公开(公告)号：US20130122112A1

公开(公告)日：2013-05-16

申请号：US13581463

申请日：2011-03-01

Applicant: Helen M. Burt ,  Donald Brooks ,  Jayachandran Kizhakkedathu ,  Richard Liggins ,  Dechi Guan ,  Lu Ye ,  Clement Mugabe ,  Alan So ,  Martin E. Gleave ,  John K. Jackson ,  Rajesh Kumar Kainthan

Inventor： Helen M. Burt ,  Donald Brooks ,  Jayachandran Kizhakkedathu ,  Richard Liggins ,  Dechi Guan ,  Lu Ye ,  Clement Mugabe ,  Alan So ,  Martin E. Gleave ,  John K. Jackson ,  Rajesh Kumar Kainthan

IPC: A61K47/10 ,  C08G65/333

CPC classification number: A61K47/10 ,  A61K9/0034 ,  A61K9/006 ,  A61K9/5146 ,  A61K31/337 ,  A61K31/407 ,  A61K33/24 ,  A61K47/34 ,  A61K47/60 ,  C08G65/33306 ,  C08G65/33337 ,  C08G65/34 ,  C08G65/48 ,  C08G83/005 ,  C08G83/006 ,  C08G2650/54

Abstract: Herein are provided derivatized hyperbranched polyglycerols (“dHPGs”). The dHPG comprises a core comprising a hyperbranched polyglycerol derivatized with C1C20 alkyl chains and a shell comprising at least one hydrophilic substituent bound to hydroxyl groups of the core, wherein the hyperbranched polyglycerol comprises from about 1 to about 200 moles of the at least one hydrophilic substituent. The dHPGs are for use as agents for the delivery of a drug or other biologically active moiety to the urinary tract, the digestive tract, the airways, the vaginal cavity and cervix and the peritoneal cavity to treat indications such as cancer, which may be useful in the treatment of or the manufacture of a medicament, in the preparation, of a pharmaceutical composition for the treatment of cancer, as a pre-treatment or co-treatment to improve drug uptake in a tissue. Furthermore, there are provided methods of making dHPGs.

Abstract translation: 本文提供衍生的超支化聚甘油（“dHPG”）。 dHPG包含核心，其包含用C1C20烷基链衍生的超支化聚甘油和包含至少一个与核心羟基结合的亲水取代基的壳，其中超支化聚甘油包含约1至约200摩尔的至少一个亲水取代基 。 dHPG用作将药物或其他生物活性部分递送至尿路，消化道，气道，阴道腔和子宫颈以及腹膜腔以治疗诸如癌症的适应症的药剂，其可能是有用的 在制备中用于治疗癌症的药物组合物的治疗或制造中，作为用于改善组织中药物摄取的预处理或共处理。 此外，还提供了制备dHPG的方法。

公开(公告)号：US09186410B2

公开(公告)日：2015-11-17

申请号：US13581463

申请日：2011-03-01

Applicant: Helen Burt ,  Donald Brooks ,  Jayachandran Kizhakkedathu ,  Richard Liggins ,  Dechi Guan ,  Lu Ye ,  Clement Mugabe ,  Alan So ,  Martin E. Gleave ,  John K. Jackson ,  Rajesh Kumar Kainthan

Inventor： Helen Burt ,  Donald Brooks ,  Jayachandran Kizhakkedathu ,  Richard Liggins ,  Dechi Guan ,  Lu Ye ,  Clement Mugabe ,  Alan So ,  Martin E. Gleave ,  John K. Jackson ,  Rajesh Kumar Kainthan

IPC: A61K33/24 ,  C07C217/00 ,  C07D207/46 ,  A61K47/10 ,  A61K9/51 ,  A61K47/34 ,  C08G65/34 ,  C08G65/48 ,  C08G83/00 ,  C08G65/333 ,  A61K9/00

CPC classification number: A61K47/10 ,  A61K9/0034 ,  A61K9/006 ,  A61K9/5146 ,  A61K31/337 ,  A61K31/407 ,  A61K33/24 ,  A61K47/34 ,  A61K47/60 ,  C08G65/33306 ,  C08G65/33337 ,  C08G65/34 ,  C08G65/48 ,  C08G83/005 ,  C08G83/006 ,  C08G2650/54

Abstract: Herein are provided derivatized hyperbranched polyglycerols (“dHPGs”). The dHPG comprises a core comprising a hyperbranched polyglycerol derivatized with C1C20 alkyl chains and a shell comprising at least one hydrophilic substituent bound to hydroxyl groups of the core, wherein the hyperbranched polyglycerol comprises from about 1 to about 200 moles of the at least one hydrophilic substituent. The dHPGs are for use as agents for the delivery of a drug or other biologically active moiety to the urinary tract, the digestive tract, the airways, the vaginal cavity and cervix and the peritoneal cavity to treat indications such as cancer, which may be useful in the treatment of or the manufacture of a medicament, in the preparation, of a pharmaceutical composition for the treatment of cancer, as a pre-treatment or co-treatment to improve drug uptake in a tissue. Furthermore, there are provided methods of making dHPGs.

Abstract translation: 本文提供衍生的超支化聚甘油（“dHPG”）。 dHPG包含核心，其包含用C1C20烷基链衍生的超支化聚甘油和包含至少一个与核心羟基结合的亲水取代基的壳，其中超支化聚甘油包含约1至约200摩尔的至少一个亲水取代基 。 dHPG用作将药物或其他生物活性部分递送至尿路，消化道，气道，阴道腔和子宫颈以及腹膜腔以治疗诸如癌症的适应症的药剂，其可能是有用的 在制备中用于治疗癌症的药物组合物的治疗或制造中，作为用于改善组织中药物摄取的预处理或共处理。 此外，还提供了制造dHPG的方法。