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21. 发明公开

EP2598483A1 AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME 无效
标题翻译： AMPK激活杂环化合物和使用方法
公开(公告)号：EP2598483A1
公开(公告)日：2013-06-05
申请号：EP11746709.2
申请日：2011-07-29
申请人： Rigel Pharmaceuticals, Inc.
发明人： GOFF, Dane , PAYAN, Donald , SINGH, Rajinder , SHAW, Simon , CARROLL, David , HITOSHI, Yasumichi
IPC分类号： C07D213/82 , C07D295/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61P3/10 , A61P9/10
摘要： wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

22. 发明公开

EP1573026A2 MRE11: MODULATION OF CELLULAR PROLIFERATION 审中-公开
标题翻译： MRE11：调制细胞增殖
公开(公告)号：EP1573026A2
公开(公告)日：2005-09-14
申请号：EP02791559.4
申请日：2002-07-31
申请人： Rigel Pharmaceuticals, Inc.
发明人： DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： C12Q1/00
CPC分类号： C12Q1/34 , G01N33/5011 , G01N33/573 , G01N2333/922 , G01N2500/02

23. 发明公开

EP1497461A2 METHODS OF ASSAYING FOR CELL CYCLE MODULATORS 审中-公开
标题翻译：检验方法对细胞周期调节剂
公开(公告)号：EP1497461A2
公开(公告)日：2005-01-19
申请号：EP03719802.5
申请日：2003-04-15
申请人： Rigel Pharmaceuticals, Inc.
发明人： HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： C12Q1/68
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.

24. 发明授权

EP2387395B1 AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER 有权
标题翻译： AXL抑制剂用于联合疗法预防，治疗或处理转移性肿瘤组织
公开(公告)号：EP2387395B1
公开(公告)日：2014-10-15
申请号：EP10700686.8
申请日：2010-01-15
申请人： Rigel Pharmaceuticals, Inc.
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

25. 发明公开

EP2661621A1 WHOLE BLOOD ASSAY FOR MEASURING AMPK ACTIVATION 有权
标题翻译：全血测试测量AMPK的活化
公开(公告)号：EP2661621A1
公开(公告)日：2013-11-13
申请号：EP11811474.3
申请日：2011-12-22
申请人： Rigel Pharmaceuticals, Inc.
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.

26. 发明公开

EP2387395A1 AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER 有权
标题翻译： AXL抑制剂用于联合疗法预防，治疗或处理转移性肿瘤组织
公开(公告)号：EP2387395A1
公开(公告)日：2011-11-23
申请号：EP10700686.8
申请日：2010-01-15
申请人： Rigel Pharmaceuticals, Inc.
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 Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents.

27. 发明授权

EP2598483B1 AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME 无效
公开(公告)号：EP2598483B1
公开(公告)日：2020-07-29
申请号：EP11746709.2
申请日：2011-07-29
申请人： Rigel Pharmaceuticals, Inc.
发明人： GOFF, Dane , PAYAN, Donald , SINGH, Rajinder , SHAW, Simon , CARROLL, David , HITOSHI, Yasumichi
IPC分类号： C07D213/82 , C07D295/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61P3/10 , A61P9/10

28. 发明公开

EP3500558A1 BENZIMIDAZOLE DIRECT AMPK ACTIVATORS 有权
公开(公告)号：EP3500558A1
公开(公告)日：2019-06-26
申请号：EP17758349.9
申请日：2017-08-15
申请人： Rigel Pharmaceuticals, Inc.
发明人： SHAW, Simon , XU, Xiang , ISSAKANI, Sarkiz , SINGH, Rajinder , HITOSHI, Yasumichi , DUNCTON, Matthew , LIN, Nan
IPC分类号： C07D235/26 , C07D403/04 , C07D403/12 , A61K31/41 , A61K31/4184 , A61P3/10 , A61P9/00

29. 发明授权

EP1549760B1 SAK: MODULATION OF CELLULAR PROLIFERATION FOR TREATMENT OF CANCER 有权
标题翻译： SAK：调制癌症治疗的细胞增殖
公开(公告)号：EP1549760B1
公开(公告)日：2008-12-31
申请号：EP02750377.0
申请日：2002-07-31
申请人： Rigel Pharmaceuticals, Inc.
发明人： DEMO, Susan , HITOSHI, Yasumichi , JENKINS, Yonchu
IPC分类号： C12Q1/68 , C12Q1/48 , G01N33/53 , A61K39/395 , A61K48/00
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.

30. 发明公开

EP1576173A2 MODULATORS OF CELLULAR PROLIFERATION 审中-公开
标题翻译：细胞增殖的调节剂
公开(公告)号：EP1576173A2
公开(公告)日：2005-09-21
申请号：EP03764711.2
申请日：2003-07-14
申请人： Rigel Pharmaceuticals, Inc.
发明人： HITOSHI, Yasumichi , JENKINS, Yonchu , MARKOVTSOV, Vadim
IPC分类号： C12Q1/00
CPC分类号： G01N33/5011
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.

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