Jenkem Technologyco., Ltd.. (tianjin)

Jenkem Technology Co., Ltd. (beijing)

Jenkem Technology Co., Ltd.

Jenkem Technology Co., Ltd., Tianjin Branch

Cansino (shanghai) Biological Research Co., Ltd.

Meina Lin

Xuan Zhao

Hui Zhu

Zhen Wei

Xiaomeng Chen

Jinliang Wang

Zewang Feng

Yanping Song

Yang Wang

Yan Liu

Wen Li

Jian Liu

Xuefeng Yu

Yu Sun

Qingbin Wang

Kun Zheng

Rujun Zhang

Leimin Wang

Jinghui Du

Junye Li

Zhen'gang Zhu

Jing Hao

Haomeng Wang

Zhihong Yan

Dongxu Qiu

Shengyong Yan

Yanli Xiong

Jun Guo

Tao Zhu

Being used for drug modification, the multi-arm single molecular weight polyethylene glycol active derivative provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the multi-arm single molecular weight polyethylene glycol active derivative provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.

Multi-arm single molecular weight polyethylene glycol active derivative and application thereof

The present invention provides a composition of a polyethylene glycol maleimide derivative and a polymerization inhibitor. In particular, the present invention provides a composition of an 8-arm polyethylene glycol maleimide derivative and a phenolic polymerization inhibitor. The ingredient and content of the polymerization inhibitor in the composition are reasonably chosen, thereby significantly increasing stability of the polyethylene glycol maleimide derivative, effectively avoiding the undesirable effect of gel solidifying due to polymerization during storage and transportation, and extending a pot life and shelf life of a product thereof.

Composition of polyethylene glycol maleimide derivative and polymerization inhibitor

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-{R-PEG2-{Y4}}&#x2003;&#x2003;(I)TM-{R-PEG1-{R-PEG2-{R-A'-drug}}}&#x2003;&#x2003;(II)

Peg linker and ligand drug conjugate

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.-{-1-[-2-(-'-)]}&#x2003;&#x2003;(I

Multi-drug-loading-site, high drug-loading capacity ligand-drug conjugate

Being used for drug modification, the multi-arm single molecular weight polyethylene glycol and an active derivative thereof provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the active derivative of the multi-arm single molecular weight polyethylene glycol provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.

Multi-arm single molecular weight polyethylene glycol, active derivative thereof, and preparation and application thereof

Disclosed in the present invention is a method for preparing a Y-branched hydrophilic polymer carboxylic acid derivative, in particular a method for preparing a Y-branched polyethylene glycol carboxylic acid derivative having a high purity and high molecular weight. The preparation steps are simple, the product of the reaction is easy to be separated, the cost for separation is low, and the purity and yield of the product are high, facilitating the subsequent preparation of other derivatives and medicament conjugates based on the preparation of the carboxylic acid derivative, which is advantageous for industrial scale-up and commercial applications. The prepared Y-branched hydrophilic polymer carboxylic acid derivative (in particular the Y-branched polyethylene glycol carboxylic acid derivative having a high molecular weight) product has a high purity and high commercial application value, in particular in the use of the preparation of medicaments for preventing and/or treating diseases.

Method for preparing Y-branched hydrophilic polymer carboxylic acid derivative

The present invention discloses a branched polyethylene glycol epoxy derivative crosslinked sodium hyaluronate gel, preparation and application thereof. The crosslinking agent used in the crosslinked sodium hyaluronate gel prepared by the present invention is a polyethylene glycol epoxy derivative, due to the existence of multiple ether bonds in the molecule of the crosslinking agent, there are more hydrogen bonds in the gel system; meanwhile, due to the particularity of the space structure of the branched polyethylene glycol epoxy derivative, the gel prepared has a more complex winding structure in its space, thus achieving better stability. Moreover, the branched polyethylene glycol epoxy derivative involved in the present invention is a compound with single molecular weight, therefore, the gel prepared thereby has better batch stability.

Branched polyethylene glycol epoxy derivative crosslinked sodium hyaluronate gel, preparation and application thereof

The present invention discloses polyglycol epoxide crosslinked sodium hyaluronate gel for injection and a preparation method thereof. A polyglycol epoxide is a compound with single molecular weight preferably; a plurality of ether bonds are present in the molecule of the polyglycol epoxide, the water solubility is good, and thus, the polyglycol epoxide is more easily subjected to a crosslinking reaction with polysaccharides; and meanwhile, polyglycol is relatively easy in adjustment of the number of repeating units and relatively easy in control of length, and thus, the sodium hyaluronate gel prepared by taking the polyglycol epoxide as a crosslinker is relatively easy in regulation and control of properties. The crosslinked sodium hyaluronate gel is low in toxicity, little in residual, small in squeezing and pushing force, good in shaping performance, good in enzyme resistance and long in in-vivo retention time. The present invention further discloses a mild crosslinker deactivation technology. Unreacted epoxide groups in the gel are subjected to a hydrolysis reaction in a carbonate buffer system with a pH of 8-9, so that the difficulty of impurity removal of the crosslinked sodium hyaluronate gel can be effectively lowered, and the problem of toxicity in the prior art due to the fact that BDDE is used in a crosslinking method is avoided.

Gel of sodium hyaluronate cross-linked by polyethylene glycol epoxy derivative for injection and preparation method thereof

The present invention discloses a PEGylated thioxanthone photoinitiator and a photosensitive resin composition, the PEGylated thioxanthone compound is eco-friendly and has low toxicity, high initiation efficiency and good thermal stability, meanwhile, as a kind of photoinitiator, the compound has a small amount of fragment residue after cured, and may improve the compatibility of the photoinitiator and photosensitive resin composition system. The photosensitive resin composition provided by the present invention has reasonable allocation of ingredients and content in the components thereof, capable of 3D-printing a hydrogel having a specific structure; the hydrogel has lower cytotoxicity and better biocompatibility, and may applied in bioengineering fields, e.g., 3D cell culture.

PEGylated thioxanthone photoinitiator and photosensitive resin composition

The disclosure discloses a dendritic polyethylene glycol derivative and a preparation method and an application thereof. The dendritic polyethylene glycol derivative has a structure of formula (I), has multiple end functional groups, has a stronger water solubility in comparison with linear-chain polyethylene glycol, and can solve a problem of insufficient water solubility due to the increase of load when modifying an insoluble drug by the polyethylene glycol. The preparation method of the dendritic polyethylene glycol derivative provided by the disclosure has mild reaction conditions, is green and environmentally friendly, is low in cost, and is easy to implement industrialization. 

Dendritic polyethylene glycol derivative, and preparation method and application thereof

The present invention relates to a Y-type discrete polyethylene glycol derivative as shown by Formula (I). The Y-type discrete polyethylene glycol derivative has the advantages of a determined molecular weight and number of segments in the chain, and can avoid the defects where the polyethylene glycol derivative itself is a mixture and the molecular weight is not homogeneous. The Y-type polyethylene glycol of the present invention can solve the problem of insufficient water solubility caused by an increase in the loading capacity when the discrete polyethylene glycol modifies an insoluble drug while increasing the drug loading capacity. 

Y-type discrete polyethylene glycol derivative and preparation method thereof

A conjugate represented by general formula (I), wherein Ris a Calkyl, B is an anesthetic, and A is a linking group, and a quaternary ammonium salt is formed at the linking position between B and R. The conjugate has a prolonged analgesic effect, and can be used in postoperative analgesia or treatment for chronic pain.

Conjugate of polyethylene glycol and anesthetic, and preparation method thereof

The present invention discloses a Y-type discrete polyethylene glycol derivative, which has the advantages of determined molecular weights and the number of chain segments, and can avoid the defect of heterogeneity of a PEG derivative. In addition, the Y-type discrete polyethylene glycol derivative of the present invention may increase the water solubility of the discrete polyethylene glycol, and solve the problem of insufficient water solubility of the discrete polyethylene glycol-modified insoluble drug caused by an increase of the loading capacity.

The present invention provides an alkynyl multi-arm polyethylene glycol derivative having a structure of a general formula I or general formula X VIII. In the derivative, X1, X2, X3 and X4 are linking groups, F1, F2, F3 and F4 are end groups, the end groups may be the same or may also be different, and are selected from: hydroxy, carboxyl, ester group, amino, alkynyl or the like, at least one of the end groups is alkynyl, and PEG is the same or different &#x2014;(CHCHO)&#x2014;, wherein m is an integer ranging from 3 to 250, and l is an integer greater than or equal to 1. The multi-arm polyethylene glycol derivatives have stronger application flexibility, and have good application prospect in aspects such as organic synthesis, medicine synthesis and medical instruments. 

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Tianjin, China

Meina Lin