公开(公告)号：US11324827B2

公开(公告)日：2022-05-10

申请号：US15516259

申请日：2015-09-30

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Wengui Weng ,  Chao Liu ,  Ce Yan ,  Shaofeng Wu ,  Chun Zhou

IPC分类号： A61K47/10 ,  C08G65/334 ,  C08G65/323 ,  C08G65/08 ,  C08G65/329 ,  C08G65/00

摘要： Disclosed are a multifunctionalized polyethylene glycol derivative and a preparation method therefor. The derivative has an H-shaped structure as represented by formula (1) and comprises one linear core LPEG and four PEG branch chains, where n1, n2, n3, and n4 respectively are the degrees of polymerization of the branch chains, U1 and U2 are trivalent branching groups connecting the core LPEG to two of the PEG branch chains, F1 and F2 contain a functional group or a protected form R01 thereof and may or may not contain a branched group G, correspondingly, the number of R01 is one or more, F1 and F2 are either identical or different, any one linking group in the molecule or any linking group formed with an adjacent heteroatom group can either remain stable or be degraded, and any one PEG segment in the molecule is discretely polydispersed or monodispersed. The multifunctional polyethylene glycol is flexible and diverse in terms of branch structures and the lengths of branching arms, has various parameters and performance indicators that are adjustable and easy to control, and has a broad applicability.

公开(公告)号：US10434182B2

公开(公告)日：2019-10-08

申请号：US15738761

申请日：2016-06-08

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Wengui Weng ,  Chao Liu ,  Ce Yan ,  Huihuang Su ,  Chun Zhou

IPC分类号： A61K47/60 ,  C08G65/334 ,  C08G65/332 ,  C08G65/333 ,  A61K47/50 ,  C08G83/00 ,  A61K47/10

摘要： Disclosed are an eight-arm polyethylene glycol (PEG) derivative (formula I), production method therefor and modified bio-related substance thereby. Wherein, one tetravalent group U together with four trivalent groups Ec form a highly symmetrical octavalent group CORE0; Lc connects the octavalent group to eight PEG chains having polydispersity or monodispersity and having n1 to n8 as the degree of polymerization thereof; the terminal of one PEG chain is connected to at least one functional group F (k≥1); said PEG chain and F therebetween can be directly connected (g=0) or be indirectly connected via a linking group L0 to a terminal end-branching group G (g=1); the latter provides more reactive sites for binding more drug molecules and increases the drug loading. The eight-arm polyethylene glycol derivative has a centrosymmetric or approximately centrosymmetric structure, and leads to more precise control of the molecular weight in large-scale production and much narrower distribution of molecular weight for products. The modified bio-related substance thereby has a more uniform and controllable performance.

公开(公告)号：US20240342088A1

公开(公告)日：2024-10-17

申请号：US18269728

申请日：2022-04-01

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Wengui WENG ,  Chao LIU ,  Ailan WANG ,  Sheng LIN

IPC分类号： A61K9/127 ,  A61K9/51 ,  A61K45/06 ,  C07C219/06 ,  C07C229/16 ,  C07C229/26 ,  C07C271/16 ,  C07C271/18 ,  C07D207/452 ,  C07D233/60 ,  C12N15/113

CPC分类号： A61K9/1272 ,  A61K9/5123 ,  A61K45/06 ,  C07C219/06 ,  C07C229/16 ,  C07C229/26 ,  C07C271/16 ,  C07C271/18 ,  C07D207/452 ,  C07D233/60 ,  C12N15/113 ,  C12N2310/14

摘要： A novel cationic lipid has a structure as represented by general formula (1) and specifically relates to a nitrogen-branched cationic lipid, and a liposome containing the cationic lipid, and a nucleic-acid pharmaceutical composition containing the liposome, a preparation method and application thereof, wherein, the definition of each symbol in the formula (1) is as defined herein. The cationic liposome containing the cationic lipid as represented by formula (1) can improve the loading rate and transport efficiency of nucleic-acid drugs. The formulation of the cationic liposome nucleic-acid pharmaceutical composition has good cell compatibility and higher gene transfection capability, and can improve the treatment and/or prevention effects of nucleic-acid drugs.

公开(公告)号：US20240335384A1

公开(公告)日：2024-10-10

申请号：US18700022

申请日：2022-10-13

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Sheng LIN ,  Minggui LIN ,  Ailan WANG ,  Linlin WANG ,  Wengui WENG ,  Chao LIU ,  Jinchun YUAN ,  Qian LIN

IPC分类号： A61K9/127 ,  A61K45/00 ,  A61K47/18 ,  C07C217/08 ,  C07C219/06 ,  C07C229/10 ,  C07C229/26 ,  C07C235/10

CPC分类号： A61K9/1272 ,  A61K45/00 ,  A61K47/18 ,  C07C217/08 ,  C07C219/06 ,  C07C229/10 ,  C07C229/26 ,  C07C235/10

摘要： A novel cationic lipid having a structure as represented by general formula (1), which specifically relates to a nitrogen-containing cationic lipid, and also relates to a liposome containing the cationic lipid, a liposome pharmaceutical composition containing said cationic lipid, preparation and application thereof. A cationic liposome containing the cationic lipid represented by formula (1), can improve the loading rate and transport rate of drugs, particularly nucleic acid drugs. The terminus of the novel cationic lipid can contain a fluorescent group or a targeting group, so that the cationic liposome pharmaceutical composition containing the cationic lipid can have fluorescent or targeting function. A formulation of cationic liposome pharmaceutical composition containing nucleic acid exhibiting a very good gene complexing ability and high gene transfection ability, thereby further improves the gene therapeutic and/or gene diagnostic effect of the drug, and provides more selectable cationic lipids in the field of drug delivery.

公开(公告)号：US20240197633A1

公开(公告)日：2024-06-20

申请号：US18284740

申请日：2022-04-07

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Wengui WENG ,  Chao LIU ,  Ailan WANG ,  Minggui LIN ,  Qiaoyan LIU

IPC分类号： A61K9/127

CPC分类号： A61K9/1271

摘要： A novel PEGylated lipid and preparation methods thereof, a cationic liposome containing the PEGylated lipid, a pharmaceutical composition containing the liposome, a formulation and application thereof. The PEGylated lipid can be used for modifying a liposome, and it can be further modified and coupled with a targeting group, and then used for modifying a liposome to obtain a liposome with the targeting group. Due to the presence of a long-chain PEG and the targeting group on the lipid, the modified liposome can avoid being removed by the reticuloendothelial system in a human body and realize a targeting function. Therefore, when the modified liposome delivers an active drug to cells or a patient, especially when delivering a nucleic acid or anti-tumor drug, the liposome can realize long circulation in vivo and improve the transport efficiency of drug, and has a targeting unction so the therapeutic effect of a drug is improved.

公开(公告)号：US20220118100A1

公开(公告)日：2022-04-21

申请号：US17561342

申请日：2021-12-23

申请人： Xiamen Sinopeg Biotech Co., Ltd.

发明人： WenGui WENG ,  Chao LIU ,  JinCheng LIAO ,  JinChun YUAN

IPC分类号： A61K47/60 ,  C08G65/08 ,  C08G65/331 ,  C08G65/26

摘要： The monofunctional branched poly(ethylene glycol) (PEG) has a general formula shown in formula (1), and the bio-related substance modified by the monofunctional branched PEG has a general formula shown in formula (2), wherein X1 and X2 are each independently a hydrocarbon group having 1 to 20 carbon atoms, n1 and n2 are each independently an integer selected from 1 to 1000, n3 is an integer selected from 11 to 1000, L1, L2 are each independently a linking group, p is 0 or 1, q is 0 or 1, R1 is a hydrogen atom or a hydrocarbon group having 1 to 20 carbon atoms, D is a bio-related substance, Z is a linking group, and Z can react with the bio-related substance to form a residue group L3. The PEG-modified bio-related substance maintains good biological activity, and has better solubility and a longer half-life in vivo.

公开(公告)号：US20240180951A1

公开(公告)日：2024-06-06

申请号：US18284762

申请日：2022-04-07

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Wengui WENG ,  Chao LIU ,  Ailan WANG ,  Congming LIN ,  Linlin WANG

IPC分类号： A61K31/7105 ,  A61K9/127 ,  A61K9/51 ,  A61K31/713

CPC分类号： A61K31/7105 ,  A61K9/1272 ,  A61K9/5192 ,  A61K31/713

摘要： A novel PEGylated lipid and preparation methods thereof, a cationic liposome containing the lipid, a pharmaceutical composition containing the liposome, a formulation and application thereof. The PEGylated lipid can be used for modifying a liposome, and can be further modified and coupled with a targeting group and then used for modifying a liposome to obtain a liposome having the targeting group. Due to the presence of a long-chain PEG and the targeting group on the lipid, the modified liposome can avoid being removed by the reticuloendothelial system in a human body and realize a targeting function. Therefore, when the modified liposome delivers an active drug to cells or a patient, especially when delivering a nucleic acid or anti-tumor drug, the liposome can realize long circulation in vivo and improve the transport efficiency of drug, and has a targeting function, so the therapeutic effect of a drug is improved.

公开(公告)号：US20170312363A1

公开(公告)日：2017-11-02

申请号：US15516259

申请日：2015-09-30

申请人： XIAMEN SINOPEG BIOTECH CO., LTD.

发明人： Wengui WENG ,  Chao LIU ,  Ce YAN ,  Shaofeng WU ,  Chun ZHOU

IPC分类号： A61K47/10 ,  C08G65/00

CPC分类号： A61K47/10 ,  C08G65/002 ,  C08G65/08 ,  C08G65/323 ,  C08G65/329 ,  C08G65/334 ,  C08G2650/36 ,  C08G2650/58

摘要： Disclosed are a multifunctionalized polyethylene glycol derivative and a preparation method therefor. The derivative has an H-shaped structure as represented by formula (1) and comprises one linear core LPEG and four PEG branch chains, where n1, n2, n3, and n4 respectively are the degrees of polymerization of the branch chains, U1 and U2 are trivalent branching groups connecting the core LPEG to two of the PEG branch chains, F1 and F2 contain a functional group or a protected form R01 thereof and may or may not contain a branched group G, correspondingly, the number of R01 is one or more, F1 and F2 are either identical or different, any one linking group in the molecule or any linking group formed with an adjacent heteroatom group can either remain stable or be degraded, and any one PEG segment in the molecule is discretely polydispersed or monodispersed. The multifunctional polyethylene glycol is flexible and diverse in terms of branch structures and the lengths of branching arms, has various parameters and performance indicators that are adjustable and easy to control, and has a broad applicability.

公开(公告)号：US10660969B2

公开(公告)日：2020-05-26

申请号：US16527368

申请日：2019-07-31

申请人： Xiamen Sinopeg Biotech Co., Ltd.

发明人： Wengui Weng ,  Chao Liu ,  Ce Yan ,  Huihuang Su ,  Chun Zhou

IPC分类号： A61K47/60 ,  A61K47/10 ,  C08G65/332 ,  C08G65/334 ,  A61K47/50 ,  C08G65/333 ,  C08G83/00 ,  C08L101/00

摘要： Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k≥1), and said PEG chain and F can be directly connected (g=0) or connected with a divalent linking group L0 connected with a terminal branched group G (g=1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.

公开(公告)号：US20190365910A1

公开(公告)日：2019-12-05

申请号：US16527368

申请日：2019-07-31

申请人： Xiamen Sinopeg Biotech Co., Ltd.

发明人： Wengui Weng ,  Chao Liu ,  Ce Yan ,  Huihuang Su ,  Chun Zhou

IPC分类号： A61K47/60 ,  C08G65/332 ,  C08G65/334 ,  A61K47/10 ,  C08G65/333

摘要： Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k≥1), and said PEG chain and F can be directly connected (g=0) or connected with a divalent linking group L0 connected with a terminal branched group G (g=1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.