公开(公告)号：US20160128938A9

公开(公告)日：2016-05-12

申请号：US14651840

申请日：2013-12-12

申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION

发明人： Xiang Gao ,  Song Li ,  Peter Wipf ,  Michael Wayne Epperly ,  Joel S. Greenberger

IPC分类号： A61K9/107 ,  A61K31/337 ,  A61K31/704 ,  A61K31/45

CPC分类号： A61K9/1075 ,  A61K9/1271 ,  A61K31/337 ,  A61K31/45 ,  A61K31/704

摘要： A method of creating a formulation for a compound includes determining a compound interactive agent comprising at least one group that interacts with the compound, creating a carrier agent by conjugating at least one compound interactive domain comprising the at least one group that interacts with the compound with at least one hydrophilic domain, and combining the compound and the carrier agent to create the formulation. Creating the carrier agent may further include conjugating the at least one compound interactive domain with at least one hydrophobic domain so that the at least one compound interactive domain is positioned between the at least one hydrophilic domain and the at least one hydrophobic domain.

公开(公告)号：US09855341B2

公开(公告)日：2018-01-02

申请号：US14625873

申请日：2015-02-19

申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

发明人： Song Li ,  Yixian Huang ,  Xiaolan Zhang ,  Xiang Gao

IPC分类号： A61K47/48 ,  A61K31/337 ,  A61K31/235 ,  A61K31/704 ,  A61K9/00 ,  A61K9/107 ,  C08G65/331 ,  C08G65/333 ,  C08G65/334

CPC分类号： A61K47/60 ,  A61K9/0019 ,  A61K9/1075 ,  A61K31/235 ,  A61K31/337 ,  A61K31/704 ,  C08G65/331 ,  C08G65/3311 ,  C08G65/33306 ,  C08G65/33396 ,  C08G65/334 ,  C08G65/3344 ,  C08L2203/02

摘要： A method of forming or creating a formulation for a compound to be delivered includes creating a carrier agent by conjugating at least one hydrophobic domain or hydrophobic compound with at least one hydrophilic domain or hydrophilic compound and associating the compound to be delivered with the carrier agent to create the formulation. The at least one hydrophobic compound has the formula: wherein R1 is a farnesyl group, a geranyl group or geranyl-geranyl group, X is O, S, SO, SO2, NH or Se, Z is C—R2 or N, R2 is H, CN, CO2R7, SO3R7, CONR7R8 or SO2NR7R8, wherein R7 and R8 are each independently H, an alkyl group, an alkenyl group, CO2M or SO3M, wherein M is a cation and R3, R4, and R5 are independently H, a carboxyl group, an alkyl group, an alkenyl group, an aminoalkyl group, a nitroalkyl group, a nitro group, a halo atom, an amino group, a mono-alkylamino group, a di-alkylamino group, mercapto group, a mercaptoalkyl group, an azido group or a thiocyanato group. A plurality of the carrier agents are adapted to assemble into a structure. The hydrophobic compound is cleavably conjugated to the at least one hydrophilic compound via a linkage which is labile in vivo.

公开(公告)号：US08771728B2

公开(公告)日：2014-07-08

申请号：US13712804

申请日：2012-12-12

申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

发明人： Leaf Huang ,  Xiang Gao ,  Frank L. Sorgi

IPC分类号： A61K9/127 ,  A61K38/00 ,  C07H21/04

CPC分类号： A61K47/48315 ,  A61K9/1272 ,  A61K47/543 ,  A61K47/645 ,  C12N15/88

摘要： Novel stable, concentrated, biologically active and ready-to-use lipid-comprising drug delivery complexes and methods for their production are described. The biological activity of the complexes produced are comparable to the formulations prepared according to the prior art admixture method and upon purification, the complexes produced by the method of this invention are 50 to 500 fold more concentrated than the complexes formed by admixture. The method described herein provides for the large scale production of lipid-comprising drug delivery systems useful for gene therapy and other applications.

摘要翻译： 描述了新的稳定的，浓缩的，生物活性的和即用型含脂质的药物递送复合物及其生产方法。 所生成的络合物的生物活性与根据现有技术的混合方法制备的制剂相当，并且在纯化后，通过本发明的方法制备的络合物比通过混合物形成的络合物多50至500倍。 本文所述的方法提供大规模生产用于基因治疗和其它应用的含脂质药物递送系统。

公开(公告)号：US10172795B2

公开(公告)日：2019-01-08

申请号：US14651840

申请日：2013-12-12

申请人： University of Pittsburgh—Of The Commonwealth System of Higher Education

发明人： Xiang Gao ,  Song Li ,  Peter Wipf ,  Michael Wayne Epperly ,  Joel S. Greenberger

IPC分类号： A61K31/45 ,  A61K9/107 ,  A61K9/127 ,  A61K31/337 ,  A61K31/704

摘要： A method of creating a formulation for a compound includes determining a compound interactive agent comprising at least one group that interacts with the compound, creating a carrier agent by conjugating at least one compound interactive domain comprising the at least one group that interacts with the compound with at least one hydrophilic domain, and combining the compound and the carrier agent to create the formulation. Creating the carrier agent may further include conjugating the at least one compound interactive domain with at least one hydrophobic domain so that the at least one compound interactive domain is positioned between the at least one hydrophilic domain and the at least one hydrophobic domain.

公开(公告)号：US10376591B2

公开(公告)日：2019-08-13

申请号：US15703110

申请日：2017-09-13

申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education

发明人： Song Li ,  Yixian Huang ,  Xiaolan Zhang ,  Xiang Gao

IPC分类号： A61K47/60 ,  A61K31/337 ,  A61K31/235 ,  A61K31/704 ,  A61K9/00 ,  A61K9/107 ,  C08G65/331 ,  C08G65/333 ,  C08G65/334

摘要： A formulation includes a carrier agent formed by conjugating at least one biologically active hydrophobic compound with at least one hydrophilic compound, the at least one biologically active hydrophobic compound selected from the group of farnesylthiosalicylic acid and a derivative of farnesylthiosalicylic acid which is biologically active as an RAS antagonist, wherein a plurality of the carrier agents are adapted to assemble into a structure and the at least one biologically active hydrophobic compound is conjugated with the at least one hydrophilic compound via a linkage which is labile in vivo, and a biologically active compound associated with the carrier agent.

公开(公告)号：US20190038556A1

公开(公告)日：2019-02-07

申请号：US16154881

申请日：2018-10-09

申请人： University of Pittsburgh - Of The Commonwealth System of Higher Education

发明人： Xiang Gao ,  Song Li ,  Peter Wipf ,  Michael Wayne Epperly ,  Joel S. Greenberger

IPC分类号： A61K9/107 ,  A61K31/337 ,  A61K31/45 ,  A61K31/704 ,  A61K9/127

摘要： A method of creating a formulation for a compound includes determining a compound interactive agent comprising at least one group that interacts with the compound, creating a carrier agent by conjugating at least one compound interactive domain comprising the at least one group that interacts with the compound with at least one hydrophilic domain, and combining the compound and the carrier agent to create the formulation. Creating the carrier agent may further include conjugating the at least one compound interactive domain with at least one hydrophobic domain so that the at least one compound interactive domain is positioned between the at least one hydrophilic domain and the at least one hydrophobic domain.

公开(公告)号：US20150306034A1

公开(公告)日：2015-10-29

申请号：US14651840

申请日：2013-12-12

申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION

发明人： Xiang Gao ,  Song Li ,  Peter Wipf ,  Michael Wayne Epperly ,  Joel S. Greenberger

IPC分类号： A61K9/107 ,  A61K31/337 ,  A61K31/704 ,  A61K31/45

CPC分类号： A61K9/1075 ,  A61K9/1271 ,  A61K31/337 ,  A61K31/45 ,  A61K31/704

摘要： A method of creating a formulation for a compound includes determining a compound interactive agent comprising at least one group that interacts with the compound, creating a carrier agent by conjugating at least one compound interactive domain comprising the at least one group that interacts with the compound with at least one hydrophilic domain, and combining the compound and the carrier agent to create the formulation. Creating the carrier agent may further include conjugating the at least one compound interactive domain with at least one hydrophobic domain so that the at least one compound interactive domain is positioned between the at least one hydrophilic domain and the at least one hydrophobic domain.

摘要翻译： 创建化合物制剂的方法包括确定包含与化合物相互作用的至少一个基团的化合物相互作用试剂，通过将包含与该化合物相互作用的至少一个基团的至少一个化合物相互作用结构域与 至少一个亲水结构域，并组合化合物和载体试剂以产生制剂。 产生载体试剂可以进一步包括将至少一个化合物交互结构域与至少一个疏水结构域共轭，使得至少一个化合物相互作用结构域位于至少一个亲水结构域和至少一个疏水结构域之间。

公开(公告)号：US20190210969A1

公开(公告)日：2019-07-11

申请号：US16240595

申请日：2019-01-04

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Michael W. Epperly ,  Xiang Gao ,  Joel S. Greenberger ,  Song Li ,  Peter Wipf

IPC分类号： C07D211/94 ,  C07K5/087 ,  C07F9/22 ,  A61K31/13 ,  C07D207/46 ,  A61K31/445 ,  C07D471/08

CPC分类号： C07D211/94 ,  A61K31/13 ,  A61K31/445 ,  C07D207/46 ,  C07D471/08 ,  C07F9/22 ,  C07K5/0812

摘要： Provided herein are compositions and related methods useful for prevention or mitigation of ionizing radiation-induced esophagitis. The compositions comprise compounds comprising a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent or mitigate esophageal damage caused by radiation.

公开(公告)号：US20150065443A1

公开(公告)日：2015-03-05

申请号：US14391001

申请日：2013-04-04

申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION

发明人： Song Li ,  Xiang Gao ,  Yixian Huang ,  Jianqin Lu

IPC分类号： A61K9/107 ,  A61K31/704 ,  A61K31/337 ,  A61K47/48 ,  A61K31/122

CPC分类号： A61K9/1075 ,  A61K31/122 ,  A61K31/337 ,  A61K31/436 ,  A61K31/4745 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/13 ,  A61K47/18 ,  A61K47/55 ,  A61K47/60 ,  A61K2300/00

摘要： A composition having a structure of: X-L-Y wherein X comprises at least one embelin moiety;L comprises a linker; andY comprises a hydrophilic moiety.Also disclosed is a micelle that includes:a core that includes at least one hydrophobic active agent and at least one embelin moiety; anda hydrophilic zone surrounding the core and comprising at least one hydrophilic moiety.

摘要翻译： 具有以下结构的组合物：X-L-Y，其中X包含至少一个连接子部分; L包含连接体; Y包含亲水部分。 还公开了一种胶束，其包括：核心，其包含至少一种疏水性活性剂和至少一种丝氨酸部分; 以及包围所述芯并且包含至少一个亲水部分的亲水区。