Abstract: The disclosure discloses a linker compound, a polyethylene glycol-linker conjugate and a derivative thereof, and a polyethylene glycol-linker-drug conjugate. The linker compound as well as the conjugate thereof with the polyethylene glycol and the derivative thereof may be used for modifying a drug, and a modification reaction is simple and easy to carry out. Moreover, a reaction yield is high, and an application range of the modified drug is wide. The modified drugs gradually degrade from a chain of the conjugate in vivo, and may stay in a lesion (such as a cancer site) for a longer period of time, achieving purposes of sustained and controlled release, reducing an administration frequency, and greatly improving a bioavailability of the drug and a patient compliance.

Abstract: 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.

Abstract: The disclosure provides a multi-arm multi-claw polyethylene glycol derivative suitable for click chemistry reactions of general formula I, wherein R is a polyethylene glycol residue having a linear-chain structure, a Y-type structure or a multi-branched structure, R1, R2 and R3 are linking groups, P is an terminal group of non-azido non-alkynyl group, D is —N3 or —C?CH, l is selected from an integer of 1 to 20, and m is selected from an integer of 0 to 19.

Abstract: 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.

Abstract: The invention discloses use of a conjugate of polyethylene glycol and a local anesthetic in non-anesthetic analgesia. A local anesthetic is prepared into a prodrug or a sustained release preparation, wherein a high molecular polymer such as polyethylene glycol in the prodrug is covalently bonded with a local anesthetic, and auxiliary materials with a sustained release effect in the sustained release preparation are non-covalently bonded to the local anesthetic. After administration, there is no anesthesia and analgesic effect before the release of the free local anesthetic. After the free local anesthetic is released, an analgesic effect is achieved.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The present invention discloses a method of preparing PEGylated biomolecules having controllable binding sites, including the following steps: (1) binding a blocker to a biomolecule; (2) PEGylating the biomolecule; and (3) separating the blocker from the biomolecule. In another aspect, the present invention discloses a method for preparing PEGylated IL-2 having controllable binding sites, including the following steps: (1) binding IL-2 to an IL-2? receptor, closing the a binding site of the IL-2; (2) PEGylating, coupling PEG with the IL-2; and (3) separating the IL-2 from the IL-2? receptor. By regulating IL-2 binding sites and a PEGylation process only adding one or two polyethylene glycols, the IL-2 is caused to selectively bind to an IL-2R ??-type receptor.

Abstract: The present invention provides a cell-penetrating-peptide multi-arm-PEG medicine conjugate having a general formula I, II, III, IV or V. As compared with linear-chain-type PEG-cell-penetrating-peptide conjugates, the multi-arm PEG has multiple end groups, and has introduction sites for multiple functional groups, which can connect to multiple different active groups. In addition, the cell-penetrating-peptide multi-arm-PEG medicine conjugate to enable the medicine to enter the pathogenetic cells in a targeting manner, to achieve precise treatment. The present invention further provides use of a cell-penetrating-peptide multi-arm-PEG medicine conjugate having targeting ability in preparation of a targeting medicine, especially use of a cell-penetrating-peptide multi-arm-PEG medicine conjugate having targeting ability in the treatment of eye age-related macular degeneration, asthma and pulmonary fibrosis.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The present invention discloses a conjugate of PEG (polyethylene glycol) and rapamycin and use thereof, in particular use in preparation of a medicament for reducing immune response, wherein conjugate of PEG and rapamycin can remarkably lower the generation rate of an antibody directed to foreign immunogen, and reduce excessive immune responses caused by use thereof. The conjugate of PEG and rapamycin has beneficial effects of ensuring and even improving the treatment effect of a therapeutic agent, improving the own immunity of a subject, reducing and even eliminating graft rejection, and is advantageous in a relatively simple preparation process thereof, low cost, easy industrial production, and a high application value.

Abstract: 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.

Abstract: 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.

Abstract: The invention discloses use of a conjugate of polyethylene glycol and a local anesthetic in non-anesthetic analgesia. A local anesthetic is prepared into a prodrug or a sustained release preparation, wherein a high molecular polymer such as polyethylene glycol in the prodrug is covalently bonded with a local anesthetic, and auxiliary materials with a sustained release effect in the sustained release preparation are non-covalently bonded to the local anesthetic. After administration, there is no anesthesia and analgesic effect before the release of the free local anesthetic. After the free local anesthetic is released, an analgesic effect is achieved.

Abstract: 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.