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1. 发明申请

WO2015048547A3 METHODS FOR USING AND BIOMARKERS FOR AMPK-ACTIVATING COMPOUNDS 审中-公开
标题翻译： AMPK活化化合物的使用和生物标志物的方法
公开(公告)号：WO2015048547A3
公开(公告)日：2015-06-18
申请号：PCT/US2014057861
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 , A61K31/4427 , A61K31/501 , A61K31/5377
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, D1, D2, D3, the ring system denoted by "B", T, R3, R4, w and x are as described herein.
摘要翻译：公开了使用AMPK活化化合物的方法，例如用于治疗癌症和血管血流障碍。还公开了AMPK的生物标志物及其用途，例如在诊断和治疗AMPK相关疾病中的用途。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，在此描述。

2. 发明申请

WO2004007754A2 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：WO2004007754A2
公开(公告)日：2004-01-22
申请号：PCT/US0322164
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： G01N33/50 , C12Q
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 zeta (PKC-zeta), phospholipase C-beta1 (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 zeta (PKC-zeta), 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.
摘要翻译：本发明涉及细胞增殖的调控。更具体地，本发明涉及编码蛋白激酶C zeta（PKC-zeta），磷脂酶C-β1（PLC-β1），蛋白酪氨酸激酶2（FAK），蛋白酪氨酸激酶2b（FAK2），酪蛋白激酶 2（CK2），cMET酪氨酸激酶（cMET），皮瓣结构特异性内切核酸酶1（FEN1），REV1 dCMP转移酶（REV1），无泛素/无嘧啶核酸酶1（APE1），细胞周期蛋白依赖性激酶3（CDK3），细胞分裂周期7激酶（CDC7L1），细胞周期蛋白依赖性激酶7（CDK7），细胞因子诱导型激酶（CNK），潜在的异戊烯基化蛋白酪氨酸磷酸酶（PRL-3），丝氨酸苏氨酸激酶2（STK2）或（NEK4）丝氨酸苏氨酸激酶（NKIAMRE）或组蛋白乙酰化酶（HBO1），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成，抗体，肽，环肽，核酸，RNAi，反义核酸和核酶在内的试剂的方法，其通过调节蛋白激酶Cζ来调节细胞周期停滞 PKC-zeta），磷脂酶C-β1（PLC-β1），蛋白酪氨酸激酶2（FAK），蛋白酪氨酸激酶2b（FAK2），酪蛋白激酶2（CK2），cMET酪氨酸激酶（cMET），皮瓣结构特异性内切核酸酶1 （CD1），细胞周期蛋白依赖激酶3（CDK3），PIM1激酶（PIM1），细胞分裂周期7激酶（CDC7L1），细胞周期蛋白依赖性激酶7（CDK7），细胞周期蛋白依赖激酶7 ，细胞因子诱导型激酶（CNK），潜在的异戊烯基化蛋白酪氨酸磷酸酶（PRL-3），丝氨酸苏氨酸激酶2（STK2）或（NEK4），细胞周期蛋白依赖丝氨酸苏氨酸激酶（NKIAMRE）或组蛋白乙酰化酶（HBO1）在诊断中使用表达谱和组成涉及细胞周期调节和调节细胞增殖的治疗，例如用于治疗癌症和其它细胞增殖疾病。

3. 发明申请

WO02101072A8 LETM1: MODULATORS OF CELLULAR PROLIFERATION 审中-公开
标题翻译： LETM1：细胞增殖的调节剂
公开(公告)号：WO02101072A8
公开(公告)日：2003-09-04
申请号：PCT/US0217533
申请日：2002-05-31
申请人： RIGEL PHARMACEUTICALS INC , DEMO SUSAN , HITOSHI YASUMICHI , PEARSALL DENISE
发明人： DEMO SUSAN , HITOSHI YASUMICHI , PEARSALL DENISE
IPC分类号： C07K14/47 , G01N33/574 , C12Q
CPC分类号： C07K14/47 , G01N33/574 , G01N2333/705 , G01N2500/04
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding LETM1 ("leucine zipper EF hand transmembrane receptor"), which is 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, siRNA, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of LETM1 and LETM1 related signal transduction; 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.
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LETM1（“亮氨酸拉链EF手跨膜受体”）的核酸，其涉及细胞增殖和细胞周期调节的调节。本发明还涉及用于鉴定和使用包括小分子化学组成，抗体，siRNA，反义核酸和核酶的试剂的方法，其通过调节LETM1和LETM1相关信号转导来调节细胞周期调节和细胞增殖; 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。

4. 发明申请

WO02101072A2 LETM1: MODULATORS OF CELLULAR PROLIFERATION 审中-公开
标题翻译： LETM1：细胞增殖的调节剂
公开(公告)号：WO02101072A2
公开(公告)日：2002-12-19
申请号：PCT/US0217533
申请日：2002-05-31
申请人： RIGEL PHARMACEUTICALS INC , DEMO SUSAN , HITOSHI YASUMICHI , PEARSALL DENISE
发明人： DEMO SUSAN , HITOSHI YASUMICHI , PEARSALL DENISE
IPC分类号： C07K14/47 , G01N33/574 , C12Q
CPC分类号： C07K14/47 , G01N33/574 , G01N2333/705 , G01N2500/04
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding LETM1 ("leucine zipper EF hand transmembrane receptor"), which is 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, siRNA, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of LETM1 and LETM1 related signal transduction; 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.
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LETM1（“亮氨酸拉链EF手跨膜受体”）的核酸，其涉及细胞增殖和细胞周期调节的调节。本发明还涉及用于鉴定和使用包括小分子化学组成，抗体，siRNA，反义核酸和核酶的试剂的方法，其通过调节LETM1和LETM1相关信号转导来调节细胞周期调节和细胞增殖; 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。

5. 发明专利

JP2015007135A 転移性癌の予防、治療、または管理のための併用療法に用いるためのＡＸＬ阻害薬审中-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：JP2015007135A
公开(公告)日：2015-01-15
申请号：JP2014208912
申请日：2014-10-10
申请人：ライジェルファーマシューティカルズ, インコーポレイテッド , Rigel Pharmaceuticals Inc , ライジェルファーマシューティカルズ, インコーポレイテッド
发明人： HITOSHI YASUMICHI , SACHA HOLLAND , PAYAN DONALD G
IPC分类号： A61K45/06 , A61K31/502 , A61K33/24 , A61P35/00 , A61P35/04 , A61P43/00
CPC分类号： A61K31/502 , A61K31/4196 , A61K33/24 , A61K45/06 , C07D403/04 , C07D403/14 , A61K2300/00
摘要：【課題】本発明は、Axl阻害薬を用いる現行の単剤療法またはその他の併用療法よりも優れた治療プロファイルが得られる併用療法を提供することを課題とする。【解決手段】治療的または予防的有効量のAxl阻害薬、および治療的または予防的有効量の1もしくは2つ以上の化学療法薬を含む、癌の予防、治療、または管理のための医薬を提供する。【選択図】なし
摘要翻译：要解决的问题：提供与使用Ax1抑制剂的当前单一药物疗法或其他组合疗法相比提供更好治疗特征的组合疗法。解决方案：本发明提供用于预防，治疗或治疗转移性癌症的药物，其包含治疗或预防有效量的 Axl抑制剂和治疗或预防有效量的一种或多种化学治疗剂。

6. 发明专利

PL2598483T3 ZWIĄZKI HETEROCYKLICZNE AKTYWUJĄCE AMPK I SPOSOBY ICH ZASTOSOWANIA 未知
公开(公告)号：PL2598483T3
公开(公告)日：2020-12-28
申请号：PL11746709
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 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61P3/10 , A61P9/10 , C07D295/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10

8. 发明专利

CA2823582A1 WHOLE BLOOD ASSAY FOR MEASURING AMPK ACTIVATION 未知
公开(公告)号：CA2823582A1
公开(公告)日：2012-07-12
申请号：CA2823582
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
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.

9. 发明专利

AU2003290557A1 CELL CYCLE TARGETS AND PEPTIDES 未知
公开(公告)号：AU2003290557A1
公开(公告)日：2004-06-07
申请号：AU2003290557
申请日：2003-10-30
申请人： RIGEL PHARMACEUTICALS INC
发明人： HITOSHI YASUMICHI , ANDERSON DAVID
IPC分类号： C07K20060101
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.

10. 发明专利

AU2003249284A1 MODULATORS OF CELLULAR PROLIFERATION 未知
公开(公告)号：AU2003249284A1
公开(公告)日：2004-02-02
申请号：AU2003249284
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： G01N33/50
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 zeta (PKC-zeta), phospholipase C-beta1 (PLC-beta1), 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 zeta (PKC-zeta), phospholipase C-beta1 (PLC-beta1), 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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