Chinese Academy of Sciences

Zhejiang University

Other

Suzhou Baijibugong Pharmaceutical Technology Co., Ltd.

Zibo Biopolar Changsheng Pharmaceutical Co. Ltd.

Shanghai Puyi Chemical Co., Ltd.

Shanghai Theorion Pharmaceutical Co., Ltd.

Yubo Zhou

Jia Tao Li

Anhui Gao

Mingbo Su

Zhijian Lu

Xibin Liao

Jia Li

Yongzhou Hu

Tao Liu

Xiaobei Hu

Fajun Nan

Yangming Zhang

Xiaowu Dong

Weijuan Kan

Wei Zhu

Jun Wei Zhang

Jian Ding

Hong Tao Liu

Jiang Wang

Hualiang Jiang

Kaixian Chen

Lei Xu

Bo Yang

Xin Xie

Qiaojun He

Peipei Wang

Shuni Wang

Lexian Tong

Pinrao Song

Mengmeng Zhang

Yi Chen

Meiyu Geng

Lei Feng

Yu Cheng

Fei Chen

Xiaohua Chen

Linghua Meng

Chunpu Li

Chaojun Gong

Yujie Wang

Wenhu Zhan

Qinjie Weng

Binshan Zhou

Rong Sheng

Jun Wei

Dongyan Gu

Jieyu Liu

Kaixiang Zhang

Gaoya Xu

Yuhua Zhong

Kenian Yan

Tian Mi

Hongtao Tian

Huijun Nie

Shixian Wang

Hui Chai

Jiankang Zhang

Wei Xu

Hong Liu

The present invention relates to a polysubstituted isoindoline compound as shown in general formula (I), and a preparation method, a pharmaceutical composition and the use thereof. In particular, the polysubstituted isoindoline compound is provided in the present invention as a class of novel CRL4E3 ubiquitin ligase modulators in structure, wherein same has a stronger antitumor activity and antitumor spectrum, and can be used to prepare drugs for treating CRL4E3 ligase-related diseases.

Isoindoline compound, preparation method, pharmaceutical composition and use thereof

Provided by the present disclosure are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present disclosure have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present disclosure can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b are shown as below:

Aminoquinazolinone and aminoisoquinolinone derivatives and application thereof

Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):

Bruton's tyrosine kinase inhibitors

The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

Trans-indoline cyclopropylamine chemical compound, and method for preparation, pharmaceutical composition, and use thereof

The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chk1 kinase inhibitory activity, and are promising Chk1 inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I: 

2-polysubstituted aromatic ring-pyrimidine derivatives, preparation and medical application thereof

Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I): 

Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers. 

Fluorinated cyclopropylamine compound, preparation method therefor, pharmaceutical composition thereof, and uses thereof

A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.

2-substituted aromatic ring-pyrimidine derivative and preparation and application thereof

The invention describes an aryl-2,2'-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2&#x2032;-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs. 

Aryl-2,2'-tandem bisthiazole compound and preparation method and use thereof

Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.

Substituted nitrogen-containing heterocyclic derivatives, pharmaceutical compositions comprising the same and applications of antitumor thereof

Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.

Tripeptide epoxyketone compound constructed by heterocycle and preparation method and use thereof

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Shanghai, China

Yubo Zhou