CAS: 848192-96-1; 3-(Trifluoromethyl)Azetidin-3-Ol Hydrochloride

上下游产品

1-benzhydryl-3-(trifluoromethyl)azetidin-3-ol 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(3-hydroxy-3-(trifluoromethyl)azetidin-1-yl)butan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid

📜1-二苯甲基-3-(三氟甲基)氮杂啶-3-醇置于盐酸,Palladium 10% On Activated Carbon,氢气体系中,用 甲醇 作为反应溶剂,化学反应生成 3-三氟甲基-3-吖啶醇盐酸盐
参考文献:苯并氧杂硼杂环戊烷抗疟剂.第5部分.新型酰胺吡唑基氧基苯并恶唑的前导物优化和临床前候选物的鉴定
标题:苯并氧杂硼杂环戊烷抗疟剂.第5部分.新型酰胺吡唑基氧基苯并恶唑的前导物优化和临床前候选物的鉴定
摘要:为了确定具有令人满意的抗疟活性,理化性质,药代动力学特征,体内功效和安全性特征的分子,对羧酰胺基吡嗪酰氧基苯并氧杂硼酸酯进行了研究.这项优化工作发现了46个,满足了我们的目标候选人档案.化合物46对培养的恶性疟原虫具有优异的活性,并且在感染的小鼠体内对恶性疟原虫和伯氏疟原虫具有体内活性.它在小鼠,大鼠和狗中表现出非常好的pk特性.它对其他11种恶性疟原虫非常活跃菌株,大多数对氯喹和乙胺嘧啶有抗性.46种体外快速寄生虫减少和体内寄生虫清除率特征与青蒿素和氯喹(两种速效抗疟药)相似.当口服剂量高达2000 Mg / Kg时,在ames分析,体外微核分析和体内大鼠微核分析中均无遗传毒性.这种新颖的苯并氧杂硼酸酯的综合性能支持其向临床前发展的进程.
DOI:10.1021/acs.Jmedchem.7B00621

专利信息

专利号:US-9856241-B2
优先权日:2013-07-03
标 题:Substituted benzofuranyl and benzoxazolyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

专利号:US-9428490-B2
优先权日:2011-07-29
标 题 :Nuclear transport modulators and uses thereof
发明人：SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD
权利人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD; KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.