CAS: 53981-23-0; 2-Amino-3-Fluorophenol

上下游产品

CAS号385-01-3 3-氟-2-硝基苯酚 | CAS号160564-65-8 2-benzyloxy-6-f... | CAS号384346-28-5 N-(2-fluoro-6-h... | CAS号18063-03-1 2,6-二氟苯甲酰胺 | CAS号19064-24-5 2,6-二氟硝基苯 | CAS号641-49-6 3-氟-2-硝基苯甲醚 | CAS号127682-43-3 O-(3-fluorophen...

📜2,6-二氟硝基苯置于palladium 10% On Activated Carbon,氢气,三溴化硼体系中,用 甲醇,乙醇,二氯甲烷 作为反应溶剂,-40.0~20.0 °C,101.33 Kpa 条件下,反应 33.0H,反应生成 2-氨基-3-氟苯酚
参考文献:开发一种新的结构类广泛作用的 Hcv 非核苷抑制剂,导致 Mk-8876 的发现.
标题:开发一种新的结构类广泛作用的 Hcv 非核苷抑制剂,导致 Mk-8876 的发现.
摘要:旨在开发一种广泛作用的 Hcv Ns5B 非核苷抑制剂的研究导致发现了一种新型结构类别的 5-芳基苯并呋喃,它同时与手掌 I 和手掌 Ii 结合区域相互作用.最初的候选药物在体外对 Hcv Gt1A 和 Gt1B 复制子有效,并且当对慢性 Gt1 感染的黑猩猩口服给药时,可诱导 Hcv 病毒载量多对数减少.然而,针对临床相关 Gt1A 变体的体外效力损失促使人们进一步努力开发在更广泛的 Hcv 基因型和突变体中具有持续效力的化合物.最终,生物学和药物化学的合作导致了开发候选 Mk-8876 的发现.mk-8876 表现出泛基因型效力特征,并保持对临床相关突变体的效力.它在大鼠和狗中表现出中等的生物利用度,但表现出与每日一次给药一致的低血浆清除率特征.在本文中,我们描述了导致 Mk-8876 发现的努力,该研究进入了 1 期单药治疗研究,用于评估和表征作为治疗慢性 Hcv 感染的全口服直接作用药物方案的组成部分.
DOI:10.1002/cmdc.201700228

专利信息

专利号:WO-2011106986-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO
权利人:MERCK SHARP & DOHME; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO
摘要:Compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and /or viral production in a cell-based system. Wherein Z, R 30 , R 40 , R 50 and R 60 of compounds of formula (I) are herein defined as in the description.

专利号:US-2012328569-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
权利人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
摘要:Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9549917-B2
优先权日:2011-09-08
标 题 :Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
发明人：MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS
权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9549921-B2
优先权日:2013-06-24
标 题:Heterocyclic compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)