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1. 发明申请

US20120258975A1 Potent Small Molecule Inhibitors of Autophagy, and Methods of Use Thereof 审中-公开
标题翻译：自噬的强力小分子抑制剂及其使用方法
公开(公告)号：US20120258975A1
公开(公告)日：2012-10-11
申请号：US13382572
申请日：2010-07-21
申请人： Junying Yuan , Dawei Ma , Junli Liu , Lihong Zhang
发明人： Junying Yuan , Dawei Ma , Junli Liu , Lihong Zhang
IPC分类号： A61K31/517 , A61P35/00 , A61P29/00 , A61P31/00 , C07D471/04 , A61P1/18 , A61P31/04 , A61P31/12 , C12N9/99 , A61K31/519 , C07D239/94 , A61P25/28
CPC分类号： C07D239/94 , C07D239/88 , C07D239/93 , C07D401/12 , C07D405/12 , C07D417/12 , C07D471/04
摘要： Certain aspects of the invention relates to small molecule autophagy inhibitors of the formula (I), and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity. (I)
摘要翻译：本发明的某些方面涉及式（I）的小分子自噬抑制剂及其用于治疗和预防癌症和急性胰腺炎的用途。如本文所公开的，已知生物活性文库中的基于图像的筛选鉴定了小分子自噬抑制剂。发现这种自噬抑制剂通过促进起始自噬所需的III型PI3激酶复合物的降解起作用。药物化学研究导致小分子自噬抑制剂具有改善的效力和选择性。（一世）

2. 发明申请

US20100267704A1 Autophagy Inducing Compounds and Uses Thereof in Treating Autophagy Associated Diseases 审中-公开
标题翻译：自噬诱导化合物及其用途治疗自噬相关疾病
公开(公告)号：US20100267704A1
公开(公告)日：2010-10-21
申请号：US12682468
申请日：2008-10-10
申请人： Junying Yuan , Dawei Ma , Lihong Zhang
发明人： Junying Yuan , Dawei Ma , Lihong Zhang
IPC分类号： A61K31/541 , C07D211/06 , A61K31/445 , C07D307/77 , A61K31/343 , C07D401/12 , A61K31/4545 , C07D401/04 , A61K31/454 , C07D213/80 , A61K31/44 , C07D491/16 , A61K31/407 , C07D487/10 , A61K31/438 , C07D417/06 , C12N5/02 , A61P25/28 , A61P25/16 , A61P35/00
CPC分类号： C07D211/44 , A61K31/445 , C07D211/82 , C07D401/12 , C07D491/22
摘要： This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.
摘要翻译：本发明涉及治疗由错误折叠的蛋白质聚集体引起的疾病的一类自噬诱导化合物和用于鉴定这些化合物的筛选方法。

3. 发明授权

US07491743B2 Inhibitors of cellular necrosis 有权
标题翻译：细胞坏死的抑制剂
公开(公告)号：US07491743B2
公开(公告)日：2009-02-17
申请号：US10930690
申请日：2004-08-30
申请人： Gregory D. Cuny , Junying Yuan , Prakash Jagtap , Alexei Degterev
发明人： Gregory D. Cuny , Junying Yuan , Prakash Jagtap , Alexei Degterev
IPC分类号： A61K31/415 , C07D403/02
CPC分类号： C07D409/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07D471/04
摘要： The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.
摘要翻译：本发明涉及化合物和药物制剂及其在预防或治疗与细胞死亡有关的创伤，缺血，中风和退行性疾病的治疗中的用途。本发明的方法和组合物特别可用于治疗与细胞坏死相关的神经障碍。

4. 发明授权

US07390836B2 Small molecules used to increase cell death 失效
标题翻译：小分子用于增加细胞死亡
公开(公告)号：US07390836B2
公开(公告)日：2008-06-24
申请号：US11606583
申请日：2006-11-30
申请人： Junying Yuan , Alexei Degterev , Timothy J. Mitchison
发明人： Junying Yuan , Alexei Degterev , Timothy J. Mitchison
IPC分类号： A61K31/167
CPC分类号： A61K31/10 , A61K31/167
摘要： The invention features methods for increasing cell death. The invention also features compounds used to increase cell death. The invention further features methods for identifying compounds that increase cell death.
摘要翻译：本发明的特征在于增加细胞死亡的方法。本发明还涉及用于增加细胞死亡的化合物。本发明还涉及鉴定增加细胞死亡的化合物的方法。

5. 发明申请

US20070219277A1 Small molecules used to increase cell death 失效
标题翻译：小分子用于增加细胞死亡
公开(公告)号：US20070219277A1
公开(公告)日：2007-09-20
申请号：US11606583
申请日：2006-11-30
申请人： Junying Yuan , Alexei Degterev , Timothy Mitchison
发明人： Junying Yuan , Alexei Degterev , Timothy Mitchison
IPC分类号： A61K31/10 , C12N5/06 , C12N5/08
CPC分类号： A61K31/10 , A61K31/167
摘要： The invention features methods for increasing cell death. The invention also features compounds used to increase cell death. The invention further features methods for identifying compounds that increase cell death.
摘要翻译：本发明的特征在于增加细胞死亡的方法。本发明还涉及用于增加细胞死亡的化合物。本发明还涉及鉴定增加细胞死亡的化合物的方法。

6. 发明授权

US07071302B1 Cloning sequencing and characterization of two cell death genes and uses therefor 失效
公开(公告)号：US07071302B1
公开(公告)日：2006-07-04
申请号：US09577897
申请日：2000-05-24
申请人： H. Robert Horvitz , Junying Yuan , Shai Shaham
发明人： H. Robert Horvitz , Junying Yuan , Shai Shaham
IPC分类号： C07K14/00 , C12N15/00 , C12N15/63
CPC分类号： C12N9/6475 , A61K38/00 , C07K14/43581 , C07K14/4747
摘要： Described herein are genes shown to be essential for programmed cell death in C. elegans, their encoded products (RNA and polypeptides), antibodies directed against the encoded polypeptides; probes for identifying structurally related genes and bioassays for identifying functionally related cell death genes from various organisms; methods and agents for altering (increasing or decreasing) the activity of the cell death-genes and, thus, of altering cell death; and uses therefor. Specifically, two genes shown to be essential for almost all of the cell deaths which occur in the development of C. elegans, referred to as ced-3 and ced-4, have been cloned, sequenced and characterized.

7. 发明授权

US06939850B2 Altered human interleukin-1β convertase (ICE), NEDD-2, and C. elegans ced-3 polypeptides and uses therefor 失效
标题翻译：改变人白细胞介素-1β转换酶（ICE），NEDD-2和秀丽隐杆线虫ced-3多肽，并用于其
公开(公告)号：US06939850B2
公开(公告)日：2005-09-06
申请号：US09888243
申请日：2001-06-22
申请人： H. Robert Horvitz , Junying Yuan , Shai Shaham
发明人： H. Robert Horvitz , Junying Yuan , Shai Shaham
IPC分类号： A61K38/00 , A61K38/55 , C07K14/435 , C07K14/47 , C12N9/64 , C12Q1/68 , A61K38/43
CPC分类号： C12N9/641 , A61K38/00 , C07K14/43581 , C07K14/4747 , C07K2319/00 , C12N9/6475 , C12Q1/6876 , C12Q2600/156 , C12Y304/22036 , C12Y304/22055
摘要： Described herein is the discovery that human interleukin-1β convertase (ICE) is structurally similar to the protein encoded by the C. elegans cell death gene, ced-3. Comparative and mutational analyses of the two proteins, together with previous observations, suggest that the Ced-3 protein may be a cysteine protease like ICE and that ICE may be a human equivalent of the nematode cell death gene. Another mammalian protein, the murine NEDD-2 protein, was also found to be similar to Ced-3. The NEDD-2 gene is implicated in the development of the murine central nervous system. On the basis of these findings, novel drugs for enhancing or inhibiting the activity of ICE, ced-3, or related genes are provided. Such drugs may be useful for treating inflammatory diseases and/or diseases characterized by cell deaths, as well as cancers, autoimmune disorders, infections, and hair growth and hair loss. Furthermore, such drugs may be useful for controlling pests, parasites and genetically engineered organisms. Furthermore, novel inhibitors of the activity of ced-3, ICE and related genes are described which comprise portions of the genes or their encoded products.
摘要翻译：本文描述了人白细胞介素-1β转化酶（ICE）在结构上类似于由线虫类细胞死亡基因ced-3编码的蛋白质的发现。两种蛋白质的比较和突变分析结合以前的观察结果表明，Ced-3蛋白可能是像ICE这样的半胱氨酸蛋白酶，并且ICE可能是人类等效于线虫细胞死亡基因。还发现另一种哺乳动物蛋白，鼠类NEDD-2蛋白质与Ced-3相似。 NEDD-2基因涉及鼠中枢神经系统的发展。在这些发现的基础上，提供了用于增强或抑制ICE，ced-3或相关基因活性的新型药物。这些药物可用于治疗以细胞死亡为特征的炎性疾病和/或疾病，以及癌症，自身免疫性疾病，感染和毛发生长和脱发。此外，这些药物可用于控制害虫，寄生虫和遗传工程生物体。此外，描述了包含部分基因或其编码产物的ced-3，ICE和相关基因的活性的新型抑制剂。

8. 发明授权

US09643977B2 Necroptosis inhibitors and methods of use therefor 有权
公开(公告)号：US09643977B2
公开(公告)日：2017-05-09
申请号：US14004474
申请日：2012-03-12
申请人： Junying Yuan
发明人： Junying Yuan
IPC分类号： C07D403/06 , C07D495/04 , C07D417/12 , C07D487/04 , C07D209/82 , C07D231/14 , C07D231/40 , C07D233/56 , C07D235/30 , C07D237/18 , C07D409/06 , C07D261/14 , C07D263/58 , C07D277/46 , C07D277/54 , C07C211/52 , C07C235/38 , C07D215/08 , C07D261/20 , C07D403/12 , C07D405/06
CPC分类号： C07D495/04 , C07C211/52 , C07C235/38 , C07D209/82 , C07D215/08 , C07D231/14 , C07D231/40 , C07D233/56 , C07D235/30 , C07D237/18 , C07D261/14 , C07D261/20 , C07D263/58 , C07D277/46 , C07D277/54 , C07D403/06 , C07D403/12 , C07D405/06 , C07D409/06 , C07D417/12 , C07D487/04
摘要： Described herein are compositions that inhibit the production of TNFα downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNFα production or CD40 activation.

9. 发明申请

US20120315244A1 Methods for Modulation of Autophagy Through the Modulation of Autophagy-Inhibiting Gene Products 审中-公开
标题翻译：通过调节自噬抑制基因产物调节自噬的方法
公开(公告)号：US20120315244A1
公开(公告)日：2012-12-13
申请号：US13499313
申请日：2010-09-30
申请人： Junying Yuan , Marta M. Lipinski
发明人： Junying Yuan , Marta M. Lipinski
IPC分类号： A61K31/713 , A61P25/28 , A61K38/19 , A61P5/00 , C12Q1/02 , C12N5/071 , A61P35/00
CPC分类号： C12N15/113 , C07K16/22 , C07K16/24 , C12N5/0618 , C12N2310/14 , C12N2320/10 , C12N2320/30 , G01N33/502
摘要： The present disclosure relates to methods for the modulation of autophagy and the treatment of autophagy-related diseases, including cancer, neurodegenerative diseases and pancreatitis.
摘要翻译：本公开涉及调节自噬和治疗包括癌症，神经变性疾病和胰腺炎在内的自噬相关疾病的方法。

10. 发明申请

US20100087453A1 COMPOUNDS, SCREENS, AND METHODS OF TREATMENT 审中-公开
标题翻译：化合物，筛选和治疗方法
公开(公告)号：US20100087453A1
公开(公告)日：2010-04-08
申请号：US12444822
申请日：2007-10-09
申请人： Junying Yuan , Chengye Yuan , Alexei Degterev
发明人： Junying Yuan , Chengye Yuan , Alexei Degterev
IPC分类号： A61K31/519 , C07D239/00 , C07D491/14 , A61K31/505 , A61P25/28
CPC分类号： C07D495/04
摘要： The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associated with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described.
摘要翻译：本发明的特征在于具有式（I）的化合物，药物组合物，合成方法和用于治疗与细胞坏死有关的疾病和病症的方法。还描述了用于鉴定用于治疗这些病症的化合物的筛选测定。

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