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1. 发明申请

US20140140931A1 ANTIOXIDANT, NEUROPROTECTIVE AND ANTINEOPLASTIC NANOPARTICLES COMPRISING A THERAPEUTIC AGENT ON AN AMPHIPHILIC SPACER OR AN AMPHIPHILIC POLYMER 审中-公开
标题翻译：抗氧化剂，包含治疗药物的神经保护和抗原性纳米颗粒在AMPHIPHILIC间隔剂或AMPHIPHILIC聚合物
公开(公告)号：US20140140931A1
公开(公告)日：2014-05-22
申请号：US14232871
申请日：2012-07-27
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K47/48 , A61K49/00
CPC分类号： A61K47/55 , A61K9/5123 , A61K38/00 , A61K49/0032 , A61K49/0052
摘要： This invention relates to antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer. Methods of synthesizing the antioxidant derivatives of camptothecin and anti-oxidant derivatives of camptothecin analogs, NSAIDs and statins, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant, neuroprotective and anti-neoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these neuroprotective and anti-neoplastic nanoparticles for the preparation of delivery devices of other pharmaceuticals and/or drugs.
摘要翻译：本发明涉及包含在两亲性间隔物或两亲性聚合物上的治疗剂的抗氧化剂，神经保护和抗肿瘤纳米颗粒。合成喜树碱的抗氧化剂衍生物和喜树碱类似物的抗氧化衍生物，NSAIDs和他汀类药物的自发乳化或纳米沉淀以产生抗氧化剂，神经保护和抗肿瘤纳米颗粒的方法，其包含在两亲性间隔基或两亲性聚合物上的治疗剂及其还提供用于治疗癌性疾病。本发明的另一方面是这些神经保护和抗肿瘤纳米颗粒在制备其它药物和/或药物的递送装置中的用途。

2. 发明授权

US08318795B2 Antioxidant polymers containing [1,2]-dithiolane moieties and uses thereof 有权
标题翻译：含有[1,2] - 二硫醇烷部分的抗氧化聚合物及其用途
公开(公告)号：US08318795B2
公开(公告)日：2012-11-27
申请号：US12528067
申请日：2008-02-29
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K31/385 , C07D339/04
CPC分类号： C07D339/04 , C08B37/003
摘要： The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.
摘要翻译：本发明描述了能够作为自由基，金属和活性氧的清除剂的1,2-二硫戊环的聚合物。还描述了合成抗氧化剂1,2-二硫戊环衍生物和其聚合以生产可生物降解的抗氧化聚合物的方法。本发明的抗氧化聚合物可用于治疗由氧化应激和其他自由基介导的病症引起的疾病或病症。抗氧化聚合物也可用于制备治疗剂的抗氧化剂颗粒递送装置。

3. 发明申请

US20110300187A1 ANTIOXIDANT CAMPTOTHECIN DERIVATIVES AND ANTIOXIDANT ANTINEOPLASTIC NANOSPHERES THEREOF 有权
标题翻译：抗氧化剂胶体衍生物及其抗氧化剂的抗原性纳米粒子
公开(公告)号：US20110300187A1
公开(公告)日：2011-12-08
申请号：US13114539
申请日：2011-05-24
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K31/4745 , A61K9/14 , A61P35/00 , C07D491/22
CPC分类号： C07D471/14 , C07D491/22
摘要： The present invention is directed to antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs and the preparation of nanometer-sized camptothecin prodrugs. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant camptothecin nanosphere prodrugs and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these antioxidant camptothecin nanosphere prodrugs for the preparation of delivery devices of other pharmaceuticals and/or drugs. Additionally, methods of treating cancer with the camptothecin and antioxidant derivatives of camptothecin analogs, and nanometer-sized camptothecin prodrugs are also provided.
摘要翻译：本发明涉及喜树碱的抗氧化衍生物和喜树碱类似物的抗氧化衍生物以及纳米级喜树碱前药的制备。合成喜树碱抗氧化剂衍生物和喜树碱类似物抗氧化衍生物的方法，自发乳化或其纳米沉淀法制备抗氧化喜树碱纳米球前药及其在治疗癌性疾病中的应用。本发明的另一方面是这些抗氧化喜树碱纳米球前药用于制备其它药物和/或药物的递送装置的用途。此外，还提供了用喜树碱和喜树碱类似物的抗氧化衍生物和纳米级喜树碱前药治疗癌症的方法。

4. 发明申请

US20110086073A1 NANOMETER-SIZED PRODRUGS OF NSAIDs 有权
标题翻译： NANOMETER SIZE的NSAIDs产品
公开(公告)号：US20110086073A1
公开(公告)日：2011-04-14
申请号：US12995125
申请日：2009-04-08
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K9/00 , C07D339/04 , A61K31/385 , C07C69/612 , C07C229/66 , A61P29/00 , C07D409/12 , A61K31/704 , A61K31/4188 , A61K31/513 , A61K31/4375 , A61K38/02 , A61K31/7088 , B82Y5/00
CPC分类号： A61K47/48061 , A61K9/14 , A61K47/545 , C07D339/04
摘要： The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of α-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
摘要翻译：本发明描述了非甾体抗炎药（NSAID）和α-硫辛酸和NSAIDs的纳米药物的纳米药物。这些纳米药物具有抗氧化性质和刺激响应性，可用于治疗各种疾病状况。

5. 发明授权

US08603531B2 Nanometer-sized prodrugs of NSAIDs 有权
标题翻译：纳米尺寸的NSAID前药
公开(公告)号：US08603531B2
公开(公告)日：2013-12-10
申请号：US12995125
申请日：2009-04-08
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K9/14 , A61K31/385 , A61K31/405 , A61K31/407 , A61K31/4436 , C07D409/12 , C07D339/04
CPC分类号： A61K47/48061 , A61K9/14 , A61K47/545 , C07D339/04
摘要： The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of α-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
摘要翻译：本发明描述了非甾体抗炎药（NSAID）和含α-硫辛酸和NSAIDs的纳米药物的纳米药物。这些纳米药物具有抗氧化性质和刺激响应性，可用于治疗各种疾病状况。

6. 发明申请

US20100291222A1 ANTIOXIDANT NANOSPHERE COMPRISING [1,2]-DITHIOLANE MOIETIES 有权
标题翻译：包含[1,2] - 二羟基苯甲酸酯的抗氧化剂纳米粒子
公开(公告)号：US20100291222A1
公开(公告)日：2010-11-18
申请号：US12811197
申请日：2008-12-30
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K9/14 , C07D409/12 , C07D409/14 , A61K31/497 , A61K31/385 , A61K31/4375 , A61K31/4188 , A61K38/02 , A61K31/7088
CPC分类号： C07D339/04 , A61K9/0014 , A61K9/1075 , A61K9/5146 , A61K47/24
摘要： The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.
摘要翻译：本发明涉及能够作为自由基清除剂，金属和活性氧（ROS）的多种含有α-硫辛酸的疏水性化合物（mALA）。还描述了合成新型抗氧化剂mALA，自发乳化或其纳米沉淀以产生抗氧化剂纳米球的方法及其在预防或治疗由氧化应激和其他自由基介导的条件引起的疾病或病症中的用途。本发明的另一方面是这些抗氧化剂纳米球用于制备治疗剂的抗氧化剂颗粒递送系统的用途。

7. 发明授权

US09028874B2 Antioxidant nanosphere comprising [1,2]-dithiolane moieties 有权
标题翻译：含有[1,2] - 二硫戊环部分的抗氧化纳米球
公开(公告)号：US09028874B2
公开(公告)日：2015-05-12
申请号：US12811197
申请日：2008-12-30
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K9/14 , C07D409/12 , A61K31/497 , A61K38/02 , C07D339/04 , A61K9/107 , A61K9/51 , A61K47/24 , A61K9/00
CPC分类号： C07D339/04 , A61K9/0014 , A61K9/1075 , A61K9/5146 , A61K47/24
摘要： The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.
摘要翻译：本发明涉及能够作为自由基清除剂，金属和活性氧（ROS）的多种含有α-硫辛酸的疏水性化合物（mALA）。还描述了合成新型抗氧化剂mALA，自发乳化或其纳米沉淀以产生抗氧化剂纳米球的方法及其在预防或治疗由氧化应激和其他自由基介导的条件引起的疾病或病症中的用途。本发明的另一方面是这些抗氧化剂纳米球用于制备治疗剂的抗氧化剂颗粒递送系统的用途。

8. 发明授权

US08697743B2 Antioxidant camptothecin derivatives and antioxidant antineoplastic nanospheres thereof 有权
标题翻译：抗氧化喜树碱衍生物及其抗氧化抗肿瘤纳米球
公开(公告)号：US08697743B2
公开(公告)日：2014-04-15
申请号：US13114539
申请日：2011-05-24
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K38/00 , A61K31/44 , A61K31/385 , A61K31/38 , A61K31/27 , A61P35/00 , A01N43/42 , A01N43/40 , A01N43/26 , A01N43/06 , A01N47/10
CPC分类号： C07D471/14 , C07D491/22
摘要： The present invention is directed to antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs and the preparation of nanometer-sized camptothecin prodrugs. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant camptothecin nanosphere prodrugs and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these antioxidant camptothecin nanosphere prodrugs for the preparation of delivery devices of other pharmaceuticals and/or drugs. Additionally, methods of treating cancer with the camptothecin and antioxidant derivatives of camptothecin analogs, and nanometer-sized camptothecin prodrugs are also provided.
摘要翻译：本发明涉及喜树碱的抗氧化衍生物和喜树碱类似物的抗氧化衍生物以及纳米级喜树碱前药的制备。合成喜树碱抗氧化剂衍生物和喜树碱类似物抗氧化衍生物的方法，自发乳化或其纳米沉淀法制备抗氧化喜树碱纳米球前药及其在治疗癌性疾病中的应用。本发明的另一方面是这些抗氧化喜树碱纳米球前药用于制备其它药物和/或药物的递送装置的用途。此外，还提供了用喜树碱和喜树碱类似物的抗氧化衍生物和纳米级喜树碱前药治疗癌症的方法。

9. 发明申请

US20100098653A1 ANTIOXIDANT POLYMERS CONTAINING [1,2]-DITHIOLANE MOIETIES AND USES THEREOF 有权
标题翻译：含有[1,2] - 二羟基苯并咪唑的抗氧化剂聚合物及其用途
公开(公告)号：US20100098653A1
公开(公告)日：2010-04-22
申请号：US12528067
申请日：2008-02-29
申请人： John S. Yu , Bong Seop Lee
发明人： John S. Yu , Bong Seop Lee
IPC分类号： A61K47/30 , C07D339/04 , C07D409/02 , C08F216/06 , C08G75/00 , C08B37/08 , C08B37/00 , C08B37/02 , C08B37/16 , A61P35/00
CPC分类号： C07D339/04 , C08B37/003
摘要： The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.
摘要翻译：本发明描述了能够作为自由基，金属和活性氧的清除剂的1,2-二硫戊环的聚合物。还描述了合成抗氧化剂1,2-二硫戊环衍生物和其聚合以生产可生物降解的抗氧化聚合物的方法。本发明的抗氧化聚合物可用于治疗由氧化应激和其他自由基介导的病症引起的疾病或病症。抗氧化聚合物也可用于制备治疗剂的抗氧化剂颗粒递送装置。

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