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    Chemical compounds
    2.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US06436691B1

    公开(公告)日：2002-08-20

    申请号：US09011769

    申请日：1998-02-13

    申请人： Anthony Michael Slater ,  David Charles Blakey ,  David Huw Davies ,  John Frederick Hennam ,  Laurent Francois Andre Hennequin ,  Peter Robert Marsham ,  Robert Ian Dowell

    发明人： Anthony Michael Slater ,  David Charles Blakey ,  David Huw Davies ,  John Frederick Hennam ,  Laurent Francois Andre Hennequin ,  Peter Robert Marsham ,  Robert Ian Dowell

    IPC分类号： C12N964

    CPC分类号： B82Y5/00 ,  A61K47/6899 ,  C12N9/48

    摘要： Antibody Directed Enzyme Prodrug Therapy (ADEPT) systems for use in cancer based on mutated carboxypeptidase B (CPB) enzymes. Enzyme conjugates for ADEPT are substantially non-immunogenic in humans comprising a targeting moiety (for example an antibody) capable of binding with a tumor associated antigen, the targeting moiety being linked to a mutated form of a CPB enzyme capable of converting a prodrug into an antineoplastic drug wherein the prodrug is not significantly convertible into antineoplastic drug in humans by natural unmutated enzyme. A preferred enzyme mutant is human pancreatic CPB comprising a Lys or Arg residue at position 253. Suitable mustard prodrugs are disclosed in the specification.

    摘要翻译： 基于突变的羧肽酶B（CPB）酶的用于癌症的抗体定向酶前药治疗（ADEPT）系统。 用于ADEPT的酶缀合物在人中基本上是非免疫原性的，其包含能够与肿瘤相关抗原结合的靶向部分（例如抗体），所述靶向部分与能够将前药转化成为前体药物的CPB酶的突变形式连接 抗肿瘤药物，其中前药在天然未突变酶中不能显着转化成人类的抗肿瘤药物。 优选的酶突变体是人胰腺CPB，其包含位置253处的Lys或Arg残基。合适的芥子酰胺前药在说明书中公开。

    4-Mercaptopyrrolidine derivatives as farnesyl transferase inhibitors
    3.
    发明授权
    4-Mercaptopyrrolidine derivatives as farnesyl transferase inhibitors 失效
    4-巯基吡咯烷衍生物作为法呢基转移酶抑制剂

    公开(公告)号：US06232338B1

    公开(公告)日：2001-05-15

    申请号：US09011135

    申请日：1998-02-03

    申请人： David Huw Davies ,  Francis Thomas Boyle ,  James Michael Wardleworth ,  Peter Wedderburn Kenny ,  Peter Beverley Scholes ,  Zbigniew Stanely Matusiak

    发明人： David Huw Davies ,  Francis Thomas Boyle ,  James Michael Wardleworth ,  Peter Wedderburn Kenny ,  Peter Beverley Scholes ,  Zbigniew Stanely Matusiak

    IPC分类号： A61K3140

    CPC分类号： C07D401/12 ,  C07D207/12 ,  C07D409/12

    摘要： Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.

    摘要翻译： 包含式（I）的ras法呢基酯化抑制剂的药物组合物，其中R1为例如本说明书中定义的其它值; R2是例如H和说明书中定义的其它值; R3是例如H或具有本说明书中定义的值的取代基; p为0-3，其中R3值可以相同或不同; L是例如-CO-NH 2的连接部分和如说明书中定义的进一步的值; A选自苯基; 萘基; 含有多达5个杂原子的5-10元单环或双环杂芳基环，其中杂原子独立地选自O，N和S; 或其-S-S-二聚体时，R 2 = H; 或其对映体，非对映异构体，药学上可接受的盐，前药或溶剂合物以及药学上可接受的稀释剂或载体。 一个特别的用途是癌症治疗。

    4-mercaptopyrrolidine derivatives as farnesyl transferase inhibitors
    4.
    发明授权
    4-mercaptopyrrolidine derivatives as farnesyl transferase inhibitors 失效
    4-巯基吡咯烷衍生物作为法呢基转移酶抑制剂

    公开(公告)号：US06541491B1

    公开(公告)日：2003-04-01

    申请号：US09725964

    申请日：2000-11-30

    申请人： David Huw Davies ,  Francis Thomas Boyle ,  James Michael Wardleworth ,  Peter Wedderburn Kenny ,  Peter Beverley Scholes ,  Zbigniew Stanely Matusiak

    发明人： David Huw Davies ,  Francis Thomas Boyle ,  James Michael Wardleworth ,  Peter Wedderburn Kenny ,  Peter Beverley Scholes ,  Zbigniew Stanely Matusiak

    IPC分类号： A61K3140

    CPC分类号： C07D401/12 ,  C07D207/12 ,  C07D409/12

    摘要： Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S-dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.

    摘要翻译： 包含式（I）的ras法呢基酯化抑制剂的药物组合物，其中R1为例如本说明书中定义的其它值; R2是例如H和说明书中定义的其它值; R3是例如H或具有本说明书中定义的值的取代基; p为0-3，其中R3值可以相同或不同; L是例如-CO-NH 2的连接部分和如说明书中定义的进一步的值; A选自苯基; 萘基; 含有多达5个杂原子的5-10元单环或双环杂芳基环，其中杂原子独立地选自O，N和S; 或其-S-S-二聚体时，R 2 = H; 或其对映体，非对映异构体，药学上可接受的盐，前药或溶剂合物以及药学上可接受的稀释剂或载体。 一个特别的用途是癌症治疗。