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    Selective serine/threonine kinase inhibitors
    1.
    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

    申请人： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    发明人： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

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

    CPC分类号： C07D487/04 ,  C07D239/42 ,  C07D403/06 ,  C07D487/14 ,  C07D519/00

    摘要： 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.

    摘要翻译： 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
    2.
    发明申请
    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：US20070082884A1

    公开(公告)日：2007-04-12

    申请号：US10552847

    申请日：2004-04-12

    申请人： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    发明人： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    IPC分类号： A61K31/55 ,  A61K31/519 ,  A61K31/517 ,  A61K31/407 ,  A61K31/404

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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
    3.
    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：US07687506B2

    公开(公告)日：2010-03-30

    申请号：US10552847

    申请日：2004-04-12

    申请人： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    发明人： Jack Taunton ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    IPC分类号： C07D487/04 ,  A61K31/52

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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，使得它们能够被这样的化合物抑制，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
    4.
    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：US08034821B2

    公开(公告)日：2011-10-11

    申请号：US12698027

    申请日：2010-02-01

    申请人： John William Taunton, Jr. ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    发明人： John William Taunton, Jr. ,  Michael Cohen ,  Kevan Shokat ,  Chao Zhang

    IPC分类号： C07D487/04 ,  A61K31/52

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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
    5.
    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

    申请人： Jack Taunton ,  Michael Cohen ,  Kevin Shokat ,  Chao Zhang

    发明人： Jack Taunton ,  Michael Cohen ,  Kevin Shokat ,  Chao Zhang

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

    CPC分类号： C07D487/04 ,  C07D239/42 ,  C07D403/06 ,  C07D487/14 ,  C07D519/00

    摘要： 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.

    摘要翻译： 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。

    Hand stand
    7.
    外观设计
    Hand stand 有权

    公开(公告)号：USD968138S1

    公开(公告)日：2022-11-01

    申请号：US29832941

    申请日：2022-03-31

    申请人： Chao Zhang

    设计人： Chao Zhang

    GAME THEORY MODEL FOR PATROLLING AN AREA THAT ACCOUNTS FOR DYNAMIC UNCERTAINTY
    10.
    发明申请
    GAME THEORY MODEL FOR PATROLLING AN AREA THAT ACCOUNTS FOR DYNAMIC UNCERTAINTY 审中-公开
    用于计算动态不确定性帐户的游戏理论模型

    公开(公告)号：US20140279818A1

    公开(公告)日：2014-09-18

    申请号：US14216449

    申请日：2014-03-17

    申请人： Albert Xin Jiang ,  Zhengyu Yin ,  Chao Zhang ,  Milind Tambe ,  Sarit Kraus

    发明人： Albert Xin Jiang ,  Zhengyu Yin ,  Chao Zhang ,  Milind Tambe ,  Sarit Kraus

    IPC分类号： G06N5/04

    CPC分类号： G06N5/048 ,  G06N7/005 ,  G06Q10/047

    摘要： Game theory models may be used for producing a strategy and schedule for patrolling an area like a rail transportation system. In some instances, the model may account for events that cause a patrol unit to deviate from a patrol schedule and route. For example, a patrol schedule may be generated for one or more patrol units using a Bayesian Stackelberg game theory model based on a map of the public transportation system, a schedule of the transports, a list of the one or more patrolling units, a probability distribution for the occurrence of the passenger not paying to ride the transports, a list of the one or more possible events that would delay the patrol units, and a probability distribution for the occurrence of the one or more possible events that would delay the patrolling units represented by a Markov-decision process.

    摘要翻译： 游戏理论模型可用于制定巡视像铁路运输系统这样的区域的战略和时间表。 在某些情况下，该模型可能会导致巡视单位偏离巡逻进度和路线的事件。 例如，可以使用基于公共交通系统的地图，运输时间表，一个或多个巡逻单元的列表，一个或多个巡逻单元的列表，使用贝叶斯Stackelberg游戏理论模型来生成针对一个或多个巡逻单元的巡逻时间表 分配用于不支付乘坐运输工具的乘客的发生，将延迟巡逻单位的一个或多个可能的事件的列表，以及发生一个或多个可能的事件的概率分布，这些事件将延迟巡逻单位 由马尔科夫决定过程代表。