公开(公告)号：US09572892B2

公开(公告)日：2017-02-21

申请号：US14772981

申请日：2014-03-07

Applicant: POLYACTIVA PTY LTD

Inventor： Sarah Man Yee Ng ,  Andrew Craig Donohue ,  Russell John Tait ,  Stephen Lonsdale Birkett ,  Adrian Sulistio ,  Anton Blencowe

IPC: C08G73/00 ,  A61K47/48 ,  A61K9/00 ,  A61K31/5377 ,  A61K31/5575

CPC classification number: A61K31/5575 ,  A61K9/0051 ,  A61K31/5377 ,  A61K47/58 ,  A61K47/59 ,  A61K47/60

Abstract: The present invention relates in general to polymer-bioactive agent conjugates for delivering a bioactive agent to a subject. The polymer-bioactive agent conjugates contain triazole moieties in the polymer backbone and a bioactive moiety selected from prostaglandin analogs, β-blockers and mixtures thereof. The present invention also relates to methods for preparing the polymer conjugates using click chemical reactions, to monomer-bioactive agent conjugates suitable for preparing the polymer conjugates, and to pharmaceutical products comprising the polymer conjugates for the treatment of glaucoma.

Abstract translation: 本发明一般涉及将生物活性剂递送至受试者的聚合物 - 生物活性剂缀合物。 聚合物 - 生物活性剂缀合物在聚合物主链中含有三唑部分和选自前列腺素类似物，β-阻断剂及其混合物的生物活性部分。 本发明还涉及使用点击化学反应制备聚合物共轭物的方法，适用于制备聚合物缀合物的单体 - 生物活性剂缀合物以及包含用于治疗青光眼的聚合物缀合物的药物产品。

公开(公告)号：US20170035796A1

公开(公告)日：2017-02-09

申请号：US15229314

申请日：2016-08-05

Applicant: Arrowhead Pharmaceuticals, Inc.

Inventor： Christine I. Wooddell ,  David B. Rozema ,  David L. Lewis ,  Darren H. Wakefield ,  Lauren J. Almeida

IPC: A61K31/713 ,  A61K38/16

CPC classification number: A61K31/713 ,  A61K38/16 ,  A61K47/549 ,  A61K47/554 ,  A61K47/59 ,  A61K2300/00

Abstract: Described are compositions and methods for inhibition of Hepatitis B virus gene expression. RNA interference (RNAi) triggers and RNAi trigger conjugates for inhibiting the expression of Hepatitis B virus gene are described. Pharmaceutical compositions comprising one or more HBV RNAi triggers optionally with one or more additional therapeutics are also described. Delivery of the described HBV RNAi triggers to infected liver in vivo provides for inhibition of HBV gene expression and treatment.

Abstract translation: 描述了用于抑制乙型肝炎病毒基因表达的组合物和方法。 描述了用于抑制乙型肝炎病毒基因表达的RNA干扰（RNAi）触发剂和RNAi触发偶联物。 还描述了包含一种或多种HBV RNAi的药物组合物任选地与一种或多种另外的治疗剂触发。 所描述的HBV RNAi在体内传染给感染的肝脏可以抑制HBV基因的表达和治疗。

公开(公告)号：US20160339108A1

公开(公告)日：2016-11-24

申请号：US15164607

申请日：2016-05-25

Applicant: Nektar Therapeutics

Inventor： Lin Cheng ,  Jennifer Riggs-Sauthier ,  Neel K. Anand

IPC: A61K47/48 ,  A61K31/166 ,  C07C237/44

CPC classification number: A61K47/59 ,  A61K31/166 ,  A61K47/60 ,  C07C231/12 ,  C07C237/44

Abstract: The invention relates to (among other things) oligomer-containing benzamide-based compound compounds. A compound of the invention exhibits one or more advantages over corresponding compounds lacking the oligomer.

Abstract translation: 本发明涉及（尤其是）含低聚物的苯甲酰胺类化合物。 本发明的化合物相对于缺乏低聚物的相应化合物显示出一个或多个优点。

公开(公告)号：US20160317673A1

公开(公告)日：2016-11-03

申请号：US15205671

申请日：2016-07-08

Applicant: SERINA THERAPEUTICS, INC.

Inventor： J Milton HARRIS ,  Kunsang Yoon ,  Michael David Bentley ,  Zhihao Fang ,  Tacey Viegas

IPC: A61K47/48 ,  A61K31/7072 ,  A61K31/4745 ,  C08G69/00 ,  A61K31/7068 ,  A61K38/09 ,  A61K31/196 ,  C08G69/48 ,  A61K31/7008 ,  A61K31/519

CPC classification number: A61K38/09 ,  A61K47/59 ,  C08G73/0233

Abstract: The present disclosure provides copolymers of 2-substituted-2-oxazolines possessing two or three reactive functional groups which are also chemically orthogonal. The copolymers described may be random copolymers, block copolymers or a mixture of random and block copolymer configurations. Furthermore, the present disclosure provides novel methods for synthesizing the above polymers and for conjugating to molecules such as targeting, diagnostic and therapeutic agents.

Abstract translation: 本公开提供了具有两个或三个也是化学正交的反应性官能团的2-取代-2-恶唑啉的共聚物。 所述共聚物可以是无规共聚物，嵌段共聚物或无规嵌段共聚物构型的混合物。 此外，本公开提供了用于合成上述聚合物并用于与靶标，诊断和治疗剂等分子缀合的新方法。

公开(公告)号：US20160287717A1

公开(公告)日：2016-10-06

申请号：US15023093

申请日：2014-09-18

Applicant: STC.UNM ,  SANDIA CORPORATION

Inventor： Charles Jeffrey Brinker ,  Jason TOWNSON ,  Yu-Shen LIN ,  Paul N. DURFEE

IPC: A61K47/48 ,  A61K9/51

CPC classification number: A61K47/6929 ,  A61K9/0019 ,  A61K9/1271 ,  A61K9/5115 ,  A61K9/5146 ,  A61K47/02 ,  A61K47/59 ,  A61K47/60 ,  A61K47/6923

Abstract: In one aspect, the invention provides mesoporous silica nanoparticles (MSNPs), monodisperse populations of MSNPs and related protocells which exhibit single cell binding specificity to the substantial exclusion of non-targeted cells. For example, MSNPs and protocells of the invention may be used to target specific delivery of therapeutic agents to cancer cells or to specific blood vessel types (e.g. in the arterial, venous and/or capillary vessels or any combination of vessels). Related protocells, pharmaceutical compositions and therapeutic and diagnostic methods are also provided.

Abstract translation: 一方面，本发明提供介孔二氧化硅纳米颗粒（MSNP），MSNP的单分散群体和相关的原细胞，其显示出对非靶向细胞的实质排除的单细胞结合特异性。 例如，本发明的MSNPs和原细胞可用于靶向治疗剂到癌细胞或特定血管类型（例如在动脉，静脉和/或毛细血管或血管的任何组合中）的特异性递送。 还提供了相关的原细胞，药物组合物和治疗和诊断方法。

公开(公告)号：US20160228572A9

公开(公告)日：2016-08-11

申请号：US13911727

申请日：2013-06-06

Applicant: Robert Vestberg

Inventor： Robert Vestberg

IPC: A61K47/48

CPC classification number: A61K47/61 ,  A61K47/58 ,  A61K47/59 ,  A61K47/6957 ,  A61L33/0029

Abstract: There is described inter alia a medical device having a surface which comprises a coating layer, said coating layer being a biocompatible composition comprising an anti-coagulant entity capable of interacting with mammalian blood to prevent coagulation or thrombus formation, which anti-coagulant entity is covalently attached to said surface through a linker comprising a thioether.

公开(公告)号：US20160220696A1

公开(公告)日：2016-08-04

申请号：US15001119

申请日：2016-01-19

Applicant: Mersana Therapeutics, Inc.

Inventor： Aleksandr V. Yurkovetskiy ,  Mao Yin ,  Timothy B. Lowinger ,  Joshua D. Thomas ,  Charles E. Hammond ,  Cheri A. Stevenson ,  Natalya D. Bodyak ,  Patrick R. Conlon ,  Dimitry R. Gumerov

IPC: A61K47/48 ,  A61K31/4745 ,  C07K16/32

CPC classification number: A61K47/59 ,  A61K31/4745 ,  A61K47/64 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6883 ,  C07K7/02 ,  C07K16/32 ,  C08G65/33396 ,  C08G65/334

Abstract: Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

公开(公告)号：US09403851B2

公开(公告)日：2016-08-02

申请号：US14573099

申请日：2014-12-17

Applicant: The University of North Carolina at Chapel Hill

Inventor： Mark H. Schoenfisch ,  Jae Ho Shin ,  Nathan Stasko

IPC: A61K47/18 ,  C07F7/18 ,  A61K9/14 ,  A61K33/00 ,  C07F7/10 ,  A61K9/16 ,  A61K9/51 ,  A61K41/00 ,  A61K47/48 ,  B82Y5/00 ,  B82Y10/00 ,  B82Y30/00 ,  A61K31/695

CPC classification number: C07F7/10 ,  A61K9/14 ,  A61K9/167 ,  A61K9/5115 ,  A61K31/695 ,  A61K41/0042 ,  A61K47/59 ,  A61K47/6923 ,  A61K47/6929 ,  B82Y5/00 ,  B82Y10/00 ,  B82Y30/00 ,  C07F7/18

Abstract: The presently disclosed subject matter relates to nitric oxide-releasing particles for delivering nitric oxide, and their use in biomedical and pharmaceutical applications.

公开(公告)号：US20160199502A1

公开(公告)日：2016-07-14

申请号：US15056386

申请日：2016-02-29

Applicant: Rutgers, The State University of New Jersey ,  US Army, Secretary of the Army

Inventor： David Devore ,  Charles Roth

IPC: A61K47/48 ,  A61K31/713 ,  A61K31/711

CPC classification number: A61K47/59 ,  A61K9/1272 ,  A61K31/70 ,  A61K31/711 ,  A61K31/713 ,  A61K47/6911 ,  C08F265/02 ,  C08G81/025

Abstract: Graft copolymer polyelectrolyte complexes are disclosed for the efficient delivery of anionic, cationic or polyelectrolyte therapeutic agents into biological cells, and for maintaining the biological activity of these molecules while in serum and other aqueous environments are provided. Such complexes comprise (1) an anionic graft copolymer containing an anionic polymer backbone, with pendent carboxylic acid groups and pendant chains containing amphipathic or hydrophilic polymers covalently bonded to a portion of the pendant carboxylic acid groups, (2) one or more anionic, cationic or polyelectrolyte therapeutic agents, and (3) optionally a liposome optionally containing an additional therapeutic agent. Also disclosed are functional nanoparticles containing the complexes.

Abstract translation: 公开了接枝共聚物聚电解质络合物，用于将阴离子，阳离子或聚电解质治疗剂有效递送到生物细胞中，并且在提供血清和其它水性环境的同时保持这些分子的生物学活性。 这样的络合物包含（1）含有阴离子聚合物主链和侧链羧酸基团的阴离子接枝共聚物和含有共价键合到一部分羧酸侧基的两亲性或亲水性聚合物的侧链，（2）一种或多种阴离子阳离子 或聚电解质治疗剂，和（3）任选地含有另外的治疗剂的脂质体。 还公开了含有复合物的功能纳米粒子。

公开(公告)号：US20160184333A1

公开(公告)日：2016-06-30

申请号：US15070657

申请日：2016-03-15

Applicant: University of Massachusetts

Inventor： Dario C. Altieri ,  Byoung Heon Kang

IPC: A61K31/675

CPC classification number: A61K31/675 ,  A61K47/54 ,  A61K47/549 ,  A61K47/55 ,  A61K47/59 ,  A61K47/645 ,  A61K47/6455 ,  C07D225/06

Abstract: Described are mitochondria-targeted anti-tumor agents, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.