CAS: 1243244-14-5; 2-(2',3-Dimethyl-[2,4'-Bipyridin]-5-yl)-N-(5-(Pyrazin-2-yl)Pyridin-2-yl)Acetamide

上下游产品

5-bromo-2-chloro-3-methylpyridine

2-氨基吡啶-5-硼酸,频哪醇酯置于4-二甲氨基吡啶,四(三苯基膦)钯,Sodium Carbonate,N,N'-二环己基碳二亚胺体系中,用 乙醇,水,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 30.0H,反应生成2',3-二甲基-N-[5-(2-吡嗪基)-2-吡啶基]-[2,4'-联吡啶]-5-乙酰胺
参考文献:发现作为有效,选择性和口服生物利用性豪猪抑制剂的吡啶基乙酰胺衍生物.
标题:发现作为有效,选择性和口服生物利用性豪猪抑制剂的吡啶基乙酰胺衍生物.
摘要:异常wnt信号传导的阻断是多种癌症中的一种有吸引力的治疗方法.我们开发并执行了针对wnt分泌和途径激活抑制剂的细胞高通量筛选.从屏幕上识别出引线结构(gnf-1331).进一步的研究确定了gnf-1331的分子靶标为豪猪(一种膜结合的o-酰基转移酶).结构-活性关系研究导致发现了一系列新型的有效和选择性豪猪抑制剂.在小鼠mmtv-Wnt1异种移植肿瘤模型中,化合物19 Gnf-6231表现出出色的途径抑制作用,并诱导了强大的抗肿瘤功效.
Doi:10.1021/acsmedchemlett.6B00038

专利信息

专利号:US-12358903-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-11739065-B2
优先权日:2016-06-13
标题 :FXR (NR1H4) modulating compounds
发明人：BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN
权利人:GILEAD SCIENCES INC
摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人：SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.