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1. 发明申请

US20130101672A1 NANOCONJUGATES AND NANOCONJUGATE FORMULATIONS 有权
标题翻译：纳米结晶和纳米结晶配方
公开(公告)号：US20130101672A1
公开(公告)日：2013-04-25
申请号：US13518836
申请日：2010-12-23
申请人： Jianjun Cheng , Rong Tong
发明人： Jianjun Cheng , Rong Tong
IPC分类号： A61K9/16
CPC分类号： A61K9/1658 , A61K9/0019 , A61K9/5169 , A61K47/593 , A61K47/60 , A61K47/6935
摘要： The invention provides a drug-polymer nanoconjugate that includes a drug covalently bonded to a polymer. The nanoconjugate can include a block copolymer coating and/or an albumin coating. The drug of the drug-polymer nanoconjugate can be one or more of a variety of therapeutic agents linked to the polymer through ether or thioether linkages formed from hydroxyl or thiol groups of the drug. The albumin coating can substantially or completely retard or prevent aggregation of the nanoconjugates in solid form or in solution. The invention further provides compositions that include a plurality of drug-polymer nanoconjugates, as well as methods for using the drug-polymer nanoconjugates, such as in therapeutic or diagnostic applications.
摘要翻译：本发明提供药物 - 聚合物纳米缀合物，其包括共价键合到聚合物上的药物。纳米缀合物可以包括嵌段共聚物涂层和/或白蛋白涂层。药物 - 聚合物纳米缀合物的药物可以是通过由药物的羟基或硫醇基团形成的醚或硫醚键与聚合物连接的各种治疗剂中的一种或多种。白蛋白涂层可以基本上或完全地延迟或阻止纳米缀合物以固体形式或溶液中的聚集。本发明还提供了包括多种药物 - 聚合物纳米缀合物的组合物，以及用于使用药物 - 聚合物纳米缀合物的方法，例如在治疗或诊断应用中。

2. 发明申请

US20110085974A1 SMALL MOLECULE LIGAND-DRUG CONJUGATES FOR TARGETED CANCER THERAPY 审中-公开
标题翻译：小分子药物配方药物治疗癌症治疗
公开(公告)号：US20110085974A1
公开(公告)日：2011-04-14
申请号：US12995417
申请日：2009-06-12
申请人： Leland W.K. Chung , Xiaojian Yang , Jianjun Cheng , Rong Tong
发明人： Leland W.K. Chung , Xiaojian Yang , Jianjun Cheng , Rong Tong
IPC分类号： A61K51/00 , C07D403/08 , C07D403/14 , A61K31/404 , A61P35/00 , A61K49/06 , A61K49/00
CPC分类号： A61K47/545 , A61K47/546 , A61K49/0002 , A61K49/0032 , A61K49/0052
摘要： The present invention describes small molecule ligand-drug conjugates and methods of using the small molecule ligand-drug conjugates for targeted treatment of cancer in a patient in need thereof. Further described are methods of sterilizing circulating tumor cells and determining drug concentration in cancer tissue.
摘要翻译：本发明描述了小分子配体 - 药物偶联物以及在有需要的患者中使用小分子配体 - 药物偶联物靶向治疗癌症的方法。进一步描述了对循环肿瘤细胞进行灭菌和确定癌组织中的药物浓度的方法。

3. 发明授权

US09295651B2 Nanoconjugates and nanoconjugate formulations 有权
标题翻译：纳米缀合物和纳米缀合物配方
公开(公告)号：US09295651B2
公开(公告)日：2016-03-29
申请号：US13518836
申请日：2010-12-23
申请人： Jianjun Cheng , Rong Tong
发明人： Jianjun Cheng , Rong Tong
IPC分类号： A61K9/14 , A61K38/38 , A61K47/30 , A61K47/42 , A61K47/48 , A61K9/16 , A61K9/00 , A61K9/51
CPC分类号： A61K9/1658 , A61K9/0019 , A61K9/5169 , A61K47/593 , A61K47/60 , A61K47/6935
摘要： The invention provides a drug-polymer nanoconjugate that includes a drug covalently bonded to a polymer. The nanoconjugate can include a block copolymer coating and/or an albumin coating. The drug of the drug-polymer nanoconjugate can be one or more of a variety of therapeutic agents linked to the polymer through ether or thioether linkages formed from hydroxyl or thiol groups of the drug. The albumin coating can substantially or completely retard or prevent aggregation of the nanoconjugates in solid form or in solution. The invention further provides compositions that include a plurality of drug-polymer nanoconjugates, as well as methods for using the drug-polymer nanoconjugates, such as in therapeutic or diagnostic applications.
摘要翻译：本发明提供药物 - 聚合物纳米缀合物，其包括共价键合到聚合物上的药物。纳米缀合物可以包括嵌段共聚物涂层和/或白蛋白涂层。药物 - 聚合物纳米缀合物的药物可以是通过由药物的羟基或硫醇基团形成的醚或硫醚键与聚合物连接的各种治疗剂中的一种或多种。白蛋白涂层可以基本上或完全地延迟或阻止纳米缀合物以固体形式或溶液中的聚集。本发明还提供了包括多种药物 - 聚合物纳米缀合物的组合物，以及用于使用药物 - 聚合物纳米缀合物的方法，例如在治疗或诊断应用中。

4. 发明申请

US20080248126A1 PARTICULATE DRUG DELIVERY 审中-公开
标题翻译：颗粒药物递送
公开(公告)号：US20080248126A1
公开(公告)日：2008-10-09
申请号：US12041529
申请日：2008-03-03
申请人： Jianjun Cheng , Rong Tong
发明人： Jianjun Cheng , Rong Tong
IPC分类号： A61K9/14 , A61K38/02 , A61K31/70 , A61K31/7052 , C08G63/08 , C08G79/04 , C08G77/04 , C08G69/26
CPC分类号： A61K47/59 , A61K9/5146 , A61K9/5192 , A61K31/337 , A61K31/4355 , A61K31/704 , A61K38/09 , A61K38/13 , A61K47/593 , A61K47/60 , A61K47/605 , A61K47/6803 , A61K47/6809 , A61K47/6811 , A61K47/6851 , A61K47/6855 , A61K47/6857 , A61K47/6877 , A61K47/6927 , A61K47/6935 , A61K47/6937 , C08G63/823 , C08G81/00
摘要： Methods for efficient preparation of drug-polymer (or oligomer) conjugates which are useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications. The invention additionally provides certain drug-polymer and drug-oligomer conjugates which are useful in the preparation of particles for delivery of the drug in vivo. The invention also provides nanoparticles of this invention prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention.The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.
摘要翻译：药物 - 聚合物（或低聚物）缀合物的有效制备方法，其可用于制备颗粒，包括微粒和纳米颗粒，用于在体内递送药物用于治疗应用。本发明另外提供某些药物 - 聚合物和药物 - 低聚物共轭物，其可用于制备用于在体内递送药物的颗粒。本发明还提供使用本发明的药物 - 聚合物/低聚物共轭物通过纳米沉淀制备的本发明的纳米颗粒。在聚合物或低聚物的聚合过程中形成药物共轭物，其中药物被用作形成聚合物和/或低聚物的单体聚合的引发剂。更具体地说，通过在合适的开环聚合催化剂和引发剂（药物）的存在下，环状单体的开环聚合形成药物偶联物。该方法特别适用于与含有一个或多个羟基或硫醇基团的药物和其它化学物质形成聚合物/低聚物缀合物。

5. 发明申请

US20140206679A1 HETEROCYCLIC PYRIDONE COMPOUND, AND INTERMEDIATE, PREPARATION METHOD AND USE THEREOF 有权
标题翻译：杂环吡啶类化合物及其中间体，制备方法及其用途
公开(公告)号：US20140206679A1
公开(公告)日：2014-07-24
申请号：US14124628
申请日：2012-05-28
申请人： Jianjun Cheng , Jihong Qin , Bin Ye
发明人： Jianjun Cheng , Jihong Qin , Bin Ye
IPC分类号： C07D513/04 , C07D498/04 , C07D471/04
CPC分类号： C07D513/04 , C07D471/04 , C07D498/04
摘要： The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament.
摘要翻译：本发明涉及由通式（I）表示的杂环吡啶酮化合物，其中杂环吡啶酮化合物用作酪氨酸激酶抑制剂，特别是c-Met抑制剂。本发明还涉及制备杂环吡啶酮化合物的中间体及其制备方法。本发明还涉及含有杂环吡啶酮化合物作为活性成分的药物组合物，以及该药物组合物用于治疗与酪氨酸激酶c-Met相关疾病，特别是与c-Met相关的癌症作为药物的用途。

6. 发明授权

US08680202B2 Cyclodextrin-based polymers for therapeutics delivery 有权
标题翻译：用于治疗输送的基于环糊精的聚合物
公开(公告)号：US08680202B2
公开(公告)日：2014-03-25
申请号：US13572294
申请日：2012-08-10
申请人： Jianjun Cheng , Mark E. Davis , Kay T. Khin
发明人： Jianjun Cheng , Mark E. Davis , Kay T. Khin
IPC分类号： A61K47/48 , C08B37/16 , A61K9/51 , A61P35/00
CPC分类号： C08G69/44 , A61K31/337 , A61K31/7048 , A61K47/48176 , A61K47/48192 , A61K47/482 , A61K47/48215 , A61K47/4823 , A61K47/48338 , A61K47/48969 , A61K47/58 , A61K47/59 , A61K47/60 , A61K47/61 , A61K47/6951 , B82Y5/00 , C08B30/00 , C08B31/00 , C08B37/0012 , C08F220/28 , C08F220/58 , C08F222/22 , C08F2220/282 , C08G81/02 , G06F19/00 , G06F19/3456 , G06Q50/22 , Y02A90/22 , Y02A90/26
摘要： The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.
摘要翻译：本发明涉及设计为小分子治疗剂递送载体的治疗性环糊精含有聚合物的组合物及其药物组合物。这些含环糊精的聚合物改善药物稳定性和溶解性，并且在体内使用时降低小分子治疗剂的毒性。此外，通过从各种接头基团和靶向配体中选择，聚合物呈现用于治疗剂的受控递送的方法。本发明还涉及用本文所述的治疗组合物治疗受试者的方法。本发明还涉及用于进行药物业务的方法，包括制造，许可或分发包含或涉及本文所述的聚合物的试剂盒。

7. 发明授权

US08404662B2 Cyclodextrin-based polymers for therapeutics delivery 有权
公开(公告)号：US08404662B2
公开(公告)日：2013-03-26
申请号：US13572283
申请日：2012-08-10
申请人： Jianjun Cheng , Mark Davis , Kay T. Khin
发明人： Jianjun Cheng , Mark Davis , Kay T. Khin
IPC分类号： A61K31/337 , A61K31/4745 , C08G2/30 , C08G69/08 , C08L5/16
CPC分类号： C08G69/44 , A61K31/337 , A61K31/7048 , A61K47/48176 , A61K47/48192 , A61K47/482 , A61K47/48215 , A61K47/4823 , A61K47/48338 , A61K47/48969 , A61K47/58 , A61K47/59 , A61K47/60 , A61K47/61 , A61K47/6951 , B82Y5/00 , C08B30/00 , C08B31/00 , C08B37/0012 , C08F220/28 , C08F220/58 , C08F222/22 , C08F2220/282 , C08G81/02 , G06F19/00 , G06F19/3456 , G06Q50/22 , Y02A90/22 , Y02A90/26
摘要： The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

8. 发明授权

US08389499B2 Cyclodextrin-based polymers for therapeutics delivery 有权
公开(公告)号：US08389499B2
公开(公告)日：2013-03-05
申请号：US13553400
申请日：2012-07-19
申请人： Jianjun Cheng , Mark E. Davis , Kay T. Khin
发明人： Jianjun Cheng , Mark E. Davis , Kay T. Khin
IPC分类号： A61K31/337 , C08G2/30 , C08G69/08 , C08G69/10 , C08L5/16
CPC分类号： C08G69/44 , A61K31/337 , A61K31/7048 , A61K47/48176 , A61K47/48192 , A61K47/482 , A61K47/48215 , A61K47/4823 , A61K47/48338 , A61K47/48969 , A61K47/58 , A61K47/59 , A61K47/60 , A61K47/61 , A61K47/6951 , B82Y5/00 , C08B30/00 , C08B31/00 , C08B37/0012 , C08F220/28 , C08F220/58 , C08F222/22 , C08F2220/282 , C08G81/02 , G06F19/00 , G06F19/3456 , G06Q50/22 , Y02A90/22 , Y02A90/26
摘要： The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

9. 发明授权

US08092833B2 Compositions containing inclusion complexes 有权
标题翻译：含有复合物的组合物
公开(公告)号：US08092833B2
公开(公告)日：2012-01-10
申请号：US12846344
申请日：2010-07-29
申请人： Suzie Hwang Pun , Hector Gonzalez , Mark E. Davis , Nathalie C. Bellocq , Jianjun Cheng
发明人： Suzie Hwang Pun , Hector Gonzalez , Mark E. Davis , Nathalie C. Bellocq , Jianjun Cheng
IPC分类号： A61K31/74 , A61K9/14 , C12P19/30 , C12N15/63
CPC分类号： A61K47/48215 , A61K38/44 , A61K47/60 , A61K47/6949 , A61K47/6951 , A61K48/0041 , B82Y5/00 , C08B37/0012 , C08G65/33396 , C08G65/48 , C08G2650/04 , C08G2650/38 , C12Y113/12007
摘要： The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent. According to the method, a therapeutically effective amount of a therapeutic composition of the invention is administered to a mammal (e.g. person or animal) in recognized need of the therapeutic. Also disclosed are compounds having the formula:
摘要翻译：本发明提供了含有聚合物和治疗剂的颗粒复合物的组合物。该组合物还含有络合剂。聚合物与宿主客体或客体 - 宿主相互作用中的络合剂相互作用以形成包合物。本发明的治疗组合物可用于递送治疗剂并治疗各种疾病。颗粒复合材料的聚合物和络合剂都可用于将功能性引入治疗组合物中。本发明还涉及制备组合物的方法。该方法结合治疗剂，具有宿主或客体功能的聚合物和具有客体或宿主功能的络合剂以形成治疗组合物。络合剂与聚合物形成包合络合物。本发明还涉及递送治疗剂的方法。根据该方法，将治疗有效量的本发明的治疗组合物在公认的治疗需要中给予哺乳动物（例如人或动物）。还公开了具有下式的化合物：

10. 发明授权

US07166302B2 Complexing agents for compositions containing inclusion complexes 有权
公开(公告)号：US07166302B2
公开(公告)日：2007-01-23
申请号：US10021294
申请日：2001-12-19
申请人： Suzie Hwang Pun , Hector Gonzalez , Mark E. Davis , Nathalie Bellocq , Jianjun Cheng
发明人： Suzie Hwang Pun , Hector Gonzalez , Mark E. Davis , Nathalie Bellocq , Jianjun Cheng
IPC分类号： A61K9/14 , A61K31/74 , C12P19/30 , C12N15/63
CPC分类号： A61K47/48215 , A61K38/44 , A61K47/60 , A61K47/6949 , A61K47/6951 , A61K48/0041 , B82Y5/00 , C08B37/0012 , C08G65/33396 , C08G65/48 , C08G2650/04 , C08G2650/38 , C12Y113/12007
摘要： The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent. According to the method, a therapeutically effective amount of a therapeutic composition of the invention is administered to a mammal (e.g. person or animal) in recognized need of the therapeutic. Also disclosed are compounds having the formula:

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