IMIDAZO [1,2-A]PYRIDINE COMPOUNDS FOR USE IN THERAPY
    2.
    发明申请
    IMIDAZO [1,2-A]PYRIDINE COMPOUNDS FOR USE IN THERAPY 审中-公开
    咪达唑[1,2-A]吡啶化合物用于治疗

    公开(公告)号:WO2012130322A1

    公开(公告)日:2012-10-04

    申请号:PCT/EP2011/055059

    申请日:2011-03-31

    CPC classification number: C07D471/04 A61K31/496 A61K31/551 A61K45/06

    Abstract: The present invention provides novel imidazo[1,2-a]pyridine compounds that are useful in therapy of diseases and disorders. The novel compounds inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders. wherein X is CH 2 , CH 2 CH 2 or C=O; R 1 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R 1a which are identical or different; R 2 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2, 3, 4 or 5 radicals R 2a which are identical or different; R 3 is hydrogen, C 1 -C 6 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl C(O)R 4 ; where R 1a , R 2a and R 4 are as defined in the claims and the specification.

    Abstract translation: 本发明提供可用于治疗疾病和病症的新的咪唑并[1,2-a]吡啶化合物。 该新型化合物在低氧条件下抑制缺氧诱导因子(HIF)介导的转录和信号传导的活化。 一方面,本发明的化合物可用于制备用于治疗或预防选自以下的疾病或病症的药物:炎性疾病,过度增殖性疾病或病症,缺氧相关病理学和 一种以血管过度为特征的疾病。 还提供了包含本发明化合物和第二治疗剂或辐射的药物组合物,其可用于治疗或预防所述疾病或病症。 其中X是CH 2,CH 2 CH 2或C = O; R 1是苯基或C键的单环5或6元杂芳基,其中苯基和单环5或6元杂芳基是未取代的或带有相同或不同的1,2,3,4或5个基团R 1a; R 2是苯基或C结合的单环5或6元杂芳基,其中苯基和单环5或6元杂芳基是未取代的或带有相同或不同的1,2,3,4或5个基团R2a; R 3是氢,C 1 -C 6烷基,C 1 -C 4烷氧基-C 1 -C 4烷基,氟化C 1 -C 2烷基C(O)R 4; 其中R1a,R2a和R4如权利要求和说明书中所定义。

    DETECTION OF REINFORCEMENT METAL CORROSION
    4.
    发明申请
    DETECTION OF REINFORCEMENT METAL CORROSION 审中-公开
    检测加固金属腐蚀

    公开(公告)号:WO2011153628A1

    公开(公告)日:2011-12-15

    申请号:PCT/CA2011/000679

    申请日:2011-06-08

    CPC classification number: G01N17/04 B60L1/00 H03H1/00 H03H3/00

    Abstract: Systems, devices, and/or methods for use in detection of reinforcement metal corrosion within material, such as concrete, are described. The systems, devices, and/or methods may use a passive sensor located within the material and an interrogator located outside of the material that may be used to interrogate the passive sensor and to receive a signal from the passive sensor representative of corrosion potential of reinforcement metal.

    Abstract translation: 描述了用于检测材料(例如混凝土)中的钢筋金属腐蚀的系统,装置和/或方法。 系统,装置和/或方法可以使用位于材料内的无源传感器和位于材料外部的询问器,所述询问器可用于询问无源传感器并从被动传感器接收代表加固腐蚀电位的信号 金属。

    BICYCLIC 2,3-DIHYRDOBENZAZINE COMPOUNDS FOR USE IN THERAPY
    5.
    发明申请
    BICYCLIC 2,3-DIHYRDOBENZAZINE COMPOUNDS FOR USE IN THERAPY 审中-公开
    双酚2,3-二羟基苯并嗪化合物用于治疗

    公开(公告)号:WO2012130306A1

    公开(公告)日:2012-10-04

    申请号:PCT/EP2011/054959

    申请日:2011-03-30

    Abstract: The present invention provides novel 2,3-dihydrobenzazine compounds of formula (I) and to their salts. The compounds inhibit cell proliferation and cell division and they also inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions (I) wherein X is O or S(=O)n; n is 0, 1 or 2; R 1 is an optionally substituted C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring having either 1, 2 or 3 nitrogen atoms as heteroatom ring members or 1 oxygen or 1 sulfur atom and 0, 1 or 2 nitrogen atoms as heteroatom ring members, and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring having 1, 2 or 3 heteroatom ring members selected from oxygen, sulfur and nitrogen, where sulfur atoms, if present, may be present as S, S(O) or S(O) 2 and where the saturated or unsaturated carbocyclic or heterocyclic second ring may also have 1 or 2 carbonyl groups or thiocarbonyl groups as ring members; R 2 is an optionally substituted aromatic radical selected from phenyl, C-bound mono- cyclic 5- or 6-membered heteroaryl or C-bound bicyclyl comprising a first ring which is a benzene ring or a 5- or 6-membered heteroaromatic ring and a second ring, which is fused to the first ring, where the second ring is a 5-, 6- or 7-membered carbocyclic ring or a 5-, 6- or 7-membered heterocyclic ring.

    Abstract translation: 本发明提供新的式(I)的2,3-二氢苯并嗪化合物及其盐。 这些化合物抑制细胞增殖和细胞分裂,并且还在低氧条件下(I)抑制缺氧诱导因子(HIF)介导的转录和信号传导的活化,其中X是O或S(= O)n; n为0,1或2; R1是任选取代的C结合的双环,其包含第一环,其是苯环或具有1,2或3个氮原子作为杂原子环成员或1个氧或1个硫原子的5或6元杂芳环和0 ,1或2个氮原子作为杂原子环成员,和第二个环,其与第一个环稠合,其中第二个环是5-,6-或7-元碳环或5-,6-或7 含有1,2或3个选自氧,硫和氮的杂原子环成员的杂环,其中硫原子(如果存在)可以S,S(O)或S(O)2存在,其中饱和或不饱和的 碳环或杂环第二环也可以具有1或2个羰基或硫代羰基作为环成员; R2是任选取代的芳基,其选自苯基,C-结合的单环5-或6-元杂芳基或C结合的双环,其包含第一环,其是苯环或5-或6-元杂芳环, 第二个环与第一个环融合,其中第二个环是5-,6-或7-元的碳环或5-,6-或7-元杂环。

    MEASURING STRAIN IN A STRUCTURE (BRIDGE) WITH A (TEMPERATURE COMPENSATED) ELECTROMAGNETIC RESONATOR (MICROWAVE CAVITY)
    8.
    发明申请
    MEASURING STRAIN IN A STRUCTURE (BRIDGE) WITH A (TEMPERATURE COMPENSATED) ELECTROMAGNETIC RESONATOR (MICROWAVE CAVITY) 审中-公开
    用A(温度补偿)电磁谐振器(微波炉)测量结构(桥)中的应变

    公开(公告)号:WO2004003500A1

    公开(公告)日:2004-01-08

    申请号:PCT/CA2003/000952

    申请日:2003-06-26

    Abstract: The system (10) comprises a sensor (18) 90x90x90x30 mm as an electromagnetic microwave cavity (20) with a coupler (22) with a wire (40) and an antenna (42). Cavity (20) produces a response signal (26) in response to an interrogation signal (24) from interrogator (16). Sensor (18) is coupled to a structure (14) to allow a strain to alter the resonance properties. 3.6 GHz is used with a detection of a 2.5 kHz change. If not temperature via strain is detected a mechanical amplifier is used with cavity (20) for temperature compensation. Continuous or intermittent narrowband signals are used as interrogation signals (24). Used with bridges for structural health monitoring. Also for aircrafts, dams, buildings, vehicles.

    Abstract translation: 系统(10)包括具有耦合器(22)和电线(40)和天线(42)的电磁微波空腔(20)的90×90×90×30mm的传感器(18)。 腔(20)响应于来自询问器(16)的询问信号(24)产生响应信号(26)。 传感器(18)耦合到结构(14)以允许应变改变谐振特性。 使用3.6 GHz,检测到2.5 kHz的变化。 如果没有检测到温度通过应变,机械放大器与空腔(20)一起用于温度补偿。 连续或间歇的窄带信号被用作询问信号(24)。 与桥梁一起用于结构健康监测。 也适用于飞机,水坝,建筑物,车辆。

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