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1. 发明申请

WO2010107519A1 TERMINALLY-FUNCTIONALIZED CONJUGATES AND USES THEREOF 审中-公开
标题翻译：终端功能结合及其用途
公开(公告)号：WO2010107519A1
公开(公告)日：2010-09-23
申请号：PCT/US2010/022251
申请日：2010-01-27
申请人： SMARTCELLS, INC. , ZION, Todd, C. , LANCASTER, Thomas, M.
发明人： ZION, Todd, C. , LANCASTER, Thomas, M.
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： A61K38/28 , A61K47/58
摘要： The present disclosure provides inter alia conjugates of formula (I): wherein n, R1, R2, Rx, Z, X, Y and Z are as defined herein. A conjugate of formula (I) can also be converted to a conjugate of formulae (II) or (III) as described herein. Without limitation, the conjugates can be used to make controlled release materials and chemical sensors.
摘要翻译：本公开尤其提供式（I）的缀合物：其中n，R1，R2，Rx，Z，X，Y和Z如本文所定义。式（I）的缀合物也可以转化为如本文所述的式（II）或（III）的缀合物。不限于此，共轭物可用于制备控释材料和化学传感器。

2. 发明申请

WO2010088276A2 POLYNUCLEOTIDE APTAMER-BASED CROSS -LINKED MATERIALS AND USES THEREOF 审中-公开
标题翻译：基于APTAMER的多晶交联材料及其用途
公开(公告)号：WO2010088276A2
公开(公告)日：2010-08-05
申请号：PCT/US2010/022237
申请日：2010-01-27
申请人： SMARTCELLS, INC. , ZION, Todd, C. , LANCASTER, Thomas, M.
发明人： ZION, Todd, C. , LANCASTER, Thomas, M.
IPC分类号： A61K48/00
CPC分类号： C12N15/111 , A61K47/549 , C12N2310/16 , C12N2310/51
摘要： In one aspect, the disclosure provides cross-linked materials that include multivalent polynucleotide aptamers that bind a target molecule; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with the target molecule for binding with the aptamers and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between aptamers and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of the target molecule. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label. The drug, detectable label and affinity ligands may be covalently or non-covalently bound to the conjugate framework.
摘要翻译：一方面，本公开提供交联材料，其包括结合目标分子的多价多核苷酸适体; 以及包含与缀合物框架结合的两个或更多个分离的亲和配体的缀合物，其中所述两个或更多个亲和配体与靶分子竞争与适配体结合，并且其中结合物由于非共价键而在材料内交联适体与亲和配体在不同共轭物上的相互作用。这些材料被设计成响应于目标分子的所需浓度释放结合物的量。根据最终应用，在各种实施方案中，缀合物还可以包括药物和/或可检测标记。药物，可检测的标记和亲和配体可以共价或非共价结合到缀合物框架。

3. 发明申请

WO2010088268A1 EXOGENOUSLY TRIGGERED CONTROLLED RELEASE MATERIALS AND USES THEREOF 审中-公开
标题翻译：异构触发控制释放材料及其用途
公开(公告)号：WO2010088268A1
公开(公告)日：2010-08-05
申请号：PCT/US2010/022225
申请日：2010-01-27
申请人： SMARTCELLS, INC. , ZION, Todd, C. , LANCASTER, Thomas, M.
发明人： ZION, Todd, C. , LANCASTER, Thomas, M.
IPC分类号： A01N45/00
CPC分类号： A61K47/4823 , A61K38/00 , A61K38/28 , A61K47/26 , A61K47/48092 , A61K47/48246 , A61K47/549 , A61K47/61 , A61K47/64
摘要： The disclosure provides cross-linked materials that include multivalent cross-linking agents that bind an exogenous target molecule; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with the exogenous target molecule for binding with the cross-linking agents and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between cross-linking agents and affinity ligands on different conjugates. The conjugates also include a drug.
摘要翻译：本公开提供交联材料，其包括结合外源性靶分子的多价交联剂; 以及包含与缀合物框架结合的两个或更多个分离的亲和配体的缀合物，其中两个或更多个亲和配体与外源靶分子竞争与交联剂结合，并且其中结合物在材料内交联在交联剂和不同共轭物上的亲和配体之间的非共价相互作用。缀合物还包括药物。

4. 发明申请

WO2010088261A1 BINDING-SITE MODIFIED LECTINS AND USES THEREOF 审中-公开
标题翻译：绑定现场修改的条款及其用途
公开(公告)号：WO2010088261A1
公开(公告)日：2010-08-05
申请号：PCT/US2010/022213
申请日：2010-01-27
申请人： SMARTCELLS, INC. , ZION, Todd, C. , LANCASTER, Thomas, M.
发明人： ZION, Todd, C. , LANCASTER, Thomas, M.
IPC分类号： A01N45/00
CPC分类号： C07K14/42 , A61K38/28 , A61K47/61 , A61K47/641 , A61K47/6415 , C07K14/4726 , G01N33/66 , G01N2333/4724
摘要： In one aspect, the disclosure provides cross-linked materials that include multivalent lectins with at least two binding sites for glucose, wherein the lectins include at least one covalently linked affinity ligand which is capable of competing with glucose for binding with at least one of said binding sites; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with glucose for binding with the lectins at said binding sites and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between lectins and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of glucose. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label.
摘要翻译：一方面，本公开提供了交联材料，其包括具有至少两个葡萄糖结合位点的多价凝集素，其中所述凝集素包括至少一个共价连接的亲和配体，其能与葡萄糖竞争与至少一个所述结合位点以及包含与缀合物框架结合的两个或更多个分离的亲和配体的缀合物，其中所述两个或更多个亲和配体与葡萄糖竞争与所述结合位点处的凝集素结合，并且其中缀合物在材料内交联，在不同共轭物上的凝集素和亲和配体之间的共价相互作用。这些材料被设计为响应于期望的葡萄糖浓度释放结合物的量。取决于最终应用，在各种实施方案中，缀合物还可以包括药物和/或可检测标记。

5. 发明申请

WO2012050822A1 USES OF MACROPHAGE MANNOSE RECEPTOR TO SCREEN COMPOUNDS AND USES OF THESE COMPOUNDS 审中-公开
标题翻译：使用MACHOPHAT MANNOSE受体筛选化合物和这些化合物的用途
公开(公告)号：WO2012050822A1
公开(公告)日：2012-04-19
申请号：PCT/US2011/053390
申请日：2011-09-27
申请人： SMARTCELLS, INC. , MURIKIPUDI, Sylaja , LANCASTER, Thomas, M. , ZION, Todd, C.
发明人： MURIKIPUDI, Sylaja , LANCASTER, Thomas, M. , ZION, Todd, C.
IPC分类号： A61K38/14 , C07K17/00 , C07K1/00 , C07K14/00 , A01N25/00
CPC分类号： G01N33/5308 , A61K47/61 , C07K14/705 , G01N33/566 , G01N2333/62
摘要： Methods and associated compositions of matter (e.g., kits, cell lines, etc.) for screening compounds that bind to macrophase mannose receptor (MMR). Compounds identified by these methods and drug conjugates that includes these compounds are also encompassed as are their uses in the manufacture of medicaments.
摘要翻译：用于筛选与巨噬细胞甘露糖受体（MMR）结合的化合物的物质（例如试剂盒，细胞系等）的相关组合物。通过这些方法鉴定的化合物和包括这些化合物的药物偶联物也包括在制备药物中的用途。

6. 发明申请

WO2012015692A2 RECOMBINANTLY EXPRESSED INSULIN POLYPEPTIDES AND USES THEREOF 审中-公开
标题翻译：重组表达的胰岛素多肽及其用途
公开(公告)号：WO2012015692A2
公开(公告)日：2012-02-02
申请号：PCT/US2011/045008
申请日：2011-07-22
申请人： SMARTCELLS, INC. , LANCASTER, Thomas, M. , MURIKIPUDI, Sylaja , LALEAU, Rassol , ZION, Todd, C.
发明人： LANCASTER, Thomas, M. , MURIKIPUDI, Sylaja , LALEAU, Rassol , ZION, Todd, C.
IPC分类号： C07K14/62
CPC分类号： C07K14/62 , A61K38/28
摘要： The present disclosure provides recombinantly expressed insulin polypeptides that comprise an N-linked glycan motif. The N-linked glycan motif is not present in wild-type insulins and enables the recombinant expression of glycosylated insulin polypeptides (e.g., in yeast cells). Based on results obtained with synthetic glycosylated insulin conjugates we predict that when these recombinant glycosylated insulin polypeptides are administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the glycosylated insulin polypeptide will be sensitive to serum concentrations of glucose (or an exogenous saccharide such as alpha-methyl mannose). Exemplary insulin polypeptides, polynucleotides encoding these insulin polypeptides, glycosylated insulin polypeptides, pharmaceutical formulations and sustained release formulations are provided in addition to methods of use and preparation.
摘要翻译：本公开提供了包含N-连接的聚糖基序的重组表达的胰岛素多肽。 N-连接的聚糖基序不存在于野生型胰岛素中并且能够重组表达糖基化胰岛素多肽（例如在酵母细胞中）。基于用合成糖基化胰岛素缀合物获得的结果，我们预测当将这些重组糖基化胰岛素多肽施用于哺乳动物时，糖基化胰岛素多肽的至少一种药代动力学或药效学性质将对血清葡萄糖浓度（或外源糖类作为α-甲基甘露糖）。除了使用和制备方法外，还提供了示例性的胰岛素多肽，编码这些胰岛素多肽的多核苷酸，糖基化的胰岛素多肽，药物制剂和缓释制剂。

7. 发明申请

WO2012015691A2 RECOMBINANT LECTINS, BINDING-SITE MODIFIED LECTINS AND USES THEREOF 审中-公开
标题翻译：重组蛋白，结合位点修饰的蛋白及其用途
公开(公告)号：WO2012015691A2
公开(公告)日：2012-02-02
申请号：PCT/US2011/044989
申请日：2011-07-22
申请人： SMARTCELLS, INC. , LANCASTER, Thomas, M. , BUTTERS, Robert , CHOODNOVSKIY, Naomi, R. , ZION, Todd, C.
发明人： LANCASTER, Thomas, M. , BUTTERS, Robert , CHOODNOVSKIY, Naomi, R. , ZION, Todd, C.
IPC分类号： C07K14/42
CPC分类号： C07K14/42
摘要： In one aspect, the disclosure provides cross-linked materials that include multivalent lectins with at least two binding sites for glucose, wherein the lectins include at least one affinity ligand which is capable of competing with glucose for binding with at least one of said binding sites and is covalently linked to a cysteine residue of the lectins; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with glucose for binding with the lectins at said binding sites and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between lectins and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of glucose. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label.
摘要翻译：一方面，本公开提供了交联材料，其包括具有至少两个葡萄糖结合位点的多价凝集素，其中所述凝集素包括至少一种亲和配体，其能够与葡萄糖竞争与至少一个所述结合位点并与凝集素的半胱氨酸残基共价连接; 以及包含与缀合物框架结合的两个或多个分离的亲和配体的缀合物，其中所述两个或更多个亲和配体与葡萄糖竞争与所述结合位点处的凝集素结合，并且其中缀合物在材料内交联，在不同共轭物上的凝集素和亲和配体之间的共价相互作用。这些材料被设计为响应于期望的葡萄糖浓度释放结合物的量。根据最终应用，在各种实施方案中，缀合物还可以包括药物和/或可检测标记。

8. 发明申请

WO2012015687A2 DRUG-LIGAND CONJUGATES, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO 审中-公开
标题翻译：药物与药物联合治疗药物合成及其中间体
公开(公告)号：WO2012015687A2
公开(公告)日：2012-02-02
申请号：PCT/US2011/044961
申请日：2011-07-22
申请人： SMARTCELLS, INC. , KANE, John , LANCASTER, Thomas, M. , ZION, Todd, C.
发明人： KANE, John , LANCASTER, Thomas, M. , ZION, Todd, C.
IPC分类号： C07K14/62
CPC分类号： C07C237/12 , A61K38/28 , A61K47/549 , C07K14/62
摘要： The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: (I) wherein each of X, Alk, and W are as defined and described herein.
摘要翻译：本发明涉及合成式I化合物或其药学上可接受的盐的方法：（I）其中X，Alk和W各自如本文所定义和描述。

9. 发明申请

WO2012015681A2 DRUG-LIGAND CONJUGATES, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO 审中-公开
标题翻译：药物与药物联合治疗药物合成及其中间体
公开(公告)号：WO2012015681A2
公开(公告)日：2012-02-02
申请号：PCT/US2011/044936
申请日：2011-07-22
申请人： SMARTCELLS, INC. , CHEN, Zhiyu , LANCASTER, Thomas, M. , ZION, Todd, C.
发明人： CHEN, Zhiyu , LANCASTER, Thomas, M. , ZION, Todd, C.
IPC分类号： C07K14/62
CPC分类号： A61K47/48092 , A61K47/549 , C07H13/04 , C07H15/04 , C07H15/26
摘要： The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: I wherein each of X, Alk 1 , Alk 2 , and W are as defined and described herein.
摘要翻译：本发明涉及合成式I化合物或其药学上可接受的盐的方法：其中X，Alk1，Alk2和W中的每一个如本文所定义和描述。

10. 发明申请

WO2010088300A1 CRYSTALLINE INSULIN-CONJUGATES 审中-公开
标题翻译：结晶胰岛素结合
公开(公告)号：WO2010088300A1
公开(公告)日：2010-08-05
申请号：PCT/US2010/022277
申请日：2010-01-27
申请人： SMARTCELLS, INC. , ZION, Todd, C. , LANCASTER, Thomas, M.
发明人： ZION, Todd, C. , LANCASTER, Thomas, M.
IPC分类号： C07K14/62 , A61K38/28
CPC分类号： C07K14/62 , A61K38/28 , A61K47/48092 , A61K47/549
摘要： The present disclosure provides crystalline insulin-conjugates. The present disclosure also provides formulations, methods of treatment, methods of administering, and methods of making that encompass these crystalline insulin-conjugates.
摘要翻译：本公开提供结晶胰岛素缀合物。本公开还提供了制剂，治疗方法，施用方法以及制备其包括这些结晶性胰岛素缀合物的方法。

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