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1. 发明授权

US06753177B1 P-glycoproteins and uses thereof 失效
标题翻译： P-糖蛋白及其用途
公开(公告)号：US06753177B1
公开(公告)日：2004-06-22
申请号：US09672725
申请日：2000-09-28
申请人： Penny J. Stocker , Dorothy T. Steimel-Crespi , Charles L. Crespi , Timothy C. Reif , Christopher J. Patten
发明人： Penny J. Stocker , Dorothy T. Steimel-Crespi , Charles L. Crespi , Timothy C. Reif , Christopher J. Patten
IPC分类号： C12P2106
CPC分类号： C07K14/705
摘要： The invention pertains to dog P-glycoproteins and related P-glycoproteins which include dog-specific amino acids, as well as nucleic acids which encode those polypeptides. The present invention also includes fragments and biologically functional variants of the dog P-glycoprotein. The invention further relates to methods of using such dog P-glycoprotein nucleic acids and polypeptides, especially in methods for determining bioavailability of drugs and for screening for inhibitors of dog PGP. Also included are dog PGP inhibitors which inhibit dog PGP activity by inhibiting the expression or function of dog PGP.
摘要翻译：本发明涉及狗P-糖蛋白和包括狗特异性氨基酸的相关P-糖蛋白，以及编码那些多肽的核酸。本发明还包括狗P-糖蛋白的片段和生物功能变体。本发明还涉及使用这种狗P-糖蛋白核酸和多肽的方法，特别是在确定药物生物利用度和筛选狗PGP抑制剂的方法中。还包括通过抑制狗PGP的表达或功能来抑制狗PGP活性的狗PGP抑制剂。

2. 发明授权

US06617450B1 P-glycoproteins and uses thereof 失效
标题翻译： P-糖蛋白及其用途
公开(公告)号：US06617450B1
公开(公告)日：2003-09-09
申请号：US09672810
申请日：2000-09-28
申请人： Penny J. Stocker , Dorothy T. Steimel-Crespi , Charles L. Crespi
发明人： Penny J. Stocker , Dorothy T. Steimel-Crespi , Charles L. Crespi
IPC分类号： C07H2104
CPC分类号： C07K14/705
摘要： The invention pertains to cynomologous monkey P-glycoproteins and related P-glycoproteins which include cynomologous-specific amino acids, as well as nucleic acids which encode those polypeptides. The present invention also includes fragments and biologically functional variants of the cynomologous monkey P-glycoprotein. The invention further relates to methods of using such cynomologous monkey P-glycoprotein nucleic acids and polypeptides, especially in methods for determining bioavailability of drugs and for screening for inhibitors of cynomologous PGP. Also included are cynomologous PGP inhibitors which inhibit cynomologous PGP activity by inhibiting the expression or function of cynomologous PGP.
摘要翻译：本发明涉及包括人类特异性氨基酸的同源猴P-糖蛋白和相关P-糖蛋白，以及编码这些多肽的核酸。本发明还包括食蟹猴P-糖蛋白的片段和生物学功能变体。本发明进一步涉及使用这种cynomologous猴P-糖蛋白核酸和多肽的方法，特别是用于确定药物的生物利用度和筛选cynomologous PGP抑制剂的方法。还包括通过抑制cynomologous PGP的表达或功能来抑制Cynomologous PGP活性的cynomologous PGP抑制剂。

3. 发明申请

US20070269850A1 ELASTOMERIC DEVICE FOR CELL SEEDING ON THE BOTTOM OF A FILTER 有权
标题翻译：用于在过滤器底部进行细胞接种的弹性装置
公开(公告)号：US20070269850A1
公开(公告)日：2007-11-22
申请号：US11750067
申请日：2007-05-17
申请人： Charles L. Crespi , Xiaoxi (Kevin) Chen
发明人： Charles L. Crespi , Xiaoxi (Kevin) Chen
IPC分类号： C12Q1/24 , C12M1/34
CPC分类号： C12M23/20 , C12M25/04 , C12M33/06 , Y10T436/25375
摘要： An article is provided herein for use in seeding cells on at least one filter extending across at least one well of an assay device. The article includes an elastomeric body having spaced-apart first and second surfaces, and at least one channel extending between, and through the first and second surfaces. The channel is formed to sealingly, and detachably, engage an outer surface of the well with the filter being at least partially encompassed by the channel. Advantageously, with the subject invention, a cell monolayer can be formed on the exterior surface of the filter. The assay device may be a multiwell plate, an insert plate, a column a test tube, or a pipette.
摘要翻译：本文提供了用于在至少一个穿过测定装置的至少一个孔延伸的过滤器上接种细胞的制品。该制品包括具有间隔开的第一和第二表面的弹性体，以及在第一和第二表面之间延伸并穿过第一和第二表面的至少一个通道。通道形成为密封地且可拆卸地与孔的外表面接合，过滤器至少部分地被通道包围。有利地，通过本发明，可以在过滤器的外表面上形成细胞单层。测定装置可以是多孔板，插入板，柱，试管或移液管。

4. 发明授权

US08986781B2 Immobilized multi-layer artificial membrane for permeability measurements (PAMPA) 有权
标题翻译：固定多层人造膜渗透测量（PAMPA）
公开(公告)号：US08986781B2
公开(公告)日：2015-03-24
申请号：US11552606
申请日：2006-10-25
申请人： Xiaoxi (Kevin) Chen , Charles L. Crespi
发明人： Xiaoxi (Kevin) Chen , Charles L. Crespi
IPC分类号： B01D61/36 , B01D61/38 , B01D69/10 , G01N15/08 , B01L3/00
CPC分类号： B01D69/144 , B01D61/38 , B01D67/0002 , B01D69/10 , B01D71/34 , B01D71/50 , B01D71/74 , B01D71/82 , B01D2323/04 , B01L3/50255 , G01N15/08 , G01N15/082 , G01N2001/4016 , G01N2015/084 , G01N2015/086 , Y10T436/255
摘要： With the subject invention, a method is provided for preparing a filter membrane including the steps of dispersing a liquid which is generally hydrophobic into the pores of a porous membrane, and applying a solution containing lipids onto at least a first surface of the porous membrane containing the liquid. Advantageously, the subject invention allows for filter membranes to be prepared which can be stored for periods of time without degradation in performance. The subject invention may have applicability in various contexts, but is well-suited for preparing filter membranes for permeability screening, particularly Parallel Artificial Membrane Permeability Assay (PAMPA).
摘要翻译：对于本发明，提供了一种制备滤膜的方法，包括以下步骤：将通常是疏水性的液体分散到多孔膜的孔中，并将含有脂质的溶液施加到多孔膜的至少第一表面上，该第一表面含有液体。有利地，本发明允许制备可以储存一段时间而不降低性能的滤膜。本发明可以在各种情况下具有适用性，但是非常适用于制备用于渗透性筛选的滤膜，特别是平行人造膜渗透性测定法（PAMPA）。

5. 发明授权

US06420131B1 Use of fluorescein aryl ethers in high throughput cytochrome P450 inhibition assays 有权
标题翻译：在高通量细胞色素P450抑制测定中使用荧光素芳基醚
公开(公告)号：US06420131B1
公开(公告)日：2002-07-16
申请号：US09636332
申请日：2000-08-10
申请人： Vaughn P. Miller , David Streser , Charles L. Crespi
发明人： Vaughn P. Miller , David Streser , Charles L. Crespi
IPC分类号： C12Q126
CPC分类号： C12Q1/26 , C07D311/82 , G01N2333/795 , G01N2333/80 , G01N2333/90245 , Y10S435/968
摘要： Novel fluorescent substrates of human cytochrome P450 enzymes are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing cytochrome P450 enzyme activity and in selecting compounds which inhibit cytochrome P450 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of cytochrome P450 enzyme activity.
摘要翻译：提供人类细胞色素P450酶的新型荧光底物。还提供了用于其制造和使用的方法。这些底物可用于评估细胞色素P450酶活性和选择抑制细胞色素P450酶活性的化合物，特别是鉴定由抑制细胞色素P450酶活性介导的潜在不良药物相互作用。

6. 发明授权

US4532204A Mutation assays involving blood cells that metabolize toxic substances 失效
标题翻译：涉及代谢有毒物质的血细胞的突变测定
公开(公告)号：US4532204A
公开(公告)日：1985-07-30
申请号：US399851
申请日：1982-07-19
申请人： Charles L. Crespi , William G. Thilly
发明人： Charles L. Crespi , William G. Thilly
IPC分类号： C12N5/00 , C02F1/02 , C12N5/02 , C12N5/06 , C12Q1/02 , C12R1/91 , F24D11/02 , F24J3/00 , F25B30/00 , G01N33/50 , C12N15/00
CPC分类号： C02F1/02 , F24D11/025 , F24J3/00 , F25B30/00 , G01N33/5017 , Y02B30/126 , Y02B30/52 , Y10S435/948
摘要： A line of human blood cells which have high levels of oxidative activity (such as oxygenase, oxidase, peroxidase, and hydroxylase activity) is disclosed. Such cells grow in suspension culture, and are useful to determine the mutagenicity of xenobiotic substances that are metabolized into toxic or mutagenic substances. Mutation assays using these cells, and other cells with similar characteristics, are also disclosed.
摘要翻译：公开了一系列具有高水平氧化活性（例如加氧酶，氧化酶，过氧化物酶和羟化酶活性）的人类血细胞。这种细胞在悬浮培养物中生长，并且可用于确定被代谢为有毒或致突变物质的异种生物物质的致突变性。还公开了使用这些细胞和具有相似特征的其它细胞的突变测定。

7. 发明授权

US06207404B1 Coumarin-based CYP3A fluorescent assay reagents 有权
标题翻译：基于香豆素的CYP3A荧光测定试剂
公开(公告)号：US06207404B1
公开(公告)日：2001-03-27
申请号：US09410212
申请日：1999-09-30
申请人： Vaughn P. Miller , Charles L. Crespi
发明人： Vaughn P. Miller , Charles L. Crespi
IPC分类号： C12Q126
CPC分类号： C12Q1/26 , C07D311/16 , Y10S435/968
摘要： Novel fluorescent substrates of human cytochrome P450 enzymes are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing cytochrome P450 enzyme activity and in selecting compounds which inhibit cytochrome P450 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of cytochrome P450 enzyme activity. The compounds are particularly useful for assessing cytochrome P450 CYP3A enzyme activity.
摘要翻译：提供人类细胞色素P450酶的新型荧光底物。还提供了用于其制造和使用的方法。这些底物可用于评估细胞色素P450酶活性和选择抑制细胞色素P450酶活性的化合物，特别是鉴定由抑制细胞色素P450酶活性介导的潜在不良药物相互作用。该化合物特别可用于评估细胞色素P450 CYP3A酶活性。

8. 发明授权

US6130342A CYP2D fluorescent assay reagents 有权
标题翻译： CYP2D荧光检测试剂
公开(公告)号：US6130342A
公开(公告)日：2000-10-10
申请号：US352576
申请日：1999-07-12
申请人： Vaughn P. Miller , Charles L. Crespi
发明人： Vaughn P. Miller , Charles L. Crespi
IPC分类号： C07D311/12 , C07D311/16 , C07D311/18 , C12Q1/26
CPC分类号： C07D311/16 , C12Q1/26
摘要： Novel fluorescent substrates of the human P450 enzyme CYP2D6 are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing CYP2D6 enzyme activity and in selecting compounds which inhibit CYP2D6 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of CYP2D6 enzyme activity.
摘要翻译：提供人P450酶CYP2D6的新型荧光底物。还提供了用于其制造和使用的方法。这些底物可用于评估CYP2D6酶活性和选择抑制CYP2D6酶活性的化合物，特别是鉴定由抑制CYP2D6酶活性介导的潜在不良药物相互作用。

9. 发明授权

US5429948A Human cell line stably expressing 5cDNAS encoding procarcinogen-activating enzymes and related mutagenicity assays 失效
标题翻译：稳定表达编码致癌活化酶的5cDNAS的人细胞系和相关致突变性测定
公开(公告)号：US5429948A
公开(公告)日：1995-07-04
申请号：US997455
申请日：1992-12-28
申请人： Charles L. Crespi , Bruce W. Penman , Robin L. Davies
发明人： Charles L. Crespi , Bruce W. Penman , Robin L. Davies
IPC分类号： C12N9/02 , C12N9/14 , C12Q1/26 , G01N33/50 , C12N15/00
CPC分类号： C12N9/0077 , C12N9/14 , C12Q1/26 , G01N33/5011 , G01N2500/00
摘要： An immortal human cell line stably expressing a multiplicity of cytochrome P450s is provided. Preferably, the cell line is MCL-5, which stably expresses cytochrome P450 IA1, IA2, IIA3, IIIA4, and IIE1, as well as microsomal epoxide hydrolase. The cell line is useful in mutagenicity, toxicity and metabolism studies.
摘要翻译：提供稳定表达多种细胞色素P450的永生人细胞系。优选地，细胞系是MCL-5，其稳定表达细胞色素P450 IA1，IA2，IIA3，IIIA4和IIE1，以及微粒体环氧化物水解酶。细胞系可用于致突变性，毒性和代谢研究。

10. 发明授权

US07879607B2 Elastomeric device for cell seeding on the bottom of a filter 有权
标题翻译：用于细胞播种过滤器底部的弹性装置
公开(公告)号：US07879607B2
公开(公告)日：2011-02-01
申请号：US11750067
申请日：2007-05-17
申请人： Charles L. Crespi , Xiaoxi (Kevin) Chen
发明人： Charles L. Crespi , Xiaoxi (Kevin) Chen
IPC分类号： C12N5/00 , C12N5/02 , B01L99/00 , G01N1/18
CPC分类号： C12M23/20 , C12M25/04 , C12M33/06 , Y10T436/25375
摘要： An article is provided herein for use in seeding cells on at least one filter extending across at least one well of an assay device. The article includes an elastomeric body having spaced-apart first and second surfaces, and at least one channel extending between, and through, the first and second surfaces. The channel is formed to sealingly, and detachably, engage an outer surface of the well with the filter being at least partially encompassed by the channel. Advantageously, with the subject invention, a cell monolayer can be formed on the exterior surface of the filter. The assay device may be a multiwell plate, an insert plate, a column, a test tube, or a pipette.
摘要翻译：本文提供了用于在至少一个穿过测定装置的至少一个孔延伸的过滤器上接种细胞的制品。该制品包括具有间隔开的第一和第二表面的弹性体，以及在第一和第二表面之间延伸并穿过第一和第二表面的至少一个通道。通道形成为密封地且可拆卸地与孔的外表面接合，过滤器至少部分地被通道包围。有利地，通过本发明，可以在过滤器的外表面上形成细胞单层。测定装置可以是多孔板，插入板，柱，试管或移液管。

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