- DIHYDROPYRIMIDINYLTHIAZOLE FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The present invention provides novel compounds having the general formula: wherein R1, R2, X, Y and A are as described herein, compositions including the compounds and methods of using the compounds.
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- 4 - Methyl dihydro pyrimidine compounds and their use in medicine
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The invention relates to a 4-methyl dihydropyrimidine compound and an application thereof as a drug, especially a drug used for treating and preventing hepatitis B, and in particular relates to a compound shown in a general formula (I) or general formula (Ia) in the specification or enantiomers, diastereoisomers, tautomers, hydrates, solvates or pharmaceutically acceptable salts of the compound. All the variables are defined in the specification. The invention also relates to an application of the compound shown in the general formula (I) or general formula (Ia) in the specification or the enantiomers, diastereoisomers, tautomers, hydrates, solvates or pharmaceutically acceptable salts of the compound as drugs, especially drugs used for treating and preventing hepatitis B.
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Paragraph 0448; 0450-0451
(2019/04/30)
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- Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors
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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
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supporting information
p. 3352 - 3371
(2017/05/05)
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- PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
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The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The process of the invention has simple operation, high optical purity o
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Paragraph 00121
(2015/06/11)
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- PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
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The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (la), as well as a intermediate thereof. The process of the invention has simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.
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Paragraph 00121
(2015/06/11)
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- PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
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The present invention relates to processes for preparing a dihydropyrimidine derivative having Formula (I) or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The processes of the invention have simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.
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Paragraph 00114
(2015/06/11)
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- DIHYDROPYRIMIDINE COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS
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Provided herein are dihydropyrimidine compounds and their pharmaceutical applications, especially for use in treating and preventing HBV diseases. Specifically, provided herein are compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer,
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Paragraph 00197
(2015/11/24)
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- AROYL-PIPERAZINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS TACHYKININ ANTAGONISTS
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This invention relates to piperazine derivatives of formula (I), wherein Y is bond or lower alkylene, R1 is aryl which may have substituent(s), R2 is aryl or indolyl, each of which may have substituent(s), R3 is hydrogen or lower alkyl, and R4 is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human beings or animals. 1
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