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    MULTI-ARMED FORMS OF ACTIVATED POLYOXAZOLINE AND METHODS OF SYNTHESIS THEREOF
    1.
    发明申请
    MULTI-ARMED FORMS OF ACTIVATED POLYOXAZOLINE AND METHODS OF SYNTHESIS THEREOF 审中-公开
    活性多环芳烃的多臂形式及其合成方法

    公开(公告)号：WO2009043027A2

    公开(公告)日：2009-04-02

    申请号：PCT/US2008/078159

    申请日：2008-09-29

    Applicant: SERINA THERAPEUTICS, INC. ,  HARRIS, J., Milton ,  BENTLEY, Michael, David ,  YOON, Kunsang ,  FANG, Zhihao

    Inventor： HARRIS, J., Milton ,  BENTLEY, Michael, David ,  YOON, Kunsang ,  FANG, Zhihao

    IPC: C07D263/10 ,  C08G73/00 ,  C08L79/04

    CPC classification number: C07D263/12 ,  A61K47/59 ,  A61K47/64 ,  C08G73/0233 ,  C08L79/02

    Abstract: 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.

    Abstract translation: 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想要的副反应（例如但不限于链转移）产生的杂质的减少量。

    MULTIFUNCTIONAL FORMS OF POLYOXAZOLINE COPOLYMERS AND DRUG COMPOSITIONS COMPRISING THE SAME
    2.
    发明申请
    MULTIFUNCTIONAL FORMS OF POLYOXAZOLINE COPOLYMERS AND DRUG COMPOSITIONS COMPRISING THE SAME 审中-公开
    聚氧杂环丁烷共聚物的多功能形式和包含其的药物组合物

    公开(公告)号：WO2009089542A3

    公开(公告)日：2009-10-01

    申请号：PCT/US2009030762

    申请日：2009-01-12

    Applicant: SERINA THERAPEUTICS INC ,  HARRIS J MILTON ,  BENTLEY MICHAEL DAVID ,  YOON KUNSANG

    Inventor： HARRIS J MILTON ,  BENTLEY MICHAEL DAVID ,  YOON KUNSANG

    IPC: C08G69/44

    CPC classification number: C08G73/0233 ,  C08G73/028

    Abstract: 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.

    Abstract translation: 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
    5.
    发明申请
    POLYOXAZOLINES WITH INERT TERMINATING GROUPS, POLYOXAZOLINES PREPARED FROM PROTECTED INITIATING GROUPS AND RELATED COMPOUNDS 审中-公开
    带有末端终止组的聚氧杂环己烷，由保护的起始组合制备的聚氧杂环戊烯和相关化合物

    公开(公告)号：WO2010006282A3

    公开(公告)日：2010-07-22

    申请号：PCT/US2009050286

    申请日：2009-07-10

    Applicant: SERINA THERAPEUTICS INC ,  HARRIS J MILTON ,  BENTLEY MICHAEL DAVID ,  YOON KUNSANG ,  REIF MICHAEL ,  JORDAN RAINER

    Inventor： HARRIS J MILTON ,  BENTLEY MICHAEL DAVID ,  YOON KUNSANG ,  REIF MICHAEL ,  JORDAN RAINER

    IPC: C08G73/06 ,  A61K9/127 ,  C08L79/04

    CPC classification number: C08G73/0233 ,  A61K9/1272 ,  C08L79/02

    Abstract: 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.

    Abstract translation: 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。

    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 审中-公开
    含有惰性末端基团的聚恶唑啉，由受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：WO2010006282A2

    公开(公告)日：2010-01-14

    申请号：PCT/US2009/050286

    申请日：2009-07-10

    Applicant: SERINA THERAPEUTICS, INC. ,  HARRIS, J., Milton ,  BENTLEY, Michael, David ,  YOON, Kunsang ,  REIF, Michael ,  JORDAN, Rainer

    Inventor： HARRIS, J., Milton ,  BENTLEY, Michael, David ,  YOON, Kunsang ,  REIF, Michael ,  JORDAN, Rainer

    CPC classification number: C08G73/0233 ,  A61K9/1272 ,  C08L79/02

    Abstract: 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.

    Abstract translation: 本公开提供了通过用惰性化学基团终止聚恶唑啉聚合制备的新型官能聚恶唑啉衍生物。 此外，本公开内容证明具有能够引发恶唑啉聚合且能够存活聚合条件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他聚恶唑啉。 此外，本公开提供了使用这种聚恶唑啉 - 脂质缀合物制备的聚恶唑啉 - 脂质缀合物和脂质体组合物。 还公开了使用前述方法制备与靶分子的缀合物的方法。

    MULTIFUNCTIONAL FORMS OF POLYOXAZOLINE COPOLYMERS AND DRUG COMPOSITIONS COMPRISING THE SAME
    7.
    发明申请
    MULTIFUNCTIONAL FORMS OF POLYOXAZOLINE COPOLYMERS AND DRUG COMPOSITIONS COMPRISING THE SAME 审中-公开
    多羟基化合物共聚物的多功能形式和包含它们的药物组合物

    公开(公告)号：WO2009089542A2

    公开(公告)日：2009-07-16

    申请号：PCT/US2009/030762

    申请日：2009-01-12

    Applicant: SERINA THERAPEUTICS, INC. ,  HARRIS, J. Milton ,  BENTLEY, Michael David ,  YOON, Kunsang

    Inventor： HARRIS, J. Milton ,  BENTLEY, Michael David ,  YOON, Kunsang

    IPC: C08G69/44

    CPC classification number: C08G73/0233 ,  C08G73/028

    Abstract: 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.

    Abstract translation: 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，嵌段共聚物或无规和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和用于缀合分子如靶向，诊断和治疗剂的新方法。

    MULTI-ARMED FORMS OF ACTIVATED POLYOXAZOLINE AND METHODS OF SYNTHESIS THEREOF
    8.
    发明申请
    MULTI-ARMED FORMS OF ACTIVATED POLYOXAZOLINE AND METHODS OF SYNTHESIS THEREOF 审中-公开
    活性聚恶唑啉的多臂形式及其合成方法

    公开(公告)号：WO2009043027A3

    公开(公告)日：2009-06-25

    申请号：PCT/US2008078159

    申请日：2008-09-29

    Applicant: SERINA THERAPEUTICS INC ,  HARRIS J MILTON ,  BENTLEY MICHAEL DAVID ,  YOON KUNSANG ,  FANG ZHIHAO

    Inventor： HARRIS J MILTON ,  BENTLEY MICHAEL DAVID ,  YOON KUNSANG ,  FANG ZHIHAO

    IPC: C07D263/10 ,  C08G73/00 ,  C08L79/04

    CPC classification number: C07D263/12 ,  A61K47/59 ,  A61K47/64 ,  C08G73/0233 ,  C08L79/02

    Abstract: 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.

    Abstract translation: 本公开提供了新的POZ-2衍生物，用于合成POZ-2衍生物的方法和用于这些方法的中间体。 在一个实施方案中，POZ-2衍生物包含直接或间接连接至含有用于将POZ-2衍生物连接至靶分子的官能团的支化部分的本发明的两条线性POZ链。 还描述了靶分子-POZ-2缀合物。 在某些实施方案中，POZ-2衍生物具有低多分散性值和由不希望的副反应产生的杂质的量降低，例如但不限于链转移。

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