公开(公告)号：US09675556B2

公开(公告)日：2017-06-13

申请号：US14575517

申请日：2014-12-18

Applicant: Howard University

Inventor： Emmanuel Oyekanmi Akala ,  Simeon Kolawole Adesina

IPC: B01J13/06 ,  B01J13/16 ,  A61K9/16 ,  A61K31/337 ,  A61K31/704 ,  B82Y5/00 ,  B82Y15/00 ,  B82Y40/00 ,  A61K9/51 ,  C08G63/85

CPC classification number: C08G63/78 ,  A61K9/1635 ,  A61K9/5153 ,  A61K31/337 ,  A61K31/7034 ,  A61K31/704 ,  B01J13/06 ,  B01J13/16 ,  B82Y5/00 ,  B82Y15/00 ,  B82Y40/00 ,  C08F299/024 ,  C08G63/06 ,  C08G63/82 ,  C08G63/85 ,  C08G63/912 ,  Y10S977/773 ,  Y10T428/2982

Abstract: The present invention is directed to a crosslinked or non-crosslinked polymer particle, wherein the crosslinked polymer particle comprises a copolymer of poly(alklyene glycol-graft-lactate) that is crosslinked by at least one hydrolysable monomer. Another embodiment of the present invention is a polymer particle comprising a crosslinked polymer particle that is a product of starting materials comprising (a) a hydrophilic monomer, (b) a hydrophobic monomer, and (c) a hydrolysable crosslinking agent. Another embodiment of the present invention is a polymer particle comprising, a crosslinked copolymer comprises structures represented by Formulas (I), (II), and (III), where Formulas (I), (II) and (III) are defined in the specification. Yet other embodiments of the present invention include a method of preparing a methacrylate terminated macromonomer, a method of preparing a crosslinking agent, and a method of preparing a therapeutic agent loaded nanosphere by dispersion polymerization.

公开(公告)号：US11826344B2

公开(公告)日：2023-11-28

申请号：US15775986

申请日：2016-11-18

Applicant: HOWARD UNIVERSITY

Inventor： Simeon Kolawole Adesina

IPC: A61K31/366 ,  A61K31/337 ,  C07D493/20 ,  A61K47/64 ,  A61P35/00 ,  A61K38/00 ,  A61K9/51

CPC classification number: A61K31/366 ,  A61K9/5146 ,  A61K9/5184 ,  A61K31/337 ,  A61K47/64 ,  A61P35/00 ,  C07D493/20 ,  A61K38/00 ,  A61K31/337 ,  A61K2300/00 ,  A61K31/366 ,  A61K2300/00

Abstract: Disclosed are bruceolides for the treatment of cancer, and other diseases, selectively targeting unwanted cells. The disclosed bruceolides may include a site specific cleavable moiety inhibiting the chemotoxic activity until cleaved, i.e., removed, within and/or near a cancer to be treated. As to facilitate selective delivery to cancer tumors, the disclosed bruceolides may be loaded into, attached to or otherwise carried by nanoparticles.

公开(公告)号：US20180325865A1

公开(公告)日：2018-11-15

申请号：US15775986

申请日：2016-11-18

Applicant: HOWARD UNIVERSITY

Inventor： Simeon Kolawole Adesina

IPC: A61K31/366 ,  A61K9/51 ,  A61K47/64 ,  A61P35/00

CPC classification number: A61K31/366 ,  A61K9/5146 ,  A61K9/5184 ,  A61K31/337 ,  A61K38/00 ,  A61K47/64 ,  A61P35/00 ,  C07D493/20 ,  A61K2300/00

Abstract: Disclosed are bruceolides for the treatment of cancer, and other diseases, selectively targeting unwanted cells. The disclosed bruceolides may include a site specific cleavable moiety inhibiting the chemotoxic activity until cleaved, i.e., removed, within and/or near a cancer to be treated. As to facilitate selective delivery to cancer tumors, the disclosed bruceolides may be loaded into, attached to or otherwise carried by nanoparticles.

公开(公告)号：US20150209287A1

公开(公告)日：2015-07-30

申请号：US14575517

申请日：2014-12-18

Applicant: Howard University

Inventor： Emmanuel Oyekanmi Akala ,  Simeon Kolawole Adesina

IPC: A61K9/16 ,  A61K31/337 ,  C08G63/85

CPC classification number: C08G63/78 ,  A61K9/1635 ,  A61K9/5153 ,  A61K31/337 ,  A61K31/7034 ,  A61K31/704 ,  B01J13/06 ,  B01J13/16 ,  B82Y5/00 ,  B82Y15/00 ,  B82Y40/00 ,  C08F299/024 ,  C08G63/06 ,  C08G63/82 ,  C08G63/85 ,  C08G63/912 ,  Y10S977/773 ,  Y10T428/2982

Abstract: The present invention is directed to a crosslinked or non-crosslinked polymer particle, wherein the crosslinked polymer particle comprises a copolymer of poly(alklyene glycol-graft-lactate) that is crosslinked by at least one hydrolysable monomer. Another embodiment of the present invention is a polymer particle comprising a crosslinked polymer particle that is a product of starting materials comprising (a) a hydrophilic monomer, (b) a hydrophobic monomer, and (c) a hydrolysable crosslinking agent. Another embodiment of the present invention is a polymer particle comprising, a crosslinked copolymer comprises structures represented by Formulas (I), (II), and (III), where Formulas (I), (II) and (III) are defined in the specification. Yet other embodiments of the present invention include a method of preparing a methacrylate terminated macromonomer, a method of preparing a crosslinking agent, and a method of preparing a therapeutic agent loaded nanosphere by dispersion polymerization.

Abstract translation: 本发明涉及交联或非交联聚合物颗粒，其中交联聚合物颗粒包含由至少一种可水解单体交联的聚（烷二醇 - 接枝 - 乳酸）共聚物。 本发明的另一个实施方案是包含交联聚合物颗粒的聚合物颗粒，其是起始材料的产物，其包含（a）亲水性单体，（b）疏水性单体和（c）可水解交联剂。 本发明的另一个实施方案是包含交联共聚物的聚合物颗粒，其包含由式（I），（II）和（III）表示的结构，其中式（I），（II）和（III） 规范。 本发明的其它实施方案包括制备甲基丙烯酸酯封端的大分子单体的方法，制备交联剂的方法，以及通过分散聚合制备负载纳米球的治疗剂的方法。