- Anti-apoptosis protein Bcl - 2 inhibitor as well as preparation method and application thereof
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The invention provides an anti-apoptotic protein Bcl - 2 inhibitor and a preparation method and application thereof, and particularly provides a compound shown by the following formula (I) or an optical isomer thereof. A tautomer, or a pharmaceutically acceptable salt thereof. The compounds have excellent Bcl - 2 inhibitory activity and are therefore useful in the treatment or prevention of related mammalian diseases or disorders due to abnormal expression of anti-apoptotic protein Bcl - 2.
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- Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor
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Ziresovir (RO-0529, AK0529) is reported here for the first time as a promising respiratory syncytial virus (RSV) fusion (F) protein inhibitor that currently is in phase 2 clinical trials. This article describes the process of RO-0529 as a potent, selective, and orally bioavailable RSV F protein inhibitor and highlights the in vitro and in vivo anti-RSV activities and pharmacokinetics in animal species. RO-0529 demonstrates single-digit nM EC50 potency against laboratory strains, as well as clinical isolates of RSV in cellular assays, and more than one log viral load reduction in BALB/c mouse model of RSV viral infection. RO-0529 was proven to be a specific RSV F protein inhibitor by identification of drug resistant mutations of D486N, D489V, and D489Y in RSV F protein and the inhibition of RSV F protein-induced cell-cell fusion in cellular assays.
- Zheng, Xiufang,Gao, Lu,Wang, Lisha,Liang, Chungen,Wang, Baoxia,Liu, Yongfu,Feng, Song,Zhang, Bo,Zhou, Mingwei,Yu, Xin,Xiang, Kunlun,Chen, Li,Guo, Tao,Shen, Hong C.,Zou, Gang,Wu, Jim Zhen,Yun, Hongying
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p. 6315 - 6329
(2019/07/09)
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- HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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- 1,3-BENZOTHIAZINONE DERIVATIVE AND USE THEREOF
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The present invention provides compounds represented by formula (I): wherein R1 independently represents a halogen atom, hydroxy, nitro, an optionally halogenated alkyl, alkenyl or alkynyl, an optionally substituted alkoxy, an acyl, or an optionally substituted amino; R2 represents hydrogen atom or an optionally substituted hydrocarbon group; R3 represents an electron-withdrawing group; n represents an integer of 0 to 2; and m represents an integer of 1 to 6 (hereinafter sometimes briefly referred to as Compound (I)); or salts thereof. These compounds are capable of binding to macrophage migration inhibitory factor (MIF) and useful as agents for preventing/treating diseases induced by oxidative stress.
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Page/Page column 21
(2008/06/13)
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