SELECTIVE SERINE/THREONINE KINASE INHIBITORS
    1.
    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

    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

    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
    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:US08748601B2

    公开(公告)日:2014-06-10

    申请号:US12088059

    申请日:2006-09-26

    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
    4.
    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

    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

    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。

    Image-based localization
    6.
    发明授权
    Image-based localization 有权
    基于图像的本地化

    公开(公告)号:US08798357B2

    公开(公告)日:2014-08-05

    申请号:US13544817

    申请日:2012-07-09

    IPC分类号: G06K9/00

    摘要: Image-based localization technique embodiments are presented which provide a real-time approach for image-based video camera localization within large scenes that have been reconstructed offline using structure from motion or similar techniques. From monocular video, a precise 3D position and 3D orientation of the camera can be estimated on a frame by frame basis using only visual features.

    摘要翻译: 提出了基于图像的定位技术实施例,其提供了使用已经使用运动或类似技术的结构离线重建的大场景内基于图像的摄像机定位的实时方法。 从单眼视频,可以使用仅视觉特征逐帧估计摄像机的精确3D位置和3D取向。

    COMPOSITIONS AND METHODS FOR GROWING HUMAN EMBRYONIC CELLS
    7.
    发明申请
    COMPOSITIONS AND METHODS FOR GROWING HUMAN EMBRYONIC CELLS 审中-公开
    用于生长人胚胎细胞的组合物和方法

    公开(公告)号:US20130302887A1

    公开(公告)日:2013-11-14

    申请号:US13947884

    申请日:2013-07-22

    IPC分类号: C12N5/0735

    摘要: Methods for deriving and cultivating human embryonic stem (ES) cells and maintaining their pluripotency in culture is provided by utilizing secreted products obtained from the culture medium of human embryonic gem (EG) cell derivatives, such as embryoid body-derived cells. Substrates include compounds such as collagen I, fibronectin, or superfibronectin, or extracellular matrix, typically human derived.

    摘要翻译: 通过使用从人胚胎宝石(EG)细胞衍生物(例如胚状体衍生细胞)的培养基获得的分泌产物,提供用于衍生和培养人胚胎干(ES)细胞并维持其培养多能性的方法。 底物包括诸如胶原I,纤连蛋白或超纤连蛋白的化合物,或通常人衍生的细胞外基质。

    System and method for avoiding synchronization bugs through virtualization
    8.
    发明授权
    System and method for avoiding synchronization bugs through virtualization 有权
    通过虚拟化避免同步错误的系统和方法

    公开(公告)号:US08572606B1

    公开(公告)日:2013-10-29

    申请号:US11365012

    申请日:2006-03-01

    IPC分类号: G06F9/455

    摘要: A system and method for reducing the likelihood of concurrency errors by identifying vulnerable segments of computer code and stalling other virtual machine threads of execution. According to one embodiment of the present invention, the vulnerable segment is identified at runtime, for example in a dynamic translator. According to another embodiment of the present invention, the vulnerable segment is identified ahead of time, for example in a static translator. According to yet another embodiment of the present invention, the vulnerable segment is identified in the binary translator of a virtual machine monitor.

    摘要翻译: 通过识别计算机代码的易受攻击的部分并拖延执行其他虚拟机线程来减少并发错误的可能性的系统和方法。 根据本发明的一个实施例,在运行时识别易受攻击的段,例如在动态翻译器中。 根据本发明的另一个实施例,提前识别易受攻击的段,例如在静态转换器中。 根据本发明的另一个实施例,在虚拟机监视器的二进制转换器中识别易受攻击的段。

    COMPOSITIONS AND METHODS FOR GROWING EMBRYONIC STEM CELLS
    9.
    发明申请
    COMPOSITIONS AND METHODS FOR GROWING EMBRYONIC STEM CELLS 审中-公开
    用于生长胚胎干细胞的组合物和方法

    公开(公告)号:US20120034183A1

    公开(公告)日:2012-02-09

    申请号:US12448435

    申请日:2007-12-19

    摘要: Compositions including topical formulations comprising secreted products obtained from the culture medium of human embryonic germ (EG) cell derivatives and particular combinations of components therefrom are provided for treatment of various dermatological conditions, such as adverse consequences of aging, wrinkling, altered pigmentation, altered viscoelasticity, and altered thickness, among others. Methods for using the compositions and topical formulations for treating adverse or undesirable dermatological conditions are also provided, as well as preventing the appearance of undesirable dermatological conditions.

    摘要翻译: 提供包括由人类胚胎(EG)细胞衍生物的培养基获得的分泌产物和其组分的特定组合的包含局部制剂的组合物用于治疗各种皮肤病学条件,例如老化,起皱,改变的色素沉着,改变的粘弹性的不良后果 ,厚度变化等。 还提供了使用组合物和局部制剂治疗不利或不期望的皮肤病学条件的方法,以及防止不期望的皮肤病学病症的出现。

    TOWEL TWIRLING MECHANISM
    10.
    发明申请
    TOWEL TWIRLING MECHANISM 失效
    TOWEL TWIRLING机制

    公开(公告)号:US20110173851A1

    公开(公告)日:2011-07-21

    申请号:US12691382

    申请日:2010-01-21

    申请人: Michael Cohen

    发明人: Michael Cohen

    IPC分类号: G09F17/00 G09F19/02

    CPC分类号: G09F19/02

    摘要: An article, such as a towel, having an opening to secure a twirling mechanism thereto. The twirling mechanism having a handle extending from a bottom portion thereof and having a mechanism to permit rotating of the handle with respect to the fabric-article, such that the fabric article is capable of twirling around the twirling mechanism. The twirling mechanism may in other embodiments include noise maker when the handle is rotated.

    摘要翻译: 诸如毛巾的物品,具有用于固定旋转机构的开口。 旋转机构具有从其底部延伸的手柄,并且具有允许手柄相对于织物制品旋转的机构,使得织物制品能够绕旋转机构旋转。 在其他实施例中,旋转机构可以包括手柄旋转时的噪音制造器。