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：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.