Chinese Academy of Sciences

Dalian University of Technology

East China University of Science and Technology

Cisen Pharmaceutical Co., Ltd.

Shanghai Acebright Pharmaceuticals Co., Ltd.

Fukang (shanghai) Health Technology Co., Ltd.

Fukang Health Technology Co., Ltd.

Zehong Miao

Gang Liu

Jian Ding

Ao Zhang

Yi Chen

Shanshan Song

Xiajuan Huan

Chunhao Yang

Zilan Song

Cun Tan

Jinxue He

Jia Tao Li

Hong Iris Zhu

Fajun Nan

Jingkang Shen

Meng Wang

Tao Meng

Yufang Xu

Xuhong Qian

Bing Xiong

Yong Gan

Jianping Hu

Liping Lin

Chaodong Xiong

Jia Li

Baoyuan Qu

Yonggang Li

Wanyi Tai

Chuanming Xie

Chuanhuizi Chen

Na Ye

Zhoulong Fan

Pingyuan Wang

Yingqing Wang

Li Gao

Shiyan Guo

The present disclosure relates to triazolopyrimidine compounds and salts, compositions and uses thereof, and the triazolopyrimidine compounds have the structures represented by the formula (I): the above-mentioned triazolopyrimidine compounds have good activity and high selectivity for NAE.

Triazolopyrimidine compound and salt, composition and use thereof

Disclosed is an SOMCL-9112 solid dispersion. The SOMCL-9112 solid dispersion is characterized by being prepared from the following raw materials in percentage by weight: 5 percent to 60 percent of SOMCL-9112, 5 percent to 90 percent of pharmaceutically acceptable matrix polymer, 0 percent to 20 percent of surfactant, 0 percent to 20 percent of flow aid and 0 percent to 20 percent of plasticizer. Also disclosed are a preparation method of the SOMCL-9112 solid dispersion, a solid medicinal preparation containing the solid dispersion and application of the solid dispersion for preparing a medicine for treating cancer.

SOMCL-9112 solid dispersion and preparation method thereof and SOMCL-9112 solid preparation containing SOMCL-9112 solid dispersion

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

The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein. 

Dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof

A class of substituted triazolopiperazine compounds represented by formula (I), tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers. 

Substituted triazolopiperazine PARP inhibitor, preparation method therefor and use 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

Provided is a piperazinotriazole compound represented by general formula I or a pharmaceutically acceptable salt, stereoisomer, tautomer or hydrate thereof. Also provided are a pharmaceutical composition comprising the compound, a method for preparing the compound and a method of use thereof as a high-selectivity poly(adenosine diphosphate-ribose)polymerase-1 (PARP-1) inhibitor in the preparation of drugs for the prevention and/or treatment of PARP-related diseases. 

Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors

Disclosed are a series of &#x3b1;-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The &#x3b1;-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers. 

Alpha-amino-N-substituted amides, pharmaceutical composition containing them and uses thereof

The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.

Sulfur-containing naphthalimide derivatives

Growing community of inventors

Shanghai, China

Zehong Miao