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1. 发明授权

US08629136B2 Bisfluoroalkyl-1,4-benzodiazepinone compounds 有权
标题翻译：双氟烷基-1,4-苯并二氮杂酮化合物
公开(公告)号：US08629136B2
公开(公告)日：2014-01-14
申请号：US13426730
申请日：2012-03-22
申请人： Ashvinikumar V. Gavai , Claude A. Quesnelle , Soong-Hoon Kim , Francis Y. Lee
发明人： Ashvinikumar V. Gavai , Claude A. Quesnelle , Soong-Hoon Kim , Francis Y. Lee
IPC分类号： C07D243/24 , A61K31/5513 , A61P35/00
CPC分类号： C07D243/24 , A61K31/138 , A61K31/337 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K45/06 , A61K2300/00
摘要： Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
摘要翻译：公开了式（I）的化合物或其前药; 其中：R1是-CH2CF3或-CH2CH2CF3; R2是-CH2CF3，-CH2CH2CF3或-CH2CH2CH2CF3; R3是H或-CH3; 每个R a独立地是F，Cl，-CN，-OCH 3和/或-NHCH 2 CH 2 OCH 3; 并且z为零，1或2.还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。

2. 发明申请

US20120121604A1 COMBINATION OF ANTI-CTLA4 ANTIBODY WITH DIVERSE THERAPEUTIC REGIMENS FOR THE SYNERGISTIC TREATMENT OF PROLIFERATIVE DISEASES 有权
标题翻译：抗CTLA4抗体与多种治疗方案的联合治疗增殖性疾病的协同治疗
公开(公告)号：US20120121604A1
公开(公告)日：2012-05-17
申请号：US13384900
申请日：2009-10-29
申请人： Maria Jure-Kunkel , Francis Y. Lee
发明人： Maria Jure-Kunkel , Francis Y. Lee
IPC分类号： A61K39/395 , A61P35/00
CPC分类号： A61K47/48384 , A61K31/505 , A61K31/555 , A61K31/7068 , A61K33/24 , A61K39/39541 , A61K39/3955 , A61K45/06 , A61K2300/00
摘要： Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. Such Compositions comprise inter alia an anti-CTLA-4 agent, e.g. ipilimumab or tremelimumab in combination with other chemotherapeutic agents such as dasatinib, imatinib, paclitaxel, gemcitabine, cisplatin or etoposide.
摘要翻译：公开了可用于治疗和预防增殖性疾病的组合物和方法。这样的组合物尤其包括抗CTLA4剂，例如， ipilimumab或tremelimumab与其他化学治疗剂如达沙替尼，伊马替尼，紫杉醇，吉西他滨，顺铂或依托泊苷组合使用。

3. 发明授权

US07799788B2 Method of treating chronic myelogenous leukemia cells 有权
标题翻译：治疗慢性骨髓性白血病细胞的方法
公开(公告)号：US07799788B2
公开(公告)日：2010-09-21
申请号：US12364009
申请日：2009-02-02
申请人： Kapil N. Bhalla , Francis Y. Lee
发明人： Kapil N. Bhalla , Francis Y. Lee
IPC分类号： A61K31/497
CPC分类号： A61K31/4745 , A61K31/506 , A61K45/06 , A61K2300/00
摘要： Here, the inventors disclose the treatment of imatinib mesylate resistant chronic myelogenous leukemia cells with a cotreatment of vorinostat (SAHA, suberoylanilide hydroxamic acid) and dasatinib, a dual Abl/Src kinase (TK) inhibitor. Combined treatment of cultured human CML and BaF3 cells with vorinostat and dasatinib induced more apoptosis than either agent alone, as well as synergistically induced loss of clonogenic survival, which was associated with greater depletion of Bcr-Abl, p-CrkL and p-STAT5 levels. Co-treatment with dasatinib and vorinostat also attenuated the levels of Bcr-AblE255K and Bcr-AblT315I and induced apoptosis of BaF3 cells with ectopic expression of the mutant forms of Bcr-Abl. Finally, co-treatment of the primary CML cells with vorinostat and dasatinib induced more loss of cell viability and depleted Bcr-Abl or Bcr-AblT315I, p-STAT5 and p-CrkL levels than either agent alone.
摘要翻译：在这里，发明人公开了通过联合维生素（SAHA，辛二酰苯胺异羟肟酸）和达沙替尼（双重Abl / Src激酶（TK））抑制剂的治疗来治疗甲磺酸伊马替尼耐药性慢性骨髓性白血病细胞。培养的人CML和BaF3细胞与伏立诺他和达沙替尼的联合治疗诱导出比单独的任一种更多的凋亡，以及协同诱导的克隆形成存活的损失，其与Bcr-Abl，p-CrkL和p-STAT5水平的更大的消耗相关。与dasatinib和伏立诺他治的联合治疗也减弱了Bcr-AblE255K和Bcr-AblT315I的水平，并诱导了Bcr-Abl突变形式异位表达BaF3细胞凋亡。最后，原代CML细胞与伏立诺他和达沙替尼的共同治疗比单独使用任一试剂诱导更多的细胞活力丧失和消耗Bcr-Abl或Bcr-AblT315I，p-STAT5和p-CrkL水平。

4. 发明申请

US20100098701A1 Combination of anti-CTLA4 antibody with dasatinib for the treatment of proliferative diseases 有权
标题翻译：抗CTLA4抗体与达沙替尼联合用于治疗增殖性疾病
公开(公告)号：US20100098701A1
公开(公告)日：2010-04-22
申请号：US12462168
申请日：2009-07-30
申请人： Maria Jure-Kunkel , Francis Y. Lee
发明人： Maria Jure-Kunkel , Francis Y. Lee
IPC分类号： A61K39/395 , A61K31/7048 , A61K31/7088 , A61K31/7068 , A61K31/506 , A61K31/427 , A61K31/337 , A61P35/00
CPC分类号： A61K47/48384 , A61K31/505 , A61K31/555 , A61K31/7068 , A61K33/24 , A61K39/39541 , A61K39/3955 , A61K45/06 , A61K2300/00
摘要： Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.
摘要翻译：公开了可用于治疗和预防增殖性疾病的组合物和方法。

5. 发明申请

US20090197893A1 Methods of Identifying and Treating Individuals Exhibiting Complex Karyotypes 审中-公开
标题翻译：识别和处理复杂核型的个体的方法
公开(公告)号：US20090197893A1
公开(公告)日：2009-08-06
申请号：US12085733
申请日：2006-11-30
申请人： Francis Y. Lee , Charles L. Sawyers , Neil P. Shah
发明人： Francis Y. Lee , Charles L. Sawyers , Neil P. Shah
IPC分类号： A61K31/496 , C12Q1/68 , A61P35/00 , A61P35/02
CPC分类号： C12Q1/6886 , C12Q2600/106 , C12Q2600/156
摘要： The invention described herein relates to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that harbor complex karyotypes. The present invention also related to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins.
摘要翻译：本文描述的发明涉及可用于治疗病症（例如涉及携带复杂核型的细胞的癌症）的诊断和治疗方法和组合物。本发明还涉及突变体BCR-ABL激酶蛋白，以及可用于治疗病症（例如涉及表达这种突变型BCR-ABL激酶蛋白的细胞）的癌症的诊断和治疗方法和组合物。

6. 发明授权

US07504211B2 Methods of using EPHA2 for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in breast cells 有权
标题翻译：使用EPHA2预测与乳腺细胞相互作用和/或调节蛋白酪氨酸激酶和/或蛋白酪氨酸激酶途径的化合物的活性的方法
公开(公告)号：US07504211B2
公开(公告)日：2009-03-17
申请号：US10648593
申请日：2003-08-26
申请人： Fei Huang , Xia Han , Karen A. Reeves , Lukas C. Amler , Craig R. Fairchild , Francis Y. Lee , Peter Shaw
发明人： Fei Huang , Xia Han , Karen A. Reeves , Lukas C. Amler , Craig R. Fairchild , Francis Y. Lee , Peter Shaw
IPC分类号： C12Q1/00 , C12Q1/68
CPC分类号： C07K14/47 , A61K38/00 , C12Q1/6837 , C12Q1/6886 , C12Q2600/106 , C12Q2600/136 , C12Q2600/158
摘要： The present invention describes polynucleotides that have been discovered to correlate to the relative sensitivity or resistance of cells, e.g., breast cell lines, to treatment with compounds that interact with and modulate, e.g., inhibit, protein tyrosine kinases, such as, for example, members of the Src family of tyrosine kinases, e.g., Src, Fgr, Fyn, Yes, Blk, Hck, Lck and Lyn, as well as other protein tyrosine kinases, including, Bcr-abl, Jak, PDGFR, c-kit and Eph receptors. These polynucleotides have been shown to have utility in predicting the resistance and sensitivity of breast cell lines to the compounds. Such polynucleotides comprise polynucleotide predictor or marker sets useful in methods of predicting drug response, and as prognostic or diagnostic indicators in disease management, particularly in those disease areas, e.g., breast cancer, in which signaling through one or more of the aforementioned Src tyrosine and protein tyrosine kinases is involved with the disease process.
摘要翻译：本发明描述了已被发现与将细胞例如乳腺细胞系的相对敏感性或抗性相关的多核苷酸与用蛋白酪氨酸激酶相互作用并调节，例如抑制蛋白酪氨酸激酶的化合物的治疗，酪氨酸激酶Src家族成员，如Src，Fgr，Fyn，Yes，Blk，Hck，Lck和Lyn，以及其他蛋白酪氨酸激酶，包括Bcr-abl，Jak，PDGFR，c-kit和Eph 受体。已经显示这些多核苷酸可用于预测乳腺细胞系对化合物的抗性和敏感性。这样的多核苷酸包括可用于预测药物反应的方法的多核苷酸预测物或标志物组，以及疾病管理中的预后或诊断指标，特别是在那些疾病领域，例如乳腺癌中，其中通过一种或多种上述Src酪氨酸和蛋白酪氨酸激酶参与疾病过程。

7. 发明申请

US20130012519A1 Biomarker Identifying the Reactivation of STAT3 After Src Inhibition 审中-公开
标题翻译：生物标志物识别STAT3在Src抑制后的重新激活
公开(公告)号：US20130012519A1
公开(公告)日：2013-01-10
申请号：US13617992
申请日：2012-09-14
申请人： Faye M. Johnson , Nicholas J. Donato , Francis Y. Lee
发明人： Faye M. Johnson , Nicholas J. Donato , Francis Y. Lee
IPC分类号： A61K31/506 , A61P35/00 , G01N33/573 , G01N33/566 , G01N33/574
CPC分类号： G01N33/574
摘要： A method of identifying cancer or an associated disorder comprising identifying and quantifying STAT3 occurring in a biological sample taken from a subject after administering a SFK inhibitor to said subject.
摘要翻译：一种鉴定癌症或相关疾病的方法，其包括鉴定和定量在向所述受试者施用SFK抑制剂之后，从取自受试者的生物样品中发生的STAT3。

8. 发明申请

US20110230528A1 Use of Epothilone D in Treating Tau-Associated Diseases Including Alzheimer's Disease 有权
标题翻译：使用埃坡霉素D治疗包括阿尔茨海默氏病在内的au相关疾病
公开(公告)号：US20110230528A1
公开(公告)日：2011-09-22
申请号：US13150671
申请日：2011-06-01
申请人： Charles F. Albright , Donna Marie Barten , Francis Y. Lee
发明人： Charles F. Albright , Donna Marie Barten , Francis Y. Lee
IPC分类号： A61K31/427 , A61P25/28
CPC分类号： A61K31/427
摘要： Methods of treating Tau-associated diseases, preferably tauopathies, are described using epothilone D that exhibit good brain penetration, long half-life, and high selective retention in brain, and provides effective therapies in treating tauopathies including Alzheimer's disease.
摘要翻译：使用表现出良好的脑渗透性，长半衰期和脑中高选择性保留的埃坡霉素D来描述治疗Tau相关疾病，优选tau蛋白病的方法，并且提供有效治疗包括阿尔茨海默氏病在内的tau蛋白病的疗法。

9. 发明申请

US20100173426A1 BIOMAKER IDENTIFYING THE REACTIVATION OF STAT3 AFTER SRC INHIBITION 审中-公开
标题翻译：生物标志物鉴定SRC抑制后STAT3的反应
公开(公告)号：US20100173426A1
公开(公告)日：2010-07-08
申请号：US12519848
申请日：2007-12-18
申请人： Faye M. Johnson , Nicholas J. Donato , Francis Y. Lee
发明人： Faye M. Johnson , Nicholas J. Donato , Francis Y. Lee
IPC分类号： G01N33/574
CPC分类号： G01N33/574
摘要： A method of identifying cancer or an associated disorder comprising identifying and quantifying STAT3 occurring in a biological sample taken from a subject after administering a SFK inhibitor to said subject.
摘要翻译：一种鉴定癌症或相关疾病的方法，其包括鉴定和定量在向所述受试者施用SFK抑制剂之后，从取自受试者的生物样品中发生的STAT3。

10. 发明授权

US07622472B2 Combination of Src kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases 失效
标题翻译：组合Src激酶抑制剂和化疗药物治疗增殖性疾病
公开(公告)号：US07622472B2
公开(公告)日：2009-11-24
申请号：US12047623
申请日：2008-03-13
申请人： Francis Y. Lee
发明人： Francis Y. Lee
IPC分类号： A61K31/497 , A61K31/426 , A61P35/00 , C07D277/02
CPC分类号： A61K45/06 , A61K31/426 , A61K31/427 , A61K2300/00
摘要： Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.
摘要翻译：公开了可用于治疗和预防增殖性疾病的组合物和方法。

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