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    Multifunctional Forms of Polyoxazoline Copolymers and Drug Compositions Comprising the Same
    5.
    发明申请
    Multifunctional Forms of Polyoxazoline Copolymers and Drug Compositions Comprising the Same 审中-公开
    多官能团形式的聚恶唑啉共聚物和药物组合物组成

    公开(公告)号：US20140066577A1

    公开(公告)日：2014-03-06

    申请号：US13957989

    申请日：2013-08-02

    申请人： Serina Therapeutics, Inc.

    发明人： Kunsang YOON ,  J. Milton HARRIS ,  Michael David BENTLEY ,  Zhihac FANG ,  Tacey VIEGAS

    IPC分类号： A61K47/48

    CPC分类号： A61K47/59 ,  A61K38/09 ,  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.

    摘要翻译： 本公开提供了具有两个或三个也是化学正交的反应性官能团的2-取代-2-恶唑啉的共聚物。 所述共聚物可以是无规共聚物，嵌段共聚物或无规嵌段共聚物构型的混合物。 此外，本公开提供了用于合成上述聚合物并用于与靶标，诊断和治疗剂等分子缀合的新方法。

    Polyoxazolines with Inert Terminating Groups, Polyoxazolines Prepared from Protected Initiating Groups and Related Compounds
    6.
    发明申请
    Polyoxazolines with Inert Terminating Groups, Polyoxazolines Prepared from Protected Initiating Groups and Related Compounds 有权
    具有惰性终止基团的聚恶唑啉，由保护起始基团和相关化合物制备的聚恶唑啉

    公开(公告)号：US20110123453A1

    公开(公告)日：2011-05-26

    申请号：US13003306

    申请日：2009-07-10

    申请人： Michael David Bentley ,  J. Milton Harris ,  Michael Reif ,  Rainer Jordon ,  Kunsang Yoon

    发明人： Michael David Bentley ,  J. Milton Harris ,  Michael Reif ,  Rainer Jordon ,  Kunsang Yoon

    IPC分类号： A61K49/00 ,  C08G73/06 ,  A61K9/127 ,  A61K31/787

    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 poly-oxazolines 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多 - 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。

    Polyoxazoline antibody drug conjugates
    7.
    发明授权
    Polyoxazoline antibody drug conjugates 有权

    公开(公告)号：US11065340B2

    公开(公告)日：2021-07-20

    申请号：US16126798

    申请日：2018-09-10

    申请人： Serina Therapeutics, Inc.

    发明人： Randall W. Moreadith ,  Michael D. Bentley ,  Zhihao Fang ,  Tacey Viegas

    IPC分类号： A61K47/60 ,  A61K47/68 ,  A61K47/54 ,  A61K47/59

    摘要： In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.

    Polyoxazolines with inert terminating groups, polyoxazolines prepared from protected initiating groups and related compounds
    8.
    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：US08883211B2

    公开(公告)日：2014-11-11

    申请号：US13003306

    申请日：2009-07-10

    申请人： Michael David Bentley ,  J. Milton Harris ,  Michael Reif ,  Rainer Jordon ,  Kunsang Yoon

    发明人： Michael David Bentley ,  J. Milton Harris ,  Michael Reif ,  Rainer Jordon ,  Kunsang Yoon

    IPC分类号： A61K9/14 ,  C08G73/02 ,  A61K9/127 ,  C08L79/02

    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。

    Multi-armed forms of activated polyoxazoline and methods of synthesis thereof
    10.
    发明授权
    Multi-armed forms of activated polyoxazoline and methods of synthesis thereof 有权
    多种形式的活性聚恶唑啉及其合成方法

    公开(公告)号：US08088884B2

    公开(公告)日：2012-01-03

    申请号：US12680448

    申请日：2008-09-29

    申请人： J. Milton Harris ,  Michael David Bentley ,  Kunsang Yoon ,  Zhihao Fang

    发明人： J. Milton Harris ,  Michael David Bentley ,  Kunsang Yoon ,  Zhihao Fang

    IPC分类号： C08G73/06

    CPC分类号： C07D263/12 ,  A61K47/59 ,  A61K47/64 ,  C08G73/0233 ,  C08L79/02

    摘要： The present disclosure provides novel POZ-2 derivatives, methods for synthesizing POZ-2 derivatives and intermediates useful in such methods. In one embodiment, the POZ-2 derivative comprises two linear POZ chains of the present disclosure linked directly or indirectly to a branching moiety that contains a functional group for linking the POZ-2 derivative to the target molecule. Target molecule-POZ-2 conjugates are also described. In certain embodiment, the POZ-2 derivatives have low polydispersity values and a decreased amount of impurities produced by unwanted side reactions, such as, but not limited to, chain transfer.

    摘要翻译： 本公开提供新的POZ-2衍生物，用于合成POZ-2衍生物的方法和可用于这些方法的中间体。 在一个实施方案中，POZ-2衍生物包含本公开的两个线性POZ链，其直接或间接连接到支链部分，其包含用于将POZ-2衍生物与靶分子连接的官能团。 还描述了靶分子-POZ-2缀合物。 在某些实施方案中，POZ-2衍生物具有低的多分散性值和由不希望的副反应（例如但不限于链转移）产生的杂质量的降低。