CAS: 1242156-23-5; 6-Cyclopropyl-8-Fluoro-2-(2-(Hydroxymethyl)-3-(1-Methyl-5-((5-(4-Methylpiperazin-1-yl)Pyridin-2-yl)Amino)-6-Oxo-1,6-Dihydropyridin-3-yl)Phenyl)Isoquinolin-1(2H)-One

上下游产品

2-(3-chloro-2-(hydroxymethyl)phenyl)-6-cyclopropyl-8-fluoroisoquinoline-1(2H)-one 1-methyl-3-[5-(4-methyl-piperazin-1-yl)-pyridin-2-ylamino]-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyridin-2-one 6-bromo-8-fluoro-3,4-dihydroisoquinolin-1(2H)-one 6-cyclopropyl-8-fluoro-3,4-dihydroisoquinolin-1(2H)-one

📜1-甲基-4-(6-氨基吡啶-3-基)哌嗪置于tris-(Dibenzylideneacetone)Dipalladium(0),Palladium Diacetate,Potassium Carbonate,Caesium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽,2-二环己基磷-2,4,6-三异丙基联苯,三环己基膦体系中,用 1,4-二氧六环 用作溶剂,化学反应 11.0H,反应生成Rn486抑制剂
参考文献:Structure-Based Drug Design Of Rn486,A Potent And Selective Bruton's Tyrosine Kinase (Btk) Inhibitor,For The Treatment Of Rheumatoid Arthritis
标题:Structure-Based Drug Design Of Rn486,A Potent And Selective Bruton's Tyrosine Kinase (Btk) Inhibitor,For The Treatment Of Rheumatoid Arthritis
摘要:Structure-Based Drug Design Was Used To Guide The Optimization Of A Series Of Selective Btk Inhibitors As Potential Treatments For Rheumatoid Arthritis. Highlights Include The Introduction Of A Benzyl Alcohol Group And A Fluorine Substitution,Each Of Which Resulted In Over 10-Fold Increase In Activity. Concurrent Optimization Of Drug-Like Properties Led To Compound 1 (Rn486) ( J. Pharmacol. Exp. Ther. 2012,341,90),Which Was Selected For Advanced Preclinical Characterization Based On Its Favorable Properties.
Doi:10.1021/jm500305P

专利信息

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2025049968-A1
优先权日:2022-04-21
标 题 :Therapeutic and imaging agents for targeting myocardial tissue
发明人：EEDA VENKATESWARARAO; AWASTHI VIBHUDUTTA
权利人:UNIV OKLAHOMA
摘要:Analogs and derivatives of omecamtiv mecarbil (OM), including an 18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an 18F-labeled analog of OM.