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1. 发明申请

WO1992017784A1 METHOD FOR ANALYTE CLASSIFICATION BY SC PROFILES 审中-公开
标题翻译： SC概要分析分类方法
公开(公告)号：WO1992017784A1
公开(公告)日：1992-10-15
申请号：PCT/US1992002716
申请日：1992-04-02
申请人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M. , AMBLER, Stuart, M.
发明人： TERRAPIN TECHNOLOGIES, INC.
IPC分类号： G01N33/563
CPC分类号： G01N33/53 , G01N30/02 , Y10S435/975 , Y10S436/808 , Y10S436/815 , Y10S436/816 , Y10S436/817 , Y10S436/901 , B01D15/422 , B01D15/3804
摘要： The precision of identification of analyte composition in a sample, where the possible analytes each provide a series of values for characteristic parameters; in particular where the parameters are generated by cross-reaction with specific binding reagents, is enhanced by applying pattern recognition techniques. Samples to be tested are evaluated with respect to each survey parameter to obtain a pattern of parameter values with respect to each analyte at a given concentration. In the case of the use of a panel of specific binding reagents, the samples to be tested are reacted with this panel and the affinities at various analyte concentrations are determined. This results in a databank of "SC profiles" for known concentrations of each analyte. This databank is stored in a computationally accessible form, which then can be matched against SC profiles obtained by testing unknown samples.
摘要翻译：样品中分析物组成的鉴定精度，其中可能的分析物各自提供一系列特征参数值; 特别是通过与特异性结合试剂进行交叉反应产生参数时，通过应用模式识别技术得到增强。针对每个测量参数评估要测试的样品，以获得相对于给定浓度下的每个分析物的参数值的模式。在使用一组特异性结合试剂的情况下，待测试样品与该面板反应，并确定各种分析物浓度下的亲和力。这导致每个分析物的已知浓度的“SC概况”的数据库。该数据库以计算可访问的形式存储，然后可以与通过测试未知样本获得的SC简档进行匹配。

2. 发明申请

WO1996023879A1 GLUBODIES - MULTIPLICITIES OF PROTEINS CAPABLE OF BINDING A VARIETY OF SMALL MOLECULES 审中-公开
标题翻译： GLUBODIES - 能够绑定一小部分小分子的蛋白质的多样性
公开(公告)号：WO1996023879A1
公开(公告)日：1996-08-08
申请号：PCT/US1996001567
申请日：1996-01-30
申请人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M. , TRAINER, John, A. , VILLAR, Hugo, O. , NAPOLITANO, Eugene, W.
发明人： TERRAPIN TECHNOLOGIES, INC.
IPC分类号： C12N15/11
CPC分类号： C12N9/003 , C07K14/245 , C07K14/36 , C07K14/42 , C07K14/79 , C12N9/1029 , C12N9/1088 , C12N9/90 , C12N15/11 , G01N33/68
摘要： Certain naturally occurring proteins contain regions, designated protogludomains, which can be modified randomly or systematically to generate families of protein ligates, termed glubodies, which have ranges and variations in binding specificities comparable to those of the antibody repertoire. Methods for constructing such families of glubodies and for their use are described.
摘要翻译：某些天然存在的蛋白质含有区域，指定的原肠蛋白酶，其可以随机或系统地修饰以产生称为葡萄糖的蛋白质连接物家族，其具有与抗体库相似的结合特异性的范围和变化。描述了构建这样的葡萄糖族家族及其用途的方法。

3. 发明申请

WO1992019767A1 METHODS TO PROFILE AND TREAT ABNORMAL CELLS 审中-公开
标题翻译：描述和治疗异常细胞的方法
公开(公告)号：WO1992019767A1
公开(公告)日：1992-11-12
申请号：PCT/US1992003537
申请日：1992-04-29
申请人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M.
发明人： TERRAPIN TECHNOLOGIES, INC.
IPC分类号： C12Q01/48
CPC分类号： G01N33/573 , G01N30/02 , G01N33/57496 , G01N2333/91177 , B01D15/3804 , B01D15/422
摘要： Advantage is taken of identifying the differences in glutathione-S-transferase (GST) complements of unwanted tissues and cells as compared to normal tissues and cells to evaluate therapeutic protocols designed to treat conditions characterized by, for example, tumor cells or infectious agents. Therapeutic modulators which affect preferentially the GST complement of normal or unwanted cells or tissues can thereby also be selected for use in combination with drugs which serve as substrates for GST.
摘要翻译：与正常组织和细胞相比，鉴定与不正常组织和细胞的谷胱甘肽-S-转移酶（GST）互补物的差异的优点是为了评估设计用于治疗特征在于例如肿瘤细胞或感染因子的病症的治疗方案。因此，优选影响正常或不需要的细胞或组织的GST补体的治疗性调节剂也可以选择与用作GST的底物的药物组合使用。

4. 发明申请

WO1997014106A1 IDENTIFICATION OF COMMON CHEMICAL ACTIVITY THROUGH COMPARISON OF SUBSTRUCTURAL FRAGMENTS 审中-公开
标题翻译：通过比较结构化片段来识别共同化学活性
公开(公告)号：WO1997014106A1
公开(公告)日：1997-04-17
申请号：PCT/US1996016196
申请日：1996-10-10
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , VILLAR, Hugo, O. , BONE, Richard, G., A.
IPC分类号： G06F17/30
CPC分类号： B01J19/00 , C07K1/00 , G06F19/704 , G06F19/709
摘要： A process for preparing a database of molecule fragments contained by a molecule, the process including the steps of (1) selecting a molecule comprising molecule fragments; (2) identifying substantially all molecule fragments within the molecule; (3) counting the occurrence of each unique molecule fragment identified in step 2; and (4) storing in a computer-readable storage medium information correlating molecule fragment count with molecule fragment identity. The invention also relates to a computer-implemented process for identifying a molecule likely to have a desired trait, the process including the steps of (1) selecting a test molecule comprising molecule fragments; (2) identifying substantially all test molecule fragments within the molecule; (3) counting the occurrence of each unique test molecule fragment identified in step 2; (4) comparing test molecule fragment counts from step 3 with fragment counts for identical fragments from a plurality of molecules having known activity; and (5) presenting the results of the comparing step as an output. The invention also includes a data processing system implementing these processes and computer-readable media having recorded thereon databases containing standardized representations of substantially all fragments of one or more molecules.
摘要翻译：一种制备分子含有的分子片段的数据库的方法，所述方法包括以下步骤：（1）选择包含分子片段的分子; （2）基本上确定分子内的所有分子片段; （3）计算步骤2中鉴定的每个独特分子片段的出现; 和（4）在计算机可读存储介质中存储相关分子片段计数与分子片段同一性的信息。本发明还涉及用于鉴定可能具有所需性状的分子的计算机实施方法，所述方法包括以下步骤：（1）选择包含分子片段的测试分子; （2）确定分子内基本上所有测试分子片段; （3）计算步骤2中鉴定的每个独特的测试分子片段的发生情况; （4）将来自步骤3的测试分子片段计数与来自具有已知活性的多个分子的相同片段的片段计数进行比较; 和（5）将比较步骤的结果呈现为输出。本发明还包括实现这些过程的数据处理系统和其上记录有包含一个或多个分子的基本上所有片段的标准化表示的数据库的计算机可读介质。

5. 发明申请

WO1996040735A1 p-NITROBENZYL SIDE-CHAIN PROTECTION FOR SOLID-PHASE SYNTHESIS 审中-公开
标题翻译：用于固相合成的对硝基苯侧链保护
公开(公告)号：WO1996040735A1
公开(公告)日：1996-12-19
申请号：PCT/US1996007300
申请日：1996-05-21
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , LYTTLE, Matthew, H. , HOCKER, Michael, D.
IPC分类号： C07K01/06
CPC分类号： C07K1/063 , C07K1/062 , C07K1/064 , C07K1/065 , C07K1/067 , Y02P20/55
摘要： The solid-phase supported synthesis of peptides using p-nitrobenzyl esters, thioethers, ethers and carbamates for side-chain protection is described. Protected amino acids are utilized in the synthesis of peptides using standard solid-phase synthesis methodologies and deprotected.
摘要翻译：描述了使用对硝基苄基酯，硫醚，醚和氨基甲酸酯进行固相支持的肽合成，用于侧链保护。保护氨基酸用于使用标准固相合成方法合成肽并脱保护。

6. 发明申请

WO1995008563A1 GLUTATHIONE ANALOGS AND PARALOG PANELS COMPRISING GLUTATHIONE MIMICS 审中-公开
标题翻译： GLUTATHIONE模拟和包含GLUTATHIONE MIMICS的对话面板
公开(公告)号：WO1995008563A1
公开(公告)日：1995-03-30
申请号：PCT/US1994010797
申请日：1994-09-23
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M. , LYTTLE, Matthew, H.
IPC分类号： C07K05/037
CPC分类号： A61K38/06 , C07K5/0215 , C12N9/1088 , G01N30/02 , G01N33/573 , G01N33/57496 , G01N2333/91177 , B01D15/3804 , B01D15/422
摘要： A compound of formula (1) and the alkyl-type (1-10C), alkenyl-type (1-10C), and arylalkyl-type (7-12C) esters, amides and mixed ester/amides thereof; wherein Z is selected from the group consisting of S, O, and C; n is 1, 2 or 3; wherein when Z is O or S and n is 1, X is a mono- or disubstituted or unsubstituted hydrocarbyl (1-20C) moiety optionally containing 1 or 2 nonadjacent heteroatoms (O, S or N), and wherein said substitution is selected from the group consisting of halo, -NO, -NO2, -NR2, OR, and SR, wherein each R is independently H or lower alkyl (1-4C); wherein when Z is S and n is 2, one X is as above defined and the other X is lower alkyl (1-4C); and wherein when Z is C and n is 3, one X is as above defined and the other two X are independently H or lower alkyl (1-4C); Y-CO is selected from the group consisting of gamma -Glu, beta -Asp, Glu, Asp, gamma Glu-Gly, beta -Asp-Gly, Glu-Gly, and Asp-Gly, and AAC is an amino acid coupled through a peptide bond to the remainder of the compound of formula (1), are useful as affinity ligands, elution reagents, solution inhibitors, diagnostic reagents and therapeutics. These compounds and analogous tripeptide glutathione analogs can be used as members of panels to obtain specific characteristic profiles for various glutathione-S-transferases.
摘要翻译：式（1）的化合物和烷基型（1-10C），链烯基（1-10C）和芳基烷基（7-12C）酯，酰胺和其混合酯/酰胺; 其中Z选自S，O和C; n为1,2或3; 其中当Z为O或S且n为1时，X为任选含有1或2个不相邻杂原子（O，S或N）的单取代或未取代的烃基（1-20C）部分，并且其中所述取代选自由卤素，-NO，-NO 2，-NR 2，OR和SR组成的基团，其中每个R独立地为H或低级烷基（1-4C）; 其中当Z为S且n为2时，一个X如上定义，另一个X为低级烷基（1-4C）; 并且其中当Z为C且n为3时，一个X如上定义，另外两个X独立地为H或低级烷基（1-4C）; Y-CO选自γ-Glu，β-Asp，Glu，Asp，γ-Glu-Gly，β-Asp-Gly，Glu-Gly和Asp-Gly，AAC是通过与式（1）化合物的其余部分的肽键可用作亲和配体，洗脱试剂，溶液抑制剂，诊断试剂和治疗剂。这些化合物和类似的三肽谷胱甘肽类似物可用作面板的成员以获得各种谷胱甘肽-S-转移酶的特定特征。

7. 发明申请

WO1994023298A1 DETERMINATION OF CONCENTRATION BY AFFINITY TITRATION AND COMPETITIVE DISPLACEMENT IN DRUG DELIVERY 审中-公开
标题翻译：通过精神量化和药物递送中的竞争性位移来确定浓度
公开(公告)号：WO1994023298A1
公开(公告)日：1994-10-13
申请号：PCT/US1994003490
申请日：1994-03-30
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M.
IPC分类号： G01N33/543
CPC分类号： G01N33/54306 , A61K47/6817 , G01N33/53
摘要： A method for determining the amount of analyte in a sample utilizes a series of test regions with systematically varied, preferably monotonically increasing, affinity for a specific binding partner for an analyte or for the analyte itself. By determining the portion of test regions which are capable of binding specific binding partner in competition with the analyte in the sample, or which bind the analyte, the amount of analyte may be estimated. Thus, titration of affinity replaces titration of concentration, allowing assays to be performed without the need for serial dilution steps. Alternatively, advantage is taken of competition of various ligands for components of complexes to regulate the release of desired components from the complexes. In one embodiment, clearance of small moieties can be delayed by combining them with size-enhancing agents which can be released or dissociated on cue by action of a releasing agent. In other embodiments, a target itself is a successful competitor in releasing the active form of the moiety from the complex.
摘要翻译：用于确定样品中分析物的量的方法利用一系列测试区域，其对于分析物或分析物本身的特异性结合配偶体系统地改变，优选单调递增的亲和力。通过确定能够结合特异性结合配偶体与样品中分析物竞争或测量结合分析物的部分测试区域，可以估计分析物的量。因此，亲和力的滴定取代浓度的滴定，允许进行测定而不需要连续稀释步骤。或者，优点是各种配体竞争复合物的组分以调节所需组分从配合物的释放。在一个实施方案中，小部分的清除可以通过将它们与尺寸增强剂组合来延迟，所述尺寸增强剂可以通过释放剂的作用在提示上释放或解离。在其它实施方案中，靶自身是从复合物释放部分活性形式的成功竞争者。

8. 发明申请

WO1998029744A2 METHOD TO CLASSIFY GENE PRODUCTS 审中-公开
标题翻译：分类基因产物的方法
公开(公告)号：WO1998029744A2
公开(公告)日：1998-07-09
申请号：PCT/US1997023762
申请日：1997-12-23
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M. , VILLAR, Hugo, O.
IPC分类号： G01N33/42
CPC分类号： C12N15/1089 , C40B30/04 , G01N33/6845
摘要： Methods for classifying large numbers of proteins contained in a collection of interest are described. The collection may represent the repertoire of proteins encoded by the genome of an organism including a higher organism or those expressed by a particular tissue or type of cell. Classification is based on ability to bind ligands contained in a panel representative of the range of physiological interactions. The methods of the invention may also be used to evaluate relative binding of proteins in a set of proteins with respect to a physiologically significant ligand so as to permit the modification of specificity of a desired ligand/receptor interaction.
摘要翻译：描述了用于分类感兴趣的集合中包含的大量蛋白质的方法。该集合可以表示由生物体的基因组编码的蛋白质的所有组成成分，包括较高生物体或由特定组织或细胞类型表达的生物体。分类基于结合包含在代表生理相互作用范围的面板中的配体的能力。本发明的方法还可以用于评价蛋白质相对于生理学上重要的配体的蛋白质的相对结合，从而允许改变所需配体/受体相互作用的特异性。

9. 发明申请

WO1991006356A1 METHOD TO IDENTIFY ANALYTE-BINDING LIGANDS 审中-公开
标题翻译：识别分析结合配体的方法
公开(公告)号：WO1991006356A1
公开(公告)日：1991-05-16
申请号：PCT/US1990006333
申请日：1990-10-31
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M.
IPC分类号： B01D15/08
CPC分类号： C07K7/06 , B01D15/08 , B01J20/264 , B01J20/28033 , B01J20/286 , B01J20/289 , B01J20/29 , B01J20/3204 , B01J20/3208 , B01J20/3219 , B01J20/3274 , B01J20/328 , B01J20/3285 , B01J2220/58 , B01J2220/66 , C07K1/22 , C07K7/56 , C07K16/44 , G01N30/00 , G01N30/02 , G01N30/48 , G01N33/53 , G01N33/68 , G01N2030/027 , B01D15/422 , B01D15/3804
摘要： The invention provides methods to obtain panels of low molecular weight polymers resulting from varying constituent monomers, which panels are systematically diverse with respect to two or more variables. The panels can be screened for members (paralogs) which are capable of specifically binding a target moiety. Such paralogs are useful for chromatographic separations and purifications of desired analytes and in binding assays, such as immunoassays, involving said analytes, as well as for any purpose which requires said specific binding. The invention also provides kits for these determinations, and methods to synthesize panels of candidate paralogs and use of these panels to generate analyte profiles and cross reactivity matrices.
摘要翻译：本发明提供了获得由不同构成单体产生的低分子量聚合物的面板的方法，该面板相对于两个或多个变量系统地多样化。可以对能够特异性结合目标部分的成员（旁系同源物）进行筛选。这样的旁系同源物可用于所需分析物的色谱分离和纯化以及结合测定，例如涉及所述分析物的免疫测定，以及需要所述特异性结合的任何目的。本发明还提供用于这些测定的试剂盒，以及合成候选旁系同源板的方法以及使用这些面板产生分析物谱和交叉反应性基质。

10. 发明申请

WO1996040205A1 METABOLIC EFFECTS OF CERTAIN GLUTATHIONE ANALOGS 审中-公开
标题翻译：某些谷胱甘肽类似物的代谢作用
公开(公告)号：WO1996040205A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009057
申请日：1996-06-05
申请人： TERRAPIN TECHNOLOGIES, INC.
发明人： TERRAPIN TECHNOLOGIES, INC. , KAUVAR, Lawrence, M. , LYTTLE, Matthew, H. , MORGAN, Amy, S. , BORCH, Richard, F.
IPC分类号： A61K38/06
CPC分类号： A61K38/06 , A61K38/063
摘要： Compounds of formula (1) and the esters, amides, amide/esters and salts thereof, wherein YCO is gamma -glu or beta -asp; G* is phenylglycine or glycine; Z is CH2, O or S; and X is a hydrocarbon radical of 1-20C; are useful in modulating hematopoiesis in bone marrow, mitigating the bone-marrow-destructive effects of a chemotherapeutic agent, and in potentiating the toxicity of chemotherapeutic agents.
摘要翻译：式（1）的化合物及其酯，酰胺，酰胺/酯和盐，其中YCO是γ-Glu或β-asp; G *是苯基甘氨酸或甘氨酸; Z是CH 2，O或S; X为1-20C的烃基; 可用于调节骨髓造血功能，减轻化疗药物的骨髓破坏作用，以及增强化学治疗剂的毒性。

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