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    CONJUGATION REAGENTS
    3.
    发明公开
    CONJUGATION REAGENTS 有权
    缀合试剂

    公开(公告)号：EP2861260A1

    公开(公告)日：2015-04-22

    申请号：EP13731436.5

    申请日：2013-06-17

    申请人： Polytherics Limited

    发明人： GODWIN, Antony

    IPC分类号： A61K47/48 ,  C08G65/329

    CPC分类号： C08G65/3346 ,  A61K47/60 ,  C08G65/329 ,  C08G65/3326 ,  C08G65/33337 ,  C08G2650/50 ,  C08L2203/02

    摘要： The invention provides a compound of the general formula: in which each X independently represents a polymer chain; p represents an integer from 1 to 6; Y represents an amide group; and Z represents either -CH.(CH
    2 L)
    2 or -C(CH
    2 L)(=CH
    2 ), in which each L independently represents a leaving group. The compounds are useful reagents for the conjugation of polymers to proteins, the resulting conjugates being novel and also forming part of the invention.

    摘要翻译： 本发明提供了下列通式的化合物：其中每个X独立地代表聚合物链; p表示1至6的整数; Y代表酰胺基团; Z表示-CH（CH 2 L）2或-C（CH 2 L）（= CH 2），其中每个L独立地表示离去基团。 这些化合物是聚合物与蛋白质缀合的有用试剂，所得到的缀合物是新颖的并且也构成本发明的一部分。

    NOVEL REAGENTS AND METHOD FOR CONJUGATING BIOLOGICAL MOLECULES
    4.
    发明公开
    NOVEL REAGENTS AND METHOD FOR CONJUGATING BIOLOGICAL MOLECULES 有权
    新试剂和方法用于结合生物分子

    公开(公告)号：EP2326349A1

    公开(公告)日：2011-06-01

    申请号：EP09784718.0

    申请日：2009-07-17

    申请人： Polytherics Limited

    发明人： GODWIN, Anthony

    IPC分类号： A61K47/48

    CPC分类号： C07C317/50 ,  A61K47/60 ,  C07C49/20 ,  C07C233/73 ,  C07C317/32 ,  C07D295/155

    摘要： The invention relates to a process for the conjugation of a molecule containing a thiol or amino group to a polymer, which comprises reacting said molecule with a compound of the general formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ X-[Q-W-(CH=CH) n -CH=CH 2 ] m €ƒ€ƒ€ƒ€ƒ€ƒ(V) in which X represents a polymer; Q represents a linking group; W represents a keto group or an ester group -O-CO-; n represents 0 or an integer of from 1 to 4; and m represent an integer of from 1 to 8. The invention also relates to a compound of the general formula €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ X-[NH-CO-Ar-W-(CH=CH) n -CH=CH 2 ] m €ƒ€ƒ€ƒ€ƒ€ƒ(Va) in which X, W, n and m have the meanings given above; and Ar represents an unsubstituted or substituted aryl group.

    UNIFORM MOLECULAR WEIGHT POLYMERS
    6.
    发明授权
    UNIFORM MOLECULAR WEIGHT POLYMERS 有权
    具有均匀分子量的聚合物

    公开(公告)号：EP1222217B1

    公开(公告)日：2005-06-15

    申请号：EP00958841.9

    申请日：2000-09-08

    申请人： Polytherics Limited

    发明人： BROCCHINI, Stephen, James, School of Pharmacy ,  GODWIN, Antony

    IPC分类号： C08F246/00 ,  C08F20/34 ,  C08F20/36 ,  A61K47/48

    CPC分类号： C08F20/36 ,  C08F20/34 ,  C08F246/00

    摘要： A polymer comprising the unit (I) wherein R is selected form the group consisting of hydrogen, C1-C18 alkyl, C1-C18 alkenyl, C1-C18 aralkyl, C1-C18 alkaryl, carboxylic acid, carboxy-C1-6alkyl, or any one of the C1-C18 alkyl, C1-C18 alkenyl, C1-C18 aralkyl, C1-C18 alkaryl substituted with a heteroatom within, or attached to, the carbon backbone; R1 is selected from the group consisting of hydrogen, C¿1?-C6 alkyl groups; X is an acylating agent and wherein the polymer has a polydispersity of less than 1.4, preferably less than 1.2 and a molecular weight (Mw) of less than 100,000, the polymer is preferably made by controlled radical polymerisation and is useful in the production of polymer drug conjugates with desirable biological profiles.

    Novel reagents and method for conjugating biological molecules
    9.
    发明授权
    Novel reagents and method for conjugating biological molecules 有权
    新试剂和方法用于缀生物分子

    公开(公告)号：EP2374481B1

    公开(公告)日：2015-11-04

    申请号：EP11171786.4

    申请日：2009-07-17

    申请人： Polytherics Limited

    发明人： Godwin, Anthony

    IPC分类号： A61K47/48

    CPC分类号： C07C317/50 ,  A61K47/60 ,  C07C49/20 ,  C07C233/73 ,  C07C317/32 ,  C07D295/155

    摘要： The invention relates to a process for the conjugation of a molecule containing a thiol or amino group to a polymer, which comprises reacting said molecule with a compound of the general formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ X-[Q-W-(CH=CH) n -CH=CH 2 ] m €ƒ€ƒ€ƒ€ƒ€ƒ(V) in which X represents a polymer; Q represents a linking group; W represents a keto group or an ester group -O-CO-; n represents 0 or an integer of from 1 to 4; and m represent an integer of from 1 to 8. The invention also relates to a compound of the general formula €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ X-[NH-CO-Ar-W-(CH=CH) n -CH=CH 2 ] m €ƒ€ƒ€ƒ€ƒ€ƒ(Va) in which X, W, n and m have the meanings given above; and Ar represents an unsubstituted or substituted aryl group.