Chinese Academy of Sciences

Shanghai Haihe Pharmaceutical Co., Ltd.

Emory University

The Florida State University Research Foundation, Inc

Children's Healthcare of Atlanta, Inc.

Cisen Pharmaceutical Co., Ltd.

Fukang (shanghai) Health Technology Co., Ltd.

Children's Heatlhcare of Atlanta

Fukang Health Technology Co., Ltd.

Chunhao Yang

Yi Chen

Cun Tan

Jian Ding

Xiang Wang

Linghua Meng

Zehong Miao

Jiapeng Li

Yanhong Chen

Jing Li

Binghe Wang

Xi Zhang

Meng Wang

Chaofeng Dai

Xiajuan Huan

Nanting Ni

Weixuan Chen

Alexander Draganov

Qian He

Guojing Sun

Jinxue He

Xiaochuan Yang

Lubing Gu

Muxiang Zhou

Haoyue Xiang

The present disclosure relates to 7-substituted pyrrolo[2,1-f][1,2,4]triazine compounds or pharmaceutically acceptable salts thereof, and preparation methods and uses thereof. These compounds show good PI3K inhibitory activity, can effectively inhibit the activity of PI3K kinase, and has significant enhancement and improvement of pharmacokinetic properties, such as bioavailability, due to the introduction of the 7-position group; furthermore, the compounds of the present disclosure exhibit an unpredictable high selectivity and strong inhibitory activity on PI3K&#x3b4;, and thus these compounds can be used for treating diseases related to PI3K pathway, especially for anti-cancer or for the treatment of tumors, leukemias and autoimmune diseases. After further optimizing and screening, the compounds are expected to be developed into a new type of anti-tumor drugs.

7-site substituted pyrrole triazine compounds or pharmaceutically acceptable salts thereof, and preparation method thereof and uses thereof

Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs. 

2-[4-(meihylaminomethyl)phenyl]-5-fluoro- benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof

Rhein analogues that exhibit anti-proliferative activity, particular against cancer cells, are described herein. In some embodiments, the compounds contain a flat or planar ring system. Such rings system by facilitate non-covalent binding of the compounds to the DNA complex, such as by intercalation. In some embodiment, the compounds contain a flat or planar ring system as described above and one or more substituents which are alkylating moieties, electrophilic groups or Michael acceptors or groups which contain one or more alkylating moieties, electrophilic groups and/or Michael acceptors. The compounds described herein can also contain one more functional groups to improve the solubility of the compounds.

Anthraquinone analogs and methods of making and using thereof

The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.

Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof

Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein Rand Rare each independently hydrogen, straight or branched chained C-Calkyl, C-Ccycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or Rand Rtogether with N form an unsubstituted or substituted saturated 5- or 6-membered heterocyclyl containing at least one heteroatom, wherein the heteroatom is O, N and S, the substituent is a methyl on N; Ris a hydrogen atom or a chlorine atom; Ris a hydrogen atom or a fluorine atom; X is CH, CF or N; and Y is CH, CF or N. 

2-arylbenzofuran-7-formamide compounds, preparation method and use thereof

[object Object]

Growing community of inventors

Shanghai, China

Chunhao Yang