PHARMACEUTICAL COMBINATIONS
    42.
    发明申请
    PHARMACEUTICAL COMBINATIONS 有权
    药物组合

    公开(公告)号:US20100179145A1

    公开(公告)日:2010-07-15

    申请号:US12445180

    申请日:2007-10-12

    CPC classification number: A61K31/403 A61K31/4035 A61K45/06 A61K2300/00

    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.

    Abstract translation: 本发明提供包含(或基本上由)一种或多种辅助化合物和式(I)化合物或其盐,互变异构体,溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1,R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - (O)n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基,其中多达5个环成员是选自氧,氮和硫的杂原子。 这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶抑制剂的活性。

    COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S
    43.
    发明申请
    COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S 审中-公开
    用于抑制CDKS和GSK'S的吡唑衍生物的组合

    公开(公告)号:US20100021420A1

    公开(公告)日:2010-01-28

    申请号:US12373827

    申请日:2007-07-13

    CPC classification number: A61K31/454 A61K45/06 A61K2300/00

    Abstract: A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NR9(C═O) or 0(C═O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 to 3 carbon atoms; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or an optionally substituted C1-8 hydrocarbyl group wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; and (b) a compound of formula (I′″) or salts, tautomers, solvates and N-oxides thereof: wherein R1 is 2,6-dichlorophenyl; R2a and R2b are both hydrogen; and R3 is a group: formula (A) where R4 is C1-4 alkyl.

    Abstract translation: 包含(a)式(O)化合物或其盐或互变异构体或其N-氧化物或溶剂合物的组合; 其中X为R 1 -A-NR 4 - 或5或6元碳环或杂环; A为键,SO 2,C-O,NR 9(C-O)或O(C-O),其中R 9为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是1〜3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选取代的C 1-8烃基,其中烃基中的1或2个碳原子可以任选地被选自O,S,NH,SO,SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基; 或任选被卤素,羟基或C 1-4烷氧基取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; R4是氢或任选被卤素,羟基或C 1-4烷氧基取代的C 1-4烃基; 和(b)式(I“)的化合物或其盐,互变异构体,溶剂化物和N-氧化物:其中R1是2,6-二氯苯基; R2a和R2b都是氢; 并且R 3是下式:其中R 4是C 1-4烷基的式(A)。

    Pharmaceutical Compounds
    44.
    发明申请
    Pharmaceutical Compounds 审中-公开
    药物化合物

    公开(公告)号:US20090036435A1

    公开(公告)日:2009-02-05

    申请号:US11814461

    申请日:2006-01-20

    Abstract: The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NR9(C═O) or 0(C═O) wherein R9 is hydrogen or Ĉhydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, Ĉhydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; Ĉalkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a Ĉhydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

    Abstract translation: 本发明提供了辅助剂和具有式(O)的化合物或其盐或互变异构体或N-氧化物或溶剂合物的组合: 其中所述辅助剂选自:单克隆抗体,烷化剂,抗癌剂,另外的CDK抑制剂和激素,激素激动剂,激素拮抗剂或激素调节剂; X是R1-A-NR4-基团或5或6元碳环或杂环; A是键,SO 2,C-O,NR 9(C-O)或O(C-O),其中R 9是氢或任选被羟基或C 1-4烷氧基取代的羟基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素(例如氟),羟基,羟基氧基,氨基,单 - 或二-C 1-4烃基氨基的取代基取代的C 1-8烃基和具有3-12个环成员的碳环或杂环基 并且其中烃基中的1或2个碳原子可以任选地被选自O,S,NH,SO,SO 2的原子或基团取代; R2是氢; 卤素; Ĉ烷氧基(如甲氧基); 或任选被卤素(例如氟),羟基或C 1-4烷氧基(例如甲氧基)取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素(例如氟),羟基或C 1-4烷氧基(例如甲氧基)取代的烃基。

    Virtual beverage bar design and analysis system
    46.
    发明申请
    Virtual beverage bar design and analysis system 有权
    虚拟饮料酒吧设计与分析系统

    公开(公告)号:US20060080349A1

    公开(公告)日:2006-04-13

    申请号:US10538596

    申请日:2003-12-12

    Inventor: Thomas Thompson

    CPC classification number: G06Q10/04 G06Q10/043 G06Q10/06

    Abstract: A system, method and computer program product for planning an arrangement of beverage equipment on a virtual surface or counter. The system allows a user to create a virtual surface of chosen dimension (32) and then select one or more beverage machines (36) to place on that surface while verifying that there is sufficient open space for the selected beverage machine (38). Also disclosed is a method of determining projected profit (48) based on the selection of beverage machines, entered values related to costs, and entered values related to serving size and pricing. The system reports on projected profits and/or how long the equipment needs to be operated to pay off the equipment's cost.

    Abstract translation: 一种用于在虚拟表面或计数器上规划饮料设备的布置的系统,方法和计算机程序产品。 该系统允许用户创建所选尺寸的虚拟表面(32),然后选择一个或多个饮料机(36)放置在该表面上,同时验证所选择的饮料机(38)是否具有足够的开放空间。 还公开了一种基于饮料机的选择,与成本相关的输入值以及与服务大小和定价相关的输入值来确定预计利润(48)的方法。 系统报告设备需要运行的预计利润和/或设备的成本。

    Wettable polyester fibers and fabrics
    47.
    发明申请
    Wettable polyester fibers and fabrics 失效
    可湿性聚酯纤维和织物

    公开(公告)号:US20060020066A1

    公开(公告)日:2006-01-26

    申请号:US11185993

    申请日:2005-07-20

    Abstract: The present invention is aimed at a method of providing wettability to polyester fibers or filaments, to woven or nonwoven fabrics made therefrom and to resultant articles of manufacture. The method comprises melt extruding a mixture comprising a polyester and one or more alkyl metal sulfonates where the metal is Na, Li or K and the alkyl is straight or branched chain alkyl of 12 to 15 carbon atoms, or is straight or branched chain alkenyl of 12 to 18 carbon atoms. The alkyl metal sulfonates are present from about 2% to about 5% by weight based on the weight of the polyester. A post treatment step such as an alkaline treatment step is not included. The melt extrusion mixtures do not include certain additives such as polyoxyalkylene compounds, alkylmonoethonolamide compounds, alkyldiethanolamine compounds and polyetheramide compounds.

    Abstract translation: 本发明的目的在于提供对聚酯纤维或长丝的润湿性,由其制成的织造或非织造织物以及所得制品。 该方法包括将包含聚酯和一种或多种烷基金属磺酸盐的混合物熔融挤出,其中金属是Na,Li或K,并且烷基是12至15个碳原子的直链或支链烷基,或是直链或支链链烯基 12至18个碳原子。 基于聚酯的重量,烷基金属磺酸盐的存在量为约2重量%至约5重量%。 不包括碱处理步骤等后处理步骤。 熔融挤出混合物不包括某些添加剂,例如聚氧化烯化合物,烷基一乙醇胺化合物,烷基二乙醇胺化合物和聚醚酰胺化合物。

    Zipper sheathing tie down
    48.
    发明授权
    Zipper sheathing tie down 失效
    拉链护套系紧

    公开(公告)号:US06415575B1

    公开(公告)日:2002-07-09

    申请号:US09389677

    申请日:1999-09-02

    Inventor: Thomas Thompson

    CPC classification number: E04C3/12 E04B1/2608 E04H9/14

    Abstract: An improved metal connector that securely ties together sheathing and underlying structural members on a building to prevent hurricane and earthquake damage. The connector has alternating sheathing tabs for securing adjacent sheathing edges. Connected underneath the sheathing tabs, a rib separates the sheathing and correctly spaces each adjoining sheet with a slight gap to avoid buckling. Below the rib, rafter webs alternate with the sheathing tabs to prevent movement of the sheathing and rafter. The large surface area and precise nail holes on the sheathing tab avoids sheathing splitting and assures correct attachment to the underlying structural member.

    Abstract translation: 一种改进的金属连接器,将建筑物上的护套和基础结构构件牢固地连接在一起,以防止飓风和地震损坏。 连接器具有用于固定相邻护套边缘的交替护套。 连接在护套的下方,肋骨分开护套,并以相当的间隙将每个相邻的片材正确地隔开以避免屈曲。 在肋下方,椽腹板与护套接合,以防止护套和椽子移动。 护套上的大表面积和精确的钉孔避免了护套分裂,并确保与底层结构构件的正确连接。

    Resilient scraping blade attachment
    49.
    发明授权
    Resilient scraping blade attachment 失效
    弹性刮刀附件

    公开(公告)号:US06315056B1

    公开(公告)日:2001-11-13

    申请号:US09628000

    申请日:2000-07-28

    CPC classification number: E01H1/105 E02F3/8152 Y10S37/903

    Abstract: The resilient scraping blade attachment is provided that includes an attachment hook-up assembly adapted to be mounted on a vehicle. The attachment hook-up assembly includes an elongated central support member and a vehicle interface component. In addition, the attachment hook-up assembly includes a pair of diagonal supports that link the central support member to the vehicle interface component. A mounting plate is secured at an end of the central support member. A resilient blade assembly is attached to the attachment hook-up assembly by means of a bearing bracket and bearing means. The resilient blade assembly includes an elongated blade mounting channel having a pair of resilient blades mounted thereon. The resilient blade assembly includes extension blades that may be mounted at the ends of the blade mounting channel in order to increase the effective width of the resilient blade assembly. The extension blades may be contoured to approximate different surfaces such as a roadside curb. A hydraulic cylinder is mounted on the attachment hook-up assembly and includes a piston that is mounted on the resilient blade assembly to control and pivot the resilient blade assembly. Angle limiter chains are provided to limit the pivoting movement of the resilient blade assembly.

    Abstract translation: 提供弹性刮刀附件,其包括适于安装在车辆上的附接挂钩组件。 附件连接组件包括细长的中央支撑构件和车辆接口部件。 此外,附件连接组件包括将中央支撑构件连接到车辆接口部件的一对对角支架。 安装板固定在中央支撑件的一端。 弹性叶片组件借助于轴承支架和轴承装置附接到附件挂钩组件。 弹性叶片组件包括细长的叶片安装通道,其具有安装在其上的一对弹性叶片。 弹性叶片组件包括可以安装在叶片安装通道的端部处的延伸叶片,以便增加弹性叶片组件的有效宽度。 延伸叶片可以被轮廓化以近似不同的表面,例如路边路边缘。 液压缸安装在附件挂钩组件上并且包括安装在弹性叶片组件上以控制和枢转弹性叶片组件的活塞。 提供角度限制器链以限制弹性叶片组件的枢转运动。

    Hurricane/storm protection for windows/doors
    50.
    发明授权
    Hurricane/storm protection for windows/doors 失效
    飓风/风雨保护窗/门

    公开(公告)号:US06205713B1

    公开(公告)日:2001-03-27

    申请号:US09087728

    申请日:1998-05-29

    CPC classification number: E06B9/02

    Abstract: A shutter for withstanding hurricane wind and pressures has permanent hardware attached to a structure and a temporary shutter that can be stored until needed. Hardware consists of brackets mounted above or below a window and sliding latches at the edges of the window. Sliding latches have a key way for a carriage bolt to enter and attach. Brackets allow a shutter that has attached hinges to latch and pivot around a bridge. The shutter can be made from any material. Hinges are attached to shutter and are able to be latched and pivoted on the brackets mounted on the house. The shutter can also be swung up to protect a high window. The shutter is swung over the window and locked down to sliding latches and carriage bolts with wing nuts through holes in shutter.

    Abstract translation: 用于承受飓风和压力的快门具有连接到结构的永久硬件和可以存储直到需要的临时快门。 硬件由安装在窗户上方或下方的支架组成,并在窗口边缘滑动闩锁。 滑动闩锁具有滑架螺栓进入和连接的关键方式。 支架允许具有附接铰链的快门来锁定并围绕桥枢转。 快门可以由任何材料制成。 铰链连接到挡板上,并且能够在安装在房屋上的支架上锁定和枢转。 快门也可以向上摆动以保护高窗户。 快门在窗口上摆动,并锁定到滑动闩锁和托架螺栓,带有螺母通过快门孔。

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