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11. 发明申请

US20070141624A1 ACTIVITY-BASED PROBES AND METHODS OF THEIR PREPARATION ANS USE 有权
标题翻译：基于活动的探索及其准备工作使用的方法
公开(公告)号：US20070141624A1
公开(公告)日：2007-06-21
申请号：US10530646
申请日：2003-10-08
申请人： David Winn
发明人： David Winn
IPC分类号： C40B30/06 , C40B40/04 , C12Q1/37 , C07D311/88
CPC分类号： C07D311/90 , C07D311/82 , C12Q1/37
摘要： The present invention provides compositions and methods for assessing profiles of catalytically active enzymes in compositions containing a plurality of proteins. In preferred embodiments, the enzyme is a hydrolase, most preferably a cysteine protease. The methods described herein use activity based probes (“ABPs”) that have an affinity moiety for directing the binding of the ABP to one or more catalytically active target enzymes, a reactive group for forming a covalent bond at an active site of the target enzyme(s), and a TAG (e.g., a detectable label, preferably a fluorophore). One or more ABPs may be combined with a protein-containing sample under conditions for binding and reaction of the ABP(s) with target enzyme(s) that are present in the sample. The resulting products may then be used to assess the active enzyme profile of the sample, and can be correlated to the presence, amount, or activity of one or more target enzyme(s) present in the original complex protein mixture.
摘要翻译：本发明提供了用于在含有多种蛋白质的组合物中评估催化活性酶的谱的组合物和方法。在优选的实施方案中，酶是水解酶，最优选半胱氨酸蛋白酶。本文描述的方法使用具有亲和部分的活性基探针（“ABP”），该亲和部分用于引导ABP与一种或多种催化活性靶酶的结合，用于在靶酶的活性位点形成共价键的反应性基团（例如，可检测标记，优选荧光团）。可以在ABP与样品中存在的目标酶的结合和反应的条件下，将一种或多种ABP与含蛋白质的样品组合。然后可以将所得产物用于评估样品的活性酶谱，并且可与存在于原始复合蛋白混合物中的一种或多种目标酶的存在，量或活性相关。

12. 发明申请

US20060264401A1 METHYL AND ETHYL SUBSTITUTED PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 有权
标题翻译：甲基和乙基取代的吡咯烷酮化合物及其选择性抑制DIPEPTIDYL PEPTIDASE-IV的方法
公开(公告)号：US20060264401A1
公开(公告)日：2006-11-23
申请号：US11381090
申请日：2006-05-01
申请人： David Campbell , David Winn , Juan Betancort
发明人： David Campbell , David Winn , Juan Betancort
IPC分类号： A61K31/69 , C07F5/02
CPC分类号： C07F5/025
摘要： The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.
摘要翻译：本发明涉及显示选择性，有效的二肽基肽酶IV抑制活性的吡咯烷基氨基乙酰基吡咯烷硼酸化合物。这些化合物可用于治疗可以通过抑制DPP-IV调节或归一化的疾病，包括以血糖控制受损为特征的糖尿病和相关病症。化合物可以单独施用或与另外一种显示用于治疗这些和其它疾病的药理活性的药物一起施用。

13. 发明申请

US20060264400A1 PYRROLIDINE COMPOUNDS AND METHODS FOR SELECTIVE INHIBITION OF DIPEPTIDYL PEPTIDASE-IV 有权
标题翻译：吡咯啉化合物和选择性抑制DIPEPTIDYL PEPTIDASE-IV的方法
公开(公告)号：US20060264400A1
公开(公告)日：2006-11-23
申请号：US11381085
申请日：2006-05-01
申请人： David Campbell , David Winn , Juan Betancort
发明人： David Campbell , David Winn , Juan Betancort
IPC分类号： A61K31/69 , C07F5/02
CPC分类号： C07F5/025
摘要： The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.
摘要翻译：本发明涉及显示选择性，有效的二肽基肽酶IV抑制活性的吡咯烷基氨基乙酰基吡咯烷硼酸化合物。这些化合物可用于治疗可以通过抑制DPP-IV调节或归一化的疾病，包括以血糖控制受损为特征的糖尿病和相关病症。化合物可以单独施用或与另外一种显示用于治疗这些和其它疾病的药理活性的药物一起施用。

14. 发明申请

US20070185061A1 HETEROCYCLIC BORONIC ACID COMPOUNDS 审中-公开
标题翻译：杂环硼酸化合物
公开(公告)号：US20070185061A1
公开(公告)日：2007-08-09
申请号：US11556944
申请日：2006-11-06
申请人： David Campbell , David Winn , Juan Betancort , Kevin Shreder , Yi Hu , Bei Li , Melissa Wong , Lifu Ma , William Ripka , Min Wu
发明人： David Campbell , David Winn , Juan Betancort , Kevin Shreder , Yi Hu , Bei Li , Melissa Wong , Lifu Ma , William Ripka , Min Wu
IPC分类号： A61K31/69 , C07F5/02
CPC分类号： C07F5/025
摘要： Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CRiRii, R1, R2, R3, R4 and R5 are as described herein.
摘要翻译：提供二肽基肽酶IV（DPP-IV）抑制化合物，其具有式I：其中n为1至3; X是CH 2 2; S; O; CF 2或C（CH 3）2）2。 Z是H; 卤素; 羟; （C 1-6）烷氧基; （C 1-12）烷基; （C 3-12）环烷基; 苯基; 或杂芳基; 其中苯基和杂芳基任选被R 7独立或独立地取代; 任选地，X与相邻的环碳一起形成稠合的环丙基; 并且任选地，含有X的环中的一个键是双键; 和R 1，R 2，R 2，R 3，R 3， R 4和R 5如本文所述。

15. 发明申请

US20050200205A1 On-site power generation system with redundant uninterruptible power supply 审中-公开
标题翻译：具有冗余不间断电源的现场发电系统
公开(公告)号：US20050200205A1
公开(公告)日：2005-09-15
申请号：US11048621
申请日：2005-01-31
申请人： David Winn , Alfredo Hernandez , Gary Carr
发明人： David Winn , Alfredo Hernandez , Gary Carr
IPC分类号： H02J9/00 , H02K7/02 , H02P11/00
CPC分类号： H02J9/062 , H02J3/42 , H02J9/066 , H02J9/08 , Y10T307/615
摘要： Disclosed is a method and system for providing constant critical AC electrical load with primary, secondary, and in some cases a tertiary source of power with higher reliability and lower operating and capital costs and lower emissions than the traditional utility supply, uninterruptible power supply (UPS), and battery primary power source, and diesel generator back-up systems that are predominately used today. Specifically, the disclosed system utilizes on-site power generation to provide primary power and includes full utility and UPS/DC storage back-up systems.
摘要翻译：公开了一种方法和系统，用于在传统的公用电源，不间断电源（UPS）中提供具有较高可靠性和更低运行和资本成本以及更低排放的三次电源的一次，二次和三次电源，）和电池一次电源，以及今天主要使用的柴油发电机备用系统。具体地说，所公开的系统利用现场发电来提供一次电力，并且包括完整的公用事业和UPS / DC存储备用系统。

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