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公开(公告)号：US20170022262A1
公开(公告)日：2017-01-26
申请号：US15288362
申请日：2016-10-07
Applicant: SmartCells, Inc.
Inventor： Thomas M. Lancaster , Todd C. Zion
CPC classification number: C07K14/62 , A61K38/28 , A61K47/549
Abstract: 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.
Abstract translation: 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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公开(公告)号：US09463249B2
公开(公告)日：2016-10-11
申请号：US14280793
申请日：2014-05-19
Applicant: SmartCells, Inc.
Inventor： Thomas M. Lancaster , Todd C. Zion
CPC classification number: C07K14/62 , A61K38/28 , A61K47/549
Abstract: 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.
Abstract translation: 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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公开(公告)号：US09095623B2
公开(公告)日：2015-08-04
申请号：US14095068
申请日：2013-12-03
Applicant: SmartCells, Inc.
Inventor： Todd C. Zion , Thomas M. Lancaster
CPC classification number: A61K47/48261 , A61K38/28 , A61K47/48176 , A61K47/58
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20140121159A1
公开(公告)日：2014-05-01
申请号：US14095068
申请日：2013-12-03
Applicant: SmartCells, Inc.
Inventor： Todd C. Zion , Thomas M. Lancaster
CPC classification number: A61K47/48261 , A61K38/28 , A61K47/48176 , A61K47/58
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20180064824A1
公开(公告)日：2018-03-08
申请号：US15680262
申请日：2017-08-18
Applicant: SmartCells, Inc.
Inventor： Todd C. Zion , Thomas M. Lancaster
IPC: A61K38/28
CPC classification number: A61K47/61 , A61K38/28 , A61K47/549
Abstract: Conjugates which comprise a drug and a ligand which includes a first saccharide; wherein the conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the conjugate is sensitive to serum concentration of a second saccharide. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
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Patent Agency Ranking
公开(公告)号：US09265838B2
公开(公告)日：2016-02-23
申请号：US14291021
申请日：2014-05-30
Applicant: SmartCells, Inc.
Inventor： Todd C. Zion , Thomas M. Lancaster
CPC classification number: A61K47/61 , A61K38/28 , A61K47/549
Abstract: Conjugates which comprise a drug and a ligand which includes a first saccharide; wherein the conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the conjugate is sensitive to serum concentration of a second saccharide. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
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公开(公告)号：US09114176B2
公开(公告)日：2015-08-25
申请号：US14266868
申请日：2014-05-01
Applicant: SmartCells, Inc.
Inventor： Todd C. Zion , Thomas M. Lancaster
CPC classification number: A61K47/4823 , A61K38/00 , A61K38/28 , A61K47/26 , A61K47/48092 , A61K47/48246 , A61K47/549 , A61K47/61 , A61K47/64
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20140037699A1
公开(公告)日：2014-02-06
申请号：US14055911
申请日：2013-10-17
Applicant: SmartCells, Inc.
Inventor： Todd C. Zion , Thomas M. Lancaster
IPC: C07K14/62
CPC classification number: C07K14/62 , A61K38/28 , A61K47/549 , A61K47/6415 , C07K14/4713 , C07K14/4743 , C07K14/65
Abstract: In one aspect, the disclosure provides a conjugate comprising an insulin molecule having an A-chain and a B-chain; an affinity ligand covalently bound to the A-chain; and a monovalent glucose binding agent covalently bound to the B-chain, wherein the affinity ligand competes with glucose for non-covalent binding with the monovalent glucose binding agent. In the absence of glucose, the monovalent glucose binding agent binds the affinity ligand to produce a “closed” inactive form of the insulin molecule. When free glucose is added, it competes with the affinity ligand for binding with the monovalent glucose binding agent to produce an “open” active form of the insulin molecule. The monovalent glucose binding agent and affinity ligand are covalently bound to the insulin molecule. The disclosure also provides methods of using these conjugates and methods of making these conjugates. In another aspect, the disclosure provides exemplary conjugates. The disclosure also provides alternative conjugates that are not necessarily activated by glucose.
Abstract translation: 一方面，本公开提供了包含具有A链和B链的胰岛素分子的缀合物; 与A链共价结合的亲和配体; 与B链共价结合的一价葡萄糖结合剂，其中亲和配体与葡萄糖竞争与单价葡萄糖结合剂的非共价结合。 在没有葡萄糖的情况下，一价葡萄糖结合剂结合亲和配体以产生胰岛素分子的“封闭”无活性形式。 当加入游离葡萄糖时，其与亲和配体竞争与单价葡萄糖结合剂结合以产生胰岛素分子的“开放”活性形式。 一价葡萄糖结合剂和亲和配体与胰岛素分子共价结合。 本公开还提供了使用这些缀合物的方法和制备这些缀合物的方法。 在另一方面，本公开提供了示例性缀合物。 本公开还提供了不一定被葡萄糖激活的替代共轭物。
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公开(公告)号：US11413352B2
公开(公告)日：2022-08-16
申请号：US16771819
申请日：2018-12-13
Applicant: Merck Sharp & Dohme LLC , SmartCells,Inc.
Inventor： Chris Moyes , Songnian Lin
Abstract: The present disclosure provides conjugates which comprise an insulin molecule conjugated via a conjugate framework to one or more separate ligands that include a first saccharide, and wherein the conjugate framework also comprises a fatty chain (e.g., a C8-30 fatty chain). In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
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公开(公告)号：US20210177981A1
公开(公告)日：2021-06-17
申请号：US16771819
申请日：2018-12-13
Applicant: Merck Sharp & Dohme Corp. , SmartCells,Inc.
Inventor： Lin Yan , Pei Huo , Ahmet Kekec , Yuping Zhu , Dmitri Pissarnitski , Danqing D. Feng , Chris Moyes , Zhiqiang Zhao , David N. Hunter , Songnian Lin , Thomas M. Lancaster , Benjamin Chen
Abstract: The present disclosure provides conjugates which comprise an insulin molecule conjugated via a conjugate framework to one or more separate ligands that include a first saccharide, and wherein the conjugate framework also comprises a fatty chain (e.g., a C8-30 fatty chain). In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
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