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    SELECTIVE SERINE/THREONINE KINASE INHIBITORS
    6.
    发明申请
    SELECTIVE SERINE/THREONINE KINASE INHIBITORS 有权
    选择性丝氨酸/螺旋激酶抑制剂

    公开(公告)号：US20090221614A1

    公开(公告)日：2009-09-03

    申请号：US12088059

    申请日：2006-09-26

    Applicant: Jack Taunton ,  Michael Cohen ,  Kevin Shokat ,  Chao Zhang

    Inventor： Jack Taunton ,  Michael Cohen ,  Kevin Shokat ,  Chao Zhang

    IPC: A61K31/519 ,  C07D487/02 ,  C07D209/56 ,  C07D239/72 ,  C07D223/14 ,  C07D209/36 ,  C12N9/99 ,  C12N9/12 ,  C12N5/00 ,  C40B40/04 ,  A61P35/00

    CPC classification number: C07D487/04 ,  C07D239/42 ,  C07D403/06 ,  C07D487/14 ,  C07D519/00

    Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.

    Abstract translation: 在ATP结合位点内具有一个或多个半胱氨酸残基的蛋白激酶的抑制通过使本身或细胞或受试者中的激酶与抑制有效量的具有由两个或更多个的杂环核心结构组成的化合物接触来实现 含有至少一个氮环原子的稠环，以及能够与激酶的ATP结合位点内的半胱氨酸残基反应的亲电取代基。 优选的化合物包括具有这样的亲电子取代基的某些吡咯并嘧啶和羟吲哚，以及任选的能够与位于激酶的关守位置的苏氨酸或更小残基相互作用的芳族或杂芳族取代基。 缺乏这种半胱氨酸残基的激酶可以被改造或修饰，使得它们能够被这种化合物抑制，通过用半胱氨酸残基替换ATP结合位点内的缬氨酸或其它氨基酸残基。

    Selective serine/threonine kinase inhibitors
    9.
    发明授权
    Selective serine/threonine kinase inhibitors 有权
    选择性丝氨酸/苏氨酸激酶抑制剂

    公开(公告)号：US08748601B2

    公开(公告)日：2014-06-10

    申请号：US12088059

    申请日：2006-09-26

    Applicant: Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    Inventor： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    IPC: C07D487/00 ,  C07D411/02 ,  C07D487/04

    CPC classification number: C07D487/04 ,  C07D239/42 ,  C07D403/06 ,  C07D487/14 ,  C07D519/00

    Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.

    Abstract translation: 在ATP结合位点内具有一个或多个半胱氨酸残基的蛋白激酶的抑制通过使本身或细胞或受试者中的激酶与抑制有效量的具有由两个或更多个的杂环核心结构组成的化合物接触来实现 含有至少一个氮环原子的稠环，以及能够与激酶的ATP结合位点内的半胱氨酸残基反应的亲电取代基。 优选的化合物包括具有这样的亲电子取代基的某些吡咯并嘧啶和羟吲哚，以及任选的能够与位于激酶的关守位置的苏氨酸或更小残基相互作用的芳族或杂芳族取代基。 缺乏这种半胱氨酸残基的激酶可以被改造或修饰，使得它们能够被这种化合物抑制，通过用半胱氨酸残基替换ATP结合位点内的缬氨酸或其它氨基酸残基。

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