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1. 发明申请

WO2010083465A1 AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER 审中-公开
标题翻译：用于组合治疗的AXL抑制剂用于预防，治疗或管理分子癌
公开(公告)号：WO2010083465A1
公开(公告)日：2010-07-22
申请号：PCT/US2010/021275
申请日：2010-01-15
申请人： RIGEL PHARMACEUTICALS, INC. , HITOSHI, Yasumichi , HOLLAND, Sacha , PAYAN, Donald, G.
发明人： HITOSHI, Yasumichi , HOLLAND, Sacha , PAYAN, Donald, G.
IPC分类号： A61K31/00
CPC分类号： A61K31/502 , A61K31/4196 , A61K33/24 , A61K45/06 , C07D403/04 , C07D403/14 , A61K2300/00
摘要： This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an AxI inhibitor in combination with the administation of an effective amount of one or more chemotherapeutic agents.
摘要翻译：本发明涉及在患者体内预防，治疗或控制癌症，优选转移性癌症的方法。所述方法包括与施用有效量的一种或多种化学治疗剂组合施用有效量的AxI抑制剂。

2. 发明申请

WO2003012055A2 SAK: MODULATION OF CELLULAR PROLIFERATION FOR TREATMENT OF CANCER 审中-公开
标题翻译： SAK：用于治疗癌症的细胞增殖的调节
公开(公告)号：WO2003012055A2
公开(公告)日：2003-02-13
申请号：PCT/US2002/024312
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS, INC. , DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
发明人： DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： C12N
CPC分类号： G01N33/57484 , A61K38/00 , A61K2039/505 , G01N2333/912
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding SAK, which is a protein kinase involved in modulation of cellular proliferation and cell cycle regulation. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of SAK; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.
摘要翻译：本发明涉及细胞增殖的调控。更具体地，本发明涉及编码SAK的核酸，其是参与调节细胞增殖和细胞周期调节的蛋白激酶。本发明还涉及用于鉴别和使用通过调节SAK调节细胞周期调节和细胞增殖的试剂，包括小分子化学组合物，抗体，肽，环肽，核酸，RNAi，反义核酸和核酶的方法; 以及在细胞周期调控和细胞增殖调节相关的诊断和治疗中使用表达谱和组合物，例如用于治疗癌症和其它细胞增殖疾病。

3. 发明申请

WO2015048547A2 METHODS FOR USING AND BIOMARKERS FOR AMPK-ACTIVATING COMPOUNDS 审中-公开
标题翻译：用于AMPK激活化合物的方法和生物标志物
公开(公告)号：WO2015048547A2
公开(公告)日：2015-04-02
申请号：PCT/US2014/057861
申请日：2014-09-26
申请人： RIGEL PHARMACEUTICALS, INC. , HITOSHI, Yasumichi , JENKINS, Yonchu , MARKOVTSOV, Vadim , KINSELLA, Todd , SUN, Tian-Qiang
发明人： HITOSHI, Yasumichi , JENKINS, Yonchu , MARKOVTSOV, Vadim , KINSELLA, Todd , SUN, Tian-Qiang
IPC分类号： A61P35/00
CPC分类号： A61K31/4545 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , G01N33/573 , G01N2500/04 , A61K2300/00
摘要： Disclosed are are methods of using AMPK-activating compounds, for example, in the treatment of cancer and disorders of vascular flow. Also disclosed are biomarkers for AMPK and uses thereof, for example, in the diagnosis and treatment of AMPK-linked disorders. In certain embodiments, the AMPK-activating compounds have the structural formula (I), wherein E, J, T, D 1 , D 2 , D 3 , the ring system denoted by "B", T, R 3 , R 4 , w and x are as described herein.
摘要翻译：公开的是使用AMPK活化化合物的方法，例如用于治疗癌症和血管流动障碍。还公开了AMPK的生物标志物及其用途，例如在AMPK相关疾病的诊断和治疗中。在某些实施方案中，AMPK活化化合物具有结构式（I），其中E，J，T，D1，D2，D3，由“B”，T，R3，R4，w和x表示的环系为在此描述。

4. 发明申请

WO2004007754A3 MODULATORS OF CELLULAR PROLIFERATION 审中-公开
公开(公告)号：WO2004007754A3
公开(公告)日：2004-01-22
申请号：PCT/US2003/022164
申请日：2003-07-14
申请人： RIGEL PHARMACEUTICALS, INC. , HITOSHI, Yasumichi , JENKINS, Yonchu , MARKOVTSOV, Vadim
发明人： HITOSHI, Yasumichi , JENKINS, Yonchu , MARKOVTSOV, Vadim
IPC分类号： C12Q1/00
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding protein kinase C ζ (PKC-ζ), phospholipase C-β1 (PLC-ß1), protein tyrosine kinase 2 (FAK), protein tyrosine kinase 2b (FAK2), casein kinase 2 (CK2), cMET tyrosine kinase (cMET), flap structure specific endonuclease 1 (FEN1), REV1 dCMP transferase (REV1), apurinic/apyrimidinic nuclease 1 (APE1), cyclin dependent kinase 3 (CDK3), PIM1 kinase (PIM1), cell division cycle 7 kinase (CDC7L1), cyclin dependent kinase 7 (CDK7), cytokine inducible kinase (CNK), potentially prenylated protein tyrosine phosphatase (PRL-3), serine threonine kinase 2 (STK2) or (NEK4), cyclin dependent serine threonine kinase (NKIAMRE), or histone acetylase (HBO1), which are involved in modulation of cell cycle arrest. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle arrest via modulation of protein kinase C ζ (PKC-ζ), phospholipase C-ß1 (PLC-ß1), protein tyrosine kinase 2 (FAK), protein tyrosine kinase 2b (FAK2), casein kinase 2 (CK2), cMET tyrosine kinase (cMET), flap structure specific endonuclease 1 (FEN1), REV1 dCMP transferase (REV1), apurinic/apyrimidinic nuclease 1 (APE1), cyclin dependent kinase 3 (CDK3), PIM1 kinase (PIM1), cell division cycle 7 kinase (CDC7L1), cyclin dependent kinase 7 (CDK7), cytokine inducible kinase (CNK), potentially prenylated protein tyrosine phosphatase (PRL-3), serine threonine kinase 2 (STK2) or (NEK4), cyclin dependent serine threonine kinase (NKIAMRE), or histone acetylase (HBO1), as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

5. 发明申请

WO2008061201A1 METHODS FOR TREATING RENAL TUMORS USING 2,4-PYRIMIDINEDIAMINE DRUG AND PRODRUG COMPOUNDS 审中-公开
标题翻译：使用2,4-二吡啶二胺药物和制剂化合物治疗肾上腺肿瘤的方法
公开(公告)号：WO2008061201A1
公开(公告)日：2008-05-22
申请号：PCT/US2007/084855
申请日：2007-11-15
申请人： RIGEL PHARMACEUTICALS, INC. , HITOSHI, Yasumichi , GROSSBARD, Elliott , ARGADE, Ankush , SINGH, Rajinder , LI, Hui , CARROLL, David , CATALANO, Susan
发明人： HITOSHI, Yasumichi , GROSSBARD, Elliott , ARGADE, Ankush , SINGH, Rajinder , LI, Hui , CARROLL, David , CATALANO, Susan
IPC分类号： A61K31/5365 , A61P35/00
CPC分类号： A61K31/5365
摘要： The present disclosure provides methods for the inhibiting proliferation of tumor cells, and methods for treating solid tumor cancers in a subject by administration of 2,4-pyrimidinediamine compounds.
摘要翻译：本公开提供了抑制肿瘤细胞增殖的方法，以及通过施用2,4-嘧啶二胺化合物治疗受试者的实体瘤癌症的方法。

6. 发明申请

WO2004041844A2 CELL CYCLE TARGETS AND PEPTIDES 审中-公开
标题翻译：细胞周期目标和肽
公开(公告)号：WO2004041844A2
公开(公告)日：2004-05-21
申请号：PCT/US2003/034669
申请日：2003-10-30
申请人： RIGEL PHARMACEUTICALS, INC. , HITOSHI, Yasumichi , ANDERSON, David
发明人： HITOSHI, Yasumichi , ANDERSON, David
IPC分类号： C07K
CPC分类号： G01N33/5011 , C07K7/06 , C07K7/08 , C07K2319/60 , G01N33/502 , G01N2510/00
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention binding partners of peptides that block the cell cycle. These binding partners are targets for drug discovery, e.g., for small molecule cancer therapeutics.
摘要翻译：本发明涉及细胞增殖的调控。更具体地，本发明结合阻断细胞周期的肽的结合物。这些结合配偶体是用于药物发现的靶标，例如用于小分子癌症治疗剂。

7. 发明申请

WO2003088910A2 METHODS OF ASSAYING FOR CELL CYCLE MODULATORS 审中-公开
标题翻译：细胞周期调节剂的测定方法
公开(公告)号：WO2003088910A2
公开(公告)日：2003-10-30
申请号：PCT/US2003/011867
申请日：2003-04-15
申请人： RIGEL PHARMACEUTICALS, INC. , HITOSHI, Yasumichi , JENKINS, Yonchu
发明人： HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： A61K
CPC分类号： G01N33/5091 , C12Q1/6886 , C12Q2600/158 , G01N33/5008 , G01N33/5011 , G01N33/574 , G01N33/6872 , G01N2333/4703 , G01N2500/00
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding BRCA-1-Associated Protein-1 (BAP-1), Nuclear Protein 95 (NP95), Fanconi anemia group A protein (FANCA), DEAD/H box polypeptide 9 (DDX9), insulin-like growth factor 1 receptor (IGF1R), ubiquitin-conjugating enzyme E2 variant 1 (UBE2V1), aldehyde dehydrogenase, pyruvate kinase, glucose-6-phosphate dehydrogenase, HCDR-3, DEAD/H box polypeptide 21 (DDX21), serine threonine kinase 15 (ARK2), transmembrane 4 superfamily member 1, or ERCC1, which are involved in modulation of cell cycle arrest. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle arrest via modulation of BRCA-1-Associated Protein-1 (BAP-1), Nuclear Protein 95 (NP95), Fanconi anemia group A protein (FANCA), DEAD/H box polypeptide 9 (DDX9), insulin-like growth factor 1 receptor (IGF1R), ubiquitin-conjugating enzyme E2 variant 1 (UBE2V1), aldehyde dehydrogenase, pyruvate kinase, glucose-6-phosphate dehydrogenase, HCDR-3, DEAD/H box polypeptide 21 (DDX21), serine threonine kinase 15 (ARK2), transmembrane 4 superfamily member 1, or ERCC1, as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.
摘要翻译：本发明涉及细胞增殖的调控。更具体地，本发明涉及编码BRCA-1相关蛋白-1（BAP-1），核蛋白95（NP95），Fanconi贫血A组蛋白（FANCA），DEAD / H盒多肽9（DDX9）），胰岛素样生长因子1受体（IGF1R），泛素结合酶E2变体1（UBE2V1），醛脱氢酶，丙酮酸激酶，葡萄糖-6-磷酸脱氢酶，HCDR-3，DEAD / H盒多肽21（DDX21），丝氨酸苏氨酸激酶15（ARK2），跨膜4超家族成员1或ERCC1，其参与调节细胞周期停滞。本发明还涉及用于鉴定和使用包括小分子化学组合物，抗体，肽，环肽，核酸，RNAi，反义核酸和核酶在内的试剂的方法，其通过调节BRCA-1相关的调节细胞周期阻滞蛋白-1（BAP-1），核蛋白95（NP95），Fanconi贫血组A蛋白（FANCA），DEAD / H盒多肽9（DDX9），胰岛素样生长因子1受体（IGF1R），泛素缀合酶 E2变体1（UBE2V1），醛脱氢酶，丙酮酸激酶，葡萄糖-6-磷酸脱氢酶，HCDR-3，DEAD / H盒多肽21（DDX21），丝氨酸苏氨酸激酶15（ARK2），跨膜4超家族成员1或ERCC1 ，以及在与细胞周期调节和细胞增殖调节相关的诊断和治疗中使用表达谱和组合物，例如用于治疗癌症和其他细胞增殖疾病。

8. 发明申请

WO2003012125A9 MRE11: MODULATION OF CELLULAR PROLIFERATION 审中-公开
公开(公告)号：WO2003012125A9
公开(公告)日：2003-02-13
申请号：PCT/US2002/024422
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS, INC. , DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
发明人： DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： C12Q1/68 , C12N9/00 , C12N9/22 , C12N5/06 , A61K38/43 , A61K48/00

9. 发明申请

WO2003012055A3 SAK: MODULATION OF CELLULAR PROLIFERATION FOR TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2003012055A3
公开(公告)日：2003-02-13
申请号：PCT/US2002/024312
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS, INC. , DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
发明人： DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： C12Q1/68
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding SAK, which is a protein kinase involved in modulation of cellular proliferation and cell cycle regulation. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of SAK; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

10. 发明申请

WO2012094173A1 WHOLE BLOOD ASSAY FOR MEASURING AMPK ACTIVATION 审中-公开
标题翻译：用于测量AMPK激活的全血测定
公开(公告)号：WO2012094173A1
公开(公告)日：2012-07-12
申请号：PCT/US2011/066946
申请日：2011-12-22
申请人： RIGEL PHARMACEUTICALS, INC. , MARKOVSTOV, Vadim , HITOSHI, Yasumichi
发明人： MARKOVSTOV, Vadim , HITOSHI, Yasumichi
IPC分类号： G01N33/50 , C12N9/12
CPC分类号： G01N33/573 , G01N33/49 , G01N33/4915 , G01N33/5041 , G01N33/53 , G01N2333/912 , G01N2333/91205 , G01N2800/02
摘要： A method of sample analysis is provided. In certain embodiments, the method comprises: a) labeling cells of a blood sample using an antibody that specifically binds to phospho-AMPK or a phosphorylated target thereof, to produce a labeled sample; and b) measuring antibody binding by a population of blood cells of the labeled sample using flow cytometry. In particular embodiments, the method may further comprise, prior to the labeling step: contacting blood with a test agent ex vivo or in vivo ; and comparing the evaluation to results obtained from a reference sample of blood cells.
摘要翻译：提供了样品分析的方法。在某些实施方案中，所述方法包括：a）使用特异性结合磷酸化AMPK或其磷酸化靶标的抗体标记血液样品的细胞，以产生标记的样品; 和b）使用流式细胞术测量标记样品的血细胞群体的抗体结合。在具体实施方案中，该方法还可以包括在标记步骤之前：离体或体内使血液与测试试剂接触; 并将评估与从血细胞的参考样品获得的结果进行比较。

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