Pyrimidin-4-YL-3, 4-thione compounds and their use in therapy

    公开(公告)号:US20070021452A1

    公开(公告)日:2007-01-25

    申请号:US11408463

    申请日:2006-04-21

    IPC分类号: A61K31/506 C07D417/04

    CPC分类号: C07D417/04 C07D417/14

    摘要: The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj′) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa′CORg′, Rf′, (CH2)rNRb′SO2Rh′, SO2NRd′Ri′, SO2NRe′(CH2)sORc′, heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg′, Rh′, Ri′ and Rj′ are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; n and s are each independently 1, 2, or 3; and Ra-n and Ra′-f′ are each independently H or alkyl. Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes.

    Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy
    2.
    发明授权
    Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy 有权
    嘧啶-4-基-3,4-硫酮化合物及其在治疗中的应用

    公开(公告)号:US07902361B2

    公开(公告)日:2011-03-08

    申请号:US11408463

    申请日:2006-04-21

    CPC分类号: C07D417/04 C07D417/14

    摘要: The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj′) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa′CORg′, Rf′, (CH2)rNRb′SO2Rh′, SO2NRd′Ri′, SO2NRe′(CH2)sORc′, heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg′, Rh′, Ri′ and Rj′ are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; n and s are each independently 1, 2, or 3; and Ra-n and Ra′-f′ are each independently H or alkyl. Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes.

    摘要翻译: 本发明涉及式I化合物或其药学上可接受的盐,其中R 1和R 5各自独立地为H,C(OR j')或任选被一个或多个R 6基团取代的烃基; R 2,R 3和R 4各自独立地为H,烷基或烯基,其各自可以任选被一个或多个R 7基团取代; R6和R7各自独立地为卤素,NO2,CN,(CH2)mORa,O(CH2)nORb,(CH2)pNRcRd,CF3,COORe,CONRfRg,CORh,SO3H,SO2Ri,SO2NRjRk,(CH2)qNRa'CORg' Rf',(CH2)rNRb'SO2Rh',SO2NRd'Ri',SO2NRe'(CH2)sORc',杂环烷基或杂芳基,其中所述杂环烷基和杂芳基可以任选地被一个或多个选自芳烷基,磺酰基,R m和 玉米; R'',R'',R''和R“'各自独立地选自烷基,芳基,芳烷基和杂芳基,它们各自可以被一个或多个选自卤素,OH,NO 2,NH 2 CF 3和COOH的取代基取代; m,p,q和r各自独立地为0,1,2或3; n和s各自独立地为1,2或3; 和Ra-n和Ra'-f'各自独立地为H或烷基。 本发明的其它方面涉及包含这些化合物的药物组合物及其在制备用于治疗以下一种或多种的药物中的用途:增殖性病症,病毒病症,CNS病症,中风,脱发和糖尿病。

    Stowable Arcuate Detector Array
    4.
    发明申请
    Stowable Arcuate Detector Array 有权
    可存储的弧形检测器阵列

    公开(公告)号:US20130028376A1

    公开(公告)日:2013-01-31

    申请号:US13548431

    申请日:2012-07-13

    IPC分类号: G01N23/04

    CPC分类号: G01V5/0008

    摘要: A mobile scanning system and methods for inspecting contents of a container. Multiple detector plates are arrayed along an arcuate member coupled to a conveyance with wheels, capable of road travel. A source generates high-energy penetrating radiation that irradiates each of the detector plates from a single position. The arcuate member is disposed, during the course of operation of the system, in a vertical plane. The system has one actuator for rotating the arcuate member about a horizontal pivot into a horizontal plane, and a second actuator for further rotating the arcuate member, once rotated into the horizontal plane, about a vertical pivot, so that the arcuate member is contained, for purposes of transport, entirely within a volume defined by a rectangular prism that does not extend horizontally outward from the conveyance beyond any of its wheels.

    摘要翻译: 移动扫描系统和检查容器内容物的方法。 多个检测器板沿着弓形构件排列,弓形构件联接到具有车轮的运输工具,能够行驶。 源产生从单个位置照射每个检测器板的高能穿透辐射。 在系统的操作过程中,弓形构件设置在垂直平面中。 该系统具有一个致动器,用于将弓形构件围绕水平枢轴旋转到水平平面中;以及第二致动器,用于使弓形构件一旦旋转到水平面中,围绕垂直枢轴旋转,使得弓形构件被包含, 为了运输的目的,完全在由直角棱镜限定的体积内,该矩形棱镜不会从输送机水平向外延伸超过其任何轮子。

    CONTINUOUS BAG CLOSING APPARATUS AND METHOD
    5.
    发明申请
    CONTINUOUS BAG CLOSING APPARATUS AND METHOD 失效
    连续袋封闭装置和方法

    公开(公告)号:US20050091943A1

    公开(公告)日:2005-05-05

    申请号:US10701903

    申请日:2003-11-05

    申请人: David Blake Cory Muhm

    发明人: David Blake Cory Muhm

    摘要: An packaging apparatus and method to uncuff a package assembly is disclosed. The package assembly includes a container with at least one upstanding sidewall defining an open top. A bag is disposed within the container and a top portion of the bag is folded over the at least one sidewall at the open top to define a cuff. The packaging apparatus includes a first fluid jet directed substantially upward that is configured to uncuff the top portion of the bag from the container. An automatic bag closer gathers the top portion of the bag and applies a clip to close the bag. A second fluid jet is directed substantially downward and is configured to push the top portion of the bag substantially within the container.

    摘要翻译: 公开了一种无包装组件的包装装置和方法。 包装组件包括具有限定开口顶部的至少一个直立侧壁的容器。 袋子设置在容器内,并且袋的顶部在开口顶部折叠在至少一个侧壁上以限定袖带。 包装装置包括基本向上指向的第一流体喷射,其构造成从容器中取出袋的顶部。 自动包装袋收集袋的顶部并施加夹子以关闭袋子。 第二流体射流基本向下引导,并且构造成基本上在容器内推动袋的顶部。

    Build Automation and Verification for Modular Servers
    6.
    发明申请
    Build Automation and Verification for Modular Servers 有权
    构建模块化服务器的自动化和验证

    公开(公告)号:US20080177711A1

    公开(公告)日:2008-07-24

    申请号:US12055545

    申请日:2008-03-26

    IPC分类号: G06F9/445 G06F17/30

    CPC分类号: G06F8/61 Y10S707/966

    摘要: A system and method for managing and verifying the installation of software on a modular information handling system includes a bar file database and an installation management module. The bar file database stores bar files. The bar files each are related to a component of a modular information handling system. The installation management module is able to receive a bar file and communicate with the bar file database to identify and access each bar file associated with the modular information handling system.

    摘要翻译: 用于管理和验证在模块化信息处理系统上安装软件的系统和方法包括条形文件数据库和安装管理模块。 条形文件数据库存储条形文件。 每个条形码文件都与模块化信息处理系统的组件相关。 安装管理模块能够接收条形文件并与条形文件数据库进行通信,以识别和访问与模块化信息处理系统相关联的每个条形文件。

    Markers for cyclin dependent kinase inhibitors
    7.
    发明申请
    Markers for cyclin dependent kinase inhibitors 审中-公开
    细胞周期蛋白依赖性激酶抑制剂的标记

    公开(公告)号:US20060204975A1

    公开(公告)日:2006-09-14

    申请号:US11242244

    申请日:2005-10-03

    IPC分类号: C12Q1/68 A61K31/522

    CPC分类号: C12Q1/6886 C12Q2600/136

    摘要: The present invention relates to pharmacodynamic markers for CDKIs including the candidate 2,6,9-tri-substituted purine known as roscovitine. The identity of these markers facilitates the convenient identification of roscovitine-like activity both in vitro and in vivo.

    摘要翻译: 本发明涉及CDKI的药效学标志物,其包括称为roscovitine的候选2,6,9-三取代嘌呤。 这些标记的身份有助于在体外和体内方便地鉴定类似罗素维生素的活性。

    Stowable arcuate detector array
    9.
    发明授权
    Stowable arcuate detector array 有权
    可储存的弓形探测器阵列

    公开(公告)号:US08971487B2

    公开(公告)日:2015-03-03

    申请号:US13548431

    申请日:2012-07-13

    IPC分类号: G01V5/00

    CPC分类号: G01V5/0008

    摘要: A mobile scanning system and methods for inspecting contents of a container. Multiple detector plates are arrayed along an arcuate member coupled to a conveyance with wheels, capable of road travel. A source generates high-energy penetrating radiation that irradiates each of the detector plates from a single position. The arcuate member is disposed, during the course of operation of the system, in a vertical plane. The system has one actuator for rotating the arcuate member about a horizontal pivot into a horizontal plane, and a second actuator for further rotating the arcuate member, once rotated into the horizontal plane, about a vertical pivot, so that the arcuate member is contained, for purposes of transport, entirely within a volume defined by a rectangular prism that does not extend horizontally outward from the conveyance beyond any of its wheels.

    摘要翻译: 移动扫描系统和检查容器内容物的方法。 多个检测器板沿着弓形构件排列,弓形构件联接到具有车轮的运输工具,能够行驶。 源产生从单个位置照射每个检测器板的高能穿透辐射。 在系统的操作过程中,弓形构件设置在垂直平面中。 该系统具有一个致动器,用于将弓形构件围绕水平枢轴旋转到水平平面中;以及第二致动器,用于使弓形构件一旦旋转到水平面中,围绕垂直枢轴旋转,使得弓形构件被包含, 为了运输的目的,完全在由直角棱镜限定的体积内,该矩形棱镜不会从输送机水平向外延伸超过其任何轮子。

    Drug targeting
    10.
    发明授权
    Drug targeting 失效
    药物靶向

    公开(公告)号:US07829555B1

    公开(公告)日:2010-11-09

    申请号:US09367261

    申请日:1998-02-13

    IPC分类号: A61K31/573 C07J5/00

    CPC分类号: A61K47/559

    摘要: The invention provides a method of targeting a drug to areas of hypoxic and/or ischemic tissue within the body in which the desired drug species is linked to a non-cytotoxic bioreductive carrier. Also provided by the invention are novel bioreductive conjugates comprising a non-cytotoxic bioreductive moiety with linked-thereto at least one therapeutic agent. The compounds of the invention are particularly suitable for the treatment of rheumatoid arthritis and other arthritic conditions, diabetes, atherosclerosis, stroke, sepsis, Alzheimer's disease and other neurological disorders, cancer, kidney disease, digestive diseases, liver disease, chronic periodontitis or ischemia following tissue transplantation.

    摘要翻译: 本发明提供了将药物靶向体内缺氧和/或缺血组织的区域的方法,其中所需药物物种与非细胞毒性生物还原载体连接。 本发明还提供了包含与至少一种治疗剂连接的非细胞毒性生物还原性部分的新型生物还原性缀合物。 本发明的化合物特别适用于治疗类风湿性关节炎和其他关节炎病症,糖尿病,动脉粥样硬化,中风,败血症,阿尔茨海默病和其他神经障碍,癌症,肾脏疾病,消化系统疾病,肝病,慢性牙周炎或缺血后续 组织移植。