Brightgene Bio-Medical Technology Co., Ltd.

Brightgene Pharmaceutical (Suzhou) Co. Ltd.

Yangqing Huang

Jiandong Yuan

Yunsong Song

Jianing Gu

Zhanli Sun

Linfeng Miao

Chaohua Liang

Zhengye Wang

Fang Yuan

Zhiyuan Zhong

Fenghua Meng

Haifeng Ding

Yinan Zhong

Jianwen Chi

Yue Cai

Wenteng Zhen

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

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

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.

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Suzhou, China

Yangqing Huang