Jenkem Technologyco., Ltd.. (tianjin)

Jenkem Technology Co., Ltd. (beijing)

Beijing Tide Pharmaceutical Co., Ltd.

Jenkem Technology Co., Ltd.

Jenkem Technology Co., Ltd., Tianjin Branch

Zewang Feng

Xuan Zhao

Jinliang Wang

Zhenguo Wang

Lihua Xu

Yanli Xiong

Yang Wang

Meina Lin

Yan Liu

Jianhuan Jia

Zhen'guo Wang

Kai Liu

Hongjun Wang

Yanping Zhao

Liying Zhou

Yanan Liu

Jie Meng

Wen Li

Huai Huang

Jianmei Pang

Xuelian Liu

Shenzhen Fu

Xichao Chen

Nana Tian

Yanping Song

Hui Zhu

Zhen Wei

Kun Zheng

Lihui Zheng

Qingbin Wang

Leimin Wang

Jinghui Du

Juan Shi

CheungLing Cheng

Zhixiong Guo

The present invention relates to a salt of 5-((2-ethynyl-5-isopropylpyridin-4-yl)oxy)pyrimidine-2,4-diamine and a solid form thereof, a method for preparing the solid form and a pharmaceutical composition comprising the solid form, as well as a use of the solid form for preventing or treating diseases modulated by P2X3 and/or P2X2/3 receptor antagonists.

Salt of diaminopyrimidine compounds, and solid form thereof, preparation method therefor and use thereof

The present invention relates to a solid form of 5-((2-ethynyl-5-isopropylpyridin-4-yl)oxy)pyrimidine-2,4-diamine or a hydrate thereof, a method for preparing the solid form, a pharmaceutical composition comprising the solid form, and a use of the solid form for the prevention or treatment of a disease modulated by P2X3 and/or P2X2/3 receptor antagonists.

Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof

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

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

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

A conjugate represented by general formula (I), wherein Ris a Calkyl, B is an anesthetic, and A is a linking group, and a quaternary ammonium salt is formed at the linking position between B and R. The conjugate has a prolonged analgesic effect, and can be used in postoperative analgesia or treatment for chronic pain.

Conjugate of polyethylene glycol and anesthetic, and preparation method thereof

A pharmaceutical composition of a polyethylene glycol-modified camptothecin derivative and a preparation method thereof. The pharmaceutical composition is prepared mainly from following components: a camptothecin derivative modified by polyethylene glycol, a pH value adjustment agent and water for injection. The pharmaceutical composition has high stability.

Pharmaceutical composition of polyethylene glycol-modified camptothecin derivative and preparation method thereof

The present invention provides compounds represented by formula (I) and pharmaceutical acceptable salts thereof, preparation method therefor and pharmaceutical composition containing the compounds represented by formula (I) and pharmaceutical acceptable salts thereof. In the compounds of the present invention, each terminal group of polyethylene glycol molecule can bond with a plurality of rapamycin molecules by cactus oligopeptide, with the loading rate of the pharmaceutical being increased. The compounds can be used to induce immunosuppression and treat graft rejection, autoimmune disease, solid tumors, fungal infection, and cardiovascular and cerebrovascular disease. 

Polyethylene glycol-cactus oligopeptide bonding rapamycin derivatives

Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.

Low molecular weight polyethylene glycol drug conjugates having improved drug biological activity

Disclosed are a compound of Formula I, having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, Rand Rare the same or different, each being independently chosen from the halogens, the C-Calkoxyl group, the C-Calkyl group, the C-Calkenyl group, and the C-Calkynyl group; Ris chosen from H, the halogens, the substituted or unsubstituted C-Calkyl group, C-Ccycloalkyl group, C-Calkenyl group, and C-Calkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.

Compound having higher inhibitory activity on protein kinase G and preparation method thereof

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Beijing, China

Zewang Feng