公开(公告)号：US11759528B2

公开(公告)日：2023-09-19

申请号：US16213485

申请日：2018-12-07

申请人： JenKem Technology Co., Ltd. (Beijing)

发明人： Yanping Song ,  Wen Li ,  Jinliang Wang ,  Yan Liu ,  Kun Zheng ,  Meina Lin ,  Zhen Wei ,  Zewang Feng ,  Xuan Zhao

IPC分类号： A61K47/68 ,  A61K31/4745 ,  C08G65/48 ,  A61P37/02 ,  A61P31/00 ,  A61P35/00 ,  C08G65/334 ,  C07C69/708 ,  A61K47/60 ,  C08G65/333 ,  A61K31/436 ,  A61K47/10 ,  A61K47/34 ,  C07C59/125 ,  C07C247/04 ,  C07C309/65 ,  C07D207/452 ,  C07D207/46 ,  C07K16/28 ,  C07K16/32

CPC分类号： A61K47/6855 ,  A61K31/436 ,  A61K31/4745 ,  A61K47/10 ,  A61K47/34 ,  A61K47/60 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6883 ,  A61P31/00 ,  A61P35/00 ,  A61P37/02 ,  C07C59/125 ,  C07C69/708 ,  C07C247/04 ,  C07C309/65 ,  C07D207/452 ,  C07D207/46 ,  C07K16/2809 ,  C07K16/32 ,  C08G65/334 ,  C08G65/3332 ,  C08G65/3344 ,  C08G65/33303 ,  C08G65/33317 ,  C08G65/48 ,  C07K2317/94

摘要： A PEG linker as represented by formula (I), wherein n and m are respectively an integer from 1 to 7, providing the PEG linker with 1 to 49 linking sites. A ligand drug conjugate as represented by formula (II). The conjugate uses the PEG linker to increase a drug loading capacity and drug loading diversity, thereby improving pharmaceutical efficacy.

Y1-PEG1-{R1-PEG2-{Y4}n}m  (I)

TM-{R2-PEG1-{R1-PEG2-{R3-A′-drug}n}m}l  (II)

公开(公告)号：US10098870B2

公开(公告)日：2018-10-16

申请号：US15170894

申请日：2016-06-01

申请人： JENKEM TECHNOLOGY CO., LTD. (BEIJING)

发明人： Jianhuan Jia ,  Zewang Feng ,  Jinliang Wang ,  Yan Liu ,  Zhenguo Wang ,  Xuan Zhao

IPC分类号： A61K31/436 ,  A61K47/48 ,  A61P35/00 ,  A61P37/00 ,  C07D498/18 ,  C08G65/331 ,  C08G65/333

摘要： The present invention provides compounds represented by formula (I) and pharmaceutical acceptable salts thereof, preparation method therefor and pharmaceutical composition containing the compounds represented by formula (I) and pharmaceutical acceptable salts thereof. In the compounds of the present invention, each terminal group of polyethylene glycol molecule can bond with a plurality of rapamycin molecules by cactus oligopeptide, with the loading rate of the pharmaceutical being increased. The compounds can be used to induce immunosuppression and treat graft rejection, autoimmune disease, solid tumors, fungal infection, and cardiovascular and cerebrovascular disease.

公开(公告)号：US10596268B2

公开(公告)日：2020-03-24

申请号：US16446872

申请日：2019-06-20

申请人： JenKem Technology Co., Ltd. (Beijing)

发明人： Zewang Feng ,  Jinliang Wang ,  Yanli Xiong ,  Xuan Zhao

IPC分类号： A61K47/60 ,  A61K31/135 ,  A61P25/04 ,  C07C215/64 ,  A61K47/55 ,  A61K47/56

摘要： The present invention relates to the technical field of medicine, in particular to a conjugate of dezocine and polyethylene glycol and a pharmaceutical composition thereof. The conjugate of dezocine and water-soluble oligomer provided by the present invention has better pharmacokinetic properties and a high drug absorption degree, may reduce the side effects of the drug, and achieve a smaller administration dosage and a more diverse mode of administration, such as oral administration, in clinic. Compared with dezocine, the conjugate of the present invention has a stronger analgesic effect and a longer analgesic duration, may reduce the frequency of drug administration, improve patient compliance, and has advantages in effectiveness and safety of the drug, as well as drug tolerance, etc.

公开(公告)号：US11564990B2

公开(公告)日：2023-01-31

申请号：US16588010

申请日：2019-09-30

申请人： JenKem Technology Co., Ltd. (Beijing)

发明人： Yanping Song ,  Jinghui Du ,  Leimin Wang ,  Jinliang Wang ,  Meina Lin ,  Zewang Feng ,  Xuan Zhao

IPC分类号： A61K47/60 ,  A61K31/436 ,  A61K47/65 ,  A61K47/68

摘要： The present invention provides a multi-drug-loading site and high drug-loading capacity ligand-drug conjugate. The ligand-drug conjugate has a structure of general formula (I). The ligand-drug conjugate has the characteristics of high loading capacity, high drug efficacy, low toxicity, and low risks. The ligand-drug conjugate can be used particularly to connect to a low toxicity chemical molecule, thereby extending a therapeutic window. Furthermore, the present invention provides an antibody-drug conjugate molecule. The antibody-drug conjugate molecule has the characteristics of multiple drug-loading ability and high drug-loading capacity, such that the antibody-drug conjugate can carry a large amount of a low toxicity chemical molecule and achieve a therapeutic effect without depending on antibody targeting or high toxicity chemicals. TM-{R2-PEG1-[R1-PEG2-(R3-A′-D)n]m}l  (I