Chinese Academy of Sciences

Topharman Shanghai Co., Ltd.

Suzhou Vigonvita Life Sciences Co., Ltd.

Topharman Shandong Co., Ltd.

Vigonvita Life Sciences Co., Ltd.

Boehringer Ingelheim Pharma Gmbh & Co Kg

Weifang Tehua Chemical Co., Ltd.

Shanghai Institute of Materia Medica, Chines Academy of Sciences

Henan Topfond Pharmaceutical Co., Ltd.

Jingshan Shen

Guanghui Tian

Jianfeng Li

Hualiang Jiang

Zhen Wang

Rongxia Zhang

Zheng Liu

Yang He

Xiangrui Jiang

Weiming Chen

Yi Jing Zhu

Yongjian Liu

Yu Ying Wang

Xiaojun Yang

Chunhui Wu

Fuqiang Zhu

Jin Suo

Jingkang Shen

Guan Zhong Wang

Jin Zheng

Haji Akber Aisa

Weiliang Zhu

Leike Zhang

Gengfu Xiao

Yuanchao Xie

Haihong Li

Feipu Yang

Chao Li

Qiang Zhang

Jing Shi

Rolf Dach

Wei Wang

Jinfeng Zhang

Ye Li

Yi Zhu

Xianguo Zhao

Xudong Gong

Minghao Bi

Yu Wang

Yanjun Pan

Jingjing Yin

Zhu Xie

Xiaoguang Kong

Aixiang Liu

Yongjun Mao

Tiema Yan

Kai Xie

Guozhang Jin

Wenzhong Wang

Ruyun Ji

Xinjian Chen

Qing Jin

Weixi Jin

Heping Lv

Shunan Lai

Yurong Ji

Jinping Liu

Guan Wang

The present invention relates to an antiviral application of nucleoside analogs. Specifically, the present invention relates to uses of nucleoside analogs and a pharmaceutical composition thereof as: (a) inhibitors for inhibiting the replication of coronaviruses, influenza viruses, respiratory syncytial viruses, flaviviridae viruses, filoviridae viruses and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and mitigating diseases caused by coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV) infections. The nucleoside analogs according to the invention may treat and/or prevent and mitigate respiratory infection, pneumonia (COVID-19) and other related diseases caused by 2019 novel coronavirus infection.

Antiviral application of nucleoside analog or combination formulation containing nucleoside analog

The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.

Tetrahydroprotoberberine compound, preparation method therefor and uses thereof, and pharmaceutical composition

The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof. 

Salt and polymorph of benzopyrimidinone compound and pharmaceutical composition and use thereof

The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation. 

Maleate salt of benzothiophene compound, crystalline form thereof, and use thereof

The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease. 

Heterocyclic compounds, process for preparation of the same and use thereof

The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

Methods for preparing brexpiprazole, key intermediates thereof and salts thereof

Disclosed are aminosulfonyl-based compounds represented by the general formula I or tautomers, enantiomers, racemates or pharmaceutically acceptable salts thereof, a method for preparing the same, pharmaceutical compositions and uses thereof. The compounds can be used to treat epilepsy, convulsions, obesity and the like. 

Amino sulfonyl-based compounds, the preparation method therefor and use thereof

The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms. 

Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical composition containing the same, preparation method and use thereof

The present invention relates to a (2R,3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process. 

Substituted n-pentanamide compounds, preparation method and the use thereof

Provided is a process for preparing racemic nicotine from 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof using one-pot process. The process comprises the following steps: 1) in a reaction vessel, reacting 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof in the presence of a suitable solvent and a strong acid by heat; after the reaction is complete, cooling the same and adjusting the pH to 7-8 with alkali; and 2) directly adding a reductant into the above vessel, and after the reaction, purifying the product so as to obtain high purity racemic nicotine or a salt thereof.

Process for preparing racemic nicotine

The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like. 

Phenylpyrimidone compounds, the pharmaceutical compositions, preparation methods and uses thereof

Subject of the present invention is a new improved process for the preparation of nitroorotic acid via nitration of orotic acid.

Process for the preparation of nitroorotic acid

The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia. 

Tetrahydroprotoberberine compounds, the synthetic method and the use thereof

The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity. 

Preparation methods of 6 substituted amino-3 cyanoquinoline compounds and the intermediates thereof

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Shanghai, China

Jingshan Shen