Chinese Academy of Sciences

Zhejiang University

Weijuan Kan

Yubo Zhou

Jia Tao Li

Mengmeng Zhang

Wei Zhu

Jun Wei Zhang

Hong Tao Liu

Jiang Wang

Hualiang Jiang

Kaixian Chen

Lei Feng

Yu Cheng

Xiaohua Chen

Mingbo Su

Yongzhou Hu

Xiaobei Hu

Shuni Wang

Jia Li

Chunpu Li

Yujie Wang

Huijun Nie

Dongyan Gu

Jun Wei

Rong Sheng

Jieyu Liu

Kaixiang Zhang

Gaoya Xu

Yuhua Zhong

Binshan Zhou

Kenian Yan

Tian Mi

Hongtao Tian

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

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

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Shanghai, China

Weijuan Kan