DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
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Page/Page column 39; 132-133
(2020/01/24)
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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Page/Page column 84; 85
(2019/01/17)
Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors
Described herein are the discovery and structure-activity relationship (SAR) studies of the third-generation 4-H heteroaryldihydropyrimidines (4-H HAPs) featuring the introduction of a C6 carboxyl group as novel HBV capsid inhibitors. This new series of 4-H HAPs showed improved anti-HBV activity and better drug-like properties compared to the first- and second-generation 4-H HAPs. X-ray crystallographic study of analogue 12 (HAP_R01) with Cp149 Y132A mutant hexamer clearly elucidated the role of C6 carboxyl group played for the increased binding affinity, which formed strong hydrogen bonding interactions with capsid protein and coordinated waters. The representative analogue 10 (HAP_R10) was extensively characterized in vitro (ADMET) and in vivo (mouse PK and PD) and subsequently selected for further development as oral anti-HBV infection agent.
Qiu, Zongxing,Lin, Xianfeng,Zhang, Weixing,Zhou, Mingwei,Guo, Lei,Kocer, Buelent,Wu, Guolong,Zhang, Zhisen,Liu, Haixia,Shi, Houguang,Kou, Buyu,Hu, Taishan,Hu, Yimin,Huang, Mengwei,Yan, S. Frank,Xu, Zhiheng,Zhou, Zheng,Qin, Ning,Wang, Yue Fen,Ren, Shuang,Qiu, Hongxia,Zhang, Yuxia,Zhang, Yi,Wu, Xiaoyue,Sun, Kai,Zhong, Sheng,Xie, Jianxun,Ottaviani, Giorgio,Zhou, Yuan,Zhu, Lina,Tian, Xiaojun,Shi, Liping,Shen, Fang,Mao, Yi,Zhou, Xue,Gao, Lu,Young, John A. T.,Wu, Jim Zhen,Yang, Guang,Mayweg, Alexander V.,Shen, Hong C.,Tang, Guozhi,Zhu, Wei
p. 3352 - 3371
(2017/05/05)
Novel 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.
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(2015/02/19)
6-AMINO ACID HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
The invention provides novel compounds having the general formula:, wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.
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(2014/03/26)
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