CAS: 425637-18-9; 3-(1H-Indol-3-yl)-4-(2-(4-Methylpiperazin-1-yl)Quinazolin-4-yl)-1H-Pyrrole-2,5-Dione

上下游产品

2-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-acetamide 2-(2-chloroquinazolin-4-yl)acetamide 2,4-dichloroquinazoline 1,2,3,4-tetrahydro-quinazoline-2,4-dione 3-(1H-indol-3-yl)-4-[2-(4-methyl-piperazin-1-yl)-quinazolin-4-yl]-1H-pyrrole-2,5-dione acetate

📜2,4-喹唑啉二酮置于potassium Tert-Butylate,Sodium Hydride,N,N-二甲基苯胺,三氯氧磷体系中,用 四氢呋喃,N-甲基吡咯烷酮,Mineral Oil 作为反应溶剂,化学反应 4.75H,反应生成 3-(1H-吲哚-3-基)-4-[2-(4-甲基哌嗪-1-基)喹唑啉-4-基]吡咯-2,5-二酮
参考文献:Structure-activity Relationship And Pharmacokinetic Studies Of Sotrastaurin (Aeb071),A Promising Novel Medicine For Prevention Of Graft Rejection And Treatment Of Psoriasis
标题:Structure-activity Relationship And Pharmacokinetic Studies Of Sotrastaurin (Aeb071),A Promising Novel Medicine For Prevention Of Graft Rejection And Treatment Of Psoriasis
摘要:Protein Kinase C (Pkc) Isotypes Have Emerged As Key Targets For The Blockade Of Early T-Cell Activation. Herein,We Report On The Structure-Activity Relationship And The Detailed Physicochemical And In Vivo Pharmacokinetic Properties Of Sotrastaurin (Aeb071,1),A Novel Maleimide-Based Pkc Inhibitor Currently In Phase Ii Clinical Trials. Most Notably,The Preferred Uptake Of Sotrastaurin Into Lymphoid Tissues Is An Important Feature,Which Is Likely To Contribute To Its In Vivo Efficacy.
DOI:10.1021/jm200469U

专利信息

专利号:US-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-10308615-B2
优先权日:2015-05-29
标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-2018230127-A1
优先权日:2015-08-13
标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds
发明人：ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

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.

专利号:US-10316018-B2
优先权日:2015-08-27
标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators
发明人：LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.