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    • 92. 发明申请
    • INDOLINE SCAFFOLD SHP-2 INHIBITORS AND CANCER TREATMENT METHOD
    • INDOLINE SCAFFLE SHP-2抑制剂和癌症治疗方法
    • US20110190315A1
    • 2011-08-04
    • US13055113
    • 2009-07-21
    • Jie WuNicholas J. LawrenceSaid M. Sebti
    • Jie WuNicholas J. LawrenceSaid M. Sebti
    • A61K31/496C07D403/12C12N5/071C12N5/09A61P35/00A61P35/02
    • C07D405/06C07D209/08C07D215/36
    • The subject invention concerns methods and compounds for inhibiting Shp2. In one embodiment, a compound of the invention has a chemical structure as shown in formula I or II: wherein X, Y, and Z are independently N or S; R1 is cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, any of which can be optionally substituted with one or more of halogen; alkyl; heteroalkyl; —COOH; —C(R3)3, wherein R3 can independently be any of —H or halogen; or —OR4, wherein R4 can be any of H, alkyl, or heteroalkyl; R2 is alkyl, alkylcarbonyl, heteroalkylcarbonyl, aryl, arylcarbonyl, heterocycloalkylcarbonyl, cycloalkylcarbonyl, or —C(O)NR6R7, any of which can be optionally substituted with one or more of halogen; alkyl; heteroalkyl; carbonyl; —OR4, wherein R4 can be —H, alkyl, or heteroalkyl; —OH; —C(R3)3, wherein R3 can independently be any of —H or halogen; aryl, which can be substituted with one or more of halogen or —OR4; heterocycloalkyl; or —C(O)OR5, wherein R5 can be —H or alkyl; R6 and R7 are independently —H, alkyl, heteroalkyl, aryl, or heteroaryl; and R′ is H or alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
    • 本发明涉及抑制Shp2的方法和化合物。 在一个实施方案中,本发明的化合物具有如式I或II所示的化学结构:其中X,Y和Z独立地为N或S; R 1是环烷基,杂环烷基,芳基或杂芳基,其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; -COOH; -C(R 3)3,其中R 3可以独立地为-H或卤素; 或-OR 4,其中R 4可以是H,烷基或杂烷基中的任何一个; R 2是烷基,烷基羰基,杂烷基羰基,芳基,芳基羰基,杂环烷基羰基,环烷基羰基或-C(O)NR 6 R 7,其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; 羰; -OR4,其中R4可以是-H,烷基或杂烷基; -哦; -C(R 3)3,其中R 3可以独立地为-H或卤素; 芳基,其可被一个或多个卤素或-OR 4取代; 杂环烷基; 或-C(O)OR 5,其中R 5可以是-H或烷基; R6和R7独立地是-H,烷基,杂烷基,芳基或杂芳基; 和R'是H或烷基; 或其药学上可接受的盐或水合物。
    • 93. 发明授权
    • Method and device for suppressing narrowband interference
    • 用于抑制窄带干扰的方法和装置
    • US07957495B2
    • 2011-06-07
    • US11817553
    • 2006-02-24
    • Jie WuJinlin ZhangShijie Yang
    • Jie WuJinlin ZhangShijie Yang
    • H03D1/04H03D1/06H03K5/01H03K6/04H04B1/10H04L1/00H04L25/08
    • H04B1/1036H04B1/7102
    • The method obtains an interference detection result by detecting sampled digital signals in real time in a transform domain, then maps the interference detection result into an interference suppression pulse function on the basis of a unit noise pulse function, and carries out interference suppression filtering in the transform domain according to the interference suppression pulse function. The present invention is capable of detecting narrowband interference such as monotone, frequency modulation, and phase modulation interferences in a receive channel adaptively in real-time, and suppressing the interference adaptively according to the quantity, energy and bandwidth of the interference, so as to reduce the influence of the interference. Therefore, the present invention may enhance robustness of the communication system against interference. Moreover, the present invention does not need multiple notch devices, costs low and may be implemented simply and reliably.
    • 该方法通过在变换域中实时检测采样数字信号,获得干扰检测结果,然后基于单位噪声脉冲函数将干扰检测结果映射到干扰抑制脉冲功能,并在干扰抑制滤波中进行干扰抑制滤波 根据干扰抑制脉冲函数变换域。 本发明能够实时地自适应地检测接收信道中的单调,调频和相位调制干扰等窄带干扰,并根据干扰的数量,能量和带宽自适应地抑制干扰,从而 减少干扰的影响。 因此,本发明可以提高通信系统的抗干扰性。 此外,本发明不需要多个切口装置,成本低廉并且可以简单可靠地实现。
    • 94. 发明授权
    • Iptakalim hydrochloride for decreasing nicotine use
    • 盐酸伊曲他滨用于减少尼古丁的使用
    • US07879913B2
    • 2011-02-01
    • US11168156
    • 2005-06-28
    • Jie Wu
    • Jie Wu
    • A01N33/02A01N33/18A01N33/24A61K31/13A61K31/04
    • A61K31/13
    • A method for decreasing nicotine and other substance use in humans is disclosed. Iptakalim hydrochloride (IPT) is a novel nicotine acetylcholine receptor (nAChR) blocker. According to the disclosed method, IPT is used to block human α4β2-nAChR function. Specifically, IPT exhibits a selective blockade of α4 subunit-containing human nAChR subtypes. According to the disclosed method, IPT is thus used to block the major nicotine targets in the brain, the α4β2-nAChRs natively expressed in midbrain (VTA) DA system, the brain reward center, and in turn to reduce the nicotine-induced reward signals, namely dopamine level increase in nucleus accumbens. Therefore, IPT is capable of servicing as a nAChR antagonist agent and thus is a novel treatment for decreasing nicotine dependence in humans.
    • 公开了一种减少人体中尼古丁和其他物质使用的方法。 盐酸依普卡林(IPT)是一种新型的尼古丁乙酰胆碱受体(nAChR)阻滞剂。 根据所公开的方法,IPT用于阻断人α4和bgr2-nAChR功能。 具体来说,IPT表现出对含有α4亚基的人类nAChR亚型的选择性阻断。 根据所公开的方法,IPT因此用于阻断大脑中的主要尼古丁靶标,在中脑(VTA)DA系统中本征表达的α4和bGR2-nAChRs,脑回报中心,从而减少尼古丁诱导 奖励信号,即伏隔核多巴胺水平升高。 因此,IPT能够作为nAChR拮抗剂进行维护,因此是降低人类尼古丁依赖性的新型治疗方法。
    • 96. 发明申请
    • Method for Decreasing Nicotine and Other Substance Use in Humans
    • US20080171096A1
    • 2008-07-17
    • US12013224
    • 2008-01-11
    • Jie Wu
    • Jie Wu
    • A61K31/435A61K36/00A61P25/18
    • A61K36/185
    • A method for decreasing nicotine and other substance use in humans is disclosed. Tetrahydroberberine (THB) and its analogs, l-Tetrahydropalmatine (l-THP) and l-Stepholidine (l-SPD), are present in and can be isolated from several plants in the Magnoliidae superorder. According to the disclosed method, THB and its analogs are used to block nicotine-induced DA release, and modulate heterologous or homoeric expression of human nicotinic acetylcholine receptors (nAChR) in humans. Specifically, THB exhibits bi-directory modulation of α4β2-nAChR-mediated currents induced by nicotine. THB also shows predominant inhibition on homologously expressed α7-nAChR function. Thus, according to the disclosed method, THB is used to simultaneous blockade midbrain DA system function, the brain reward center, and neuronal α4β2- and α7-nAChR function, the major nicotine targets in the brain. Therefore, THB and its analogs serve as a novel class of natural compounds to decrease nicotine dependence in humans. Furthermore other substances, such as alcohol, cocaine, and opiates, also operate by triggering the brain reward center, resulting in a cycle of substance or alcohol abuse. THB and its analogs can be used to decrease use of substances such as alcohol, cocaine, and opiates. Finally, because THB and its analogs are DA antagonists, THB and its analogs can also be used as a treatment for Parkinson's Disease, Alzheimer's Disease and Schizophrenia.
    • 97. 发明申请
    • Iptakalim hydrochloride for decreasing nicotine use
    • 盐酸伊曲他滨用于减少尼古丁的使用
    • US20060293393A1
    • 2006-12-28
    • US11168156
    • 2005-06-28
    • Jie Wu
    • Jie Wu
    • A61K31/13
    • A61K31/13
    • A method for decreasing nicotine and other substance use in humans is disclosed. Iptakalim hydrochloride (IPT) is a novel nicotine acetylcholine receptor (nAChR) blocker. According to the disclosed method, IPT is used to block human α4β2-nAChR function. Specifically, IPT exhibits a selective blockade of α4 subunit-containing human nAChR subtypes. According to the disclosed method, IPT is thus used to block the major nicotine targets in the brain, the α4β2-nAChRs natively expressed in midbrain (VTA) DA system, the brain reward center, and in turn to reduce the nicotine-induced reward signals, namely dopamine level increase in nucleus accumbens. Therefore, IPT is capable of servicing as a nAChR antagonist agent and thus is a novel treatment for decreasing nicotine dependence in humans.
    • 公开了一种减少人体中尼古丁和其他物质使用的方法。 盐酸依普卡林(IPT)是一种新型的尼古丁乙酰胆碱受体(nAChR)阻滞剂。 根据所公开的方法,IPT用于阻断人α4β2-nAChR功能。 具体来说,IPT表现出对含有α4亚基的人类nAChR亚型的选择性阻断。 根据所公开的方法,IPT因此被用于阻断大脑中的主要尼古丁靶标,中脑(VTA)DA系统中本征表达的α4β2-nAChRs,脑回报中心,进而减少尼古丁诱导的奖励信号 ,即伏隔核多巴胺水平升高。 因此,IPT能够作为nAChR拮抗剂进行维护,因此是降低人类尼古丁依赖性的新型治疗方法。
    • 100. 发明申请
    • BRAKE MEASURING GAUGE AND METHOD
    • 制动测量仪和方法
    • US20170059431A1
    • 2017-03-02
    • US14843859
    • 2015-09-02
    • CHENG-JIE WU
    • CHENG-JIE WU
    • G01L5/28
    • B60T7/102B60T11/046F16D2125/60F16D2125/64G01B5/00G01B5/0028
    • A brake measuring gauge and method are disclosed. The measuring gauge comprises two measuring rods and a horizontal rule. Each of the two measuring rod has at least a connecting rod formed at an end of the measuring rod to engage with a nut. The horizontal ruler has a central hole formed at a central portion of a surface thereof, and two through holes are formed at relative positions on two ends of the horizontal ruler, and two scales are separately formed at a lateral side of the horizontal ruler. By using the measuring gauge to measure and calculate the dimensions of components of the brake rotor, the user can obtain precise sizes of the adapter bases for different types of the calipers or the brake discs.
    • 公开了一种制动测量计和方法。 测量计包括两个测量棒和一个水平规则。 两个测量杆中的每一个具有形成在测量杆的端部处的至少一个连杆,以与螺母啮合。 水平尺具有形成在其表面的中心部分的中心孔,并且在水平尺的两端的相对位置处形成两个通孔,并且在水平尺的横向侧分开形成两个标尺。 通过使用测量计来测量和计算制动转子部件的尺寸,用户可以获得不同类型的卡钳或制动盘的适配器底座的精确尺寸。