4433 , C07C233/54 , C07C233/63 , C07C233/81 , C07C237/22 , C07C275/42 , C07C309/66 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/40 , C07D277/28 , C07D307/46 , C07D311/04 , C07D311/22 , C07D311/64 , C07D311/68 , C07D317/58 , C07D333/20 , C07D333/22 , C07D407/12 , C07D409/12
摘要： The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
摘要翻译：胆固醇合成，代谢，获取和运输的有效调节是脂质体内平衡的重要组成部分。法呢蛋白X受体（FXR）是胆汁酸的转录传感器，胆汁酸是胆固醇代谢的主要产物。因此，FXR的有效的，选择性的，小分子激动剂，部分激动剂和拮抗剂的开发将是进一步去卷积FXR生理学中的重要步骤。根据本发明，描述了新型有效的FXR活化剂的鉴定。携带二苯乙烯或联芳基部分的本发明化合物的两种衍生物含有迄今为止基于细胞的测定中报道的最有效的FXR激动剂的成员。这些化合物可用作进一步定义FXR的生理作用以及用于治疗与胆固醇，胆汁酸及其代谢和体内平衡相关的疾病的治疗用途的化学工具。

8. 发明授权

US4582238A Rivet detaining means for riveting machines 失效
标题翻译：用于铆接机的铆钉扣留装置
公开(公告)号：US4582238A
公开(公告)日：1986-04-15
申请号：US624140
申请日：1984-06-25
申请人： Alan Bennett , Paul E. Morris , Ronald Ormston , Ronald Evans
发明人： Alan Bennett , Paul E. Morris , Ronald Ormston , Ronald Evans
IPC分类号： B21J15/00 , B21J15/10 , B21J15/16 , B21J15/20 , B21J15/32 , B21J15/36
CPC分类号： B21J15/10 , B21J15/32
摘要： A riveting apparatus comprises a portable riveting assembly which may be hand held or mounted on a robot arm. The assembly comprises a C-frame having an anvil mounted on one arm and a hydraulic ram mounted on the other arm. Rivets are supplied to a head assembly located between the anvil and piston rod via a flexible tube having a T-shaped cross-section. After a rivet has been supplied it is held positively in position ready for setting within pocket members by air pressure supplied along tube. Thus, the assembly can be moved rapidly and used in various orientations without displacing the rivet. Connections between the assembly and rivet supply and hydraulic power source are by way of flexible connections.
摘要翻译：铆接装置包括可手持或安装在机器人手臂上的便携式铆接组件。组件包括具有安装在一个臂上的砧座的C形框架和安装在另一个臂上的液压柱塞。铆钉通过具有T形横截面的柔性管道供应到位于砧座和活塞杆之间的头部组件。在铆钉已经被供应之后，它被正确地保持就位，准备通过沿管提供的空气压力来设置在口袋构件内。因此，组件可以快速移动并且以各种取向使用，而不会使铆钉移位。组装和铆钉供应和液压动力源之间的连接是通过灵活的连接。

9. 发明申请

US20060223879A1 Non-steroidal farnesoid x receptor modulators 审中-公开
标题翻译：非甾体法尼醇x受体调节剂
公开(公告)号：US20060223879A1
公开(公告)日：2006-10-05
申请号：US10535041
申请日：2003-11-14
申请人： Michael Downes , Ronald Evans , Robert Hughes , Kyriacos Nicolaou , Anthony Roecker
发明人： Michael Downes , Ronald Evans , Robert Hughes , Kyriacos Nicolaou , Anthony Roecker
IPC分类号： A61K31/381 , A61K31/353 , C07D409/02
CPC分类号： C07D311/94 , A61K31/16 , A61K31/353 , A61K31/44 , A61K31/4433 , C07C233/54 , C07C233/63 , C07C233/81 , C07C237/22 , C07C275/42 , C07C309/66 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/40 , C07D277/28 , C07D307/46 , C07D311/04 , C07D311/22 , C07D311/64 , C07D311/68 , C07D317/58 , C07D333/20 , C07D333/22 , C07D407/12 , C07D409/12
摘要： The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
摘要翻译：胆固醇合成，代谢，获取和运输的有效调节是脂质体内平衡的重要组成部分。法呢蛋白X受体（FXR）是胆汁酸的转录传感器，胆汁酸是胆固醇代谢的主要产物。因此，FXR的有效的，选择性的，小分子激动剂，部分激动剂和拮抗剂的开发将是进一步去卷积FXR生理学中的重要步骤。根据本发明，描述了新型有效的FXR活化剂的鉴定。携带二苯乙烯或联芳基部分的本发明化合物的两种衍生物含有迄今为止基于细胞的测定中报道的最有效的FXR激动剂的成员。这些化合物可用作进一步定义FXR的生理作用以及用于治疗与胆固醇，胆汁酸及其代谢和体内平衡相关的疾病的治疗用途的化学工具。

10. 发明申请

US20060128764A1 Non-steroidal farnesoid x receptor modulators and methods for the use thereof 失效
标题翻译：非甾体法尼斯X受体调节剂及其使用方法
公开(公告)号：US20060128764A1
公开(公告)日：2006-06-15
申请号：US10535043
申请日：2003-11-14
申请人： Michael Downes , Ronald Evans
发明人： Michael Downes , Ronald Evans
IPC分类号： A61K31/4433 , A61K31/44 , A61K31/353 , A61K31/16
CPC分类号： C07D311/94 , A61K31/16 , A61K31/353 , A61K31/44 , A61K31/4433 , C07C233/54 , C07C233/63 , C07C233/81 , C07C237/22 , C07C275/42 , C07C309/66 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/40 , C07D277/28 , C07D307/46 , C07D311/04 , C07D311/22 , C07D311/64 , C07D311/68 , C07D317/58 , C07D333/20 , C07D333/22 , C07D407/12 , C07D409/12
摘要： The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
摘要翻译：胆固醇合成，代谢，获取和运输的有效调节是脂质体内平衡的重要组成部分。法呢蛋白X受体（FXR）是胆汁酸的转录传感器，胆汁酸是胆固醇代谢的主要产物。因此，FXR的有效的，选择性的，小分子激动剂，部分激动剂和拮抗剂的开发将是进一步去卷积FXR生理学中的重要步骤。根据本发明，描述了新型有效的FXR活化剂的鉴定。携带二苯乙烯或联芳基部分的本发明化合物的两种衍生物含有迄今为止基于细胞的测定中报道的最有效的FXR激动剂的成员。这些化合物可用作进一步定义FXR的生理作用以及用于治疗与胆固醇，胆汁酸及其代谢和体内平衡相关的疾病的治疗用途的化学工具。

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