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1. 发明申请

WO2004056311A2 STIMULI-RESPONSIVE SYSTEMS FOR CONTROLLED DRUG DELIVERY 审中-公开
标题翻译：用于控制药物递送的刺激响应系统
公开(公告)号：WO2004056311A2
公开(公告)日：2004-07-08
申请号：PCT/US0340393
申请日：2003-12-17
申请人： MASSACHUSETTS INST TECHNOLOGY , ZION TODD C , ZARUR ANDREY , YING JACKIE Y
发明人： ZION TODD C , ZARUR ANDREY , YING JACKIE Y
IPC分类号： A61K9/06 , A61K9/14 , A61K9/51 , A61K45/00 , A61K47/36 , A61K47/48 , A61K
CPC分类号： A61K9/5161 , A61K9/06 , A61K9/5192 , A61K47/36 , A61K47/61
摘要： A method of delivering a therapeutic agent by providing a cross-linked polymer encapsulating the therapeutic agent to a site in a patient. The degradation rate of the cross-linked polymer is correlated with a local concentration of an indicator, and the therapeutic agent is released as the cross-linked polymer degrades.
摘要翻译：通过将包封治疗剂的交联聚合物提供给患者部位来递送治疗剂的方法。交联聚合物的降解速率与指示剂的局部浓度相关，并且随着交联聚合物降解，治疗剂释放。

2. 发明申请

WO2007047997A2 METHODS FOR REDUCING THE MITOGENICITY OF LECTIN COMPOSITIONS 审中-公开
标题翻译：降低LECTIN组合物的毒性的方法
公开(公告)号：WO2007047997A2
公开(公告)日：2007-04-26
申请号：PCT/US2006041167
申请日：2006-10-19
申请人： SMARTCELLS INC , LANCASTER THOMAS A , CAI WENYI , FAUCETTE RYAN , PECUKONIS MATTHEW , ZION TODD C
发明人： LANCASTER THOMAS A , CAI WENYI , FAUCETTE RYAN , PECUKONIS MATTHEW , ZION TODD C
IPC分类号： A61K38/28 , C07K14/605 , C07K14/61 , C07K14/62
CPC分类号： C08B37/0084 , A61K38/25 , A61K38/26 , A61K38/28 , A61K47/60 , A61K47/61 , A61K47/6903 , C08B30/18 , C08B37/00 , C08B37/003 , C08B37/0069 , C08B37/0072 , Y10S436/827
摘要： Methods for reducing the T-cell mitogenicity of lectin compositions are provided. In one aspect this is achieved by chemically modifying mitogenic lectin compositions under optimized conditions. Additionally or alternatively, the reduction in T-cell mitogenicity is achieved by removing unmodified subunits chemically modified mixtures. Modified lectin compositions with reduced T-cell mitogenicity are also provided as are uses of the inventive compositions.
摘要翻译：提供了降低凝集素组合物的T细胞有丝分裂原性的方法。在一个方面，这通过在优化的条件下化学改变有丝分裂凝集素组合物来实现。另外或替代地，通过去除未修饰的亚基化学修饰的混合物来实现T细胞有丝分裂原的降低。本发明组合物的用途也提供具有降低的T细胞有丝分裂原性的修饰的凝集素组合物。

3. 发明申请

WO2010088276A3 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：WO2010088276A3
公开(公告)日：2011-01-27
申请号：PCT/US2010022237
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： A61K38/28 , C12P21/08
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。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。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。

4. 发明申请

WO2012015691A3 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：WO2012015691A3
公开(公告)日：2013-08-08
申请号：PCT/US2011044989
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： A61K9/14 , A61K36/00
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。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

WO2012015687A3 DRUG-LIGAND CONJUGATES, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO 审中-公开
标题翻译：药物 - 配体偶合物，其合成及其中间体
公开(公告)号：WO2012015687A3
公开(公告)日：2012-07-19
申请号：PCT/US2011044961
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： A61K47/00 , A61K38/00
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。

6. 发明申请

WO2012015681A3 DRUG-LIGAND CONJUGATES, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO 审中-公开
标题翻译：药物 - 配体偶合物，其合成及其中间体
公开(公告)号：WO2012015681A3
公开(公告)日：2012-05-24
申请号：PCT/US2011044936
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： A61K47/00 , A61K38/00
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, Alk1, Alk2, 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。

7. 发明申请

WO2012015692A3 RECOMBINANTLY EXPRESSED INSULIN POLYPEPTIDES AND USES THEREOF 审中-公开
标题翻译：重要的表达胰岛素多肽及其用途
公开(公告)号：WO2012015692A3
公开(公告)日：2012-04-19
申请号：PCT/US2011045008
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： A61K38/28
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的胰岛素多肽（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（或外源性糖类）作为α-甲基甘露糖）。除了使用和制备方法之外，还提供示例性的胰岛素多肽，编码这些胰岛素多肽的多核苷酸，糖基化胰岛素多肽，药物制剂和持续释放制剂。

8. 发明申请

WO2007047922A2 POLYMER-DRUG CONJUGATES 审中-公开
标题翻译：聚合物 - 药物共轭物
公开(公告)号：WO2007047922A2
公开(公告)日：2007-04-26
申请号：PCT/US2006041035
申请日：2006-10-19
申请人： SMARTCELLS INC , LANCASTER THOMAS A , ZION TODD C , NELAWANSKI MATTHEW
发明人： LANCASTER THOMAS A , ZION TODD C , NELAWANSKI MATTHEW
IPC分类号： A61K38/28 , C07K14/605 , C07K14/61 , C07K14/62
CPC分类号： C08B37/0084 , A61K38/25 , A61K38/26 , A61K38/28 , A61K47/60 , A61K47/61 , A61K47/6903 , C08B30/18 , C08B37/00 , C08B37/003 , C08B37/0069 , C08B37/0072 , Y10S436/827
摘要： A conjugate that includes a drag covalently linked to a polymer. Upon administration, the conjugate is digested by an enzyme that is present at the site of administration thereby releasing a therapeutic agent. The conjugate may demonstrate substantially the same pharmacokinetic and pharmacodynamic behavior as the drug itself. A material for controllably releasing a conjugate in response to the local concentration of a molecular indicator. The material includes a plurality of conjugates and a plurality of multivalent cross-linking agents. The polymers of the conjugates include an analog of the indicator within their covalent structure. The multivalent cross-linking agents include cross-link receptors that interact with the indicator analog and thereby cross-link the conjugates. These non-covalent interactions are competitively disrupted when an amount of the molecular indicator is present thereby causing the material to release the conjugate in a manner that is dependent on the local concentration of indicator.
摘要翻译：包含与聚合物共价连接的药物的偶联物。施用后，缀合物被存在于施用部位的酶消化，由此释放治疗剂。偶联物可以表现出与药物本身基本相同的药代动力学和药效学行为。响应于分子指示剂的局部浓度而可控地释放缀合物的材料。该材料包括多种缀合物和多种多价交联剂。缀合物的聚合物包括其共价结构内的指示物的类似物。多价交联剂包括与指示剂类似物相互作用从而交联缀合物的交联受体。当存在一定量的分子指示剂时，这些非共价相互作用被竞争性地破坏，从而导致材料以取决于指示剂局部浓度的方式释放缀合物。

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