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1. 发明申请

WO2012064897A3 BICYCLIC AND TRICYCLIC INHIBITORS OF SUMOYLATION ENZYMES AND METHODS FOR THEIR USE 审中-公开
公开(公告)号：WO2012064897A3
公开(公告)日：2012-05-18
申请号：PCT/US2011/060063
申请日：2011-11-09
申请人： CHEN, Yuan , LI, Yi-Jia
发明人： CHEN, Yuan , LI, Yi-Jia
IPC分类号： A61K31/40 , C07D209/56
摘要： This invention relates to bicyclic and tricyclic SUMOylation inhibitor compounds and methods for inhibiting a SUMOylation enzymes including SUMO E1 and SUMO E2 in a cell, especially for treating cancer, degenerative diseases and viral infections. Such a method may include administering an effective amount of a pharmaceutical composition containing the described herein to a subject having the cancer. The pharmaceutical composition may include a SUMOylation inhibitor compound as described herein. In some embodiments, the method for treating a disease may further comprise administering one or more DNA damaging therapies in combination with administration of the pharmaceutical composition.

2. 发明申请

WO2012064897A2 BICYCLIC AND TRICYCLIC INHIBITORS OF SUMOYLATION ENZYMES AND METHODS FOR THEIR USE 审中-公开
标题翻译：磺酰化酶的双相和三聚体抑制剂及其使用方法
公开(公告)号：WO2012064897A2
公开(公告)日：2012-05-18
申请号：PCT/US2011060063
申请日：2011-11-09
申请人： CHEN YUAN , LI YI-JIA
发明人： CHEN YUAN , LI YI-JIA
IPC分类号： A61K31/4985
CPC分类号： C07D487/04 , A61K31/34 , A61K31/555 , A61K33/24 , A61K41/00 , A61K45/06 , C07D493/08 , A61K2300/00
摘要： According to the embodiments described herein, a tricyclic SUMOylation inhibitor compound is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer is provided. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a SUMOylation inhibitor compound. In some embodiments, the method for treating a disease may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition.
摘要翻译：根据本文所述的实施方案，提供三环SUMO化抑制剂化合物。在一些实施方案中，提供了抑制细胞中SUMO化酶的方法。这种方法可以包括向细胞施用SUMO化抑制剂化合物。在一些方面，SUMO化酶是SUMO E1或SUMO E2。在一些方面，该方法可以用于体外抑制癌细胞（例如，在培养中生长）或体内（例如作为受试者的肿瘤的一部分）。在其它实施方案中，提供了治疗癌症的方法。这种方法可以包括向具有癌症的受试者施用有效量的药物组合物。药物组合物可以包括SUMO化抑制剂化合物。在一些实施方案中，用于治疗疾病的方法还可包括与药物组合物的施用组合施用一种或多种DNA损伤性治疗。

3. 发明申请

WO2012064887A1 INHIBITORS OF DESUMOYLATION ENZYMES AND METHODS FOR THEIR USE 审中-公开
标题翻译：脱乙酰壳多糖的抑制剂及其使用方法
公开(公告)号：WO2012064887A1
公开(公告)日：2012-05-18
申请号：PCT/US2011/060052
申请日：2011-11-09
申请人： CHEN, Yuan , ZAIA, John , LI, Shirley , LI, Yi-Jia , SU, Yang , WONG, Steven
发明人： CHEN, Yuan , ZAIA, John , LI, Shirley , LI, Yi-Jia , SU, Yang , WONG, Steven
IPC分类号： A01N33/26 , A61K31/655
CPC分类号： A61K31/655 , A61K45/06 , C07C309/46 , C07C309/47
摘要： In one embodiment, a deSUMOylation inhibitor is provided. In another embodiment, a method for inhibiting infectivity of a retrovirus is provided. The method may include administering an effective amount of a deSUMOylation inhibitor compound to one or more immune cells. In some embodiments, the retrovirus is human immunodeficiency virus (HIV). In another embodiment, methods for treating HIV are provided. Such methods may include administering an effective amount of a pharmaceutical compound to a subject having HIV or is at risk of being infected with HIV. The pharmaceutical composition may comprise a deSUMOylation inhibitor described herein. In some embodiments, the treatment is a preventative treatment. In some embodiments, the methods for treating HIV may further comprise administering a highly active anti-retroviral therapy (HAART) regimen in combination with the pharmaceutical composition. A HAART regimen may include three or more active anti-retroviral medivations (ARVs).
摘要翻译：在一个实施方案中，提供了脱硫酸抑制剂。在另一个实施方案中，提供了用于抑制逆转录病毒感染性的方法。该方法可以包括向一种或多种免疫细胞施用有效量的deSUMO化抑制剂化合物。在一些实施方案中，逆转录病毒是人免疫缺陷病毒（HIV）。在另一个实施方案中，提供了用于治疗HIV的方法。这样的方法可以包括向具有HIV的受试者施用有效量的药物化合物，或者有被HIV感染的风险。药物组合物可以包含本文所述的脱硫酸抑制剂。在一些实施方案中，治疗是预防性治疗。在一些实施方案中，用于治疗HIV的方法可进一步包括与药物组合物组合施用高活性抗逆转录病毒疗法（HAART）方案。 HAART方案可以包括三种或更多种活性抗逆转录病毒介质（ARV）。

4. 发明申请

WO2012064898A1 SINGLETON INHIBITORS OF SUMOYLATION ENZYMES AND METHODS FOR THEIR USE 审中-公开
标题翻译：磺化酶的辛德龙抑制剂及其使用方法
公开(公告)号：WO2012064898A1
公开(公告)日：2012-05-18
申请号：PCT/US2011/060064
申请日：2011-11-09
申请人： CHEN, Yuan , LI, Yi-Jia
发明人： CHEN, Yuan , LI, Yi-Jia
IPC分类号： A01N43/00
CPC分类号： C07D487/04 , A61K31/34 , A61K31/555 , A61K33/24 , A61K41/00 , A61K45/06 , C07D493/08 , A61K2300/00
摘要： According to the embodiments described herein, a SUMOylation inhibitor compound comprising a singleton scaffold is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer, degenerative diseases and viral infection is provided,. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a singleton SUMOylation inhibitor compound. In some embodiments, the method for treating a cancer may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition.
摘要翻译：根据本文所述的实施方案，提供了包含单体支架的SUMO化抑制剂化合物。在一些实施方案中，提供了抑制细胞中SUMO化酶的方法。这种方法可以包括向细胞施用SUMO化抑制剂化合物。在一些方面，SUMO化酶是SUMO E1或SUMO E2。在一些方面，该方法可以用于体外抑制癌细胞（例如，在培养中生长）或体内（例如作为受试者的肿瘤的一部分）。在其它实施方案中，提供了治疗癌症，退行性疾病和病毒感染的方法。这种方法可以包括向具有癌症的受试者施用有效量的药物组合物。药物组合物可以包括单一SUMO化抑制剂化合物。在一些实施方案中，用于治疗癌症的方法可进一步包括与药物组合物的施用组合施用一种或多种DNA损伤性治疗。

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