CAS: 1445993-26-9; N-(4-(2,4-Difluorophenoxy)-3-(6-Methyl-7-Oxo-6,7-Dihydro-1H-Pyrrolo[2,3-C]Pyridin-4-yl)Phenyl)Ethanesulfonamide

上下游产品

4-(5-Amino-2-(2,4-Difluorophenoxy)Phenyl)-6-Methyl-1H-Pyrrolo[2,3-C]Pyridin-7(6H)-One 1445994-28-4
4-(2-(2,4-Difluorophenoxy)-5-Nitrophenyl)-6-Methyl-1H-Pyrrolo[2,3-C]Pyridin-7(6H)-One 1445994-27-3
N-(4-(2,4-Difluorophenoxy)-3-(6-Methyl-7-Oxo-1-Tosyl-6,7-Dihydro-1H-Pyrrolo[2,3-C]Pyridin-4-yl)Phenyl)-N-(Ethylsulfonyl)Ethanesulfonamide 1446235-99-9
4-(5-Amino-2-(2,4-Difluorophenoxy)Phenyl)-6-Methyl-1-Tosyl-1H-Pyrrolo[2,3-C]Pyridin-7(6H)-One 1446235-98-8
4-(2-Fluoro-5-Nitrophenyl)-6-Methyl-1-Tosyl-1H-Pyrrolo[2,3-C]Pyridin-7(6H)-One 1445993-88-3
6-甲基-4-(4,4,5,5,-四甲基-1,3,2-二氧硼烷-2-基)-1-对苯甲磺基-1H-吡咯并[2,3-C]吡啶-7(6H)-酮 6-Methyl-4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-1-Tosyl-1H-Pyrrolo[2,3-C]Pyridin-7(6H)-One 1445993-89-4

📜4-溴-7-甲氧基-1-对甲苯磺基-1H-吡咯并[2,3-C]吡啶置于盐酸,铁粉,Sodium Hydride,Sodium Carbonate,氯化铵,Caesium Carbonate,三乙胺体系中,用 四氢呋喃,1,4-二氧六环,乙二醇二甲醚,乙醇,二氯甲烷,水,二甲基亚砜,N,N-二甲基甲酰胺,Mineral Oil 用作溶剂,化学反应 24.25H,反应生成米维布塞
参考文献:的发现ñ-(4-(2,4-二氟苯氧基)-3-(6-甲基-7-氧代-6,7-二氢-1 H ^-吡咯并[2,3-C ^ ]吡啶-4-基)苯基)乙磺酰胺(abbv-075 / Mivebresib),有效且可口服的bromodomain和extraterminal Domain(bet)家族bromodomain抑制剂
标题:的发现ñ-(4-(2,4-二氟苯氧基)-3-(6-甲基-7-氧代-6,7-二氢-1 H ^-吡咯并[2,3-C ^ ]吡啶-4-基)苯基)乙磺酰胺(abbv-075 / Mivebresib),有效且可口服的bromodomain和extraterminal Domain(bet)家族bromodomain抑制剂
摘要:溴结构域和末端外结构域(bet)溴结构域抑制剂的开发及其在临床研究中,特别是在肿瘤学领域中的检查,引起了人们的广泛关注.基于简单的吡啶酮核心的制备,人们开始努力产生具有出色效能,药物代谢和药代动力学(dmpk)特性的新型bet溴结构域抑制剂.与关键的天冬酰胺残基形成双齿相互作用的努力导致掺入了吡咯并吡啶酮核心,其效价提高了9-19倍.旨在提高效力和改善药代动力学特性的额外结构-活性关系(sar)努力导致了临床候选药物的发现63 (abbv-075 / Mivebresib),其在生化和细胞分析中显示出优异的效力,在动物模型和人类模型中均具有非常好的暴露效果和半衰期,并且在癌症进展和炎症的小鼠模型中具有体内功效.
Doi:10.1021/acs.Jmedchem.7B00746

专利信息

专利号:WO-2011148392-A1
优先权日:2010-05-28
标题 :Process for the preparation of (2s,4s,5s,7s)-n-(2-carbamyl-2- methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3- methoxypropoxy)phenyl]-octanamide hemifumarate and its intermediates thereof
发明人：SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY
权利人:MSN LAB LTD; SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY
摘要:The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.

专利号:US-3717556-A
优先权日:1969-06-14
标 题 :PROCESS FOR THE PREPARATION OF beta -HALOGENO-ALKYL-ISOCYANATES
发明人：KAMPE K
权利人:HOECHST AG
摘要:N-halogeno-alkyl- Beta -lactams are rearranged into Beta halogeno-alkyl-isocyanates by contacting them with unsaturated organic compounds, optionally under irradiation. The products are highly reactive and useful for the synthesis of heterocyclic compounds.

专利号:US-12103929-B2
优先权日:2018-06-25
标题:Tricyclic compounds
发明人：FANG HAIQUAN; CHEN MINGMING; YANG GUIQUN; DU YUELEI; WANG YANPING; WU TONG; LI QINGLONG; ZHANG LEI; HU SHAOJING
权利人:JACOBIO PHARMACEUTICALS CO LTD
摘要:Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

专利号:CN-118754894-A
优先权日:2024-07-26
标题 :JQ1 derivative containing o-naphthoquinone structure, synthesis method thereof and application of JQ1 derivative in preparation of anti-triple-negative breast cancer drugs

专利号:CN-118812557-A
优先权日:2024-07-26
标 题:BRD4/GPX4 double-target inhibitor, synthesis method thereof and application of inhibitor in preparation of triple-negative breast cancer therapeutic drug