Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Les Laboratories Servier

Shanghai Institute of Pharmaceutical Industry

Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd.

Les Laboratoires Servier

Hubo Wang

Zhedong Yuan

Xueyan Zhu

Yu Huang

Hanbin Shan

Xiong Yu

Xingdong Cheng

Xudong Jiang

Xufeng Cao

Peng Zhang

Xiquan Zhang

Hongjiang Xu

Aiming Zhang

Xiaomin Zhang

Wei Song

Meng Guo

Mingtong Hu

Zhou Zhou

Huadong Yao

Hongjuan Pan

Leilei Yang

Hui Fu

Jiude Sun

Jiasong Zhang

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production. 

Synthesis process of ruxolitinib

The present invention relates to a nintedanib diethanesulfonate salt A-type crystal represented by formula (II), and also relates to a crystalline composition and pharmaceutical composition comprising the crystal, and preparation method and use thereof. An X-ray powder diffraction spectrum of the nintedanib diethanesulfonate salt A-type crystal of the present invention has a diffraction peak at about 14.64, 18.79, 19.31, 20.11, 21.20, 22.45 and 26.71&#xb0; when represented via a 2&#x3b8; value. The nintedanib diethanesulfonate salt A-type crystal of the present invention has a stable property, is non-hygroscopic and difficult to degrade, and is particularly suitable for medicine production. 

Nintedanib diethanesulfonate salt crystal and preparation method and use thereof

Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.

Dihydroindolinone derivatives

The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2&#x3b8; 11.13&#xb0;, 11.82&#xb0;, 17.49&#xb0;, 18.29&#xb0;, 19.48&#xb0;, 19.72&#xb0;, 20.50&#xb0;, 21.76&#xb0;, 22.54&#xb0;, 22.97&#xb0;, 24.56&#xb0;, 25.36&#xb0;, 27.16&#xb0; and 31.93&#xb0;. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.

Crystalline form VI of agomelatine, preparation method and application thereof

The present invention relates to a complex of agomelatine and to preparation thereof. The hydrogen halide complex of agomelatine obtained through the present method is more soluble, more stable, and of higher purity than agomelatine itself, making it more suitable to be used in pharmaceutical preparation. Using this method, product of high purity can be obtained through a simple process, without having to incur further complicated steps.

Agomelatine hydrohalide complex and preparation method thereof

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Shanghai, China

Hubo Wang