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1. 发明授权

US06600016B1 Multifunctionalized solid support resins for synthesis of combinatorial libraries and method for using the same 失效
标题翻译：用于合成组合文库的多功能固体支持树脂及其使用方法
公开(公告)号：US06600016B1
公开(公告)日：2003-07-29
申请号：US09379848
申请日：1999-08-24
申请人： Eugene Campian , Boliang Lu , Jinfang Zhang
发明人： Eugene Campian , Boliang Lu , Jinfang Zhang
IPC分类号： C07K104
CPC分类号： C07K1/047 , C07K1/042
摘要： Multifunctionalized support resin for the solid phase synthesis of combinatorial libraries is disclosed. The support resin comprises a resin backbone to which is attached a template containing at least two more attachment points which carry mutiple functionalized benzyl-type linkers. Each linker displays differing chemical stability under cleavage conditions so that products can be selectively and sequentially cleaved and separated from the reaction vessel. The linkers are independently different benzyl-type moieties, and each product synthesized on the linkers may have a different chemical structure. The support resin may further comprise an additional linker which is directly attached to the resin backbone. This linker can benzyl-type linkers or other traditional cleavable-linkers. The invention is further directed to a method for the production of mutiple combinatorial libraries in a simultaneous fashion utilizing the above described support resin. The products are selectively cleaved under conditions where only one linker site is cleaved so that the product is individually separated from the reaction vessel.
摘要翻译：公开了用于组合文库的固相合成的多官能化支撑树脂。载体树脂包括树脂主链，其连接有含有至少两个另外的连接点的模板，其携带多个官能化的苄基型接头。每个接头在裂解条件下显示不同的化学稳定性，使得产物可以选择性地并且顺序地从反应容器中切割和分离。接头是独立不同的苄基型部分，并且在接头上合成的每种产物可具有不同的化学结构。载体树脂还可以包含直接连接到树脂主链上的另外的连接体。该接头可以是苄基型接头或其它传统的可切割接头。本发明还涉及一种利用上述载体树脂同时制备多组合文库的方法。在只有一个连接位点被切割使得产物从反应容器中分离出的条件下，选择性地裂解产物。

2. 发明授权

US06569993B1 Process for the preparation of resin-bound cyclic peptides 失效
标题翻译：制备树脂结合环肽的方法
公开(公告)号：US06569993B1
公开(公告)日：2003-05-27
申请号：US09442989
申请日：1999-11-18
申请人： Adam W. Sledeski , James J. Mencel
发明人： Adam W. Sledeski , James J. Mencel
IPC分类号： C07K104
CPC分类号： C07K5/06182 , C07K1/04 , C07K7/54 , C07K14/635
摘要： This invention is directed to a process for the solid phase, fragment-based synthesis of resin-bound cyclic peptide analogs of parathyroid hormones and analogs of parathyroid hormone-related proteins, which analogs contain at least one bridge between the side chains of two non-adjacent amino acid residues, and to peptide fragments useful therefor.
摘要翻译：本发明涉及一种用于甲状旁腺激素与甲状旁腺激素相关蛋白类似物的树脂结合环肽类似物的固相，片段基合成的方法，该类似物在两个非甲基化激素相关蛋白的侧链之间至少包含一个桥，相邻的氨基酸残基，以及对其有用的肽片段。

3. 发明授权

US06566494B1 Support material for solid phase organic synthesis 有权
标题翻译：固相有机合成支撑材料
公开(公告)号：US06566494B1
公开(公告)日：2003-05-20
申请号：US09309828
申请日：1999-05-11
申请人： Knud J. Jensen , George Barany , Micheal F. Songster , Fernando Albericio , Jordi Alsina , Josef Vágner
发明人： Knud J. Jensen , George Barany , Micheal F. Songster , Fernando Albericio , Jordi Alsina , Josef Vágner
IPC分类号： C07K104
CPC分类号： G01N33/54353 , A61K38/2026 , B01J2219/00497
摘要： A support material for solid phase synthesis is provided having an amine-containing organic group attached to it through a linker. The support material is of the following general formula (Formula I):
摘要翻译：提供用于固相合成的载体材料，其具有通过连接体连接到其上的含胺有机基团。载体材料具有以下通式（式I）：

4. 发明授权

US06228988B1 Synthesis of hydroxamic acid derivatives 失效
标题翻译：异羟肟酸衍生物的合成
公开(公告)号：US06228988B1
公开(公告)日：2001-05-08
申请号：US09328493
申请日：1999-06-09
申请人： Christopher David Floyd , Christopher Norman Lewis
发明人： Christopher David Floyd , Christopher Norman Lewis
IPC分类号： C07K104
CPC分类号： C07K1/04 , C07K1/003 , C08F8/30 , Y02P20/55
摘要： The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group —CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1): where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.
摘要翻译：本发明描述了通过形成液体反应介质和携带多个式（A1）或（B1）部分的固相反应产物的混合物来制备包含共价键合的异羟肟酸基-CONHOH的所需合成产物的方法，：其中X是所需合成产物的残留的非羟肟酸盐部分结构，P1是氢或氨基保护基，P2是氢或羟基保护基，并且指定为（a）的键共价连接部分（A1 ）或（B1）与固体底物的残留物; 通过在所得混合物中切割指定为（a）的键; 并通过将所得液体反应相与所得反应固体分离以回收所需的合成产物。

5. 发明授权

US06495314B1 Process for characterizing proteins 失效
标题翻译：表征蛋白质的方法
公开(公告)号：US06495314B1
公开(公告)日：2002-12-17
申请号：US09043877
申请日：1998-06-19
申请人： Stephen B. H. Kent , Tom W. Muir , Philip E. Dawson , Michael C. Fitzgerald
发明人： Stephen B. H. Kent , Tom W. Muir , Philip E. Dawson , Michael C. Fitzgerald
IPC分类号： C07K104
CPC分类号： C07K1/047
摘要： A protein signature analysis is obtained using a peptide ladder library. The molecular signature of a protein is defined to be that subsequence of amino acid positions within the protein which are essential for the protein to bind to a target molecule. The molecular signature may be determined by screening a peptide ladder library which corresponds to the protein against the target molecule. The peptide ladder library is a library of m peptides wherein each peptide has an amino acid sequence of length m corresponding to an amino acid sequence of the protein, with one exception, viz. peptidem has a substitute amino acid at positionm and the substitute amino acid is attached by a labile bond to its neighboring amino acid. Screening the peptide ladder library against the target molecule results in a division of the original mixture into a positive (functional) pool and a negative (non-functional) pool. The pools are separated and subjected to cleavage to obtain cleavage products. Analysis of cleavage products by mass spectrometry identifies the positions that are essential for the protein to bind to its molecular target.
摘要翻译：使用肽梯图文件获得蛋白质特征分析。蛋白质的分子标记被定义为蛋白质内蛋白质与靶分子结合所必需的氨基酸位置的亚序列。可以通过筛选与靶分子相对应的蛋白质的肽梯形文库来确定分子特征。肽梯形文库是m肽的文库，其中每个肽具有对应于蛋白质的氨基酸序列的长度m的氨基酸序列，除了一个例外，肽在位置具有替代氨基酸，替代氨基酸通过不稳定键连接到其相邻的氨基酸。针对靶分子筛选肽梯形图文库导致原始混合物分为正（功能）池和阴性（非功能）池。将池分离并进行裂解以获得裂解产物。通过质谱分析裂解产物鉴定了蛋白质与其分子靶标结合所必需的位置。

6. 发明授权

US06476186B1 Process for preparing octreotide and derivatives thereof 有权
标题翻译：制备奥曲肽及其衍生物的方法
公开(公告)号：US06476186B1
公开(公告)日：2002-11-05
申请号：US09576769
申请日：2000-05-24
申请人： Yao-Tsung Hsieh , Shiang-Rong Chang , Shyh-Yi Chyi , Hui-Lan Wu , Shu-Ling Chen , Henton Huang , Te-Wei Lee , Tian-Fu Huang
发明人： Yao-Tsung Hsieh , Shiang-Rong Chang , Shyh-Yi Chyi , Hui-Lan Wu , Shu-Ling Chen , Henton Huang , Te-Wei Lee , Tian-Fu Huang
IPC分类号： C07K104
CPC分类号： C07K14/6555 , Y02P20/55
摘要： This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Thr(ol)(tBu)-2-chlorotrityl resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2-chlorotrityl resin or D-Phe-Cys(Trt)-Tyr(tBu)-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2-chlorotrityl resin was obtained. Cleavage of the peptide from the resin was achieved by strong acid solution. The cleaved peptide reacted with charcoal to give disulfide-containing peptide of
摘要翻译：本发明涉及制备奥曲肽及其衍生物的方法。起始物质Thr（ol）（tBu）-2-氯三苯甲基树脂与各种氨基酸偶联。 D-Phe-Cys（Trt）-Phe-D-Trp（Boc）-Lys（Boc）-Thr（tBu）-Cys（Trt）-Thr（ol）（tBu）-2-氯三苯甲基树脂或D-Phe-Cys（Trt）-Tyr（tBu）-D-Trp（Boc）-Lys（Boc）-Thr（tBu）-Cys（Trt）-Thr（ol）（tBu）-2-氯三苯甲基树脂获得。通过强酸溶液从树脂中切下肽。裂解的肽与木炭反应，得到含二硫化物的肽

7. 发明授权

US06310179B1 2-or 3-dimensional geometric structures 失效
标题翻译： 2维或3维几何结构
公开(公告)号：US06310179B1
公开(公告)日：2001-10-30
申请号：US09087514
申请日：1998-05-28
申请人： Hans-Georg Batz , Troels Koch , Henrik Frydenlund Hansen
发明人： Hans-Georg Batz , Troels Koch , Henrik Frydenlund Hansen
IPC分类号： C07K104
CPC分类号： B82Y30/00 , C07H21/00 , C07K14/003 , Y10S977/704 , Y10S977/728 , Y10S977/734 , Y10S977/753 , Y10S977/792 , Y10S977/80 , Y10S977/906
摘要： Nucleic acid analogues provide a particularly useful tool for the preparation of complex polymeric structures of defined geometry because they are relatively stable to reaction conditions for the preparation of such structures and provide the opportunity to introduce reactive groups which would not be possible with usual nucleic acids. These supramolecular structures can be used to form fine networks in nanometer size, for the preparation of e.g., computer chips, new materials/polymers with conductivity and/or insulator properties, and robot arms in nanometer scale.
摘要翻译：核酸类似物为制备具有规定几何形状的复合聚合物结构提供了特别有用的工具，因为它们对于制备这种结构的反应条件相对稳定，并且提供引入与常规核酸不可能的反应性基团的机会。这些超分子结构可用于形成纳米尺寸的精细网络，用于制备例如计算机芯片，具有导电性和/或绝缘体特性的新材料/聚合物以及纳米尺度的机器人手臂。

8. 发明授权

US06809186B1 Simple method for labeled conjugate production 失效
标题翻译：标记共轭生产的简单方法
公开(公告)号：US06809186B1
公开(公告)日：2004-10-26
申请号：US09889795
申请日：2001-12-06
申请人： John P. Morseman , Xiangfei Zeng
发明人： John P. Morseman , Xiangfei Zeng
IPC分类号： C07K104
CPC分类号： G01N33/532 , Y10S530/811 , Y10S530/814 , Y10S530/816
摘要： The present invention relates to methods for coupling labels to particular target moieties. The coupling reactions of the present invention use temporal spacing of the reactants through phase change (i.e. by rapid freezing) to control the initiation and termination of reaction. This process results in a simplified and improved method for linking labels to specific binding moieties using N-hydroxysuccinimide chemistry. The present invention further relates to kits comprising all necessary components to easily and rapidly make protein conjugates.

9. 发明授权

US06787635B2 Solid phase synthesis supports and methods 有权
标题翻译：固相合成支持和方法
公开(公告)号：US06787635B2
公开(公告)日：2004-09-07
申请号：US09827107
申请日：2001-04-05
申请人： Jerald K. Rasmussen , Larry R. Krepski
发明人： Jerald K. Rasmussen , Larry R. Krepski
IPC分类号： C07K104
CPC分类号： C40B50/14 , B01J2219/00497 , B01J2219/005 , B01J2219/00527 , B01J2219/00596 , C07B2200/11 , C07H21/04 , C07K1/042
摘要： Functionalized supports and methods for solid phase synthesis. Preferably, the functionalized support is azlactone-functionalized.
摘要翻译：功能化支持和固相合成方法。优选地，功能化载体是吖内酯官能化的。

10. 发明授权

US06265552B1 Biotinylation of proteins 失效
标题翻译：蛋白质的生物素化
公开(公告)号：US06265552B1
公开(公告)日：2001-07-24
申请号：US09512983
申请日：2000-02-24
申请人： Peter J. Schatz
发明人： Peter J. Schatz
IPC分类号： C07K104
CPC分类号： C12N9/93 , A61K38/00 , C07K1/1077 , C07K2319/24 , C07K2319/80 , C12N15/62 , Y10S530/81
摘要： Biotinylation peptides can be fused to other peptides or proteins of interest using recombinant DNA techniques to provide efficient methods for biotinylating the resulting fusion proteins in vivo or in vitro.
摘要翻译：生物素化肽可以使用重组DNA技术与其他肽或目标蛋白融合，以提供在体内或体外生成生成所得融合蛋白的有效方法。

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