Nektar Therapeutics

Jenkem Technologyco., Ltd.. (tianjin)

Nektar Therapeutics Al, Corporation

Jenkem Technology Co., Ltd. (beijing)

Shearwater Corporation

Tsinghua University

Applied Research Systems Ars Holding N.v.

Debio Recherche Pharmaceutique S.a.

Other

Jenkem Technology Co., Ltd.

Jenkem Technology Co., Ltd., Tianjin Branch

Beijing Bytedance Network Technology Co., Ltd.

United Therapeutics Corporation

Cansino (shanghai) Biological Research Co., Ltd.

Xuan Zhao

Michael David Bentley

Xiaoming Shen

Zewang Feng

Meina Lin

Jinliang Wang

J Milton Harris

Tacey Viegas

Zhongxu Ren

Lihong Guo

Zhenguo Wang

William Dudley Battle, Iii

Hui Zhu

Zhen Wei

Lihua Xu

Lin Cheng

Richard R Goodin

Yanli Xiong

Yang Wang

Xiaomeng Chen

Yan Liu

Nabil El-Tayar

Kazunori Emoto

Zhen'guo Wang

Jianhuan Jia

Fuzhi Li

Meng Zhang

Wen Li

Robert G Shorr

Martine A Rothblatt

Harold Zappe

Jian Liu

Xuefeng Yu

Yanping Song

Qingbin Wang

Rujun Zhang

Shu Sun

Jinghui Du

Leimin Wang

Jiying Wei

Lihui Zheng

Kun Zheng

Yu Sun

Juan Shi

Jeremy Lloyd Clark

Zhen'gang Zhu

Yuhe Zhao

Zhixiong Guo

Kevin Burton

Tracey X Viegas

Tao Zhu

Jun Guo

Shengyong Yan

Dongxu Qiu

Zhihong Yan

Haomeng Wang

Jing Hao

Wenzhe Huang

Jingyun Hu

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

Methods of preparing monodisperse oligomer reagent compositions such as oligo(ethylene glycol) reagent compositions are described herein. The methods involve reacting a halo-terminated oligomer such as an oligo(ethylene oxide) having (m) monomers with a hydroxyl-terminated oligomer such as a hydroxyl-terminated oligo(ethylene oxide) having (n) monomers.

Methods of preparing a monodisperse oligo(ethylene glycol) reagent composition

Provided are a search method and apparatus, and an electronic device and a storage medium. The method comprises: receiving a generic query search request, the generic query search request carrying a generic query term; acquiring at least one multimedia content card corresponding to the generic query term, wherein each multimedia content card corresponds to an extension tag corresponding to the generic query search request, each multimedia content card comprises information of a plurality of multimedia content sets; and presenting information of the plurality of multimedia content sets comprised in each multimedia content card of the at least one multimedia content card. Search results related to a generic query term can be clustered from various dimensions and presented, such that a user can directly find content related to a search intention of the user, thereby improving the search efficiency and shortening a search path.

Search method and apparatus, and electronic device and storage medium

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.

Linker compound, polyethylene glycol-linker conjugate and derivative thereof and polyethylene glycol-linker-drug conjugate

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

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, R, Rand Rare linking groups, P is an terminal group of non-azido non-alkynyl group, D is &#x2014;Nor &#x2014;C&#x2261;CH, l is selected from an integer of 1 to 20, and m is selected from an integer of 0 to 19.

Multi-arm multi-claw polyethylene glycol derivative suitable for click chemistry reactions

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 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. And the prodrug or the sustained-release preparation of the local anesthetic of the present invention releases the drug slowly, and renders the drug concentration kept stable and long-lasting in the effective concentration range of non-narcotic analgesia, and the long-acting non-anesthetic analgesic effect can be achieved while significantly reducing the clinical adverse reactions of local anesthetics and reducing the number of administrations. The effectiveness of the drug is greatly enhanced and the clinical application range of local anesthetics is expanded.

Application of combination of polyethylene glycol and local anesthetic in non-narcotic analgesia

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

A novel multi-arm polyethylene glycol (PEG) (I) and preparation method thereof. Active derivatives (II) based on the multi-arm PEG. Gels formed of the active derivatives. Drug conjugates formed of the active derivatives and drug molecules and uses thereof in medical preparation. The multi-arm PEG is formed by polymerizing ethylene oxide with pentaerythritol oligomers as initiator, wherein PEG is the same or different and is a &#x2014;(CH2CH2O)m-, the average value of m is an integer of 3-1000, l is an integer more than or equal to 2. An 8-arm PEG is preferred, wherein l is equal to 3. The active derivatives (II) comprise link groups X attached to PEG and active end groups F attached to X.

Multi-arm polyethylene glycol, preparation method and uses thereof

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

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Beijing, China

Xuan Zhao