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1.发明授权公开(公告)号：US10166294B2
公开(公告)日：2019-01-01
申请号：US15205671
申请日：2016-07-08
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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2.发明公开公开(公告)号：US20240108750A1
公开(公告)日：2024-04-04
申请号：US18387528
申请日：2023-11-07
发明人： J Milton Harris , Michael Bentley , Tacey Viegas , Randall Moreadith , Robert J Sharpe , Kunsang Yoon , Zhihao Fang , Rebecca Weimer
IPC分类号： A61K47/69
CPC分类号： A61K47/6935
摘要： POZ-lipid conjugates and lipid nanoparticles (LNPs) including POZ-lipid conjugates used to facilitate delivery of an encapsulated payload. LNPs including POZ-lipid conjugates and a nucleic acid payload such as, but not limited to, mRNA or modified mRNA are disclosed. Such LNPs have no immunogenicity or reduced immunogenicity as compared to a corresponding LNP containing a PEG-lipid.
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3.发明申请公开(公告)号：US20220193243A1
公开(公告)日：2022-06-23
申请号：US17568042
申请日：2022-01-04
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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4.发明申请公开(公告)号：US20190134208A1
公开(公告)日：2019-05-09
申请号：US16235936
申请日：2018-12-28
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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公开(公告)号：US10086084B2
公开(公告)日：2018-10-02
申请号：US15453686
申请日：2017-03-08
发明人： J Milton Harris , Michael David Bentley , Kunsang Yoon , Zhihao Fang , Francesco Maria Veronese , Tacey Viegas
IPC分类号： A61K38/18 , A61K47/48 , A61K31/727 , A61K38/33 , A61K38/47 , A61K31/728 , A61K38/19 , A61K38/27 , A61K38/42 , C08G69/48
摘要： The present disclosure provides POZ derivatives having a range of active functional groups allowing conjugation of POZ derivatives to a variety of target molecules under a wide range of reaction conditions to produce a hydrolytically stable target molecule-POZ conjugate. Furthermore, the present disclosure provides novel methods of synthesis for the disclosed POZ derivatives and hydrolytically stable target molecule-POZ conjugates created using the disclosed terminally activated monofunctional POZ derivatives. In one embodiment, the POZ derivative is a terminally activated monofunctional POZ derivative.
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6.发明公开公开(公告)号：US20240277821A1
公开(公告)日：2024-08-22
申请号：US18391869
申请日：2023-12-21
发明人： Randall Moreadith , J Milton Harris , James Dahlman , David Loughrey , Kalina Paunovska , Alejandro Da Silva Sanchez
IPC分类号： A61K39/00
CPC分类号： A61K39/00 , A61K2039/53 , A61K2039/545 , A61K2039/55555 , A61K2039/6018
摘要： A method of targeting antigen-presenting cells and delivering an encapsulated payload with lipid nanoparticles including a POZ-lipid conjugate. The encapsulated payload may include, but is not limited to, a nucleic acid payload such as mRNA or modified mRNA. These LNPs are not subject to accelerated blood clearance and they have a low or reduced immunogenicity profile in vivo.
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7.发明授权公开(公告)号：US11925689B2
公开(公告)日：2024-03-12
申请号：US17568042
申请日：2022-01-04
CPC分类号： A61K47/59 , A61K38/09 , A61P35/00 , C08G73/0233
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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8.发明授权公开(公告)号：US11213588B2
公开(公告)日：2022-01-04
申请号：US16235936
申请日：2018-12-28
摘要： The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.
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9.发明授权Polyoxazolines with inert terminating groups, polyoxazolines prepared from protected initiating groups and related compounds 有权具有惰性终端基的聚恶唑啉，由保护的引发基团和相关化合物制备的聚恶唑啉公开(公告)号：US09284411B2
公开(公告)日：2016-03-15
申请号：US14537516
申请日：2014-11-10
CPC分类号： C08G73/0233 , A61K9/1272 , C08L79/02
摘要： The present disclosure provides novel functional polyoxazoline derivatives prepared by terminating polyoxazoline polymerization with inert chemical groups. In addition, the present disclosure demonstrates the synthesis of novel electrophilic initiators with protected functional groups capable of initiating oxazoline polymerization and capable of surviving the conditions of polymerization. These initiators are used to synthesize the above inert-terminal polyoxazoline derivatives as well as other polyoxazolines with active terminal groups. Furthermore, the present disclosure provides for polyoxazoline-lipid conjugates and liposomal compositions prepared using such polyoxazoline-lipid conjugates. Methods of using the foregoing to prepare conjugates with target molecules are also disclosed.
摘要翻译： 本公开提供通过用惰性化学基团终止聚恶唑啉聚合制备的新型功能性聚恶唑啉衍生物。 此外，本公开内容显示了具有能够引发恶唑啉聚合并能够在聚合条件下存活的受保护官能团的新型亲电子引发剂的合成。 这些引发剂用于合成上述惰性末端聚恶唑啉衍生物以及具有活性末端基团的其它聚恶唑啉。 此外，本公开提供使用这种聚恶唑啉 - 脂质缀合物制备的聚恶唑啉 - 脂质缀合物和脂质体组合物。 还公开了使用前述物质与靶分子制备缀合物的方法。
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