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1. 发明专利

IL254187D0 Tgf-beta inhibitors 未知
公开(公告)号：IL254187D0
公开(公告)日：2017-10-31
申请号：IL25418717
申请日：2017-08-28
申请人： RIGEL PHARMACEUTICALS INC , SQUIBB BRISTOL MYERS CO , TODD KINSELLA , MARINA GELMAN , HUI HONG , IHAB S DARWISH , RAJINDER SINGH , JIAXIN YU , ROBERT M BORZILLERI , UPENDER VELAPARTHI , PEIYING LIU , CHETAN DARNE , HASIBUR RAHAMAN , JAYAKUMAR SANKARA WARRIER
发明人： TODD KINSELLA , MARINA GELMAN , HUI HONG , IHAB S DARWISH , RAJINDER SINGH , JIAXIN YU , ROBERT M BORZILLERI , UPENDER VELAPARTHI , PEIYING LIU , CHETAN DARNE , HASIBUR RAHAMAN , JAYAKUMAR SANKARA WARRIER
IPC分类号： C07D20060101
摘要： and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

2. 发明申请

US20150087673A1 METHODS FOR USING AND BIOMARKERS FOR AMPK-ACTIVATING COMPOUNDS 审中-公开
标题翻译：用于AMPK激活化合物的方法和生物标志物
公开(公告)号：US20150087673A1
公开(公告)日：2015-03-26
申请号：US14498921
申请日：2014-09-26
申请人： Yasumichi Hitoshi , Yonchu Jenkins , Vadim Markovtsov , Todd Kinsella , Tian-Qiang Sun
发明人： Yasumichi Hitoshi , Yonchu Jenkins , Vadim Markovtsov , Todd Kinsella , Tian-Qiang Sun
IPC分类号： A61K31/4545 , C07D401/14 , A61K45/06 , G01N33/573
CPC分类号： A61K31/4545 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , G01N33/573 , G01N2500/04 , A61K2300/00
摘要： Disclosed are methods of using AMPK-activating compounds, for example, in the treatment of cancer and disorders of vascular flow. Also disclosed are biomarkers for AMPK and uses thereof, for example, in the diagnosis and treatment of AMPK-linked disorders. In certain embodiments, the AMPK-activating compounds have the structural formula wherein E, J, T, D1, D2, D3, the ring system denoted by “B”, T, R3, R4, w and x are as described herein.
摘要翻译：公开了使用AMPK活化化合物的方法，例如用于治疗癌症和血管流动障碍。还公开了AMPK的生物标志物及其用途，例如在AMPK相关疾病的诊断和治疗中。在某些实施方案中，AMPK活化化合物具有其结构式，其中E，J，T，D1，D2，D3，由“B”，T，R3，R4，w和x表示的环系统如本文所述。

3. 发明申请

US20080009076A1 METHODS OF IDENTIFYING COMPOUNDS THAT MODULATE IL-4 RECEPTOR-MEDIATED IGE SYNTHESIS UTILIZING A THIOREDOXIN-LIKE 32 KDA PROTEIN 有权
标题翻译：鉴定化合物的方法，该化合物调节IL-4受体介导的神经元合成使用类似噻二氮素的32 KDA蛋白
公开(公告)号：US20080009076A1
公开(公告)日：2008-01-10
申请号：US11608735
申请日：2006-12-08
申请人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
发明人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
IPC分类号： G01N33/567
CPC分类号： G01N33/6854 , A61K38/00
摘要： The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a thioredoxin-like 32 kDa protein (TXNL) as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.
摘要翻译：本发明提供了能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用硫氧还蛋白样32kDa蛋白（TXNL）作为替代分析物的化合物的方法和试剂盒以及在各种体外和体外上下文中使用化合物的方法。

4. 发明申请

US20070054862A1 Methods of Identifying Compounds that Modulate IL-4 Receptor-Mediated IgE Synthesis Utilizing an Adenosine Kinase 审中-公开
标题翻译：鉴定使用腺苷激酶调节IL-4受体介导的IgE合成的化合物的方法
公开(公告)号：US20070054862A1
公开(公告)日：2007-03-08
申请号：US11550731
申请日：2006-10-18
申请人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
发明人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
IPC分类号： C07K14/47 , A61K38/16
CPC分类号： C12N9/1205 , A61K31/00 , A61K31/7076
摘要： The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize an adenosine kinase as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.
摘要翻译：本发明提供能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用腺苷激酶作为替代分析物的化合物的方法和试剂盒以及使用该化合物的方法各种体外，体外和体外上下文。

5. 发明申请

US20060275751A1 Methods and compositions for screening using diphtheria toxin constructs 有权
公开(公告)号：US20060275751A1
公开(公告)日：2006-12-07
申请号：US11392434
申请日：2006-03-28
申请人： Todd Kinsella
发明人： Todd Kinsella
IPC分类号： C40B30/06 , C40B50/06
CPC分类号： C07K14/475 , C07K14/43595 , C07K14/70596
摘要： The invention relates to methods and compositions utilizing diphtheria toxin for screening purposes. The invention is particularly useful in screening for modulators of IgE synthesis, secretion and switch rearrangement.

6. 发明申请

US20050282736A1 Methods for cyclizing synthetic polymers 有权
标题翻译：环合合成聚合物的方法
公开(公告)号：US20050282736A1
公开(公告)日：2005-12-22
申请号：US11136806
申请日：2005-05-24
申请人： Todd Kinsella
发明人： Todd Kinsella
IPC分类号： A61K38/00 , A61K38/16 , C12N15/10 , C12P19/34 , C12P21/02 , C12P21/06 , G01N33/53
CPC分类号： C12P19/34 , A61K38/00 , C12N15/10 , C12P21/02
摘要： The invention provides methods and compositions for production of a cyclic polymer in a cell free system. In general, the methods of the invention involve ligating first and second recombinant intein domains to a linear synthetic polymer to form a compound containing the structure: D1-X(n)-D2, where D1 is a first catalytic domain of an intein; D2 is a second catalytic domain of an intein; where the second catalytic domain has at its N-terminus a first reactive site for the intein; and X(n) is a polymer of a number n of monomer X, where the polymer N-terminus has a second reactive site for the intein. D1-X(n)-D2 compounds autocatalytically cyclize the X(n) polymer to produce a cyclic polymer. The invention finds use in a variety of drug discovery, clinical and therapeutic applications.
摘要翻译：本发明提供了在无细胞体系中生产环状聚合物的方法和组合物。通常，本发明的方法涉及将第一和第二重组内含肽结构域连接到线性合成聚合物以形成含有以下结构的化合物：D 1 -X（n）其中D 1是内含肽的第一催化结构域; D 2是内含肽的第二催化结构域; 其中第二催化结构域在其N末端具有用于内含肽的第一反应位点; 且X（n）是数量为n的单体X的聚合物，其中聚合物N末端具有用于内含肽的第二反应位点。化合物自由催化地使X（n）聚合物环化，从而产生一个（N）环状聚合物。本发明可用于各种药物发现，临床和治疗应用。

7. 发明申请

US20050233456A1 IN VIVO PRODUCTION OF CYCLIC PEPTIDES 有权
标题翻译：循环生殖细胞生产
公开(公告)号：US20050233456A1
公开(公告)日：2005-10-20
申请号：US09800770
申请日：2001-03-06
申请人： Todd Kinsella
发明人： Todd Kinsella
IPC分类号： C12N15/10 , C12N15/867
CPC分类号： C12N15/1055 , C12N15/10
摘要： The present invention relates ti methods and compositions utilizing inteins to generated libraries of cyclic peptides in vivo.
摘要翻译：本发明涉及利用内含肽在生物体内生成环肽文库的方法和组合物。

8. 发明申请

US20050112702A1 Methods of identifying compounds that modulate IL-4 receptor mediated IgE synthesis utilizing a CLLD8 protein 有权
标题翻译：鉴定使用CLLD8蛋白调节IL-4受体介导的IgE合成的化合物的方法
公开(公告)号：US20050112702A1
公开(公告)日：2005-05-26
申请号：US11027949
申请日：2004-12-30
申请人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
发明人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
IPC分类号： A61K38/17 , C07K7/08 , C07K14/54 , G01N33/68 , G01N33/53 , G01N33/567
CPC分类号： C07K7/08 , A61K38/1709 , C07K14/5406 , G01N33/6869 , G01N2333/5406 , G01N2500/00 , Y10S435/975
摘要： The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a CLLD8 protein as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.
摘要翻译：本发明提供能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用CLLD8蛋白作为替代分析物的化合物的方法和试剂盒以及使用该化合物的方法各种体外，体外和体外上下文。

9. 发明授权

US5830725A Rapid, stable high-titre production of recombing retrovirus 失效
标题翻译：快速，稳定的高滴度生产推荐逆转录病毒
公开(公告)号：US5830725A
公开(公告)日：1998-11-03
申请号：US430813
申请日：1995-04-28
申请人： Garry P. Nolan , Todd Kinsella
发明人： Garry P. Nolan , Todd Kinsella
IPC分类号： C12N15/867 , C12N15/00 , A61K48/00 , C07K14/00 , C12N5/00
CPC分类号： C12N15/86 , C12N2740/13043
摘要： High titre helper-free recombinant retrovirus are produced by (a) growing a transfected host cell, produced by transfecting a eukaryotic host cell with a recombinant vector capable of stable episomal maintenance in the host cell, in a medium under conditions whereby the recombinant vector is stably maintained as an episome in the transfected host cell and transcripts of said vector form, with retroviral gag, pol and env gene products, an infectious retrovirus; and (b) isolating from the medium helper-free infectious retrovirus formed in the transfected host cell. The recombinant vectors comprise (i) a retroviral construct comprising an exogenous gene; (ii) a eukaryotic origin of replication sequence providing a substrate for replicase activity capable of replicating the vector in the host cell; and, (iii) a copy control sequence providing a substrate for a copy control activity capable of maintaining the vector at a stable copy number in the host cell. The transfected host cell provides retroviral pol reverse transcriptase and integrase activity, the replicase activity and copy control activity, as well as retroviral gag and env gene products capable of forming, with a transcript of the retroviral construct, an infectious retrovirus.
摘要翻译：通过以下步骤制备高滴度无辅助重组逆转录病毒：（a）通过在培养基中培养转染的宿主细胞，所述转染的宿主细胞通过在宿主细胞中能够稳定的附加型维持的重组载体转染真核宿主细胞而产生，在转染的宿主细胞中稳定地维持该转录物和所述载体形式的转录物，其具有逆转录病毒gag，pol和env基因产物，感染性逆转录病毒; 和（b）从转染的宿主细胞中形成的中等无辅助感染性逆转录病毒分离。重组载体包含（i）包含外源基因的逆转录病毒构建体; （ii）提供能够复制宿主细胞中的载体的复制酶活性的底物的真核复制起点序列; 和（iii）复制控制序列，其提供能够将载体维持在宿主细胞中稳定拷贝数的拷贝控制活性的底物。转染的宿主细胞提供逆转录病毒pol逆转录酶和整合酶活性，复制酶活性和拷贝对照活性，以及能够与逆转录病毒构建体的转录物形成感染性逆转录病毒的逆转录病毒gag和env基因产物。

10. 发明申请

US20080003620A1 METHODS OF IDENTIFYING COMPOUNDS THAT MODULATE IL-4 RECEPTOR-MEDIATED IGE SYNTHESIS UTILIZING AN ADENOSINE KINASE 审中-公开
标题翻译：鉴定化合物的方法，其调节IL-4受体介导的神经元合成使用腺苷激酶
公开(公告)号：US20080003620A1
公开(公告)日：2008-01-03
申请号：US11608788
申请日：2006-12-08
申请人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
发明人： Esteban Masuda , Todd Kinsella , Justin Warner , Taisei Kinoshita , Mark Bennett , David Anderson
IPC分类号： G01N33/566
CPC分类号： C12N9/1205 , A61K31/00 , A61K31/7076
摘要： The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize an adenosine kinase as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.
摘要翻译：本发明提供能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用腺苷激酶作为替代分析物的化合物的方法和试剂盒以及使用该化合物的方法各种体外，体外和体外上下文。

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