公开(公告)号：US20030008818A1

公开(公告)日：2003-01-09

申请号：US10021312

申请日：2001-12-19

Applicant: California Institute of Technology and Insert Therapeutics, Inc

Inventor： Suzie Hwang Pun ,  Hector Gonzalez ,  Mark E. Davis ,  Nathalie Bellocq ,  Jianjun Cheng

IPC: A61K038/16 ,  A61K031/715 ,  A61K031/66 ,  C07K014/00 ,  C08B037/00 ,  A61K031/165

CPC classification number: 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

Abstract: 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: 1

Abstract translation: 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：

公开(公告)号：US20030017972A1

公开(公告)日：2003-01-23

申请号：US10021294

申请日：2001-12-19

Applicant: California Institute of Technology and Insert Therapeutics, Inc

Inventor： Suzie Hwang Pun ,  Hector Gonzalez ,  Mark E. Davis ,  Nathalie Bellocq ,  Jianjun Cheng

IPC: A61K038/17 ,  A61K031/724 ,  C08B037/16

CPC classification number: 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

Abstract: 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: 1

Abstract translation: 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：

公开(公告)号：US20040077595A1

公开(公告)日：2004-04-22

申请号：US10656838

申请日：2003-09-05

Applicant: Insert Therapeutics, Inc.

Inventor： Jianjun Cheng ,  Mark E. Davis ,  Kay T. Khin

IPC: A61K031/724 ,  C08G063/48 ,  C08G063/91

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20040087024A1

公开(公告)日：2004-05-06

申请号：US10372723

申请日：2003-02-24

Applicant: Insert Therapeutics, Inc.

Inventor： Nathalie C. Bellocq ,  Jianjun Cheng ,  Mark E. Davis ,  Suzie Hwang Pun

IPC: A61K048/00 ,  C08G063/48 ,  C08G063/91 ,  C12N015/85 ,  A61K031/795

CPC classification number: B82Y5/00 ,  A61K9/0019 ,  A61K9/146 ,  A61K47/34 ,  A61K47/40 ,  A61K47/59 ,  A61K47/60 ,  A61K47/6951 ,  A61K48/0041 ,  C08B37/0012 ,  C08B37/0015 ,  C08G73/02 ,  C08G73/0213 ,  C08G73/0694 ,  C12N15/88

Abstract: This application discloses compositions of carbohydrate-modified polymers, such as polyethylenimine modified with cyclodextrin moieties, for carrying drugs and other active agents, such as nucleic acids. Compositions are also disclosed of carbohydrate-modified polymer carriers that release such agents under controlled conditions. The invention also discloses compositions of carbohydrate-modified polymer carriers that are coupled to biorecognition molecules for targeting the delivery of drugs to their site of action.

Abstract translation: 本申请公开了用于携带药物和其它活性剂如核酸的碳水化合物改性聚合物的组合物，例如用环糊精部分修饰的聚乙烯亚胺。 还公开了在受控条件下释放这些试剂的碳水化合物改性聚合物载体的组合物。 本发明还公开了与生物识别分子偶联的碳水化合物改性聚合物载体的组合物，用于将药物递送到其作用位点。