Jenkem Technologyco., Ltd.. (tianjin)

Jenkem Technology Co., Ltd. (beijing)

Jenkem Technology Co., Ltd.

Cansino (shanghai) Biological Research Co., Ltd.

Yanli Xiong

Xuan Zhao

Jinliang Wang

Zewang Feng

Meina Lin

Jian Liu

Xuefeng Yu

Shengyong Yan

Yanping Song

Jinghui Du

Leimin Wang

Qingbin Wang

Lihui Zheng

Juan Shi

Dongxu Qiu

Jing Hao

Zhihong Yan

Jun Guo

Tao Zhu

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 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

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 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.

Conjugate of dezocine and polyethylene glycol

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Beijing, China

Yanli Xiong