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    Conjugated biological molecules and their preparation
    2.
    发明申请
    Conjugated biological molecules and their preparation 有权
    共轭生物分子及其制备

    公开(公告)号：US20060210526A1

    公开(公告)日：2006-09-21

    申请号：US10564340

    申请日：2004-07-12

    申请人： Stephen Brocchini ,  Antony Godwin ,  Elisa Pedone ,  Jin-Won Choi ,  Sunil Shaunak

    发明人： Stephen Brocchini ,  Antony Godwin ,  Elisa Pedone ,  Jin-Won Choi ,  Sunil Shaunak

    IPC分类号： A61K38/16 ,  A61K31/785 ,  C08G63/91 ,  C08G63/48

    CPC分类号： A61K47/48215 ,  A61K47/60

    摘要： Novel biologically active compounds of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W- together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z1 and Z2 independently represents a group derived from a biological molecule, each of which is linked to A and B via a nucleophilic moiety; or Z1 and Z2 together represent a single group derived from a biological molecule which is linked to A and B via two nucleophilic moieties; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via nucleophilic groups in said molecule, preferably via a disulphide bridge.

    摘要翻译： 通式（I）的新型生物活性化合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z 1和Z 2各自独立地表示衍生自生物分子的基团，其各自通过亲核部分连接到A和B; 或Z 1和Z 2一起代表衍生自经由两个亲核部分与A和B连接的生物分子的单一基团; A是C 1-5亚烷基或亚烯基链; 和B是键或C 1-4亚烷基或亚烯基链; 通过将所述分子中的亲核基团，优选通过二硫桥将合适的聚合物与合适的生物活性分子缀合而形成。

    NOVEL CONJUGATED PROTEINS AND PEPTIDES
    3.
    发明申请
    NOVEL CONJUGATED PROTEINS AND PEPTIDES 审中-公开
    新型结合蛋白和肽

    公开(公告)号：US20100239517A1

    公开(公告)日：2010-09-23

    申请号：US12682057

    申请日：2008-10-08

    申请人： Stephen Brocchini ,  Penny Bryant ,  Yuehua Cong ,  Ji-Won Choi ,  Antony Godwin ,  Keith Powell

    发明人： Stephen Brocchini ,  Penny Bryant ,  Yuehua Cong ,  Ji-Won Choi ,  Antony Godwin ,  Keith Powell

    IPC分类号： A61K38/21 ,  C07K16/00 ,  C07K14/56 ,  C07K14/47 ,  A61K38/17 ,  A61K39/44 ,  A61P29/00

    CPC分类号： A61K47/645 ,  A61K47/60 ,  A61K47/65

    摘要： The invention provides a novel process for conjugating a polymer, especially PEG, to a protein or peptide, which comprises reacting a polymeric conjugation reagent with a protein or peptide containing a polyhistidine tag under conditions such that conjugation occurs via said polyhistidine tag. The resulting conjugates are novel. The invention further relates to novel conjugates of the general formula (I) in which one of X and X′ represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X′ represents a polymer, X-Q-W— together may represent an electron withdrawing group; and in addition, if X represents a polymer, X′ and electron withdrawing group W together with the interjacent atoms may form a ring; Z represents a protein or a peptide linked to A and B via respective histidine residues; A is a C1-5 alkylene or alkenylene chain; and B is a bond or a C1-4 alkylene or alkenylene chain.

    摘要翻译： 本发明提供了一种用于将聚合物，特别是PEG与蛋白质或肽共轭的新方法，其包括使聚合物缀合试剂与含有多组氨酸标签的蛋白质或肽在通过所述多组氨酸标签发生缀合的条件下反应。 所得到的缀合物是新颖的。 本发明还涉及通式（I）的新结合物，其中X和X'之一表示聚合物，另一个表示氢原子; 每个Q独立地表示连接基团; W表示吸电子部分或可通过还原吸电子部分制备的部分; 或者如果X'代表聚合物，则X-Q-W一起可以代表吸电子基团; 此外，如果X表示聚合物，则X'和吸电子基团W与中间原子一起可以形成环; Z表示通过相应组氨酸残基与A和B连接的蛋白质或肽; A是C 1-5亚烷基或亚烯基链; B是键或C1-4亚烷基或亚链烯基。

    Block copolymers
    4.
    发明申请
    Block copolymers 审中-公开
    嵌段共聚物

    公开(公告)号：US20050031575A1

    公开(公告)日：2005-02-10

    申请号：US10500536

    申请日：2002-12-27

    申请人： Stephen Brocchini ,  Antony Godwin

    发明人： Stephen Brocchini ,  Antony Godwin

    IPC分类号： A61K47/48 ,  A61K31/704 ,  A61P35/00 ,  C08F4/00 ,  C08F4/40 ,  C08F8/00 ,  C08F293/00 ,  C08F297/02 ,  A61K31/785 ,  C08K5/07

    CPC分类号： C08F297/026 ,  C08F293/005

    摘要： Novel block copolymers are described, together with the production therefrom of physiologically soluble polymer therapeutics. The block copolymers have the general formula (I) wherein R is selected from the group consisting of hydrogen, C1-C18 alkyl, C2-C18 alkenyl, C7-C18 aralkyl, C7-C18 alkaryl, C6-C18 aryl, carboxylic acid, C2-C18 alkoxycarbonyl, C2-C18 alkaminocarbonyl, or any one of C1-C18 alkyl, C2-C18 alkenyl, C7-C18 aralkyl, C7-C18 alkaryl, C6-C18 aryl, C2-C18 alkoxycarbonyl and C2-C18 alkaminocarbonyl substituted with a heteroatom within, or attached to, the carbon backbone: R1 is selected from the group consisting of hydrogen and C1-C6 alkyl groups; R2 is a linking group; X is an electron withdrawing group; R3 is selected from the group consisting of C1-C15 alkylene, C2-C15 alkenylene, C7-C15 aralkylene, C7-C18 alarylene and C6-C18 arylene; l, is a divalent linker joining the of C1-C18 alkylene, C2-C18 alkylene, C2-C18 aralkylene, C7-C18 alarylene and C6-C18 arylene; l, is a divalent linker joining the blocks; and m and n are each an integer of greater than 1.

    摘要翻译： 描述了新的嵌段共聚物，以及由其生产的生理可溶性聚合物治疗剂。 嵌段共聚物具有通式（I），其中R选自氢，C 1 -C 18烷基，C 2 -C 18烯基，C 7 -C 18芳烷基，C 7 -C 18烷芳基，C 6 -C 18芳基，羧酸，C 2 C 18烷氧基羰基，C 2 -C 18烷基羰基，或C 1 -C 18烷基，C 2 -C 18烯基，C 7 -C 18芳烷基，C 7 -C 18烷芳基，C 6 -C 18芳基，C 2 -C 18烷氧基羰基和C 2 -C 18烷基羰基 被碳骨架内或附着于碳骨架上的杂原子取代：R 1选自氢和C 1 -C 6烷基; R 2是连接基团; X是吸电子基团; R 3选自C 1 -C 15亚烷基，C 2 -C 15亚烯基，C 7 -C 15亚芳烷基，C 7 -C 18亚芳基和C 6 -C 18亚芳基; C1是连接C1-C18亚烷基，C2-C18亚烷基，C2-C18亚芳基，C7-C18亚芳基和C6-C18亚芳基的二价接头; 1是连接嵌段的二价连接体; m和n分别为大于1的整数。

    Polymeric drug formulations
    5.
    发明授权
    Polymeric drug formulations 有权

    公开(公告)号：US07101840B2

    公开(公告)日：2006-09-05

    申请号：US10177097

    申请日：2002-06-21

    申请人： Stephen Brocchini ,  Stephen R. Hanson ,  Joachim B. Kohn

    发明人： Stephen Brocchini ,  Stephen R. Hanson ,  Joachim B. Kohn

    IPC分类号： C07K14/00 ,  C07K16/00

    CPC分类号： A61K9/146 ,  A61K9/2031 ,  A61K9/204 ,  A61K9/7007

    摘要： A method of forming a polymeric drug formulation in which a water-soluble drug is blended with a water-insoluble tissue-compatible polymer that is miscible in the solid phase with the drug, and with a poly(alkylene oxide), in a solvent system capable of forming a homogeneous solution of the drug, the tissue-compatible polymer and the poly(alkylene oxide), after which the solution is added to a non-solvent for the drug, the tissue-compatible polymer and the poly(alkylene oxide), so that a microdomain-separated solid co-precipitate of the drug, the tissue-compatible polymer and the poly(alkylene oxide) is formed, wherein the poly(alkylene oxide) is blended in an amount effective to form phase-separated microdomains in said co-precipitate.

    Solid Dispersion of Hydrophobic Bioactive
    6.
    发明申请
    Solid Dispersion of Hydrophobic Bioactive 审中-公开
    疏水生物活性的固体分散体

    公开(公告)号：US20080227855A1

    公开(公告)日：2008-09-18

    申请号：US11815619

    申请日：2006-02-10

    申请人： Graham Buckton ,  Stephen Brocchini ,  John Fletcher ,  Hisham Al-Obaidi

    发明人： Graham Buckton ,  Stephen Brocchini ,  John Fletcher ,  Hisham Al-Obaidi

    IPC分类号： A61K31/343

    CPC分类号： A61K31/343 ,  A61K9/146 ,  A61K9/1635 ,  A61K31/352

    摘要： A stable composition of an amorphous component (such as a bioactive) and a carrier polymer is formed by mixing a bridging polymer with the bioactive and the carrier polymer, wherein the bridging polymer is a hydrogen bond donor to both the bioactive and the carrier polymer, thereby forming a composition in which the bioactive and the carrier polymer have less of a tendency to crystallise than if the bridging polymer were not present.

    摘要翻译： 通过将桥连聚合物与生物活性和载体聚合物混合形成非晶组分（例如生物活性）和载体聚合物的稳定组合物，其中桥连聚合物是生物活性载体聚合物和载体聚合物的氢键供体， 从而形成其中生物活性和载体聚合物具有比不存在桥连聚合物更少的结晶倾向的组合物。

    Polymeric drug formulations
    8.
    发明授权
    Polymeric drug formulations 失效
    聚合药物制剂

    公开(公告)号：US07005454B2

    公开(公告)日：2006-02-28

    申请号：US09257145

    申请日：1999-02-24

    申请人： Stephen Brocchini ,  Stephen R. Hanson ,  Joachim B. Kohn

    发明人： Stephen Brocchini ,  Stephen R. Hanson ,  Joachim B. Kohn

    IPC分类号： A61K47/30 ,  A61K47/32 ,  A61K47/34

    CPC分类号： A61K9/146 ,  A61K9/2031 ,  A61K9/204 ,  A61K9/7007

    摘要： Polymeric drug formulations containing a non-releasing single-phase dispersion of a water-soluble drug in a water-insoluble tissue-compatible polymer matrix. Polymeric drug formulations are also disclosed containing a single-phase dispersion of a water-soluble drug and a water-insoluble tissue-compatible polymer matrix, and a second, phase-disrupting polymer that is non-miscible with the tissue-compatible polymer and is present in an amount sufficient to form phase-separated microdomains of the second polymer in the tissue-compatible polymer matrix, so that the release rate of the water-soluble drug from the tissue-compatible polymer matrix is related to the amount of the second polymer. Methods of preparing the polymeric drug formulations are also described, as well as methods for site-specific drug delivery utilizing the polymeric drug formulations.

    摘要翻译： 含水溶性药物的非释放单相分散体在水不溶性组织相容的聚合物基质中的聚合药物制剂。 还公开了含有水溶性药物和水不溶性组织相容聚合物基质的单相分散体的聚合药物制剂，以及与组织相容的聚合物不可混溶的第二种相位破坏性聚合物，并且是 存在的量足以在组织相容性聚合物基质中形成第二聚合物的相分离微区，使得来自组织相容性聚合物基质的水溶性药物的释放速率与第二聚合物的量相关 。 还描述了制备聚合物药物制剂的方法，以及利用聚合物药物制剂的用于位点特异性药物递送的方法。

    Synthesis of tyrosine-derived diphenol monomers
    9.
    再颁专利
    Synthesis of tyrosine-derived diphenol monomers 有权
    酪氨酸衍生的二酚单体的合成

    公开(公告)号：USRE37795E1

    公开(公告)日：2002-07-16

    申请号：US09358015

    申请日：1999-07-21

    申请人： Joachim B. Kohn ,  Stephen Brocchini ,  Arthur L. Schwartz

    发明人： Joachim B. Kohn ,  Stephen Brocchini ,  Arthur L. Schwartz

    IPC分类号： C08G6800

    CPC分类号： C08G69/44 ,  C07C231/02 ,  C07C235/34 ,  C08G63/6856 ,  C08G64/12

    摘要： A method for preparing diphenol compounds, which method includes the steps of coupling a hydroxyphenyl carboxylic acid with a L-tyrosine ester in a water-miscible organic reaction solvent containing a carbodiimide capable of forming a water-soluble urea by-product, thereby forming a diphenol reaction product; and combining the reaction mixture with an amount of water effective to precipitate the diphenol as a water-immiscible organic phase, so that a water-immiscible organic phase is formed containing the diphenol reaction product. New diphenol monomers and polymers polymerized therefrom are also discussed.

    摘要翻译： 一种制备二酚化合物的方法，该方法包括将羟基苯基羧酸与L-酪氨酸酯偶联在含有可形成水溶性尿素副产物的碳二亚胺的水混溶性有机反应溶剂中，由此形成 二酚反应产物; 并将反应混合物与一定量的水组合，将水作为与水不混溶的有机相沉淀，使得形成含有二酚反应产物的与水不混溶的有机相。 还讨论了新的二酚单体和从其聚合的聚合物。