公开(公告)号：WO2015057847A1

公开(公告)日：2015-04-23

申请号：PCT/US2014/060708

申请日：2014-10-15

Applicant: CERULEAN PHARMA INC. ,  BERGSTROM, Donald ,  NG, Pei-Sze ,  SVENSON, Sonke

Inventor： BERGSTROM, Donald ,  NG, Pei-Sze ,  SVENSON, Sonke ,  ELIASOF, Scott ,  FETZER, Oliver, S. ,  HWANG, Jungyeon ,  SOO, Patrick, Lim

IPC: A61K9/14 ,  A61K31/713 ,  A61K48/00 ,  C12N15/113

CPC classification number: A61K9/146 ,  A61K9/5153 ,  A61K47/543 ,  A61K47/59 ,  A61K47/593 ,  A61K47/645 ,  A61K47/6935 ,  A61K47/6937 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2310/351 ,  C12N2310/3515 ,  C12N2320/32

Abstract: Particles and conjugates for delivering nucleic acid agents. Compositions containing the particles, the conjugates, or both. Methods of using the particles, the conjugates, and the compositions.

Abstract translation: 用于递送核酸试剂的颗粒和共轭物。 含有颗粒，共轭物或两者的组合物。 使用颗粒，共轭物和组合物的方法。

公开(公告)号：WO2008054466A2

公开(公告)日：2008-05-08

申请号：PCT/US2007/005681

申请日：2007-03-03

Applicant: DENDRITIC NANOTECHNOLOGIES, INC. ,  DEMATTEI, Cordell, R. ,  HUANG, Baohua ,  REYNA, Lori, A. ,  SVENSON, Sonke ,  SWANSON, Douglas, R. ,  TOMALIA, Donald, A. ,  ZHURAVEL, Michael, A. ,  PULGAM, Veera, Reddy

Inventor： DEMATTEI, Cordell, R. ,  HUANG, Baohua ,  REYNA, Lori, A. ,  SVENSON, Sonke ,  SWANSON, Douglas, R. ,  TOMALIA, Donald, A. ,  ZHURAVEL, Michael, A. ,  PULGAM, Veera, Reddy

IPC: A61K48/00

CPC classification number: A61K48/00 ,  A61K9/5146 ,  A61K47/59 ,  A61K47/595 ,  A61K47/60 ,  C08G83/003 ,  Y02A50/463

Abstract: The present invention concerns core-shell tecto (dendritic polymers) that are associated with biologically active materials (such as nucleic acids for use for RNAi and in transfection). Also included are formulations for their use. The constructs are useful for the delivery of drugs to an animal or plant and may be in vivo , in vitro or ex vivo .

Abstract translation: 本发明涉及与生物活性物质（例如用于RNAi和转染的核酸）相关的核 - 壳结构（树状聚合物）。 还包括它们的使用配方。 该构建体可用于将药物递送至动物或植物，并且可以在体内，体外或离体。 >

公开(公告)号：WO2012024530A2

公开(公告)日：2012-02-23

申请号：PCT/US2011048309

申请日：2011-08-18

Applicant: CERULEAN PHARMA INC ,  FETZER OLIVER S ,  HWANG JUNGYEON ,  LIM SOO PATRICK ,  NG PEI-SZE ,  SVENSON SONKE

Inventor： FETZER OLIVER S ,  HWANG JUNGYEON ,  LIM SOO PATRICK ,  NG PEI-SZE ,  SVENSON SONKE

IPC: A61K47/48 ,  A61K9/14 ,  A61P9/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00 ,  B32B5/16 ,  C08G63/91

CPC classification number: A61K38/02 ,  A61K47/593 ,  A61K47/60 ,  A61K47/6921 ,  C08L67/04 ,  Y10T428/2982 ,  C08L2666/18

Abstract: Described herein are conjugates (e.g., therapeutic peptide-polymer conjugates and protein-polymer conjugates) and particles, which can be used, for example, in the treatment of a disorder such as cancer. Also described herein are mixtures, compositions and dosage forms containing the particles, methods of using the particles (e.g., to treat a disorder), kits including the conjugates (e.g., therapeutic peptide-polymer conjugates and protein-polymer conjugates) and particles, methods of making the conjugates (e.g., therapeutic peptide-polymer conjugates and protein-polymer conjugates) and particles, methods of storing the particles and methods of analyzing the particles

Abstract translation: 本文描述的是缀合物（例如，治疗性肽 - 聚合物缀合物和蛋白质 - 聚合物缀合物）和颗粒，其可以用于例如治疗诸如癌症的病症。 本文还描述了含有颗粒的混合物，组合物和剂型，使用颗粒的方法（例如，治疗病症），包括缀合物的试剂盒（例如治疗性肽 - 聚合物缀合物和蛋白质 - 聚合物缀合物）和颗粒，方法 制备缀合物（例如，治疗性肽 - 聚合物缀合物和蛋白质 - 聚合物缀合物）和颗粒，储存颗粒的方法和分析颗粒的方法

公开(公告)号：WO2009110971A3

公开(公告)日：2009-09-11

申请号：PCT/US2009/001163

申请日：2009-02-25

Applicant: DENDRITIC NANOTECHNOLOGIES, INC. ,  PULGAM, Veera, Reddy ,  SVENSON, Sonke ,  ZHURAVEL, Michael, A.

Inventor： PULGAM, Veera, Reddy ,  SVENSON, Sonke ,  ZHURAVEL, Michael, A.

IPC: C07D301/00

Abstract: The present invention describes a single-stage process for preparing multifunctional epoxides having at least three hydroxyl groups using epichlorohydrin in the presence of freshly ground KOH, at a temperature between 10-25°C.

公开(公告)号：WO2007149500A3

公开(公告)日：2007-12-27

申请号：PCT/US2007/014402

申请日：2007-06-20

Applicant: DENDRITIC NANOTECHNOLOGIES, INC. ,  CHAUHAN, Abhay, Singh ,  SVENSON, Sonke

Inventor： CHAUHAN, Abhay, Singh ,  SVENSON, Sonke

IPC: A61K31/74 ,  A61K47/48

Abstract: The present invention concerns hybrid dendrimers comprising a mixture, at the same or different ratios, of at least two dendritic polymers or dendronized polymers that have at least one difference between them. The surfaces of the dendritic polymer or dendronized polymer may be further modified by known methods. Also included are formulations of hybrid dendrimers wherein the dendritic polymers have the same drug present at either identical or different loading concentrations but have different release profiles. Such formulations of hybrid dendrimers may have different guest molecules present at either identical or different loading concentrations but have different release profiles. Additionally a method of using a hybrid dendrimer for delivery of a drug or guest moiety in order to provide increased solubility to poorly soluble drugs or guest moieties is provided.

公开(公告)号：WO2004012711A1

公开(公告)日：2004-02-12

申请号：PCT/US2003/021884

申请日：2003-07-14

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  TUCKER, Christopher, J. ,  SVENSON, Sonke ,  HITT, James, E. ,  CURTIS, Cathy, A.

Inventor： TUCKER, Christopher, J. ,  SVENSON, Sonke ,  HITT, James, E. ,  CURTIS, Cathy, A.

IPC: A61K9/14

CPC classification number: A61K9/146

Abstract: Drug particles which are essentially crystalline and have a mean particle size below 2 microns, when dispersed in water, are described. When added to an aqueous medium at 25-95% of the equilibrium solubility of the drug substance, the drug particles show complete dissolution, as characterized by a 95% reduction in turbidity, in less than 5 minutes. Using a controlled precipitation process to prepare such drug particles is also described. Such drug particles exhibit an enhanced dissolution rate and better stability as compared to particles prepared according to processes described in the prior art.

Abstract translation: 描述了当分散在水中时基本上是结晶的并且具有低于2微米的平均粒度的药物颗粒。 当以25-95％的药物物质的平衡溶解度加入到水性介质中时，药物颗粒显示完全溶解，其特征在于在不到5分钟内95％的浊度降低。 还描述了使用受控沉淀法制备这种药物颗粒。 与根据现有技术中描述的方法制备的颗粒相比，这样的药物颗粒显示出增强的溶解速率和更好的稳定性。

公开(公告)号：WO2012024526A2

公开(公告)日：2012-02-23

申请号：PCT/US2011/048305

申请日：2011-08-18

Applicant: CERULEAN PHARMA INC. ,  ELIASOF, Scott ,  FETZER, Oliver, S. ,  HWANG, Jungyeon ,  LIM SOO, Patrick ,  NG, Pei-sze ,  SVENSON, Sonke ,  BERGSTROM, Donald, E.

Inventor： ELIASOF, Scott ,  FETZER, Oliver, S. ,  HWANG, Jungyeon ,  LIM SOO, Patrick ,  NG, Pei-sze ,  SVENSON, Sonke ,  BERGSTROM, Donald, E.

IPC: A61K48/00

CPC classification number: A61K47/482 ,  A61K9/14 ,  A61K31/713 ,  A61K47/593 ,  A61K47/60 ,  A61K47/6921 ,  C12N15/11 ,  C12N15/113 ,  C12N15/115 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/351 ,  C12N2320/32 ,  Y10T428/2982

Abstract: Particles and conjugates for delivering nucleic acid agents. Compositions containing the particles, the conjugates, or both. Methods of using the particles, the conjugates, and the compositions.

Abstract translation: 用于递送核酸试剂的颗粒和缀合物。 含有颗粒，偶联物或两者的组合物。 使用这些颗粒，缀合物和组合物的方法。

公开(公告)号：WO2008030591A2

公开(公告)日：2008-03-13

申请号：PCT/US2007019601

申请日：2007-09-07

Applicant: DENDRITIC NANOTECHNOLOGIES INC ,  SVENSON SONKE ,  CHAUHAN ABHAY SINGH

Inventor： SVENSON SONKE ,  CHAUHAN ABHAY SINGH

IPC: A61K9/18

CPC classification number: A61K47/34 ,  A61K47/6949 ,  B82Y5/00

Abstract: The present invention concerns poly(etherhydroxylamine) PEHAM dendritic polymers wherein they function as excipients for the enhancement of water solubility of poorly water soluble (hydrophobic) Active Materials or enhancement of oil solubility of poorly oil soluble (hydrophilic) Active Materials. These dendritic polymers can have Active Materials associated with them by one or more of the following: (a) by adsorption onto the surface or (b) encapsulation into the interior of the dendritic polymers or (c) a mixture of both where these interactions are driven by one or more of the following (i) electrostatic attraction, (ii) hydrogen bonding between dendritic polymers and Active Material and (iii) hydrophobic or hydrophilic interactions or mixtures of these interactions. Additionally, these associated Active Materials can be associated with dendritic polymers through chemical bonding to the surface or to internal functionalities (IF) of PEHAM dendritic polymers or both. Such bonding is done either directly between PEHAM dendritic polymers and Active Material molecules or via a linker that can have a hydrolysable bond to the Active Material. In addition, a chemical entity with strong interaction to the Active Material and dendritic polymers can be associated with the dendritic polymer prior to adsorption or encapsulation of the Active Material or together with the Active Material.

Abstract translation: 本发明涉及聚（醚羟胺）PEHAM树枝状聚合物，其中它们用作增强水溶性（疏水性）活性材料的水溶性的赋形剂，或者提高油溶性（亲水性）活性物质的油溶性。 这些树枝状聚合物可以通过一种或多种以下物质与其相关的活性材料：（a）通过吸附到表面上或（b）包封到树枝状聚合物的内部，或（c）两者的混合物，其中这些相互作用是 由以下一个或多个（i）静电吸引，（ii）树枝状聚合物和活性材料之间的氢键和（iii）疏水或亲水相互作用或这些相互作用的混合物驱动。 另外，这些相关的活性材料可以通过与表面的化学键合或PEHAM树枝状聚合物的内部功能（IF）或两者结合而与树枝状聚合物缔合。 这种键合可以直接在PEHAM树枝状聚合物和活性材料分子之间进行，或者通过可以与活性材料具有可水解键的接头进行。 此外，与活性物质和树枝状聚合物具有强相互作用的化学物质在活性物质的吸附或包封之前或与活性物质一起可与树枝状聚合物缔合。

公开(公告)号：WO2004012710A1

公开(公告)日：2004-02-12

申请号：PCT/US2003/021882

申请日：2003-07-14

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  SVENSON, Sonke ,  TUCKER, Christopher, J. ,  HITT, James, E.

Inventor： SVENSON, Sonke ,  TUCKER, Christopher, J. ,  HITT, James, E.

IPC: A61K9/14

CPC classification number: A61K9/146 ,  A61K9/145

Abstract: Particles having a plurality of crystalline domains are described. Each crystalline domain is oriented differently than any of the adjacent domains and comprises a drug substance. A plurality of interfacial regions surround the crystalline domains, each interfacial region comprising at least one stabilizer. A process used to prepare the particles of the present invention is also described. The particles of the present invention exhibit relatively fast dissolution times as compared to particles prepared by processes described in the prior art.

Abstract translation: 描述具有多个结晶域的颗粒。 每个结晶结构域的取向与任何相邻的结构域不同，并且包含药物物质。 多个界面区域围绕结晶域，每个界面区域包括至少一个稳定剂。 还描述了用于制备本发明的颗粒的方法。 与通过现有技术中描述的方法制备的颗粒相比，本发明的颗粒表现出相对较快的溶解时间。

公开(公告)号：WO2006115547A3

公开(公告)日：2009-06-04

申请号：PCT/US2005047635

申请日：2005-12-21

Applicant: DENDRITIC NANOTECHNOLOGIES INC ,  TOMALIA DONALD A ,  SWANSON DOUGLAS R ,  HUANG BAOHUA ,  PULGAM VEERA REDDY ,  HEINZELMANN JOSEPH R ,  SVENSON SONKE ,  REYNA LORI A ,  ZHURAVEL MICHAEL A ,  CHAUHAN ABHAY SINGH ,  DEMATTEI CORDELL R

Inventor： TOMALIA DONALD A ,  SWANSON DOUGLAS R ,  HUANG BAOHUA ,  PULGAM VEERA REDDY ,  HEINZELMANN JOSEPH R ,  SVENSON SONKE ,  REYNA LORI A ,  ZHURAVEL MICHAEL A ,  CHAUHAN ABHAY SINGH ,  DEMATTEI CORDELL R

IPC: C08J3/00 ,  C08J9/32 ,  C08K9/00 ,  C12N15/87

CPC classification number: C12N15/87 ,  A61K47/59 ,  A61K47/593 ,  A61K47/595 ,  A61K48/00 ,  A61K49/0002 ,  B82Y5/00 ,  B82Y10/00 ,  C08G83/003 ,  C08L101/005 ,  C09B67/0013

Abstract: Dendritic polymers of the macromolecular structure of Figure 1 are disclosed. The dendritic polymers have enhanced amplification and interior functionality. The dendritic polymers are made by use of fact, reactive ring-opening chemistry (or other fast reactions) combined with the use of branch cell reagents in a controlled manner to rapidly and precisely build dendritic structures with cleaner chemistry and often with single products. Additional benefits include lower excesses of regents, lower levels of dilution, higher capacity, more easily scaled to commercial dimensions, new ranges of materials, and lower cost. The compositions prepared have novel internal functionality, including increased thermal stability and no reverse Michael's reaction, and reach encapsulation surface densities at lower generations.

Abstract translation: 公开了图1的大分子结构的树枝状聚合物。 树枝状聚合物具有增强的扩增和内部功能。 树枝状聚合物通过使用事实，反应性开环化学（或其它快速反应）结合使用分支细胞试剂以受控方式快速和精确地构建具有更清洁化学物质的树突状结构并且经常与单一产物一起制备。 额外的好处包括摄入量过低，稀释水平降低，容量更大，容易扩展到商业尺寸，新的材料范围以及更低的成本。 制备的组合物具有新颖的内部功能，包括增加的热稳定性和没有相反的迈克尔反应，并在较低的代下达到包封表面密度。