Shanghai Yingli Pharmaceutical Co., Ltd

Chinese Academy of Sciences

280 Bio, Inc.

Yangtong Lou

Zusheng Xu

Li Chen

Qingrui Sun

Kun Zeng

Xiaoli Lei

Bing Jiang Sun

Jianfeng Wu

Aizhong Chen

Linlin Xu

Zhenyu Yang

Zhujun Yao

Zhao Ma

Jizhi Li

Tiegang Xie

Yanhang Liu

Disclosed is a five-membered heteroaromatic ring structure containing compound, pharmaceutical compositions thereof and applications thereof. The present disclosure provides a five-membered heteroaromatic ring structure containing compound of formula I, pharmaceutical compositions thereof and applications thereof and the five-membered heteroaromatic ring structure containing compound is expected to treat and/or prevent various PARG-related diseases.

Compound containing structure of a five-membered heteroaromatic ring, pharmaceutical compositions thereof and applications thereof

Disclosed are an aromatic heterocyclic compound, an intermediate thereof, a preparation method therefor, and a pharmaceutical composition and use thereof. The aromatic heterocyclic compound of the present invention is a new ALK5 inhibitor, and is used for treating and/or preventing various ALK5-mediated diseases. 

Aromatic heterocyclic compound, intermediate thereof, preparation method therefor, and pharmaceutical composition and use thereof

The present disclosure relates to a preparation method morpholinquinazoline compound and a midbody thereof. The preparation method for morpholinquinazoline compound comprises the following steps: S1, performing a Suzuki reaction of compound S and compound IV as represented by the following formula, so as to obtain compound V; step S2, performing a reaction of methylsufonyl chloride and compound V in an organic solvent as represented by the following formula, so as to obtain compound VI; and S3, performing a coupled reaction of compound VII and compound VI in a solvent as represented by the following formula, so as to obtain compound YY-20394. The preparation method has the advantages of higher yield, better selectivity, simple operation and mild reaction condition, and is applicable to industrial production. 

Preparation method for morpholinquinazoline compound and intermediates thereof

Provided are a nitrogenous heterocyclic aromatic compound, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof. The nitrogenous heterocyclic aromatic compound can be used for treating and/or preventing various diseases mediated by ALK5. 

Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof

Provided in the present application are an aromatic heterocyclic substituted olefin compound, a preparation method for same, a pharmaceutical composition of same, and applications thereof. The aromatic heterocyclic substituted olefin compound of the present invention is a novel ALK5 inhibitor and is for use in treating and/or preventing various ALK5-mediated diseases. 

Aromatic heterocyclic substituted olefin compound, preparation method for same, pharmaceutical composition of same, and applications thereof

A crystal form I of a morpholino quinazoline compound represented by the following formula A, a preparation method therefor and use thereof. The crystal form I has good stability and non-hygroscopicity, and the preparation method is simple and suitable for industrial production. 

Crystal form of morpholino quinazoline compound, preparation method therefor and use thereof

Disclosed are a fused heterocyclic compound, a preparation method therefor, a pharmaceutical composition, and uses thereof. The preparation method of the fused heterocyclic compound and/or the pharmaceutically acceptable salt thereof in the present invention comprises three synthesizing routes. The present invention also provides a pharmaceutical composition, containing one or more of the fused heterocyclic compound, the pharmaceutically acceptable salt, hydrates, solvent compounds, polymorphs and prodrugs thereof, and a pharmaceutically acceptable carrier. The present invention also relates to an application of the fused heterocyclic compound and/or the pharmaceutical composition in preparing kinase inhibitors and in preparing drugs for preventing and treating diseases related to kinase. The fused heterocyclic compound of the present invention has selective inhibition function on PI3K &#x3b4;, and can be used for preparing drugs for preventing and treating cell proliferation diseases such as cancers, infections, inflammations, or autoimmune diseases. 

Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof

The invention relates to sinomenine derivatives, methods for their synthesis and their applications. The sinomenine derivatives include oxidation derivatives, and C-10 substituted sinomenine derivatives. Based on the readily oxidizable phenol group on sinomenine structure, using oxidation, oxidative dearomatization, or conjugated addition aromatization, one can introduce C-10 substitutions to synthesize the sinomenine derivatives. The sinomenine derivatives of the invention have the following structures:  Using in vitro TNF-&#x3b1; inhibition assay, the activities of the synthetic compounds are assessed. Results from these assays shown that most compounds have anti-inflammatory effects, and some compounds have better activities than that of sinomenine. These compounds may be used in treating immune diseases such as rheumatoid arthritis (RA).

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Shanghai, China

Yangtong Lou