公开(公告)号：US10463746B2

公开(公告)日：2019-11-05

申请号：US15807602

申请日：2017-11-09

Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION ,  AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

Inventor： Dylan Boday ,  Wei Cheng ,  Jeannette M. Garcia ,  James Hedrick ,  Nathaniel H. Park ,  Rudy J. Wojtecki ,  Chuan Yang ,  YiYan Yang

IPC: A61K47/60 ,  A61K47/69 ,  A61K31/785 ,  A61P35/00

Abstract: Embodiments of the invention are directed to a macromolecular chemotherapeutic. A non-limiting example of the macromolecular chemotherapeutic includes a block copolymer. The block copolymer can include a water-soluble block, a cationic block, and a linker, wherein the linker is connected to the water-soluble bock and the charged block.

公开(公告)号：US11485823B2

公开(公告)日：2022-11-01

申请号：US16627094

申请日：2018-05-23

Applicant: Agency for Science, Technology and Research

Inventor： Yi-Yan Yang ,  Chuan Yang ,  Wei Cheng ,  Ashlynn Lee

IPC: C08G73/02 ,  A61K47/59

Abstract: The present invention mainly relates to a polymer for delivery of biologically active materials, a complex and a method of synthesis thereof. The polymer comprises a poly(ethylene imine) and at least one monomer, each monomer comprising a modified sugar moiety, preferably galactose, comprising a sulphur atom or a nitrogen atom and a chemical moiety comprising a terminal epoxide for linking the polyethylene imine to the monomer, wherein the sulphur atom or the nitrogen atom links the modified sugar moiety to the chemical moiety. The biologically active material is preferably a gene, siRNA, mRNA or plasmid DNA. Further disclosed is the medical use of said complex in treating a disease caused by a genetic disorder, for example cancer.

公开(公告)号：US09399044B2

公开(公告)日：2016-07-26

申请号：US14288782

申请日：2014-05-28

Applicant: International Business Machines Corporation ,  Agency For Science, Technology and Research

Inventor： Wei Cheng ,  Xin Ding ,  Jeannette M. Garcia ,  James L. Hedrick ,  Chuan Yang ,  Yi Yan Yang

IPC: A01N63/00 ,  A01N37/44 ,  A61K31/785 ,  C08G73/02 ,  A01N37/46 ,  A01N33/04 ,  A01N47/30

CPC classification number: A61K31/785 ,  A01N33/04 ,  A01N37/46 ,  A01N47/30 ,  C08G73/0226 ,  Y02A50/473 ,  A01N25/10

Abstract: Antimicrobial, non-hemolytic cationic polyamines were prepared by treating partially N-acylated polyethylenimines and/or partially oxidized polyethylenimines with a protic acid. The cationic polyamines can have a linear or branched polyethylenimine backbone structure. Preferably, the cationic polyamines comprise pendant urea groups, which can be introduced via a cyclic carbonate comprising a pendant urea group. The cationic polyamines can be active against a tuberculosis mycobacterium at low concentration. The cationic polyamines are also effective against Gram-negative Escherichia coli and Pseudomonas aeruginosa, Gram-positive Staphylococcus aureus, and fungus Candida albicans in solution and in the form of a film.

Abstract translation: 通过用质子酸处理部分N-酰化的聚乙烯亚胺和/或部分氧化的聚乙烯亚胺制备抗微生物，非溶血性阳离子多胺。 阳离子多胺可以具有直链或支链的聚乙烯亚胺骨架结构。 优选地，阳离子多胺包括侧链脲基团，其可以通过包含侧基脲基团的环状碳酸酯引入。 阳离子多胺对低浓度的结核分枝杆菌具有活性。 阳离子多胺对溶液中的革兰氏阴性大肠杆菌和铜绿假单胞菌，革兰氏阳性金黄色葡萄球菌和真菌白色念珠菌也是有效的。

公开(公告)号：US20150342984A1

公开(公告)日：2015-12-03

申请号：US14288782

申请日：2014-05-28

Applicant: International Business Machines Corporation ,  Agency For Science, Technology and Research

Inventor： Wei Cheng ,  Xin Ding ,  Jeannette M. Garcia ,  James L. Hedrick ,  Chuan Yang ,  Yi Yan Yang

IPC: A61K31/785 ,  A01N37/46 ,  C08G73/02

CPC classification number: A61K31/785 ,  A01N33/04 ,  A01N37/46 ,  A01N47/30 ,  C08G73/0226 ,  Y02A50/473 ,  A01N25/10

Abstract: Antimicrobial, non-hemolytic cationic polyamines were prepared by treating partially N-acylated polyethylenimines and/or partially oxidized polyethylenimines with a protic acid. The cationic polyamines can have a linear or branched polyethylenimine backbone structure. Preferably, the cationic polyamines comprise pendant urea groups, which can be introduced via a cyclic carbonate comprising a pendant urea group. The cationic polyamines can be active against a tuberculosis mycobacterium at low concentration. The cationic polyamines are also effective against Gram-negative Escherichia coli and Pseudomonas aeruginosa, Gram-positive Staphylococcus aureus, and fungus Candida albicans in solution and in the form of a film.

Abstract translation: 通过用质子酸处理部分N-酰化的聚乙烯亚胺和/或部分氧化的聚乙烯亚胺制备抗微生物，非溶血性阳离子多胺。 阳离子多胺可以具有直链或支链的聚乙烯亚胺骨架结构。 优选地，阳离子多胺包括侧链脲基团，其可以通过包含侧基脲基团的环状碳酸酯引入。 阳离子多胺对低浓度的结核分枝杆菌具有活性。 阳离子多胺对溶液中的革兰氏阴性大肠杆菌和铜绿假单胞菌，革兰氏阳性金黄色葡萄球菌和真菌白色念珠菌也是有效的。

公开(公告)号：US20200165390A1

公开(公告)日：2020-05-28

申请号：US16627094

申请日：2018-05-23

Applicant: Agency for Science, Technology and Research

Inventor： Yi-Yan Yang ,  Chuan Yang ,  Wei Cheng ,  Ashlynn Lee

IPC: C08G73/02 ,  A61K47/59

Abstract: The present invention mainly relates to a polymer for delivery of biologically active materials, a complex and a method of synthesis thereof. The polymer comprises a poly(ethylene imine) and at least one monomer, each monomer comprising a modified sugar moiety, preferably galactose, comprising a sulphur atom or a nitrogen atom and a chemical moiety comprising a terminal epoxide for linking the polyethylene imine to the monomer, wherein the sulphur atom or the nitrogen atom links the modified sugar moiety to the chemical moiety. The biologically active material is preferably a gene, siRNA, mRNA or plasmid DNA. Further disclosed is the medical use of said complex in treating a disease caused by a genetic disorder, for example cancer.

公开(公告)号：US20200023069A1

公开(公告)日：2020-01-23

申请号：US16577142

申请日：2019-09-20

Applicant: International Business Machines Corporation ,  Agency for Science, Technology and Research

Inventor： Dylan Boday ,  Wei Cheng ,  Jeannette M. Garcia ,  James Hedrick ,  Nathaniel H. Park ,  Rudy J. Wojtecki ,  Chuan Yang ,  YiYan Yang

IPC: A61K47/60 ,  C08G65/332 ,  C08G65/00 ,  C08L71/02 ,  C08G64/18 ,  C08L71/00 ,  A61K9/107 ,  A61K47/69 ,  A61K31/785 ,  A61P35/00

Abstract: Embodiments of the invention are directed to a macromolecular chemotherapeutic. A non-limiting example of the macromolecular chemotherapeutic includes a block copolymer. The block copolymer can include a water-soluble block, a cationic block, and a linker, wherein the linker is connected to the water-soluble bock and the charged block.

公开(公告)号：US11116844B2

公开(公告)日：2021-09-14

申请号：US16577142

申请日：2019-09-20

Applicant: International Business Machines Corporation ,  Agency for Science, Technology and Research

Inventor： Dylan Boday ,  Wei Cheng ,  Jeannette M. Garcia ,  James Hedrick ,  Nathaniel H. Park ,  Rudy J. Wojtecki ,  Chuan Yang ,  YiYan Yang

IPC: A61K47/60 ,  A61K47/69 ,  A61K31/785 ,  A61P35/00 ,  C08G65/332 ,  C08G65/00 ,  C08L71/02 ,  C08G64/18 ,  C08L71/00 ,  A61K9/107

Abstract: Embodiments of the invention are directed to a macromolecular chemotherapeutic. A non-limiting example of the macromolecular chemotherapeutic includes a block copolymer. The block copolymer can include a water-soluble block, a cationic block, and a linker, wherein the linker is connected to the water-soluble bock and the charged block.

公开(公告)号：US09987369B2

公开(公告)日：2018-06-05

申请号：US15340795

申请日：2016-11-01

Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION ,  AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

Inventor： Wei Cheng ,  Mareva B. Fevre ,  James L. Hedrick ,  Nor Lizawati Ibrahim ,  Ashlynn L. Z. Lee ,  Victor W. L. Ng ,  Robert J. Ono ,  Chuan Yang ,  Yi Yan Yang

IPC: A61K39/395 ,  A61K31/65 ,  A61K31/4196 ,  A61K45/06 ,  A61K9/00 ,  A61K9/06 ,  A61K31/592 ,  A61K31/355 ,  C08G64/18 ,  C07K16/32 ,  A61K47/48 ,  A61K31/455

CPC classification number: A61K47/6903 ,  A61K9/0014 ,  A61K9/0024 ,  A61K9/06 ,  A61K31/355 ,  A61K31/4196 ,  A61K31/455 ,  A61K31/592 ,  A61K31/65 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/22 ,  A61K47/34 ,  A61K47/48192 ,  A61K47/48784 ,  A61K47/59 ,  C07K16/32 ,  C08G64/183 ,  C08G2210/00

Abstract: Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks linked to the central block by linking groups bearing one or more hydrogen bond forming *—N(H)—* groups. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions have utility in depot injections for drug delivery. The hydrogen bonding *—N(H)—* group(s) provide longer in vivo lifetime of the hydrogel before degradation and a more prolonged and controlled release rate of a hydrophobic drug compared to similar hydrogels prepared from poly(ethylene glycol).

公开(公告)号：US20180117162A1

公开(公告)日：2018-05-03

申请号：US15340795

申请日：2016-11-01

Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION ,  AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

Inventor： Wei Cheng ,  Mareva B. Fevre ,  James L. Hedrick ,  Nor Lizawati Ibrahim ,  Ashlynn L.Z. Lee ,  Victor W.L. Ng ,  Robert J. Ono ,  Chuan Yang ,  Yi Yan Yang

IPC: A61K47/48 ,  A61K31/355 ,  A61K31/592 ,  A61K9/06 ,  C07K16/32 ,  A61K9/00 ,  A61K39/395 ,  A61K45/06 ,  A61K31/4196 ,  A61K31/65 ,  C08G64/18 ,  A61K31/455

CPC classification number: A61K47/6903 ,  A61K9/0014 ,  A61K9/0024 ,  A61K9/06 ,  A61K31/355 ,  A61K31/4196 ,  A61K31/455 ,  A61K31/592 ,  A61K31/65 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/22 ,  A61K47/34 ,  A61K47/48192 ,  A61K47/48784 ,  A61K47/59 ,  C07K16/32 ,  C08G64/183 ,  C08G2210/00

Abstract: Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks linked to the central block by linking groups bearing one or more hydrogen bond forming *—N(H)—* groups. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions have utility in depot injections for drug delivery. The hydrogen bonding *—N(H)—* group(s) provide longer in vivo lifetime of the hydrogel before degradation and a more prolonged and controlled release rate of a hydrophobic drug compared to similar hydrogels prepared from poly(ethylene glycol).