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    Quinazoline derivatives as VEGF inhibitors
    1.
    发明申请
    Quinazoline derivatives as VEGF inhibitors 审中-公开
    喹唑啉衍生物作为VEGF抑制剂

    公开(公告)号：US20070265286A1

    公开(公告)日：2007-11-15

    申请号：US11642979

    申请日：2006-12-21

    申请人： Andrew Thomas ,  Elaine Stokes ,  Laurent Hennequin

    发明人： Andrew Thomas ,  Elaine Stokes ,  Laurent Hennequin

    IPC分类号： A61K31/517 ,  A61P19/02 ,  A61P3/00 ,  A61P35/00 ,  A61P37/00 ,  C07D239/94

    CPC分类号： C07D401/12

    摘要： The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中m为1至3的整数; R 1表示卤代或C 1-3烷基; X 1表示-O-; R 2选自以下三个基团之一：1）C 1-5烷基R 3（其中R 3，R 3，R 3， SUP>是可以带有一个或两个选自羟基，卤代，C 1-4 - 烷基，C 1-4 - 羟基烷基和C 1-4烷氧基; 2）C 2-5烯基R 3（其中R 3如上定义）; 3）C 2-5炔基R 3（其中R 3如上定义）; 并且其中任何烷基，烯基或炔基可以具有一个或多个选自羟基，卤代和氨基的取代基; 及其盐; 其制备方法，含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物。 式（I）化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

    COMPRESSION GARMENT WITH AN INTEGRATED RECEPTACLE
    2.
    发明申请
    COMPRESSION GARMENT WITH AN INTEGRATED RECEPTACLE 有权

    公开(公告)号：US20220287392A1

    公开(公告)日：2022-09-15

    申请号：US17693050

    申请日：2022-03-11

    申请人： Andrew Thomas

    发明人： Andrew Thomas

    IPC分类号： A41D13/00

    摘要： A compression garment with an integrated receptacle that provides liquid to a user is disclosed. The compression garment has at least one exterior cavity for receiving a receptacle and at least one tube channel with tube channel openings for receiving the tube from the exterior cavity and to route the tube across the chest of a user and into a webbing loop. An o-ring that locks a breakable foil seal in place is provided when a spout is connected to the neck element and the spout secures the liquid in the reservoir by compressing the o-ring on the foil seal. A grab ridge is then used to release the reservoir from the cavity of the compression garment as desired by the user.

    Packet based DDS minimizing mathematical and DAC noise
    3.
    发明授权
    Packet based DDS minimizing mathematical and DAC noise 有权
    基于分组的DDS最小化数学和DAC噪声

    公开(公告)号：US09292035B2

    公开(公告)日：2016-03-22

    申请号：US14163600

    申请日：2014-01-24

    申请人： Andrew Thomas

    发明人： Andrew Thomas

    IPC分类号： G06F1/02 ,  G06F1/03 ,  G01N27/90

    CPC分类号： G06F1/0321 ,  G01N27/9046 ,  G06F1/022 ,  G06F17/5045

    摘要： Disclosed are a method of and an apparatus devising a packet based DDS circuitry for performing packet based a direct digital synthesizing (DDS) function within an electronic testing instrument. The circuitry comprising a DDS logic circuit configured to execute direct digital syntheses on a plurality of consecutive packets of sine-like waves, each packet having a length of a period precisely chosen such that the sine wave at the end of one packet matches up with the sine wave at the start of the immediate subsequent packet. Also disclosed is an eddy current testing circuitry using multiple outputs of the single packet based DDS, one of the output is used in a circuit producing reference signals approximating the response signals. With the usage of the packet based DDS, the reference signal can be highly effective in nulling the unchanging portion of the response signals.

    摘要翻译： 公开了一种设计基于分组的DDS电路的方法和装置，用于基于电子测试仪器内的直接数字合成（DDS）功能执行分组。 该电路包括DDS逻辑电路，该DDS逻辑电路经配置以在正弦波的多个连续分组上执行直接数字合成，每个分组具有精确选择的周期的长度，使得一个分组结束时的正弦波与 正弦波在即时后续数据包的开始。 还公开了使用基于单个分组的DDS的多个输出的涡流测试电路，其中一个输出用于产生近似响应信号的参考信号。 通过使用基于分组的DDS，参考信号可以在使响应信号的不变部分归零时非常有效。

    Bridged piperidine derivatives
    4.
    发明授权
    Bridged piperidine derivatives 有权
    桥连哌啶衍生物

    公开(公告)号：US08703763B2

    公开(公告)日：2014-04-22

    申请号：US13405404

    申请日：2012-02-27

    申请人： Karlheinz Baumann ,  Luke Green ,  Anja Limberg ,  Thomas Luebbers ,  Andrew Thomas

    发明人： Karlheinz Baumann ,  Luke Green ,  Anja Limberg ,  Thomas Luebbers ,  Andrew Thomas

    IPC分类号： A01N43/00 ,  A61K31/55 ,  C07D413/00 ,  C07D415/00 ,  C07D417/00 ,  C07D419/00

    CPC分类号： C07D451/04

    摘要： The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

    摘要翻译： 本发明涉及式I化合物，杂芳基I，杂芳基II，R 1，R 2，R 3，Y，m和o的化合物或其药物活性酸加成盐。 本发明式I化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病如脑 淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。

    1,2,3-triazole-imidazole compounds
    5.
    发明授权
    1,2,3-triazole-imidazole compounds 有权
    1,2,3-三唑 - 咪唑化合物

    公开(公告)号：US08466181B2

    公开(公告)日：2013-06-18

    申请号：US13309589

    申请日：2011-12-02

    申请人： Andrew Thomas

    发明人： Andrew Thomas

    IPC分类号： C07D249/00

    CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D491/107

    摘要： The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) wherein X, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention provides a method for the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutic agents.

    摘要翻译： 本发明涉及式（I）的新型1,2,3-三唑 - 咪唑化合物，其中X，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。 本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。 此外，本发明提供了制备式（I）化合物的方法，包含它们的药物组合物及其作为治疗剂的用途。

    Isoxazoles
    6.
    发明授权
    Isoxazoles 有权
    异恶唑

    公开(公告)号：US08227461B2

    公开(公告)日：2012-07-24

    申请号：US12766202

    申请日：2010-04-23

    申请人： Roland Jakob-Roetne ,  Matthew C. Lucas ,  Andrew Thomas

    发明人： Roland Jakob-Roetne ,  Matthew C. Lucas ,  Andrew Thomas

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/4439 ,  C07D417/14 ,  C07D413/14 ,  C07D401/12

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.

    摘要翻译： 本发明涉及式I的新型异恶唑衍生物，其中X，R 1，R 2，R 3，R 4和R 5如本文所述，以及其药学上可接受的盐和酯。 本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。 此外，本发明涉及制备式I的活性化合物，含有它们的药物组合物及其作为药物的用途。

    Isoxazolo-pyrazine derivatives
    8.
    发明授权
    Isoxazolo-pyrazine derivatives 有权
    异恶唑并吡嗪衍生物

    公开(公告)号：US07902201B2

    公开(公告)日：2011-03-08

    申请号：US12788338

    申请日：2010-05-27

    申请人： Bernd Buettelmann ,  Roland Jakob-Roetne ,  Henner Knust ,  Andrew Thomas

    发明人： Bernd Buettelmann ,  Roland Jakob-Roetne ,  Henner Knust ,  Andrew Thomas

    IPC分类号： A61K31/4965

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A α5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of the present invention are inverse agonists of GABAAα5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.

    摘要翻译： 本发明涉及异恶唑并吡嗪衍生物及其药学上可接受的盐，其对GABA Aα5受体结合位点具有亲和力和选择性，其制备和含有它们的药物组合物。 本发明的化合物是GABAAα5的反向激动剂。 本发明还涉及增强认知和治疗认知障碍如阿尔茨海默病的方法。