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1. 发明授权

US07834012B2 Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) 有权
标题翻译：药物组合物作为二肽基肽酶-IV（DPP-IV）的抑制剂
公开(公告)号：US07834012B2
公开(公告)日：2010-11-16
申请号：US11510451
申请日：2006-08-25
申请人： Zhonghua Pei , Thomas von Geldern , David J. Madar , Xiaofeng Li , Fatima Basha , Hong Yong , Kenton L. Longenecker , Bradley J. Backes , Andrew S. Judd , Mathew M. Mulhern , Kent D. Stewart
发明人： Zhonghua Pei , Thomas von Geldern , David J. Madar , Xiaofeng Li , Fatima Basha , Hong Yong , Kenton L. Longenecker , Bradley J. Backes , Andrew S. Judd , Mathew M. Mulhern , Kent D. Stewart
IPC分类号： A61K31/535 , A61K31/50 , A61K31/47 , A61K31/445 , A61K31/415 , C07D295/12 , C07D487/04 , C07D217/16 , C07D211/32 , C07D231/12
CPC分类号： C07C211/48 , C07C211/40 , C07C217/52 , C07C217/54 , C07C217/74 , C07C217/84 , C07C217/86 , C07C225/22 , C07C229/42 , C07C229/48 , C07C229/60 , C07C233/43 , C07C233/78 , C07C235/46 , C07C237/24 , C07C237/30 , C07C237/42 , C07C255/54 , C07C255/58 , C07C311/22 , C07C311/36 , C07C317/22 , C07C317/36 , C07C2601/14 , C07C2601/16 , C07D207/16 , C07D209/08 , C07D209/48 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/64 , C07D213/68 , C07D213/74 , C07D213/82 , C07D217/04 , C07D263/56 , C07D263/60 , C07D277/04 , C07D277/64 , C07D295/135 , C07D295/185 , C07D295/205 , C07D317/66 , C07D319/18 , C07D333/34 , C07D333/38 , C07D409/04 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II, as well as hyperglycemia, metabolic syndrome, hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.
摘要翻译：本发明涉及抑制二肽基肽酶IV（DPP-IV）的化合物，其可用于预防或治疗糖尿病，特别是II型糖尿病，以及高血糖症，代谢综合征，高胰岛素血症，肥胖症，动脉粥样硬化，各种免疫调节疾病，和其他疾病。

2. 发明申请

US20090023572A1 CAPACITY ALTERING DEVICE, HOLDER, AND METHODS OF SAMPLE PROCESSING 审中-公开
标题翻译：容量改变装置，夹持器和样品加工方法
公开(公告)号：US20090023572A1
公开(公告)日：2009-01-22
申请号：US11972589
申请日：2008-01-10
申请人： Bradley J. Backes , Jim Chang , John Isbell , James K. Mainquist , Christopher M. Shaw
发明人： Bradley J. Backes , Jim Chang , John Isbell , James K. Mainquist , Christopher M. Shaw
IPC分类号： B01L9/00 , B04B7/12
CPC分类号： B01L3/00 , B01L3/5085 , B01L3/563 , B01L9/523
摘要： This invention provides capacity altering devices that facilitate the processing of samples whose volume exceeds the capacity of external sample processing regions (e.g., sample tubes or wells). The invention also provides holders that can be used with such devices, e.g., to allow centrifugation of the devices and/or to minimize handling of the external processing regions. Methods of processing samples, particularly samples whose volume exceeds the capacity of the external processing regions, and methods of collecting compounds in external processing regions are another feature of the invention.
摘要翻译：本发明提供了容量改变装置，其有助于处理体积超过外部样品处理区域（例如样品管或孔）的容量的样品。本发明还提供了可以与这种装置一起使用的保持器，例如允许设备的离心和/或最小化外部处理区域的处理。处理样品的方法，特别是体积超过外部处理区域的容量的样品以及在外部处理区域中收集化合物的方法是本发明的另一个特征。

3. 发明授权

US07629437B2 Fluorogenic materials and uses thereof 有权
标题翻译：荧光材料及其用途
公开(公告)号：US07629437B2
公开(公告)日：2009-12-08
申请号：US10686884
申请日：2003-10-15
申请人： Jennifer L. Harris , Bradley J. Backes , Jonathan A. Ellman , Charles S. Craik
发明人： Jennifer L. Harris , Bradley J. Backes , Jonathan A. Ellman , Charles S. Craik
IPC分类号： C12Q1/00 , C12Q1/37 , C07K5/00 , C07K7/00
CPC分类号： C12Q1/37 , C07K1/047 , C07K5/101 , C07K5/1024
摘要： A method is presented for the preparation and use of fluorogenic peptide substrates that allows for the configuration of general substrate libraries to rapidly identify the primary and extended specificity of enzymes, such as proteases. The substrates contain a fluorogenic-leaving group, such as 7-amino-4-carbamoylmethyl-coumarin (ACC). Substrates incorporating the ACC leaving group show comparable kinetic profiles as those with the traditionally used 7-amino-4-methyl-coumarin (AMC) leaving group. The bifunctional nature of ACC allows for the efficient production of single substrates and substrate libraries using solid-phase synthesis techniques.
摘要翻译：提出了一种用于制备和使用荧光肽底物的方法，其允许构建一般底物文库以快速鉴定酶（例如蛋白酶）的主要和延伸的特异性。底物含有荧光离去基团，如7-氨基-4-氨基甲酰甲基香豆素（ACC）。结合ACC离去基团的底物显示与传统使用的7-氨基-4-甲基香豆素（AMC）离去基团相似的动力学曲线。 ACC的双功能特性允许使用固相合成技术有效地生产单个底物和底物文库。

4. 发明授权

US07329393B2 Capacity altering device, holder, and methods of sample processing 失效
标题翻译：容量更换装置，夹持器和样品处理方法
公开(公告)号：US07329393B2
公开(公告)日：2008-02-12
申请号：US10682781
申请日：2003-10-08
申请人： Bradley J. Backes , Jim Chang , John Isbell , James K. Mainquist , Christopher M. Shaw
发明人： Bradley J. Backes , Jim Chang , John Isbell , James K. Mainquist , Christopher M. Shaw
IPC分类号： B01L3/00
CPC分类号： B01L3/00 , B01L3/5085 , B01L3/563 , B01L9/523
摘要： This invention provides capacity altering devices that facilitate the processing of samples whose volume exceeds the capacity of external sample processing regions (e.g., sample tubes or wells). The invention also provides holders that can be used with such devices, e.g., to allow centrifugation of the devices and/or to minimize handling of the external processing regions. Methods of processing samples, particularly samples whose volume exceeds the capacity of the external processing regions, and methods of collecting compounds in external processing regions are another feature of the invention.
摘要翻译：本发明提供了容量改变装置，其有助于处理体积超过外部样品处理区域（例如样品管或孔）的容量的样品。本发明还提供了可以与这种装置一起使用的保持器，例如允许设备的离心和/或最小化外部处理区域的处理。处理样品的方法，特别是体积超过外部处理区域的容量的样品以及在外部处理区域中收集化合物的方法是本发明的另一个特征。

5. 发明授权

US06680178B2 Profiling of protease specificity using combinatorial fluorogenic substrate libraries 有权
标题翻译：使用组合荧光底物库分析蛋白酶特异性
公开(公告)号：US06680178B2
公开(公告)日：2004-01-20
申请号：US09866132
申请日：2001-05-25
申请人： Jennifer L. Harris , Bradley J. Backes , Jonathan A. Ellman , Charles S. Craik
发明人： Jennifer L. Harris , Bradley J. Backes , Jonathan A. Ellman , Charles S. Craik
IPC分类号： C12Q137
CPC分类号： C12Q1/37 , C07K1/047 , C07K5/101 , C07K5/1024
摘要： A method is presented for the preparation and use of fluorogenic peptide substrates that allows for the configuration of general substrate libraries to rapidly identify the primary and extended specificity of enzymes, such as proteases. The substrates contain a fluorogenic-leaving group, such as 7-amino-4-carbamoylmethyl-coumarin (ACC). Substrates incorporating the ACC leaving group show comparable kinetic profiles as those with the traditionally used 7-amino-4-methyl-coumarin (AMC) leaving group. The bifunctional nature of ACC allows for the efficient production of single substrates and substrate libraries using solid-phase synthesis techniques. The approximately 3-fold increased quantum yield of ACC over AMC permits reduction in enzyme and substrate concentrations. As a consequence, a greater number of substrates can be tolerated in a single assay, thus enabling an increase in the diversity space of the library. Soluble positional protease substrate libraries of 137,180 and 6,859 members, possessing amino acid diversity at the P4-P3-P2-P1 and P4-P3-P2 positions, respectively, were constructed. Employing this screening method the substrate specificities of a diverse array of proteases were profiled, including the serine proteases thrombin, plasmin, factor Xa, uPA, tPA, granzyme B, trypsin, chymotrypsin, human neutrophil elastase, and the cysteine proteases papain and cruzain. The resulting profiles create a pharmacophoric portrayal of the proteases allowing for the design of selective substrates and potent inhibitors.
摘要翻译：提出了一种用于制备和使用荧光肽底物的方法，其允许构建一般底物文库以快速鉴定酶（例如蛋白酶）的主要和延伸的特异性。底物含有荧光离去基团，如7-氨基-4-氨基甲酰甲基香豆素（ACC）。结合ACC离去基团的底物显示与传统使用的7-氨基-4-甲基香豆素（AMC）离去基团相似的动力学曲线。 ACC的双功能特性允许使用固相合成技术有效地生产单个底物和底物文库。 ACC超过AMC的大约3倍增加的量子产率允许酶和底物浓度的降低。因此，在单个测定中可以容忍更多数量的底物，从而能够增加文库的多样性空间。构建了分别在P4-P3-P2-P1和P4-P3-P2位置具有氨基酸多样性的137,180和6,859个成员的可溶性位置蛋白酶底物文库。使用这种筛选方法，分析各种蛋白酶的底物特异性，包括丝氨酸蛋白酶凝血酶，纤溶酶，因子Xa，uPA，tPA，粒酶B，胰蛋白酶，胰凝乳蛋白酶，人嗜中性粒细胞弹性蛋白酶和半胱氨酸蛋白酶木瓜蛋白酶和克鲁津。所得的谱产生蛋白酶的药效学描述，允许设计选择性底物和有效的抑制剂。

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