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1. 发明申请

WO2010011666A3 INDOLINE SCAFFOLD SHP-2 INHIBITORS AND CANCER TREATMENT METHOD 审中-公开
标题翻译： INDOLINE SCAFFOLD SHP-2抑制剂和癌症治疗方法
公开(公告)号：WO2010011666A3
公开(公告)日：2010-04-22
申请号：PCT/US2009051276
申请日：2009-07-21
申请人： UNIV SOUTH FLORIDA , WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M
发明人： WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M
IPC分类号： C07D403/12 , A61K31/496 , A61P35/00
CPC分类号： C07D405/06 , C07D209/08 , C07D215/36
摘要： 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(RO3)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 R1 is H or alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明涉及用于抑制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，它们中的任何一个可以任选地被一个或多个卤素取代; 烷基; 杂; -COOH; -C（R 3）3，其中R 3可以独立地为-H或卤素中的任何一个; 或-OR 4，其中R 4可以是H，烷基中的任何一个。或杂烷基; 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，它们中的任何一个可以任选地被一个或多个卤素取代; 烷基; 杂; 羰; -OR 4，其中R 4可以是-H，烷基或杂烷基; -哦; -C（RO 3）3，其中R 3可以独立地为-H或卤素中的任何一个; 芳基，其可以被一个或多个卤素或-OR 4取代; 杂环; 或-C（O）OR 5，其中R 5可以是-H或烷基; R6和R7独立地为-H，烷基，杂烷基，芳基或杂芳基; 并且R1是H或烷基; 或其药学上可接受的盐或水合物。

2. 发明申请

WO2009135000A3 INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-117199 AND ANALOGS 审中-公开
标题翻译： NSC-117199和模拟物对SHP2 / PTPN11蛋白酪氨酸磷酸化酶的抑制作用
公开(公告)号：WO2009135000A3
公开(公告)日：2010-02-18
申请号：PCT/US2009042305
申请日：2009-04-30
申请人： H LEE MOFFITT CANCER CT AND RE , UNIV SOUTH FLORIDA , WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M , LAWRENCE HARSHANI R
发明人： WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M , LAWRENCE HARSHANI R
IPC分类号： A61K31/404 , A61P35/00 , C07D209/34
CPC分类号： C07D209/40
摘要： Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. NSC-117199 was identified as a porent inhibitor of the protein tyrosine phosphatase (PTPa) Shp2. A focused library of analogs incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
摘要翻译：蛋白酪氨酸磷酸酶（PTP）Shp2是参与细胞信号传导和调节细胞增殖，分化和迁移的非受体PTP。 Shp2介导参与人类癌症发病机制的激酶活化。 NSC-117199被鉴定为蛋白酪氨酸磷酸酶（PTPa）Shp2的细胞抑制剂。设计了一个重点的掺入靛红支架的类似物库，并评估了Shp2和Shp1 PTP活性的抑制作用。鉴定出几种化合物选择性地抑制Shp1与Shp1和PTP1B的低亚微摩尔活性。还公开了抑制细胞中的蛋白质酪氨酸磷酸酶并通过选择性抑制Shp2治疗癌症的方法。

3. 发明申请

WO2010121212A2 INDOLINE SCAFFOLD SHP-2 INHIBITORS AND METHOD OF TREATING CANCER 审中-公开
标题翻译： INDOLINE SCAFFOLD SHP-2抑制剂和治疗癌症的方法
公开(公告)号：WO2010121212A2
公开(公告)日：2010-10-21
申请号：PCT/US2010031506
申请日：2010-04-16
申请人： H LEE MOFFIT CANCER CT AND RES , UNIV SOUTH FLORIDA , WU JIE , LAWRENCE NICHOLAS JAMES , SEBTI SAID M , LAWRENCE HARSHANI RITHMA
发明人： WU JIE , LAWRENCE NICHOLAS JAMES , SEBTI SAID M , LAWRENCE HARSHANI RITHMA
CPC分类号： C07D209/34 , C07D209/12 , C07D209/40 , C07D215/36
摘要： Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
摘要翻译：蛋白酪氨酸磷酸酶（PTP）Shp2是参与细胞信号传导和调节细胞增殖，分化和迁移的非受体PTP。 Shp2介导参与人类癌症发病机制的激酶活化。高通量筛选鉴定抑制PTP Shp2的化合物。鉴定了几种化合物，选择性抑制Shp2超过Shp1，具有低至亚微摩尔的活性。还公开了抑制细胞中的蛋白质酪氨酸磷酸酶并通过选择性抑制Shp2治疗癌症的方法。

4. 发明申请

WO2007117699A2 INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-87877, NSC-117199 AND THEIR ANALOGS 审中-公开
标题翻译： NSC-87877，NSC-117199及其类似物对SHP2 / PTPN11蛋白酪氨酸磷酸化酶的抑制作用
公开(公告)号：WO2007117699A2
公开(公告)日：2007-10-18
申请号：PCT/US2007008876
申请日：2007-04-09
申请人： UNIV SOUTH FLORIDA , H LEE MOFFITT CANCER CT AND RE , WU JIE , LAWRENCE NICHOLAS JAMES , SEBTI SAID M , LAWRENCE HARSHANI RITHMA
发明人： WU JIE , LAWRENCE NICHOLAS JAMES , SEBTI SAID M , LAWRENCE HARSHANI RITHMA
IPC分类号： A61K31/405
CPC分类号： A61K31/405 , C07D209/40
摘要： Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erkl/2 activation pathway. Additionally, a number of analogs of NSC-1 17199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and arc found to be potent and/or selectiv e inhibitors of Shp l and/or Shp2 protein tyrosine phosphatases.
摘要翻译：用于抑制蛋白质酪氨酸磷酸酶的化合物和相关方法。通过NCI多样性集化学库的实验和虚拟筛选的组合，NSC-87877和NSC-117199已被鉴定为Shp2 PTP抑制剂。显着地，NSC-87877在基于细胞的测定中是有活性的，并且在EGF刺激的Erk1 / 2激活途径中没有检测到的脱靶作用。此外，已经生产了许多NSC-17199的类似物。这些类似物表现出增强的蛋白酪氨酸磷酸酶抑制，并且发现弧是Shp1和/或Shp2蛋白酪氨酸磷酸酶的有效和/或选择性抑制剂。

5. 发明申请

WO2007047919A3 TREATMENT OF RESTENOSIS AND STENOSIS WITH DASATINIB 审中-公开
标题翻译：用DASATINIB治疗抑郁症和STENOSIS
公开(公告)号：WO2007047919A3
公开(公告)日：2007-06-28
申请号：PCT/US2006041031
申请日：2006-10-19
申请人： UNIV SOUTH FLORIDA , H LEE MOFFITT CANCER CT AND RE , WU JIE , CHEN ZENGMING , BHALLA KAPIL N
发明人： WU JIE , CHEN ZENGMING , BHALLA KAPIL N
IPC分类号： A61K38/00 , A61K31/70
CPC分类号： A61K31/506
摘要： A method for treating or inhibiting artery obstructive disease, such as restenosis after angioplasty and stenting procedures and stenosis after coronary artery bypass surgery, in a subject by administering to the subject a therapeutically effective amount of dasatinib or a derivative thereof. Also provided are drug-eluting medical devices, including stents, having a therapeutically effective amount of dasatinib.
摘要翻译：在受试者中通过给予受试者治疗有效量的达沙替尼或其衍生物来治疗或抑制动脉阻塞性疾病的方法，例如血管成形术后的再狭窄和冠状动脉搭桥手术后的狭窄。还提供了具有治疗有效量的达沙替尼的药物洗脱医疗装置，包括支架。

6. 发明申请

WO2009079905A8 A SELECTIVE HYDROGENATION CATALYST AND THE PREPARATION THEREOF 审中-公开
标题翻译：选择性氢化催化剂及其制备方法
公开(公告)号：WO2009079905A8
公开(公告)日：2010-07-08
申请号：PCT/CN2008001780
申请日：2008-10-22
申请人： PETROCHINA CO LTD , LIANG SHUNQIN , SUN LIMIN , LV LONGGANG , QIAN YING , ZHENG YUNDI , WU JIE , WANG TINGHAI , LI XIAOYAN
发明人： LIANG SHUNQIN , SUN LIMIN , LV LONGGANG , QIAN YING , ZHENG YUNDI , WU JIE , WANG TINGHAI , LI XIAOYAN
IPC分类号： B01J23/44 , B01J37/02 , C10G45/10
CPC分类号： B01J23/63 , B01J21/04 , B01J23/002 , B01J35/008 , B01J35/1038 , B01J37/0205 , B01J37/0207 , B01J2523/00 , C10G45/40 , C10G2400/02 , B01J2523/24 , B01J2523/31 , B01J2523/3706 , B01J2523/824 , B01J2523/22 , B01J2523/3712 , B01J2523/25
摘要： A selective hydrogenation catalyst, with alumina as carrier, and palladium as active component that distributed on the surface of the carrier in an egg-shell form, characterized in that: provided that the catalyst is weighed 100%, it comprises 0.2-0.5wt% active component Pd, 2-8wt% aids lanthanum and/or cerium, and 2-8wt% alkaline earth metal. The specific surface area of the catalyst is 70-150m2/g, the pore volume is 0.3-0.6ml/g, and the crystal form of the carrier may be ?form or ?,amixed form mainly composed of ?form. The catalyst is suitable for the selective hydrogenation of medium or low distillate oil, especially for the first stage selective hydrogenation of pyrolysis gasoline. The catalyst has good hydrogenation performance, and can keep good hydrogenation activity and stability especially under the condition that the feed contains a small quantity of water, and the content of colloid, arsenic, and diolefin is higher.
摘要翻译：以氧化铝为载体的选择性氢化催化剂和以蛋壳形式分布在载体表面上的钯作为活性组分，其特征在于：如果催化剂称重为100％，则其包含0.2-0.5wt％活性成分Pd，2-8wt％有助于镧和/或铈，以及2-8wt％碱土金属。催化剂的比表面积为70-150m2 / g，孔体积为0.3-0.6ml / g，载体的结晶形式可以是α型或β型，主要由α形式组成。该催化剂适用于中等或低馏分油的选择性氢化，特别是热解汽油的第一阶段选择氢化。该催化剂具有良好的氢化性能，特别是在含有少量水的条件下，可保持良好的氢化活性和稳定性，胶体，砷和二烯含量较高。

7. 发明申请

WO2012068553A2 METHODS OF DIAGNOSING AND TREATING NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：诊断和治疗神经损伤性疾病的方法
公开(公告)号：WO2012068553A2
公开(公告)日：2012-05-24
申请号：PCT/US2011061541
申请日：2011-11-18
申请人： DIGNITY HEALTH , WU JIE
发明人： WU JIE
IPC分类号： A61K31/4704 , A61K38/10
CPC分类号： A61K38/1703 , A61K31/13 , A61K31/439 , A61K31/47 , A61K31/4748 , A61K38/17 , C12Q1/6883 , C12Q2600/142 , C12Q2600/158 , G01N33/6896
摘要： The present invention relates to methods of diagnosing, treating and prognosing mental disorders, such as Alzheimer's Disease. In one embodiment, the present invention provides a method of treating Alzheimer's Disease by inhibiting dysfunctional signaling of a7 nAChRs in the medial septum region of an individual.
摘要翻译：本发明涉及诊断，治疗和预测精神障碍如阿尔茨海默病的方法。在一个实施方案中，本发明提供了通过抑制个体的内侧隔膜区域中的a7 nAChRs的功能障碍信号传导来治疗阿尔茨海默氏病的方法。

8. 发明申请

WO2011112334A2 COATED CERAMIC CUTTING INSERT AND METHOD OF MAKING THE SAME 审中-公开
标题翻译：涂层陶瓷切割插件及其制造方法
公开(公告)号：WO2011112334A2
公开(公告)日：2011-09-15
申请号：PCT/US2011025165
申请日：2011-02-17
申请人： KENNAMETAL INC , BAN ZHIGANG , GATES JR ALFRED , LIU YIXIONG , WU JIE
发明人： BAN ZHIGANG , GATES JR ALFRED , LIU YIXIONG , WU JIE
IPC分类号： B23B27/14 , B23B27/16 , C04B35/01 , C23C16/30
CPC分类号： B23B27/148 , B23B27/141 , B23B2226/18 , B23B2228/10 , B23B2260/144 , C04B41/009 , C04B41/52 , C04B41/89 , C23C28/044 , C23C28/42 , C23C30/005 , Y10T407/27 , C04B35/584 , C04B35/597 , C04B41/4531 , C04B41/5031 , C04B41/459 , C04B41/5061 , C04B41/5068
摘要： A coated ceramic cutting insert (20) for removing material from a workpiece, as well as a method for making the same, that includes a ceramic substrate ((40, 40A, 40B) with a rake surface (28) and at least one flank surface (30) wherein a cutting edge (32) is at the juncture therebetween. A wear-resistant coating scheme (50, 82) that includes at least one exposed alumina coating layer (50, 60, 62, 82) which exhibits a blasted stress condition ranging between about 50 MPa (tensile stress) and about - 2GPa (compressive) as measured by XRD using the Psi tilt method and the (024) reflection of alumina. The exposed alumina coating layer (50, 60, 62, 82) is the result of wet blasting a titanium-containing outer coating layer (54, 54A, 54B) region from the surface of the alumina-containing base coating layer region (50, 50A, 50B).
摘要翻译：一种用于从工件去除材料的涂覆陶瓷切削刀片（20）及其制造方法，其包括具有前刀面（28）和至少一个侧面（40,40A，40B）的陶瓷衬底（40,40A，40B）表面（30），其中切割边缘（32）处于它们之间的接合处;耐磨涂层方案（50,82），其包括至少一个露出的氧化铝涂层（50,60,62,82）暴露的氧化铝涂层（50,60,62,82）通过使用Psi倾斜法和（024）氧化铝的反射通过XRD测量的约50MPa（拉伸应力）和约-2GPa（压缩）是从含氧化铝的基底涂层区域（50,50A，50B）的表面湿式喷砂含钛外涂层（54,54A，54B）区域的结果。

9. 发明申请

WO2004069144A3 METHOD FOR DECREASING NICOTINE AND OTHER SUBSTANCE USE IN HUMANS 审中-公开
标题翻译：降低人类免疫球蛋白和其他物质使用的方法
公开(公告)号：WO2004069144A3
公开(公告)日：2005-10-27
申请号：PCT/IB2004002083
申请日：2004-02-09
申请人： ARIZONA HEALTH CONSULTING GROU , WU JIE
发明人： WU JIE
IPC分类号： A61K20060101 , A61K36/00 , A61K36/185 , A61K35/78
CPC分类号： A61K36/185
摘要： A method for decreasing nicotine and other substance use in humans is disclosed. Tetrahydroberberine (THB) and its analogs, l-Tetrahydropalmatine (1THP) 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 a4ß2-nAChR-mediated currents induced by nicotine. THB also shows predominant inhibition on homologously expressed alpha7-nAChR function. Thus, according to the disclosed method, THB is used to simultaneous blockade midbrain DA system function, the brain reward center, and neuronal a4ß2- and a7-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.
摘要翻译：公开了一种减少人体中尼古丁和其他物质使用的方法。四氢小檗碱（THB）及其类似物1-四氢al嗪（1THP）和1- Step hol啶（1-SPD）存在于并可以从Magnoliidae超级序列中的几种植物中分离出来。根据所公开的方法，泰铢及其类似物用于阻断尼古丁诱导的DA释放，并调节人类烟碱乙酰胆碱受体（nAChR）的异源或同源性表达。具体来说，泰铢表现了由尼古丁诱导的a4β2-nAChR介导的电流的双目录调制。 THB也显示出对同源表达的α7-nAChR功能的主要抑制作用。因此，根据所公开的方法，泰铢用于同时封锁中脑DA系统功能，脑回报中心和神经元a4ß2-和a7-nAChR功能，大脑中主要的尼古丁目标。因此，泰铢及其类似物作为一类新型天然化合物，可以减少人体尼古丁依赖。此外，其他物质如酒精，可卡因和阿片剂也可以通过触发脑回报中心进行操作，导致物质或酒精滥用的循环。泰铢及其类似物可用于减少酒精，可卡因和阿片剂等物质的使用。最后，由于泰铢及其类似物是DA拮抗剂，泰铢及其类似物也可用作帕金森病，阿尔茨海默病和精神分裂症的治疗。

10. 发明申请

WO2005010494A2 MULTIPLEXED ANALYTE DETECTION 审中-公开
标题翻译：多重分析检测
公开(公告)号：WO2005010494A2
公开(公告)日：2005-02-03
申请号：PCT/US2004023613
申请日：2004-07-21
申请人： WU JIE
发明人： WU JIE
IPC分类号： C12P19/34 , C12Q1/68 , G01N20060101 , G01N
CPC分类号： C12Q1/6804 , C12Q1/6834 , C12Q2563/179 , C12Q2531/113 , C12Q2565/501 , C12Q2565/549 , C12Q2561/113
摘要： The invention provides methods and kits for quantitating or detecting the presence of a plurality of different target molecules in a sample using detector molecules comprising nucleic acid tags.
摘要翻译：本发明提供用于使用包含核酸标签的检测器分子定量或检测样品中多个不同靶分子的存在的方法和试剂盒。

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