Brightgene Bio-Medical Technology Co., Ltd.

Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd.

Brightgene Bio-Medical Technology (Suzhou) Co., Ltd.

Brightgene Pharmaceutical (Suzhou) Co. Ltd.

Selectchemie Ag

Jiandong Yuan

Yangqing Huang

Zhiyuan Zhong

Fenghua Meng

Yunsong Song

Jianing Gu

Zhanli Sun

Yan Zou

Linfeng Miao

Chaohua Liang

Zhengye Wang

Fang Yuan

Haifeng Ding

Wenteng Zhen

Yue Cai

Jingcheng Hui

Qilei Cong

Xiaopei Xing

Xinliang Fu

Jianwen Chi

Yinan Zhong

Yuan Fang

Marinus Van Boven

Karlheinz Doser

A GIP and GLP-1 dual receptor agonist, a pharmaceutical composition, and the use. In particular, the present application relates to a compound represented by formula I, a pharmaceutical composition comprising the compound, and the use of the compound as a GIP and GLP-1 dual receptor agonist in the field of medicine. The compound represented by formula I exhibits excellent GIPR and GLP-1R agonist activity and excellent pharmaceutical activity in reducing blood sugar and controlling body weight, is a therapeutic drug having a clinical application prospect, and can be used for preventing and treating diseases such as diabetes, diabetes complications, obesity, or obesity complications.

GIP and GLP-1 dual receptor agonist, pharmaceutical composition, and use

The present invention provides a method for preparing an ecteinascidin compound and an intermediate thereof, and specifically provides a preparation method for a novel compound QT9, and a method of using QT9 to prepare an ecteinascidin compound. The method provided by the present invention has high reaction selectivity and high yield, the obtained compound is easy to purify, and defects in the prior art that multiple intermediates are oily substances, and the reaction selectivity is poor are solved. The method of the present invention is particularly applicable to industrial production.

Preparation method for ecteinascidin compound and intermediate thereof

A multi-branched drug conjugate of formula (I) or a pharmaceutically acceptable salt thereof. In the formula, R is an organic center, POLY is a polymer, L is a multivalent linker, T is a targeting molecule, D is an active agent, and q is any integer between 3 and 8. The symbol '*' in L represents a junction point of the multivalent linker L and the targeting molecule T, '#' represents a junction point of the multivalent linker L and the active agent D, and &#x201c;%&#x201d; represents a junction point of the multivalent linker L and POLY. 1 is any integer between 2 and 20, and m and n are each an integer between 0 and 10. T is iRGD, cRGD, tLyp-1, Lyp-1, RPARPAR, Angiopep2, or GE11. D is a camptothecin drug. 

Multi-arm targeting anti-cancer conjugate

Disclosed are an exenatide modifier for connecting the exenatide to a fatty chain with a carboxy in the terminus thereof by means of a hydrophilic connecting arm, and a use thereof in preparing drugs serving as a GLP-1 receptor agonist; a use in preparing drugs for preventing and/or treating diseases and/or symptoms associated with a low GLP-1 receptor activity; a use in preparing drugs for diseases and/or symptoms associated with glycometabolism; a use in preparing drugs for diabetes; a use in preparing drugs for fatty liver disease, and a use in preparing drugs for losing weight.

Exenatide modifier and use thereof

The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.

Phosphoramidate compound and preparation method and crystal thereof

Disclosed is a multi-arm targeting drug conjugate modified by a water-soluble polymer; the drug conjugate has the structural formula of (III). In formula (III), R is an organic core, POLY is a polymer, L is a multivalent linker, T is a targeting molecule, D is a camptothecin-based drug, and q is any integer between 3 and 8. The drug conjugate may improve the poor water solubility, high toxicity and low bioavailability of camptothecin-based drugs.

Multi-arm polymeric targeting anti-cancer conjugate

Disclosed in the present disclosure is a biodegradable amphiphilic polymer containing disulfide in the side chain, a self-crosslinked polymeric vesicle thereof and an application in the targeted therapy of lung cancer. The polymer is obtained by an activity-controllable ring-opening polymerization based on a cyclic carbonate monomer containing a functional group of dithiolane ring, which has a controllable molecular weight and a narrow molecular weight distribution, and does not require processes of protection and deprotection; the polymer obtained by the ring-opening polymerization of the cyclic carbonate monomer of the present disclosure has biodegradability and can be used to control the drug release system, the prepared lung cancer-targeted reduction-sensitive reversibly-crosslinked polymeric vesicle as a nanomedicine carrier supports stable long circulation in vivo. However, it is highly enriched in lung cancer tissues, enter cells efficiently, and rapidly decrosslinks in the cells to release drugs, so as to kill cancer cells with high potency and specificity and inhibit the growth of tumor effectively without causing toxic and side effects.

Biodegradable amphiphilic polymer, polymeric vesicles prepared therefrom, and application of biodegradable amphiphilic polymer in preparation of medicines for targeted therapy of lung cancer

Provided is a preparation method of a composition enriched in compound S-1. The method performs isomer separation on a reaction product from the first step, and then performs a two-step chemical synthesis, so as to prepare a composition comprising high-purity compound S-1, wherein the HPLC purity of the single isomer S-1 is 90% or more. Provided is a composition enriched in compound S-1. The composition has an inhibitory effect on tumor cell proliferation in vitro significantly higher than that of NUC-1031 and compound R-1. Also provided are the use of the composition, and a pharmaceutical composition comprising the composition and at least one pharmaceutically acceptable excipient.

Composition enriched in single isomer of NUC-1031 and preparation method and use thereof

Disclosed are a hyaluronic acid-based amphiphilic polymer, preparation method and application thereof. A main chain of the amphiphilic polymer is a hydrophilic hyaluronic acid and can be employed in active targeting, and a side chain thereof is a hydrophobic group represented by Formula (1). The amphiphilic polymer can carry a small molecule anticancer drug. Polymer nanoparticles are obtained via chemical crosslinking, such that the nanoparticles are not readily dissociated outside a cell or in blood, thus ensuring the stability of a drug encapsulated by the nanoparticles. Upon arriving at a tumor tissue, the hyaluronic acid on a surface of the nanoparticle can immediately combine with a CD44 receptor on a surface of a tumor cell, and effectively enter the tumor cell via endocytosis mediated by the receptor, and then quickly de-crosslink to be dissociated. The drug is quickly released, obtaining an enrichment ratio at a tumor site markedly higher than that of the prior art, resulting in a highly effective treatment, and addressing deficiencies such as drug leakage, low carrying efficiency, low occurrence of endocytosis and slow release in a cell.

Hyaluronic acid-based amphiphilic polymer, preparation method and application thereof

Apparatus relates to a carbonate polymer containing a functional group of disulfide five-membered ring in the side chain and application thereof. The polymer can be prepared from cyclic carbonate monomer containing a disulfide five-membered ring functional group through the activity controllable ring-opening polymerization. For polymer, molecular weight is controlled, molecular weight distribution is narrowed and does not require the protection and deprotection procedures. Polymer prepared from the carbonate monomer through the ring-opening polymerization has biodegradability, can be used for controlling drugs release system, and can be used to prepare tumor-targeted nano-drug carrier which is sensitive to reduction and is reversible cross-linking, can support long circulation in the body, in high concentration of cancers cells can rapidly release cross-linking in the cancer cells, to release drugs, to kill cancer cells with high efficiency and specificity. Biodegradable polymer has a good application value in the tissue engineering and bio-chip coating.

Carbonate polymer containing a functional group of disulfide five-membered ring in the side chain and application thereof

Disclosed are a cyclic carbonate monomer containing a double-sulfur five-membered ring functional group, and preparation method thereof. The cyclic carbonate monomer can be simply and efficiently synthesized without protection and deprotection processes. The cyclic carbonate monomer of the present invention can be utilized to obtain polycarbonate having a controllable molecular weight and molecular weight distribution via ring opening polymerization, and has biodegradability and reduction-sensitive reversible crosslinking properties. The present invention can be used in a carrier having controllably released drug, a biological tissue scaffold or a biochip.

Cyclic carbonate monomer containing double-sulfur five-membered ring functional group, and preparation method thereof

The present invention provides: 1) Derivative solid form of 9-[2-(R)-[bis[pivaloyloxymethoxy]-phosphinylmethoxy]propyl]adenine (bis-POM PMPA, abbreviated as TD hereinafter), including crystalline form A and form B of TD, TD fumarate salts and cyclodextrin inclusion complex of TD; 2) Synthesis and purification methods of TD and Solidification method of TD oil, including converting TD oil to crystalline TD in Form A and Form B, solid TD salts and cyclodextrin inclusion complex of TD; 3) Stable pharmaceutical compositions containing TD derivatives and their preparation; 4) The use of the above TD derivatives in the antiviral treatments, especially in the treatment of HIV, HBV, CMV, HSV-1, HSV-2 and human Herpes virus infections.

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Suzhou, China

Jiandong Yuan