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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。
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公开(公告)号:US08486967B2
公开(公告)日:2013-07-16
申请号:US13023563
申请日:2011-02-09
申请人: Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人: Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号: A01N43/42 , A61K31/44 , C07D513/02 , C07D515/02
CPC分类号: C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要: The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus 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: 本发明涉及下式的化合物,其中杂芳基I,杂芳基II,R 1,R 2,R 3,R 4,m,n和o如说明书中所定义或其药学活性的酸加成盐。 式I化合物是淀粉样蛋白β的调节剂,因此可用于治疗或预防与脑中β-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,遗传性 脑出血伴淀粉样变性,荷兰型(HCHWA-D),多发性梗死性痴呆,痴呆和唐氏综合征。
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公开(公告)号:US20120225884A1
公开(公告)日:2012-09-06
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: A61K31/4985 , C07D451/04 , C07D487/04 , A61P25/00 , A61K31/437 , A61K31/506 , A61K31/519 , A61P25/28 , C07D471/04 , A61K31/444
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。
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公开(公告)号:US20110201605A1
公开(公告)日:2011-08-18
申请号:US13023563
申请日:2011-02-09
申请人: Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人: Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号: A61K31/5365 , C07D471/04 , A61K31/437 , C07D401/14 , A61K31/454 , C07D403/14 , A61K31/506 , C07D413/14 , A61K31/5377 , C07D498/04 , A61P25/28
CPC分类号: C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要: The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus 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: 本发明涉及下式的化合物,其中杂芳基I,杂芳基II,R 1,R 2,R 3,R 4,m,n和o如说明书中所定义或其药学活性的酸加成盐。 式I的化合物是淀粉样蛋白β的调节剂,因此可用于治疗或预防与脑中淀粉样蛋白沉积相关的疾病,特别是阿尔茨海默病和其它疾病如脑淀粉样血管病, 遗传性脑出血伴淀粉样变性,荷兰型(HCHWA-D),多发性梗死性痴呆,痴呆和唐氏综合症。
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公开(公告)号:US20110190269A1
公开(公告)日:2011-08-04
申请号:US13011951
申请日:2011-01-24
申请人: Karlheinz Baumann , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人: Karlheinz Baumann , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号: A61K31/55 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61K31/4985 , A61K31/5377 , A61K31/5025 , A61K31/538
CPC分类号: C07D471/04 , C07D487/04 , C07D498/04
摘要: The invention relates to compounds of formula wherein R1, R1′, R2, R3, n, A, and hetaryl are defined herein 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: 本发明涉及下式的化合物,其中R 1,R 1',R 2,R 3,n,A和杂芳基在本文中定义或其药学活性的酸加成盐。 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。
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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.
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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
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。
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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。
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公开(公告)号:US08227461B2
公开(公告)日:2012-07-24
申请号:US12766202
申请日:2010-04-23
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。
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公开(公告)号:US08173652B2
公开(公告)日:2012-05-08
申请号:US12704548
申请日:2010-02-12
IPC分类号: A61K31/5377 , A61K31/42 , A61K31/454 , C07D413/06 , C07D413/14
CPC分类号: C07D261/18 , C07D413/14 , C07D417/12 , C07D487/10
摘要: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
摘要翻译: 本发明涉及式I的异恶唑 - 异恶唑和异恶唑 - 异噻唑,对GABA Aα5受体具有亲和性和选择性,其制备方法,含有它们的药物组合物及其作为认知增强剂的用途或用于治疗和/或预防性治疗 认知障碍如阿尔茨海默病。
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