CAS: 872-64-0; 6-Azaspiro[2.5]Octane

相似化合物

1037834-62-0 1037834-61-9 955028-67-8

📜叔-丁基6-氮杂螺[2.5]辛烷-6-羧酸酯置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 0.5H,反应生成 6-氮杂螺[2.5]辛烷
参考文献:螺环和双环 8-硝基苯并噻嗪酮治疗结核病,具有改善的理化和药代动力学特性
标题:螺环和双环 8-硝基苯并噻嗪酮治疗结核病,具有改善的理化和药代动力学特性
摘要:以第二代类似物 Pbtz169 为代表的 8-硝基苯并噻嗪酮 (Btz) 是一类新型抗结核药物.由于分子靶标 Dpre1 位于分枝杆菌细胞包膜中,因此 Btz 的活性和亲脂性紧密耦合.设计了一系列类似物来解决 Btz 臭名昭著的不溶性问题,同时保留所需的亲脂性.这是通过用螺环和双环二胺生物电子等排取代 Pbtz169 的哌嗪部分来降低分子平面性和对称性来实现的.几种具有改善的水溶性的有前途的化合物被鉴定为具有有效的抗结核活性.化合物5因其优异的抗结核活性(mic 为 32 Nm),溶解度提高超过 1000 倍,在小鼠和人类微粒体中的清除率相对于 Pbtz169 低 2 倍以及有前景的药代动力学参数而被确定为最有前途的候选药物.
DOI:10.1021/acsmedchemlett.8B00634

专利信息

专利号:US-9533959-B2
优先权日:2013-10-07
标 题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
发明人：CHARRIER JEAN-DAMIEN; O'DONNELL MICHAEL EDWARD
权利人:VERTEX PHARMA
摘要:The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.

专利号:US-10005737-B2
优先权日:2013-10-07
标题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines

专利号:US-2015099875-A1
优先权日:2013-10-07
标题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines

专利号:US-2016326157-A1
优先权日:2014-01-06
标 题:Monobactams and methods of their synthesis and use
发明人：MYERS ANDREW G; Seiple lan Bass; SUSSMAN ROBIN JUDITH
权利人:HARVARD COLLEGE
摘要:Described herein are monobactam antibiotics of Formula (I), (I′), (II), and (II′), along with methods and intermediates for preparing these compounds. Pharmaceutical compositions and methods of treating infectious diseases using the monobactams are also provided.

专利号:US-11299484-B2
优先权日:2018-10-10
标 题 :Inhibiting fatty acid synthase (FASN)
发明人：MARTIN MATTHEW W; ZABLOCKI MARY-MARGARET; MENTE SCOT; DINSMORE CHRISTOPHER; WANG ZHONGGUO; ZHENG XIAOZHANG
权利人:FORMA THERAPEUTICS INC
摘要:The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds.

专利号:US-2014309413-A1
优先权日:2013-03-11
标题 :Methods of stereoselective synthesis of substituted nucleoside analogs
发明人：ROSE PETER JAMISON; JUNG YOUNG CHUN; BLIGH CAVAN MCKEON; IBRAHIM SHEREEN; ANZALONE LUIGI; MILLER JR DAVID B; VAN ALSTEN JOHN GREGG; CURRAN TIMOTHY THOMAS
权利人:VERTEX PHARMA
摘要:The present invention relates to the novel diastereoselective syntheses for generating phosphorothioate compounds. Examples include nucleoside phosphorothioate analogs that are useful in treating diseases and/or conditions such as viral infections.