CAS: 7411-23-6; 3,5-Dibromo-1H-1,2,4-Triazole

1H-1,2,4-三唑置于溴,Potassium Bromide体系中,用 水 作为反应溶剂,化学反应生成 3,5-二溴-1,2,4-三氮唑
参考文献:乳腺癌stat3酶抑制剂1,2,4-三唑和1,3,4-恶二唑衍生物的合成
标题:乳腺癌stat3酶抑制剂1,2,4-三唑和1,3,4-恶二唑衍生物的合成
摘要:合成了双取代五元杂环化合物(1,2,4-三唑和 1,3,4 恶二唑),并研究其作为乳腺癌信号转导子和转录激活子 3 (Stat3) 酶的抑制剂.3-(苄硫基)-5-(4-氯苄基)-4 H-1,2,4-三唑-4-胺 (12D) 被发现是合成化合物中活性最强的,具有半最大抑制浓度 (对mcf7细胞的ic 50)值为1.5 µm,并且发现对stat3酶显示出非常好的抑制作用.化合物9A,B,D,E,F,11和12A,B,F,E对 Mcf7 细胞系的ic 50值在 3-12 µm 范围内.分子模型用于研究合成化合物的生物学结果.
DOI:10.1002/ardp.202300345

专利信息

专利号:US-10226449-B2
优先权日:2013-12-20
标 题:Heterocyclic modulators of lipid synthesis and combinations thereof
发明人：HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE
权利人:3 V BIOSCIENCES INC
摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.

专利号:US-9428502-B2
优先权日:2012-07-03
标题:Heterocyclic modulators of lipid synthesis
发明人：OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; WAGMAN ALLAN S
权利人:3-V BIOSCIENCES INC
摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.

专利号:US-2018222892-A1
优先权日:2012-07-03
标 题 :Heterocyclic modulators of lipid synthesis

专利号:EP-3083583-B1
优先权日:2013-12-20
标 题:Heterocyclic modulators of lipid synthesis and combinations thereof

专利号:CA-2934251-A1
优先权日:2013-12-20
标题:A combination of heterocyclic modulators of lipid synthesis and chemotherapeutic drugs in treatment of cancer

专利号:EP-3083583-A1
优先权日:2013-12-20
标题 :Heterocyclic modulators of lipid synthesis and combinations thereof