发明名称 |
Nonnucleoside inhibitors of reverse transcriptase, composite binding pocket and methods for use thereof |
摘要 |
Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. The novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.
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申请公布号 |
US6380190(B1) |
申请公布日期 |
2002.04.30 |
申请号 |
US20010904979 |
申请日期 |
2001.07.13 |
申请人 |
PARKER HUGHES INSTITUTE |
发明人 |
VIG RAKESH;MAO CHEN;UCKUN FATIH A. |
分类号 |
A61K31/426;A61K31/44;A61K31/4402;A61K31/4545;A61K31/496;A61K31/505;A61K31/5377;A61P31/12;A61P31/18;A61P43/00;C07D213/75;C07D239/46;C07D277/20;C07D277/48;(IPC1-7):C07D401/02 |
主分类号 |
A61K31/426 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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