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1. 发明申请

WO2005098025A2 HIGH THROUGHPUT REACTIVE OXYGEN SPECIES-BASED CYTOCHROME P450 INHIBITION ASSAY 审中-公开
标题翻译：高通量反应性氧化物质基于CYPCRROM的P450抑制测定
公开(公告)号：WO2005098025A2
公开(公告)日：2005-10-20
申请号：PCT/US2005/011551
申请日：2005-04-05
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , THAKKER, Dhiren, R. , ANSEDE, John, H.
发明人： THAKKER, Dhiren, R. , ANSEDE, John, H.
IPC分类号： C12Q1/26
CPC分类号： C12Q1/26
摘要： A method of screening a candidate compound for an ability to inhibit a cytochrome P450. The method includes the steps of reacting the candidate compound, an indicator compound precursor, a cytochrome P450 substrate, and the cytochrome P450, the cytochrome P450 characterized as having a side reaction associated with metabolic activity of the cytochrome P450 wherein a chemical species capable of reacting with the indicator compound precursor is produced; quantifying the amount of indicator compound produced in the presence of the candidate compound, and comparing the amount of indicator compound produced in the presence of the candidate compound to an amount of indicator produced under identical conditions in the absence of the candidate compound, the comparison indicating the ability of the candidate compound to inhibit the cytochrome P450. Also disclosed is a method for determining an inhibitory potency of a candidate compound for a cytochrome P450.
摘要翻译：筛选候选化合物以抑制细胞色素P450的能力的方法。该方法包括以下步骤：使候选化合物，指示剂化合物前体，细胞色素P450底物和细胞色素P450反应，细胞色素P450特征在于具有与细胞色素P450的代谢活性相关的副反应，其中能够反应的化学物质产生指示剂化合物前体; 量化在候选化合物存在下产生的指示剂化合物的量，并将候选化合物存在下产生的指示剂化合物的量与在不存在候选化合物的相同条件下产生的指示剂的量进行比较，比较表明候选化合物抑制细胞色素P450的能力。还公开了用于确定候选化合物对细胞色素P450的抑制效力的方法。

2. 发明申请

WO2008134063A3 ACTIVATED LIPASES AND METHODS OF USE THEREFOR 审中-公开
标题翻译：活化的脂肪及其使用方法
公开(公告)号：WO2008134063A3
公开(公告)日：2009-01-29
申请号：PCT/US2008005486
申请日：2008-04-28
申请人： UNIV NORTH CAROLINA , THAKKER DHIREN R , KLEIN RYAN R
发明人： THAKKER DHIREN R , KLEIN RYAN R
IPC分类号： C12N9/00 , C12N9/96
CPC分类号： C12P7/649 , C12N9/20 , Y02E50/13 , Y02P20/52
摘要： Methods for enhancing a biological (e.g., catalytic) activity of a lipase, are provided. In some embodiments, the methods include the step of alkylating one or more cysteine residues present within the lipase. Also provided are modified polypeptides for which a biological activity is enhanced by the disclosed methods, methods for using the disclosed polypeptides, including for the transesterification of renewable oils to produce a biofuel, and cell free systems that include a lipase, to which one or more moieties, such as steroidal moieties, are conjugated.
摘要翻译：提供了增强脂肪酶的生物（例如催化）活性的方法。在一些实施方案中，所述方法包括烷基化存在于脂肪酶内的一个或多个半胱氨酸残基的步骤。还提供了通过所公开的方法增强生物活性的修饰多肽，使用所公开的多肽的方法，包括用于可再生油的酯交换以产生生物燃料，以及包含脂肪酶的无细胞系统，一种或多种部分如甾体部分共轭。

3. 发明申请

WO2008134063A2 ACTIVATED LIPASES AND METHODS OF USE THEREFOR 审中-公开
标题翻译：活化的脂肪及其使用方法
公开(公告)号：WO2008134063A2
公开(公告)日：2008-11-06
申请号：PCT/US2008/005486
申请日：2008-04-28
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , THAKKER, Dhiren, R. , KLEIN, Ryan, R.
发明人： THAKKER, Dhiren, R. , KLEIN, Ryan, R.
IPC分类号： C12P7/64
CPC分类号： C12P7/649 , C12N9/20 , Y02E50/13 , Y02P20/52
摘要： Methods for enhancing a biological (e.g., catalytic) activity of a lipase, are provided. In some embodiments, the methods include the step of alkylating one or more cysteine residues present within the lipase. Also provided are modified polypeptides for which a biological activity is enhanced by the disclosed methods, methods for using the disclosed polypeptides, including for the transesterification of renewable oils to produce a biofuel, and cell free systems that include a lipase, to which one or more moieties, such as steroidal moieties, are conjugated.
摘要翻译：提供了增强脂肪酶的生物（例如催化）活性的方法。在一些实施方案中，所述方法包括烷基化存在于脂肪酶内的一个或多个半胱氨酸残基的步骤。还提供了通过所公开的方法增强生物活性的修饰多肽，使用所公开的多肽的方法，包括用于可再生油的酯交换以产生生物燃料，以及包含脂肪酶的无细胞系统，一种或多种部分如甾体部分共轭。

4. 发明申请

WO0210746A2 PHARMACOKINETIC TOOL AND METHOD FOR PREDICTING METABOLISM OF A COMPOUND IN A MAMMAL 审中-公开
标题翻译：药物动力学工具和用于预测化合物在代谢中的代谢的方法
公开(公告)号：WO0210746A2
公开(公告)日：2002-02-07
申请号：PCT/US0123867
申请日：2001-07-30
申请人： LION BIOSCIENCE AG , LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , HOLME KEVIN , IZHIKEVICH TATYANA , DOERR STEVENS JULIE , LECLUYSE EDWARD , THAKKER DHIREN R , GRASS GEORGE M
发明人： LEESMAN GLEN D , NORRIS DANIEL A , SINKO PATRICK J , HOLME KEVIN , IZHIKEVICH TATYANA , DOERR-STEVENS JULIE , LECLUYSE EDWARD , THAKKER DHIREN R , GRASS GEORGE M
IPC分类号： G01N33/15 , C12Q1/02 , G06F19/00 , G01N33/48
CPC分类号： G06F19/704 , G16H10/40 , G16H50/50
摘要： A system for simulating metabolism of a compound in a mammal is disclosed that includes a metabolism simulation model of a mammalian liver. This model has equations which when executed on a computer, calculate the rate of metabolism of the compound in the cells of the mammalian liver and a rate of transport of the compound into the cells, wherein the simulation model determines an amount of the metabolism product. The rate of metabolism may be a rate of depletion of the compound. The metabolism product may be an amount of the compound remaining after the compound's first passage through the mammalian liver (This is not necessarily limited to first pass, nor would it need to be limited to the liver. Intestinal metabolism could also be modeled). The rate of metabolism may alternatively be a rate of accumulation of a metabolite of the compound.
摘要翻译：公开了一种用于模拟哺乳动物中化合物代谢的系统，其包括哺乳动物肝脏的代谢模拟模型。该模型具有在计算机上执行时计算化合物在哺乳动物肝细胞中的代谢速率和化合物进入细胞的速率的方程式，其中模拟模型确定新陈代谢产物的量。代谢速率可能是化合物的消耗速率。代谢产物可以是化合物首次通过哺乳动物肝脏后残留的化合物的量（这不一定限于第一次通过，也不需要限于肝脏，也可以建模肠代谢）。代谢速率可以是化合物代谢物的积累速率。

5. 发明申请

WO2005098025A3 HIGH THROUGHPUT REACTIVE OXYGEN SPECIES-BASED CYTOCHROME P450 INHIBITION ASSAY 审中-公开
标题翻译：高通量反应性氧化物质基于CYPCRROM的P450抑制测定
公开(公告)号：WO2005098025A3
公开(公告)日：2006-03-23
申请号：PCT/US2005011551
申请日：2005-04-05
申请人： UNIV NORTH CAROLINA , THAKKER DHIREN R , ANSEDE JOHN H
发明人： THAKKER DHIREN R , ANSEDE JOHN H
IPC分类号： C12Q1/26
CPC分类号： C12Q1/26
摘要： A method of screening a candidate compound for an ability to inhibit a cytochrome P450. The method includes the steps of reacting the candidate compound, an indicator compound precursor, a cytochrome P450 substrate, and the cytochrome P450, the cytochrome P450 characterized as having a side reaction associated with metabolic activity of the cytochrome P450 wherein a chemical species capable of reacting with the indicator compound precursor is produced; quantifying the amount of indicator compound produced in the presence of the candidate compound, and comparing the amount of indicator compound produced in the presence of the candidate compound to an amount of indicator produced under identical conditions in the absence of the candidate compound, the comparison indicating the ability of the candidate compound to inhibit the cytochrome P450. Also disclosed is a method for determining an inhibitory potency of a candidate compound for a cytochrome P450.
摘要翻译：筛选候选化合物以抑制细胞色素P450的能力的方法。该方法包括以下步骤：使候选化合物，指示剂化合物前体，细胞色素P450底物和细胞色素P450反应，细胞色素P450特征在于具有与细胞色素P450的代谢活性相关的副反应，其中能够反应的化学物质产生指示剂化合物前体; 量化在候选化合物存在下产生的指示剂化合物的量，并将候选化合物存在下产生的指示剂化合物的量与在不存在候选化合物的相同条件下产生的指示剂的量进行比较，比较表明候选化合物抑制细胞色素P450的能力。还公开了用于确定候选化合物对细胞色素P450的抑制效力的方法。

6. 发明申请

WO0230408A3 COMPOSITIONS COMPRISING PHOSPHOLIPASE C INHIBITORS AND METHODS FOR ENHANCING PARACELLULAR PERMEABILITY ACROSS EPITHELIAL AND ENDOTHELIAL BARRIERS 审中-公开
标题翻译：包含磷脂酶C抑制剂的组合物和用于在上皮和内皮障碍物之间增强细胞渗透性的方法
公开(公告)号：WO0230408A3
公开(公告)日：2003-11-06
申请号：PCT/US0131501
申请日：2001-10-10
申请人： UNIV NORTH CAROLINA , THAKKER DHIREN R , WARD PETER D
发明人： THAKKER DHIREN R , WARD PETER D
IPC分类号： A61K45/00 , A61K31/353 , A61K31/37 , A61K31/56 , A61K31/58 , A61K31/661 , A61K31/685 , A61K45/06 , A61P1/14 , A61P25/00 , A61P43/00 , A61K31/00 , A61K47/22 , A61K47/24 , A61K47/28
CPC分类号： A61K45/06 , A61K31/353 , A61K31/37 , A61K31/58 , A61K31/685 , Y10S514/946
摘要： Compositions and methods for enhancing paracellular permeability at an absorption site in a subject are disclosed. The method includes: (a) administering an effective amount of a phospholipase C inhibitor to a subject at a time in which enhanced paracellular permeability is desired; and (b) enhancing paracellular permaeability in the subject at the the absorption site through the administering of the effective amount of the phospholipase C inhibitor. The disclosed compositions and methods provide enhanced absorption of a hydrophilic drug in a subject.
摘要翻译：公开了用于在受试者的吸收部位增强细胞旁渗透性的组合物和方法。该方法包括：（a）在需要增加细胞旁渗透性的时间向受试者施用有效量的磷脂酶C抑制剂; 和（b）通过施用有效量的磷脂酶C抑制剂来增强受试者在吸收部位的细胞旁通能力。所公开的组合物和方法提供了受试者中亲水药物的增强的吸收。

7. 发明申请

WO2002010746A3 PHARMACOKINETIC TOOL AND METHOD FOR PREDICTING METABOLISM OF A COMPOUND IN A MAMMAL 审中-公开
公开(公告)号：WO2002010746A3
公开(公告)日：2002-02-07
申请号：PCT/US2001/023867
申请日：2001-07-30
申请人： LION BIOSCIENCE AG , LEESMAN, Glen, D. , NORRIS, Daniel, A. , SINKO, Patrick, J. , HOLME, Kevin , IZHIKEVICH, Tatyana , DOERR-STEVENS, Julie , LECLUYSE, Edward , THAKKER, Dhiren, R. , GRASS, George, M.
发明人： LEESMAN, Glen, D. , NORRIS, Daniel, A. , SINKO, Patrick, J. , HOLME, Kevin , IZHIKEVICH, Tatyana , DOERR-STEVENS, Julie , LECLUYSE, Edward , THAKKER, Dhiren, R. , GRASS, George, M.
IPC分类号： G06F19/00
摘要： A system for simulating metabolism of a compound in a mammal is disclosed that includes a metabolism simulation model of a mammalian liver. This model has equations which when executed on a computer, calculate the rate of metabolism of the compound in the cells of the mammalian liver and a rate of transport of the compound into the cells, wherein the simulation model determines an amount of the metabolism product. The rate of metabolism may be a rate of depletion of the compound. The metabolism product may be an amount of the compound remaining after the compound's first passage through the mammalian liver (This is not necessarily limited to first pass, nor would it need to be limited to the liver. Intestinal metabolism could also be modeled). The rate of metabolism may alternatively be a rate of accumulation of a metabolite of the compound.

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