Jiangsu Jibeier Pharmaceutical Co. Ltd.

Zhenjiang San an Pharmaceutical Co. Ltd.

Zhongyi Geng

Xinghai Chen

Wei Huang

Yao Wang

Xinyuan Zhu

Yongfeng Zhou

Deyue Yan

Wei Peng

Parker Aulma

The present disclosure provides a ketone carbonyl-containing hydrophobic antitumor drug and a conjugate thereof as well as a nano preparation containing the conjugate, a preparation method therefor, and an application thereof. The conjugate is an amphipathic pH-responsive conjugate obtained by enabling a dehydration condensation reaction between a hydrazide-terminated polyethylene glycol and/or lactose hydrazide and the ketone carbonyl-introduced hydrophobic antitumor drug. The ketone carbonyl-introduced hydrophobic antitumor drug is obtained by reacting an isocyanate group in a compound containing isocyanate group and ketone carbonyl group with a hydroxyl on a hydroxyl-containing hydrophobic antitumor drug. The hydroxyl-containing hydrophobic antitumor drug includes at least one of paclitaxel, docetaxel, paclitaxel derivatives, or docetaxel derivatives. Compared with docetaxel, the ketone carbonyl-containing hydrophobic antitumor drug, the conjugate thereof and the nano preparation have higher antitumor activity.

Ketone carbonyl-containing hydrophobic antitumor drug and conjugate thereof as well as nano preparation containing conjugate, preparation method therefor, and application thereof

Provided in the present invention are a 1-[(pyridin-3-yl-sulfonyl)-1h-pyrrol-3-yl] methanamine derivative having the structure shown below in formula (I) and a pharmaceutical composition and use thereof. The 1-[(pyridin-3-yl-sulfonyl)-1h-pyrrol-3-yl] methanamine derivative provided in the present invention has good gastric acid secretion inhibitory activities and excellent pharmacodynamic properties, while having relatively low toxicity. 

1-[(pyridin-3-yl-sulfonyl)-1H-pyrrol-3-yl] methanamine derivative and pharmaceutical composition and use thereof

The present disclosure provides a deuterium substituted 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound with a structure represented by formula (I) or a derivative thereof, a pharmaceutical composition containing the compound or the derivative thereof, and an application of the compound or the derivative thereof in preparing drugs. The compound can reduce oxidative metabolism thereof, increase the drug concentration in blood and the effective bioavailability, so as to lower the dosage and reduce the toxicity and other side effects. The deuterium 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound and its derivative thereof provided by the present disclosure can be used to treat related diseases such as affective disorders, depression and anxiety. 

Deuterium substituted 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine compound or derivatives thereof, and pharmaceutical composition and use thereof

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Zhenjiang, China

Zhongyi Geng