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    MULTI-ARMED FORMS OF ACTIVATED POLYOXAZOLINE AND METHODS OF SYNTHESIS THEREOF
    2.
    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。

    CLEAVABLE CONJUGATES OF CATECHOL COMPOUNDS AND WATER-SOLUBLE POLYMERS AND METHODS OF TREATMENT USING THE SAME
    3.
    发明申请
    CLEAVABLE CONJUGATES OF CATECHOL COMPOUNDS AND WATER-SOLUBLE POLYMERS AND METHODS OF TREATMENT USING THE SAME 审中-公开

    公开(公告)号：WO2020023947A1

    公开(公告)日：2020-01-30

    申请号：PCT/US2019/043820

    申请日：2019-07-27

    Applicant: SERINA THERAPEUTICS, INC.

    Inventor： BENTLEY, Michael ,  FANG, Zhihao ,  WEIMER, Rebecca ,  VIEGAS, Tacey ,  MOREADITH, Randall

    IPC: A61K31/4192 ,  A61K31/4535 ,  A61K47/48

    Abstract: Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

    POLYOXAZOLINE ANTIBODY DRUG CONJUGATES
    4.
    发明申请
    POLYOXAZOLINE ANTIBODY DRUG CONJUGATES 审中-公开
    聚羧酰胺抗体药物联合

    公开(公告)号：WO2016019340A1

    公开(公告)日：2016-02-04

    申请号：PCT/US2015/043297

    申请日：2015-07-31

    Applicant: SERINA THERAPEUTICS, INC.

    Inventor： MOREADITH, Randall ,  BENTLEY, Michael ,  FANG, Zhihao ,  VIEGAS, Tacey

    IPC: C08G73/06 ,  C08G69/00 ,  C08G75/02

    CPC classification number: A61K47/48384 ,  A61K47/557 ,  A61K47/59 ,  A61K47/60 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6883 ,  A61K47/6889

    Abstract: 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.

    Abstract translation: 在本公开内容中，描述了聚合物缀合物，包括聚合物 - 抗体 - 药物偶联物（聚合物ADC），以及这些缀合物用于治疗人类疾病的用途。 聚合物缀合物可以含有大量的聚合物结合剂，因此有效地增加了抗体的药物抗体比例（DAR），超过目前可获得的技术。 当将低密度抗体的抗体用作靶抗体时，这可能是特别重要的。 所描述的聚合物-ADC相对于传统的ADC具有改善的药代动力学和溶解度。 试剂和聚合物之间的接头可以被定制以提供在所需位置和肿瘤内所需条件下释放毒素。 本公开的聚合物-ADC的另外的特征是纯化部分可以连接到聚合物主链以提供聚合物-ADC的简便性。

    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
    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。

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