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1. 发明授权

US06355460B1 Metal mediated serine protease inhibitors 失效
标题翻译：金属介导的丝氨酸蛋白酶抑制剂
公开(公告)号：US06355460B1
公开(公告)日：2002-03-12
申请号：US09351869
申请日：1999-07-12
申请人： James M. Clark , Kyle Elrod , Thomas E. Jenkins , Bradley A. Katz , William R. Moore , Robert M. Stroud
发明人： James M. Clark , Kyle Elrod , Thomas E. Jenkins , Bradley A. Katz , William R. Moore , Robert M. Stroud
IPC分类号： C12N999
CPC分类号： C07D401/04 , C07D235/18 , C07D235/20 , C07D401/06 , C07D403/06 , C07K14/811 , C12N9/6424 , C12Q1/37 , G01N2333/045 , G01N2333/811 , G01N2333/96433 , G01N2333/976
摘要： The present invention relates to serine protease inhibitors having a P site binding moiety and a divalent cation(s) chelating moiety which are pre-prepared as divalent cation(s) complexes or combined with the serine protease in the presence of divalent cation(s) and methods for identifying and using the inhibitors. The compounds are shown to have high inhibitory activity when complexed to divalent cation(s) and are useful in various processes associated with serine protease isolation and inhibition.
摘要翻译：本发明涉及具有P位结合部分和二价阳离子螯合部分的丝氨酸蛋白酶抑制剂，其在二价阳离子存在下预先制备为二价阳离子配合物或与丝氨酸蛋白酶组合，以及用于鉴定和使用抑制剂的方法。所述化合物与二价阳离子络合时显示出高的抑制活性，并且可用于与丝氨酸蛋白酶分离和抑制相关的各种过程。

2. 发明授权

US06448054B1 Purposeful movement of human migratory cells away from an agent source 有权
标题翻译：人类迁徙细胞有目的地移动远离代理来源
公开(公告)号：US06448054B1
公开(公告)日：2002-09-10
申请号：US09546153
申请日：2000-04-07
申请人： Mark C. Poznansky , Andrew T. Luster , David T. Scadden
发明人： Mark C. Poznansky , Andrew T. Luster , David T. Scadden
IPC分类号： C12N999
CPC分类号： G01N33/5029 , A61K38/00 , C07K14/521 , C07K14/8114 , G01N33/5008 , G01N33/5011 , G01N33/5044 , G01N33/5047 , G01N33/505 , G01N33/5058 , G01N33/5064 , G01N33/5088
摘要： This invention relates to methods and compositions for modulating movement of eukaryotic cells with migratory capacity. More specifically, the invention relates to methods and compositions for modulating movement of cells of hematopoietic, neural, epithelial, or mesenchymal origin, in a specific site in a subject. The foregoing are useful, inter alia, in the treatment of conditions characterized by a need to modulate migratory-cell movement associated with specific sites in a subject. More specifically, specific sites include sites of inflammation and modulation of migratory-cell movement is movement away from an agent source, or repulsion. Other sites include tumor sites, sites of pathogenic infection, and germ cell bearing sites.
摘要翻译：本发明涉及用迁移能力调节真核细胞运动的方法和组合物。更具体地，本发明涉及用于调节受试者的特定部位中造血，神经，上皮或间质来源的细胞运动的方法和组合物。前述内容尤其可用于治疗特征在于需要调节与受试者中特定部位相关的迁移细胞运动的病症。更具体地，特定部位包括炎症部位和迁移细胞运动的调节是远离药剂来源的运动或排斥。其他部位包括肿瘤部位，病原体感染部位和生殖细胞承载部位。

3. 发明授权

US06255091B1 Potentiating metal mediated serine protease inhibitors with cobalt or zinc ions 失效
标题翻译：加强金属介导的丝氨酸蛋白酶抑制剂与钴或锌离子
公开(公告)号：US06255091B1
公开(公告)日：2001-07-03
申请号：US08746986
申请日：1996-11-19
申请人： James M. Clark , Kyle Elrod , Thomas E. Jenkins , Bradley A. Katz , William R. Moore , Robert M. Stroud
发明人： James M. Clark , Kyle Elrod , Thomas E. Jenkins , Bradley A. Katz , William R. Moore , Robert M. Stroud
IPC分类号： C12N999
CPC分类号： C07D401/04 , C07D235/18 , C07D235/20 , C07D401/06 , C07D403/06 , C07K14/811 , C12N9/6424 , C12Q1/37 , G01N2333/045 , G01N2333/811 , G01N2333/96433 , G01N2333/976
摘要： A method is presented for determining if the inhibition of metal mediated serine proteases can be potentiated by cobalt or zinc ions.
摘要翻译：提出了一种用于确定金属介导的丝氨酸蛋白酶的抑制是否可以被钴或锌离子加强的方法。

4. 发明授权

US06709851B1 Stabilization of helicobacter urease 失效
标题翻译：螺杆菌脲酶的稳定化
公开(公告)号：US06709851B1
公开(公告)日：2004-03-23
申请号：US09338920
申请日：1999-06-23
申请人： Gopalan Soman , William D. Thomas, Jr. , Thomas P. Monath
发明人： Gopalan Soman , William D. Thomas, Jr. , Thomas P. Monath
IPC分类号： C12N999
CPC分类号： C07K14/205 , A61K38/00 , C12N9/80
摘要： The invention provides methods for stabilizing recombinant Helicobacter urease by genetically modifying a urease amino acid. The stabilized urease is prevented from the molecular aggregation or activation (e.g., in vitro activation) characteristic of untreated urease.
摘要翻译：本发明提供了通过遗传修饰脲酶氨基酸稳定重组幽门螺杆菌脲酶的方法。稳定的脲酶被阻止未经处理的脲酶的特征的分子聚集或活化（例如，体外激活）。

5. 发明授权

US06194184B1 Compounds labeled with cyanate or thiocyanate metal complexes for detection by infrared spectroscopy 失效
标题翻译：用氰酸盐或硫氰酸盐金属配合物标记的化合物用红外光谱法检测
公开(公告)号：US06194184B1
公开(公告)日：2001-02-27
申请号：US09294139
申请日：1999-04-20
申请人： David W. Conrad , Charles H. Patterson, Jr.
发明人： David W. Conrad , Charles H. Patterson, Jr.
IPC分类号： C12N999
CPC分类号： G01N33/58 , C07F15/0066
摘要： A labeled compound detectable by IR spectroscopy contains at least one histidine residue bound to a cyanate or thiocyanate metal complex that has an IR absorption band within the spectral region of 2399-1900 cm−1. An assay reagent for simultaneously detecting or determining a plurality of different analytes in a sample is made up of a plurality of different labeled compounds, each being independently distinguishable from the others by absorbing energy in a different and distinguishable region in the range of 2300 to 1900 cm−1.
摘要翻译：通过IR光谱检测的标记化合物含有至少一个与氰酸酯或硫氰酸酯金属络合物结合的组氨酸残基，其具有在2399-1900cm -1的光谱区内的IR吸收带。用于同时检测或确定样品中多种不同分析物的测定试剂由多种不同的标记化合物组成，每种化合物通过在2300至1900范围内的不同和可区分的区域中吸收能量而独立地区别于其它化合物 cm-1。

6. 发明授权

US06787342B2 Paste formulations 有权
标题翻译：糊剂配方
公开(公告)号：US06787342B2
公开(公告)日：2004-09-07
申请号：US09504741
申请日：2000-02-16
申请人： Jun Chen
发明人： Jun Chen
IPC分类号： C12N999
CPC分类号： A61K9/0014 , A61K9/0017 , A61K9/0056 , A61K47/02 , A61K47/10 , A61K47/18 , A61K47/26 , A61K47/34
摘要： This invention provides for a pharmaceutical or veterinary paste formulation comprising: an effective amount of a therapeutic agent; fumed silica; a viscosity modifier; a hydrophilic carrier; optionally, an absorbent; and optionally, a colorant, stabilizer, surfactant, or preservative. This invention also provides for methods of using these formulations for treating various disease states as well.
摘要翻译：本发明提供了一种药物或兽用糊剂制剂，其包含：有效量的治疗剂; 气相二氧化硅; 粘度调节剂; 亲水载体; 任选地，吸收剂; 和任选的着色剂，稳定剂，表面活性剂或防腐剂。本发明还提供了使用这些制剂治疗各种疾病状态的方法。

7. 发明授权

US06387673B1 Compounds useful for the modulation of processes mediated by nuclear hormone receptors, methods for the identification and use of such compounds 失效
标题翻译：可用于调节核激素受体介导的过程的化合物，用于鉴定和使用这些化合物的方法
公开(公告)号：US06387673B1
公开(公告)日：2002-05-14
申请号：US08846881
申请日：1997-05-01
申请人： Ronald M. Evans , Laszlo Nagy
发明人： Ronald M. Evans , Laszlo Nagy
IPC分类号： C12N999
CPC分类号： C12Q1/6897 , A61K38/005 , C07K14/70567 , A61K2300/00
摘要： In accordance with the present invention, it has been discovered that histone deacetylase associates with hormone receptor complexes and contributes to the repression thereof. It has further been discovered that exposure of a repressed system to histone deacetylase inhibitors relieves this repression. Thus, histone deacetylase inhibitors have been found to be useful for the activation of genes responsive to hormone receptors. In accordance with another aspect of the invention, formulations useful for modulation of hormone-mediated processes have been developed. In addition, assays have been developed for the identification of compounds useful to modulate the above-described processes.
摘要翻译：根据本发明，已经发现组蛋白脱乙酰酶与激素受体复合物缔合并有助于其抑制。进一步发现，抑制系统暴露于组蛋白脱乙酰酶抑制剂减轻了这种镇压作用。因此，已经发现组蛋白脱乙酰酶抑制剂可用于激活对激素受体有反应的基因。根据本发明的另一方面，已经开发了可用于调节激素介导的过程的制剂。此外，已经开发了用于鉴定可用于调节上述过程的化合物的测定。

8. 发明授权

US06235509B1 Process for inhibiting serine proteases using cresol or 3-hydroxypyridine and sulfonic acid derivatives or fluorophosphonates 失效
标题翻译：使用甲酚或3-羟基吡啶和磺酸衍生物或氟代膦酸盐抑制丝氨酸蛋白酶的方法
公开(公告)号：US06235509B1
公开(公告)日：2001-05-22
申请号：US09147502
申请日：1999-03-17
申请人： Erhard Fernholz
发明人： Erhard Fernholz
IPC分类号： C12N999
CPC分类号： C07K14/62 , C12N9/99
摘要： A process is provided for inhibiting serine proteases in a sample. The process involves adding to the sample a compound such as cresol or 3-hydroxypyridine and then adding to the sample a sulfonic acid derivative or a fluorophosphonate, to derivative the serine proteases. The compounds such as cresol or 3-hydroxypyridine avoid nonspecific derivatization of proteins other than the serine proteases.
摘要翻译：提供了一种抑制样品中丝氨酸蛋白酶的方法。该方法包括向样品中加入化合物如甲酚或3-羟基吡啶，然后向样品中加入磺酸衍生物或氟代膦酸酯以衍生丝氨酸蛋白酶。化合物如甲酚或3-羟基吡啶可以避免丝氨酸蛋白酶以外的蛋白质的非特异性衍生化。

9. 发明授权

US06194183B1 Phage display for detergent enzyme activity 失效
标题翻译：噬菌体展示洗涤剂酶活性
公开(公告)号：US06194183B1
公开(公告)日：2001-02-27
申请号：US09017612
申请日：1998-02-02
申请人： Peter Markvardsen , Mads Eskelund Bjornvad , Frank Mikkelsen , Borge Diderichsen
发明人： Peter Markvardsen , Mads Eskelund Bjornvad , Frank Mikkelsen , Borge Diderichsen
IPC分类号： C12N999
CPC分类号： C40B40/02 , C12N9/00 , C12N15/1037 , G01N33/573
摘要： The invention relates to a method of identifying enzymes suitable for use in detergents, especially the selection of specific enzyme variants among a large number of such variants created through random mutagenesis. The method comprises that enzyme variants to be selected are in a mixture of enzyme variants which are each displayed on the surface of cells or phage particles, and (i) introducing the mixture into a detergent composition under conditions that will have a negative impact on the activity of or inactivate most of said enzyme variants, (ii) reacting said mixture with a catcher molecule that will bind specifically only to enzyme variants that exhibit the property sought for, (iii) separating said complex from the remaining parts of said mixture, (iv) dissociate said complex to isolate such cell(s) or phage(s) that displayed said enzyme variant without the catcher molecule, (v) introducing said phage into a host wherein it will multiply, or (va)cultivating said cell under conditions conducive to its multiplication, (vi) isolating a DNA molecule coding for said enzyme variant from the genome of said cell or phage, and (vii) determining the sequence of said DNA molecule. The invention further relates to specific materials used in said method, the enzymes selected by use of the method, and to detergent compositions comprising aid enzymes.
摘要翻译：本发明涉及一种鉴定适用于洗涤剂的酶的方法，特别是通过随机诱变产生的大量这样的变体中特异性酶变体的选择。所述方法包括要选择的酶变体是酶变体的混合物，其各自显示在细胞或噬菌体颗粒的表面上，和（i）在将对所述洗涤剂组合物产生负面影响的条件下将所述混合物引入到洗涤剂组合物中（ii）使所述混合物与捕获剂分子反应，捕获剂分子将仅特异性结合于显示所要求的性质的酶变体，（iii）将所述复合物与所述混合物的其余部分分离（ iv）解离所述复合物以分离显示所述酶变体而没有捕获分子的这样的细胞或噬菌体，（v）将所述噬菌体引入其中将繁殖的宿主或（va）在条件下培养所述细胞有利于其增殖，（vi）从所述细胞或噬菌体的基因组分离编码所述酶变体的DNA分子，和（vii）确定所述DNA分子的序列。本发明还涉及所述方法中使用的具体材料，通过使用该方法选择的酶以及包含助剂酶的洗涤剂组合物。

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