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公开(公告)号：US20160038607A1
公开(公告)日：2016-02-11
申请号：US14765620
申请日：2014-02-04
发明人： Zihni Basar BILGICER , Jonathan ASHLEY , Tanyel KIZILTEPE-BILGICER , Jared STEFANICK , Nathan J. ALVES
CPC分类号： A61K38/07 , A61K9/0014 , A61K9/0019 , A61K9/008 , A61K9/1271 , A61K9/2054 , A61K9/4858 , A61K38/05 , A61K47/542 , A61K47/62 , A61K47/6911
摘要： The invention provides pharmaceutical compositions and method of using the compositions, wherein the compositions comprise liposomes or micelles that contain one or more targeting peptides and/or anticancer drugs. In various embodiments, the components of the liposomes can include a) a phospholipid and optionally a lipid that is not a phospholipid; b) a pegylated lipid; c) a peptide-ethylene glycol (EG)-lipid conjugate wherein the peptide is a targeting ligand, and d) one or more drug-conjugated lipid, encapsulated drugs, or a combination thereof. The peptide-EG-lipid conjugate can be, for example, a compound of Formula (I) or Formula (II). The ethylene glycol (EG) segments of the peptide-EG-lipid conjugate can be, for example, EG6 to about EG36; and the EG segment can be conjugated to one or more lysine moieties.
摘要翻译： 本发明提供药物组合物和使用组合物的方法，其中组合物包含含有一种或多种靶向肽和/或抗癌药物的脂质体或胶束。 在各种实施方案中，脂质体的组分可以包括a）磷脂和任选的不是磷脂的脂质; b）聚乙二醇化脂质; c）肽 - 乙二醇（EG） - 脂质缀合物，其中所述肽是靶向配体，和d）一种或多种药物结合的脂质，包封的药物或其组合。 肽-EG-脂质缀合物可以是例如式（I）或式（II）的化合物。 肽-EG-脂质缀合物的乙二醇（EG）片段可以是例如EG6至约EG36; 并且EG区段可以与一个或多个赖氨酸部分缀合。
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公开(公告)号：US20220218839A1
公开(公告)日：2022-07-14
申请号：US17465418
申请日：2021-09-02
IPC分类号： A61K47/68 , C07K16/28 , C07K16/00 , G01N33/531 , A61K31/337 , G01N33/532 , G01N33/533 , G01N33/543
摘要： A method of crosslinking a hetero-bifunctional photo crosslinking compound to an immunoglobulin having at least one heterocyclic photo reactive group and at least one non-photo reactive group where the non-photo reactive group is coupled to an effector molecule and the photo reactive group is coupled to the nucleotide binding site of an immunoglobulin. Alternatively, the photo crosslinker contains an orthogonal reactive group such as a thiol, which can be coupled to an effector molecule or functionalized ligand.
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公开(公告)号：US20240343835A1
公开(公告)日：2024-10-17
申请号：US18735637
申请日：2024-06-06
发明人： Zihni Basar BILGICER , Peter Edward DEAK , Tanyel KIZILTEPE BILGICER , Michael William HANDLOGTEN , Jonathan Darryl ASHLEY
IPC分类号： C07K16/46 , A61K9/127 , A61K38/05 , A61K38/07 , A61K47/02 , A61K47/10 , A61K47/54 , A61K47/62
CPC分类号： C07K16/46 , A61K9/127 , A61K38/05 , A61K38/07 , A61K47/02 , A61K47/10 , A61K47/54 , A61K47/62
摘要： A strategy for site specific covalent modification of antibodies using a specialized targeting covalent heterobivalent ligand (cHBL), and corresponding design for a covalent heterobivalent inhibitor (cHBI) that can be used to prevent Immunoglobulin E (IgE) mediated allergic reactions triggered by drug molecules, according to one embodiment. These molecules contain four important components: (1) an IgE antigen binding site (ABS) ligand that can be a mimotope for the allergen protein, a small molecule, or a peptidomimetic, (2) an appropriate linker, which can be any flexible or rigid chemical linker, providing spacing between the ABS binder and the other moieties, (3) a nucleotide binding site (NBS) ligand, and (4) a reactive moiety to form a covalent link with an amino acid side chain of target IgE antibodies.
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公开(公告)号：US20190328896A1
公开(公告)日：2019-10-31
申请号：US16450615
申请日：2019-06-24
IPC分类号： A61K47/68 , C07K16/00 , C07K16/28 , G01N33/531 , G01N33/532 , G01N33/533 , G01N33/543 , A61K31/337
摘要： A method of crosslinking a hetero-bifunctional photo crosslinking compound to an immunoglobulin having at least one heterocyclic photo reactive group and at least one non-photo reactive group where the non-photo reactive group is coupled to an effector molecule and the photo reactive group is coupled to the nucleotide binding site of an immunoglobulin. Alternatively, the photo crosslinker contains an orthogonal reactive group such as a thiol, which can be coupled to an effector molecule or functionalized ligand.
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公开(公告)号：US20180263909A1
公开(公告)日：2018-09-20
申请号：US15760076
申请日：2016-09-15
CPC分类号： A61K9/1271 , A61K9/0019 , A61K31/167 , A61K31/5375 , A61K31/65 , A61K31/704 , A61K38/08 , A61K47/10 , A61K47/24 , A61K47/6911 , A61P35/00
摘要： The disclosure provides pharmaceutical compositions and method of using the compositions, wherein the compositions comprise liposomes that contain two or more anticancer drugs. In various embodiments the components of the liposomes can include a) a phospholipid, b) a pegylated lipid, c) an aqueous core, and d) at least one covalently-linked drug-conjugated lipid, an encapsulated drug, or a combination thereof, wherein the drug of the lipid-drug conjugate, encapsulated drug, or both, are anticancer drugs.
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公开(公告)号：US20210138089A1
公开(公告)日：2021-05-13
申请号：US17126616
申请日：2020-12-18
发明人： Zihni Basar BILGICER , Peter Edward DEAK , Tanyel KIZILTEPE BILGICER , Jared Francis STEFANICK , Jonathan Darryl ASHLEY
摘要： Embodiments of the present disclosure provide a nanoparticle based platform, and nanoallergens for identifying, evaluating and studying allergen mimotopes as multiple copies of a single mimotope or various combinations on the same particle. The nanoparticle is extremely versatile and allows multivalent binding to IgEs specific to a variety of mimotopes, simulating allergen proteins. Nanoparticles can include various molecular ratios of components. For example, the nanoallergens can include about 0.1-40% mimotope-lipid conjugate and about 60-99.9% lipid. The mimotope-lipid conjugate includes a mimotope, a first linker, and lipid molecule. Nanoallergens can be used in in vitro and in vivo applications to identify a specific patient's sensitivity to a set of epitopes and predict a symptomatic clinical response, identify allergen epitopes through blind screening peptide sequences from allergen protein, and in a clinical application similar to a scratch test.
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公开(公告)号：US20210115157A1
公开(公告)日：2021-04-22
申请号：US17126466
申请日：2020-12-18
发明人： Zihni Basar BILGICER , Peter Edward DEAK , Tanyel KIZILTEPE BILGICER , Michael William HANDLOGTEN , Jonathan Darryl ASHLEY
IPC分类号： C07K16/46 , A61K47/62 , A61K47/54 , A61K9/127 , A61K38/05 , A61K38/07 , A61K47/02 , A61K47/10
摘要： The invention provides a strategy for site specific covalent modification of antibodies using a specialized targeting covalent heterobivalent ligand (cHBL), and corresponding design for a covalent heterobivalent inhibitor (cHBI) that can be used to prevent Immunoglobulin E (IgE) mediated allergic reactions triggered by drug molecules, according to one embodiment. These molecules contain four important components: (1) an IgE antigen binding site (ABS) ligand that can be a mimotope for the allergen protein, a small molecule, or a peptidomimetic, (2) an appropriate linker, which can be any flexible or rigid chemical linker, providing spacing between the ABS binder and the other moieties, (3) a nucleotide binding site (NBS) ligand, and (4) a reactive moiety to form a covalent link with an amino acid side chain of target IgE antibodies.
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公开(公告)号：US20180272008A1
公开(公告)日：2018-09-27
申请号：US15762260
申请日：2016-09-26
发明人： Zihni Basar BILGICER , Peter DEAK , Tanyel KIZILTEPE BILGICER , Jared Francis STEFANICK , Jonathan Darryl ASHLEY
CPC分类号： A61K49/0006 , A61K9/0014 , A61K9/1271 , A61K39/35 , A61K47/6911 , A61K2039/60 , C12Q1/40 , C12Y302/01052 , G01N33/586 , G01N33/6854 , G01N33/686 , G01N2800/24
摘要： Embodiments of the present disclosure provide a nanoparticle based platform, and nanoallergens for identifying, evaluating and studying allergen mimotopes as multiple copies of a single mimotope or various combinations on the same particle. The nanoparticle is extremely versatile and allows multivalent binding to IgEs specific to a variety of mimotopes, simulating allergen proteins. Nanoparticles can include various molecular ratios of components. For example, the nanoallergens can include about 0.1-40% mimotope-lipid conjugate and about 60-99.9% lipid. The mimotope-lipid conjugate includes a mimotope, a first linker, and lipid molecule. Nanoallergens can be used in in vitro and in vivo applications to identify a specific patient's sensitivity to a set of epitopes and predict a symptomatic clinical response, identify allergen epitopes through blind screening peptide sequences from allergen protein, and in a clinical application similar to a scratch test.
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公开(公告)号：US20180177810A1
公开(公告)日：2018-06-28
申请号：US15878295
申请日：2018-01-23
发明人： Zihni Basar BILGICER , Tanyel KIZILTEPE BILGICER , Jonathan Darryl ASHLEY , Jared Francis STEFANICK , Nathan J. ALVES , Michael W. HANDLOGTEN
IPC分类号： A61K31/704 , A61K51/04 , A61K31/351 , A61K47/69 , A61K47/62 , A61K9/107
CPC分类号： A61K31/704 , A61K9/1075 , A61K31/351 , A61K47/62 , A61K47/6907 , A61K47/6909 , A61K51/0455
摘要： Embodiments provide systems, methods, and compositions for nanoparticle-based drug delivery to target cells or tissues. A drug delivery system may include a nanoparticle with a targeting component and a therapeutic component. The nanoparticle may have a predetermined number or valence of targeting molecules for multivalent interaction with a target cell or tissue. Binding of the targeting molecules to the target cell may result in receptor-mediated uptake of the nanoparticle by the target cell. The therapeutic component may be subsequently released within an endocytic vesicle of the target cell. Nanoparticle-based drug delivery systems as described herein may provide improved efficacy and/or reduced toxicity.
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