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1. 发明申请

US20180057478A1 AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME 审中-公开
公开(公告)号：US20180057478A1
公开(公告)日：2018-03-01
申请号：US15603023
申请日：2017-05-23
申请人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
发明人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
IPC分类号： C07D401/14 , C07D213/82 , C07D405/12 , C07D213/56 , C07D213/81 , C07D495/04 , C07D487/04 , C07D471/10 , C07D451/06 , C07D417/14 , C07D413/14 , C07D409/14 , C07D409/12 , C07D405/14 , C07D401/12 , C07D401/06 , C07D401/04
CPC分类号： C07D401/14 , C07B2200/07 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure 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.

2. 发明授权

US09005909B2 Whole blood assay for measuring AMPK activation 有权
标题翻译：用于测量AMPK活化的全血测定
公开(公告)号：US09005909B2
公开(公告)日：2015-04-14
申请号：US13333817
申请日：2011-12-21
申请人： Vadim Markovtsov , Yasumichi Hitoshi
发明人： Vadim Markovtsov , Yasumichi Hitoshi
IPC分类号： G01N33/573 , G01N33/49 , G01N33/53
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。

3. 发明申请

US20140315884A1 AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME 有权
标题翻译： AMPK活化杂环化合物及其使用方法
公开(公告)号：US20140315884A1
公开(公告)日：2014-10-23
申请号：US14325766
申请日：2014-07-08
申请人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
发明人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
IPC分类号： C07D495/04 , C07D213/82 , C07D471/10 , C07D401/14 , C07D417/14 , C07D413/14 , C07D405/14 , C07D401/04 , C07D451/06 , C07D487/04 , C07D401/12 , C07D409/12
CPC分类号： C07D401/14 , C07B2200/07 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure 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.
摘要翻译：公开了取代的吡啶化合物以及药物组合物和使用方法。一个实施方案是具有其中E，J，T，由“B”，T，R3，R4，w和x表示的环系统如本文所述的结构的化合物。在某些实施方案中，本文公开的化合物激活AMPK途径，并且可用于治疗与代谢有关的病症和病症。

4. 发明申请

US20120028954A1 Substituted Pyridine, Pyridazine, Pyrazine And Pyrimidine Compounds And Methods For Using The Same 有权
标题翻译：取代的吡啶，哒嗪，吡嗪和嘧啶化合物及其使用方法
公开(公告)号：US20120028954A1
公开(公告)日：2012-02-02
申请号：US13194810
申请日：2011-07-29
申请人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
发明人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
IPC分类号： A61K31/496 , C07D401/12 , C07D401/06 , C07D471/10 , C07D413/14 , C12N5/071 , A61K31/5377 , A61K31/4439 , A61K31/444 , A61P3/10 , A61P9/10 , A61P9/00 , C07D401/14 , A61K31/4545
CPC分类号： C07D401/14 , C07B2200/07 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure 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.
摘要翻译：公开了取代的吡啶化合物以及药物组合物和使用方法。一个实施方案是具有其中E，J，T，由“B”，T，R3，R4，w和x表示的环系统如本文所述的结构的化合物。在某些实施方案中，本文公开的化合物激活AMPK途径，并且可用于治疗与代谢有关的病症和病症。

5. 发明申请

US20100029505A1 shRNA library 有权
标题翻译： shRNA文库
公开(公告)号：US20100029505A1
公开(公告)日：2010-02-04
申请号：US12221325
申请日：2008-08-01
申请人： Donald G. Payan , Mary Shen , Simon Yu , Todd M. Kinsella , Yasumichi Hitoshi
发明人： Donald G. Payan , Mary Shen , Simon Yu , Todd M. Kinsella , Yasumichi Hitoshi
IPC分类号： C40B30/06 , C40B40/08 , C40B50/06 , C12P19/34 , C40B40/02
CPC分类号： C12N15/1093 , C12N15/66 , C12P19/34 , C40B40/08 , C40B50/06
摘要： As noted above, certain aspects of this disclosure relate to a library of nucleic acid vectors, as well as a method for making the same. In certain embodiments, the library of nucleic acid vectors comprises: a plurality of nucleic acid molecules of the following formula: S1—R—S2 wherein, in each nucleic acid of the plurality: S1 and S2 are each at least 15 nucleotides in length; S1 and S2 are complementary to each other along their entire length; either S1 or S2 is complementary along its entire length to a sequence in eukaryotic mRNA; and R is a six base recognition site for a restriction endonuclease; and wherein S1 and S2 vary in nucleotide sequence between different members of the plurality. A method for amplifying a circular nucleic acid is also provided.
摘要翻译：如上所述，本公开的某些方面涉及核酸载体文库以及其制备方法。在某些实施方案中，核酸载体文库包含：多个下式的核酸分子：S1-R-S2，其中在多个的每个核酸中，S1和S2的长度各自为至少15个核苷酸; S1和S2沿其整个长度彼此互补; S1或S2在其整个长度上与真核mRNA中的序列互补; R是限制性内切核酸酶的六碱基识别位点; 并且其中S1和S2在多个不同成员之间的核苷酸序列变化。还提供了扩增环状核酸的方法。

6. 发明申请

US20070128673A1 NP95: METHODS OF ASSAYING FOR CELL CYCLE MODULATORS 有权
标题翻译： NP95：细胞周期调节剂的测定方法
公开(公告)号：US20070128673A1
公开(公告)日：2007-06-07
申请号：US11460588
申请日：2006-07-27
申请人： Yasumichi Hitoshi , Yonchu Jenkins
发明人： Yasumichi Hitoshi , Yonchu Jenkins
IPC分类号： G01N33/574
CPC分类号： G01N33/5091 , C12Q1/6886 , C12Q2600/158 , G01N33/5008 , G01N33/5011 , G01N33/574 , G01N33/6872 , G01N2333/4703
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding NP95, which is 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 NP95; 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NP95的核酸，其涉及细胞周期停滞的调节。本发明还涉及用于鉴定和使用通过调节NP95来调节细胞周期阻滞的试剂，包括小分子化学组成，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。

7. 发明申请

US20060216299A1 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：US20060216299A1
公开(公告)日：2006-09-28
申请号：US10531492
申请日：2003-10-30
申请人： Yasumichi Hitoshi , David Anderson
发明人： Yasumichi Hitoshi , David Anderson
IPC分类号： A61K48/00 , C12Q1/68 , G01N33/574 , C07K14/82 , C07K7/64 , A61K39/395
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。

8. 发明授权

US08791136B2 Substituted pyridine, pyridazine, pyrazine and pyrimidine compounds and methods for using the same 有权
标题翻译：取代的吡啶，哒嗪，吡嗪和嘧啶化合物及其使用方法
公开(公告)号：US08791136B2
公开(公告)日：2014-07-29
申请号：US13194810
申请日：2011-07-29
申请人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
发明人： Dane Goff , Donald Payan , Rajinder Singh , Simon Shaw , David Carroll , Yasumichi Hitoshi
IPC分类号： A61K31/4427 , C07D401/14
CPC分类号： C07D401/14 , C07B2200/07 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/06 , C07D471/10 , C07D487/04 , C07D495/04
摘要： Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure 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.
摘要翻译：公开了取代的吡啶化合物以及药物组合物和使用方法。一个实施方案是具有其中E，J，T，由“B”，T，R3，R4，w和x表示的环系统如本文所述的结构的化合物。在某些实施方案中，本文公开的化合物激活AMPK途径，并且可用于治疗与代谢有关的病症和病症。

9. 发明授权

US08546433B2 Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer 有权
标题翻译：用于联合治疗用于预防，治疗或治疗转移性癌症的Axl抑制剂
公开(公告)号：US08546433B2
公开(公告)日：2013-10-01
申请号：US12688746
申请日：2010-01-15
申请人： Yasumichi Hitoshi , Sacha Holland , Donald G. Payan
发明人： Yasumichi Hitoshi , Sacha Holland , Donald G. Payan
IPC分类号： A01N43/64 , A61K31/41 , C07D413/00
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.
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Axl抑制剂。

10. 发明授权

US07413870B2 SAK: modulation of cellular proliferation for treatment of cancer 失效
标题翻译： SAK：调节细胞增殖治疗癌症
公开(公告)号：US07413870B2
公开(公告)日：2008-08-19
申请号：US10026021
申请日：2001-12-21
申请人： Yasumichi Hitoshi , Susan Demo , Yonchu Jenkins
发明人： Yasumichi Hitoshi , Susan Demo , Yonchu Jenkins
IPC分类号： C12Q1/50
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。

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