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31. 发明申请

US20080176870A1 Heterobicyclic metalloprotease inhibitors 审中-公开
标题翻译：异双环金属蛋白酶抑制剂
公开(公告)号：US20080176870A1
公开(公告)日：2008-07-24
申请号：US11986622
申请日：2007-11-20
申请人： Bert Nolte , Irving Sucholeiki , Tim Feuerstein , Brian M. Gallagher , Xinyuan Wu , Christoph Steeneck , Christian Gege , Hongbo Deng , Joshua Van Veldhuizen , Arthur Taveras
发明人： Bert Nolte , Irving Sucholeiki , Tim Feuerstein , Brian M. Gallagher , Xinyuan Wu , Christoph Steeneck , Christian Gege , Hongbo Deng , Joshua Van Veldhuizen , Arthur Taveras
IPC分类号： A61K31/495 , C07D487/04 , A61P19/02 , A61P29/00 , A61P9/10
CPC分类号： C07D487/04
摘要： The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
摘要翻译：本发明一般涉及含杂环的药物，特别是涉及杂双环金属蛋白酶抑制剂化合物。更具体地，本发明提供了一类新型的杂双环金属蛋白酶抑制化合物，其与当前已知的金属蛋白酶抑制剂相比表现出增加的效力。

32. 发明授权

US5858534A Method of making and using derivatized paramagnetic polymer beads 失效
标题翻译：制造和使用衍生的顺磁性聚合物珠的方法
公开(公告)号：US5858534A
公开(公告)日：1999-01-12
申请号：US749353
申请日：1996-09-04
申请人： Irving Sucholeiki
发明人： Irving Sucholeiki
IPC分类号： G01N33/543 , B32B5/16
CPC分类号： G01N33/5434 , B01J2219/005 , G01N2446/86 , G01N2446/90 , Y10T428/2998
摘要： A solid phase magnetic support having a hydrophilic surface, a method of making the support, and a method of using the support for peptide synthesis are provided. The solid phase magnetic support is synthesized from a starting material which is a magnetic polystyrene polymer bead which has a plurality of polystyrene coated metal oxide particles randomly distributed in a polystyrene matrix having chloromethyl groups. Hydrophilic long chain hydrocarbon spacer arms, such as polyalkylene diamine molecules are coupled with sonication to the chloromethyl groups. Each spacer arm is provided with a terminal amine for linking to a first amino acid. Preferably, the terminal amine on the spacer arm is provided by a low molecular weight linker molecule which can be acid cleaved from the spacer arm. However, the spacer arm may be derivatized and linked to a first amino acid which cannot be acid cleaved from the spacer arm. The inventive support can be used for automated peptide synthesis or as a support for a bound ligand in bioassays. The support is held in place magnetically while the surrounding solution is siphoned off allowing simultaneous separation of the support bound component from the reactants in solution and washing.
摘要翻译：提供具有亲水表面的固相磁性载体，制备载体的方法和使用该载体用于肽合成的方法。固相磁性载体是由具有随机分布在具有氯甲基的聚苯乙烯基质中的多个聚苯乙烯涂覆的金属氧化物颗粒的磁性聚苯乙烯聚合物珠粒的起始材料合成的。亲水性长链烃隔离臂如聚亚烷基二胺分子与超声处理与氯甲基偶联。每个间隔臂设置有用于连接到第一氨基酸的末端胺。优选地，间隔臂上的末端胺由可以从间隔臂酸切割的低分子量连接分子提供。然而，间隔臂可以被衍生化并连接到不能从间隔臂被酸切割的第一个氨基酸。本发明的载体可用于自动肽合成或作为生物测定中结合配体的载体。将支撑体保持在磁性位置，同时虹吸掉周围的溶液，从而在溶液和洗涤中同时将载体结合的组分与反应物分离。

33. 发明授权

US5834121A Composite magnetic beads 失效
标题翻译：复合磁珠
公开(公告)号：US5834121A
公开(公告)日：1998-11-10
申请号：US585905
申请日：1996-01-16
申请人： Irving Sucholeiki , Graham Margetts , Mark Roberts
发明人： Irving Sucholeiki , Graham Margetts , Mark Roberts
IPC分类号： B03C1/01 , C02F1/48 , C02F1/68 , G01N33/543 , H01F1/00 , H01F1/37 , B32B5/16 , B05D7/00
CPC分类号： B82Y25/00 , B03C1/01 , C02F1/681 , G01N33/5434 , H01F1/37 , C02F1/48 , G01N2446/20 , G01N2446/40 , G01N2446/86 , Y10S428/90 , Y10T428/2998
摘要： This invention provides a novel composite magnetic bead and a method for making the composite magnetic bead. The composite magnetic bead is comprised of a matrix formed from vinyl monomers throughout which is distributed primary beads, each primary bead of which is a magnetizable metal oxide encapsulated in a rigid polymeric coating. The matrix structure allows the composite magnetic bead to swell in organic solvents without loss of the intermeshed primary beads. Further, the matrix can be functionalized to allow the covalent bonding of sites useful for organic syntheses. The composite magnetic beads are made utilizing a core-shell polymerization techinque under conditions which preserve the oxidation state of the magnetizable metal oxide in the primary particles. In one embodiment, primary beads, each having a hydrophobic exterior surface, are dispersed in an inert solvent with a vinyl monomer and a crosslinking agent for that monomer to form a dispersed phase. The dispersed phase is mixed into an aqueous solvent-dispersing agent phase and stirred until the desired droplet size is achieved, then polymerization is initiated. After removal of the solvent and unreacted components, the composite magnetic beads are dried and sieved.
摘要翻译：本发明提供一种新型复合磁珠及其制造方法。复合磁珠由由乙烯基单体形成的基体组成，其中分布有初级珠，每个主珠是包封在刚性聚合物涂层中的可磁化金属氧化物。基体结构允许复合磁珠在有机溶剂中溶胀而不损失相互啮合的初级珠粒。此外，基质可以官能化以允许有机合成有用的位点的共价键。在保持一次颗粒中的可磁化金属氧化物的氧化态的条件下，使用核 - 壳聚合技术制备复合磁珠。在一个实施方案中，每个具有疏水性外表面的初级珠粒分散在具有乙烯基单体和用于该单体的交联剂的惰性溶剂中以形成分散相。将分散相混合到水性溶剂分散剂相中并搅拌直到达到所需的液滴尺寸，然后开始聚合。除去溶剂和未反应的组分后，将复合磁珠干燥并过筛。

34. 发明授权

US5779985A Reaction plenum 失效
标题翻译：反应气室
公开(公告)号：US5779985A
公开(公告)日：1998-07-14
申请号：US762887
申请日：1996-12-07
申请人： Irving Sucholeiki
发明人： Irving Sucholeiki
IPC分类号： B01F11/02 , B01F13/08 , B01J19/00 , B06B3/02 , C07K1/04 , C40B40/10 , C40B50/14 , C40B60/14 , B06B1/00
CPC分类号： B06B3/02 , B01F11/0283 , B01F13/0809 , B01J19/0046 , C07K1/042 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/00328 , B01J2219/00351 , B01J2219/00414 , B01J2219/00454 , B01J2219/00459 , B01J2219/00486 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00686 , B01J2219/00691 , B01J2219/0072 , B01J2219/00725 , C40B40/10 , C40B50/14 , C40B60/14 , Y10S436/809 , Y10T436/25375
摘要： An apparatus for facilitating the running of multiple simultaneous solid phase reactions for mounting on a temperature controllable water bath and a method of using this apparatus in the presence or absence of paramagnetic beads to perform chemical syntheses resulting in separation and recovery of a final desired reaction product is provided. The apparatus comprises a reaction plate, a reaction vessel for mounting in the reaction plate, a reaction plate holder, a screw-like rod, a mounting block attached to the reaction plate holder for operably receiving the screw-like rod, a motor, a sonication region in the water bath and a magnetic separation region in the water bath. Paramagnetic beads having reaction sites are introduced into the reaction vessels along with the appropriate solvent and one or more reactants. The contents of the reaction vessel are sonicated, then moved to the magnetic separation region where the paramagnetic beads are tightly held against the reaction vessel while the solvent is aspirated off. Once the desired reaction product is attained, the reaction product is cleaved off the paramagnetic bead. In an alternative embodiment, chemical synthesis is performed in a similar manner in the absence of the paramagnetic beads.
摘要翻译：用于促进多个同步固相反应运行以安装在温度可控的水浴上的装置以及在存在或不存在顺磁珠的情况下使用该装置的方法进行化学合成，导致最终所需反应产物的分离和回收被提供。该装置包括反应板，用于安装在反应板中的反应容器，反应板保持器，螺杆状杆，安装在反作用板保持器上用于可操作地接收螺杆状杆的安装块，马达，水浴中的超声处理区域和水浴中的磁分离区域。具有反应位点的顺磁珠与合适的溶剂和一种或多种反应物一起引入反应容器中。将反应容器的内容物进行超声处理，然后移动到磁性分离区域，其中顺磁珠紧紧地保持在反应容器上，同时吸出溶剂。一旦达到所需的反应产物，反应产物就从顺磁珠上分离出来。在替代实施方案中，在不存在顺磁珠的情况下以类似的方式进行化学合成。

35. 发明授权

US5502246A Solid-phase synthesis utilizing photochemical carbon-sulfur bond cleavage of thioethers 失效
标题翻译：利用硫醚的光化学碳 - 硫键切割的固相合成
公开(公告)号：US5502246A
公开(公告)日：1996-03-26
申请号：US215607
申请日：1994-03-22
申请人： Irving Sucholeiki
发明人： Irving Sucholeiki
IPC分类号： C07C323/56 , C07C323/07
CPC分类号： C07C323/56
摘要： A method for photochemical cleavage of carbon-sulfur bonds in conjunction with solid-phase synthesis utilizing a deoxygenated solvent and light to cleave the carbon-sulfur bond from a heterogeneous support. Also disclosed are compounds for use with said photochemical cleavage and methods of preparing them.
摘要翻译：结合使用脱氧溶剂和光从固相合成裂解碳 - 硫键从不均匀载体切割碳 - 硫键的方法。还公开了用于所述光化学切割的化合物及其制备方法。

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