CB1 receptor modulators
    1.
    发明授权

    公开(公告)号:US08124634B2

    公开(公告)日:2012-02-28

    申请号:US12519432

    申请日:2007-12-17

    Abstract: Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is (i) a bond, or (ii) —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* or —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q1-A4-[Q2]w- wherein Q1, A4 Q2 and w are as defined in the specification; and R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.

    FLUID DISPENSING APPARATUS AND METHOD
    2.
    发明申请
    FLUID DISPENSING APPARATUS AND METHOD 有权
    流体分配装置和方法

    公开(公告)号:US20100181343A1

    公开(公告)日:2010-07-22

    申请号:US12663145

    申请日:2008-06-09

    Abstract: A fluid dispenser contains and dispenses metered amounts of fluid, and in some embodiments comprises a reservoir for containing fluid; a chamber positioned substantially within the reservoir for containing a quantity of fluid; and a piston moveable within the chamber in a first direction to draw fluid into the chamber from the reservoir, and movable in a second direction to discharge a metered amount of fluid from the chamber. A user-manipulatable control can be coupled to the piston to move the piston with respect to the chamber, and in some cases to select the desired metered amount of fluid to be dispensed. Also, a pawl can be used to selectively permit and inhibit movement of the piston in the first and/or second directions to prevent partial doses from being dispensed from the fluid dispenser.

    Abstract translation: 流体分配器包含并分配计量的流体,并且在一些实施例中包括用于容纳流体的储存器; 基本上位于储存器内的腔室,用于容纳一定量的流体; 以及活塞,其在所述腔室内沿第一方向移动,以将流体从所述储存器吸入所述腔室中,并且可在第二方向上移动以从所述腔室排出计量的流体。 用户可操纵的控制可以联接到活塞以相对于腔室移动活塞,并且在一些情况下选择要分配的所需计量量的流体。 而且,可以使用棘爪来选择性地允许和抑制活塞在第一和/或第二方向上的运动,以防止从流体分配器分配部分剂量。

    Novel compounds
    3.
    发明申请
    Novel compounds 审中-公开
    新型化合物

    公开(公告)号:US20060223809A1

    公开(公告)日:2006-10-05

    申请号:US11447343

    申请日:2006-06-06

    CPC classification number: C07D495/04

    Abstract: The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.

    Abstract translation: 本发明涉及式(I)的噻吩并哒嗪酮:其中:R 1是C 1-6烷基,C 2-6链烯基或C 任选被C 1-6烷基取代的,任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G,其中G是含有氮原子的5-或6-元环,和选自氧和/ 硫邻近氮,并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5,其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮,氧和硫的杂原子的5至10元单环或双环芳族环系统,所述环系统如上所述被任选地取代 在本说明书及其药学上可接受的盐和溶剂化物中。 还描述了其制备方法,含有它们的药物组合物及其在治疗中的用途,特别是在调节自身免疫疾病中。

    SPORTS PERFORMANCE TESTING AND TRAINING SYSTEMS, DEVICES AND METHODS
    6.
    发明申请
    SPORTS PERFORMANCE TESTING AND TRAINING SYSTEMS, DEVICES AND METHODS 有权
    运动性能测试和训练系统,设备和方法

    公开(公告)号:US20160220864A1

    公开(公告)日:2016-08-04

    申请号:US14609479

    申请日:2015-01-30

    Abstract: A method for collecting performance test data during a performance test of an athlete from timing devices associated with a performance test includes automatically receiving an electronic time stamp message from each of the timing devices, each electronic time stamp message incorporating a time stamp generated by the timing device in response to entering into a triggered state during the performance test; and automatically inserting time data corresponding to the received time stamps into respective fields of an electronic performance test record associated with the unique athlete identifier. A system for collecting performance test data includes a plurality of timing devices each configured to generate one or more electronic time stamp messages each incorporating a time stamp generated in response to entering into a triggered state during a performance test; a synchronizing device configured to periodically transmit electronic synchronize instructions to the timing devices to synchronize the timing devices; and a control device configured to receive the electronic time stamp messages from the timing devices and to insert time data corresponding to the time stamps into respective fields of performance test records.

    Abstract translation: 在与性能测试相关的定时设备的运动员的性能测试期间收集性能测试数据的方法包括:从每个定时设备自动接收电子时间戳消息,每个电子时间戳消息包含由定时产生的时间戳 响应于在性能测试期间进入触发状态的装置; 并且将与所接收的时间戳相对应的时间数据自动插入到与所述唯一运动员标识符相关联的电子演奏测试记录的相应字段中。 用于收集性能测试数据的系统包括多个定时设备,每个定时设备被配置为生成一个或多个电子时间戳消息,每个电子时间戳消息包含响应于在性能测试期间进入触发状态而产生的时间戳; 同步装置,被配置为周期性地向所述定时装置发送电子同步指令以同步所述定时装置; 以及控制装置,被配置为从定时装置接收电子时间戳消息,并将对应于时间戳的时间数据插入到性能测试记录的各个字段中。

    Crystalline forms of 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine
    8.
    发明申请
    Crystalline forms of 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine 审中-公开
    4-(2-氟苯基)-6-甲基-2-(哌嗪-1-基)噻吩并[2,3-d]嘧啶的结晶形式

    公开(公告)号:US20070254891A1

    公开(公告)日:2007-11-01

    申请号:US11728947

    申请日:2007-03-27

    CPC classification number: C07D495/04

    Abstract: The present invention is directed to novel crystalline forms of 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine salts, including 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine hydrochloride crystalline forms. The present invention is also directed to compositions including such crystalline forms and methods for making and using such crystalline forms, e.g., in the treatment of gastrointestinal and/or genitourinary disorders.

    Abstract translation: 本发明涉及4-(2-氟苯基)-6-甲基-2-(哌嗪-1-基)噻吩并[2,3-d]嘧啶盐的新结晶形式,包括4-(2-氟苯基) -6-甲基-2-(哌嗪-1-基)噻吩并[2,3-d]嘧啶盐酸盐结晶形式。 本发明还涉及包含这种结晶形式的组合物和用于制备和使用这种结晶形式的方法,例如用于治疗胃肠道和/或泌尿生殖系统疾病。

    Compounds
    9.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号:US06342601B1

    公开(公告)日:2002-01-29

    申请号:US09214755

    申请日:1999-01-12

    CPC classification number: C07D487/04 C07D491/04 C07D495/04

    Abstract: The invention provides certain pyrrolo-, thieno-, furano- and pyrazolo-[3,4-d]pyridazinones, processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.

    Abstract translation: 本发明提供某些吡咯并噻吩并呋喃并吡唑并[3,4-d]哒嗪酮,其制备方法,含有它们的药物组合物,制备药物组合物的方法和涉及其用途的治疗方法。

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