CAS: 1228591-30-7; N-(7-Cyano-6-(4-Fluoro-3-(2-(3-(Trifluoromethyl)Phenyl)Acetamido)Phenoxy)Benzo[d]Thiazol-2-yl)Cyclopropanecarboxamide

上下游产品

N-{5-[(2-amino-7-cyano-1,3-benzothiazol-6-yl)oxy]-2-fluorophenyl}-2-[3-(trifluoromethyl)phenyl]acetamide cyclopropanecarboxylic acid chloride 2-(3-amino-4-fluorophenoxy)-5-nitrobenzonitrile N-[5-(2-cyano-4-nitrophenoxy)-2-fluorophenyl]-2,2,2-trifluoroacetamide

📜N-[5-(4-Amino-2-Cyanophenoxy)-2-Fluorophenyl]-2,2,2-Trifluoroacetamide置于吡啶,Sodium Tetrahydroborate,溶剂黄146,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate体系中,用 四氢呋喃,甲醇,乙醇 用作溶剂,化学反应 17.17H,反应生成N-[7-氰基-6-[4-氟-3-[[[3-(三氟甲基)苯基]乙酰基]氨基]苯氧基]-1,3-苯并噻唑-2-基]环丙烷甲酰胺
参考文献:Discovery Of A Selective Kinase Inhibitor (Tak-632) Targeting Pan-Raf Inhibition: Design,Synthesis,And Biological Evaluation Of C-7-Substituted 1,3-Benzothiazole Derivatives
标题:Discovery Of A Selective Kinase Inhibitor (Tak-632) Targeting Pan-Raf Inhibition: Design,Synthesis,And Biological Evaluation Of C-7-Substituted 1,3-Benzothiazole Derivatives
摘要:With The Aim Of Discovering A Selective Kinase Inhibitor Targeting Pan-Raf Kinase Inhibition,We Designed Novel 1,3-Benzothiazole Derivatives Based On Our Thiazolo[5,4-B]Pyridine Class Raf/vegfr2 Inhibitor 1 And Developed A Regioselective Cyclization Methodology For The C-7-Substituted 1,3-Benzothiazole Scaffold Utilizing Meta-Substituted Anilines. Eventually,We Selected 7-Cyano Derivative 8B (Tak-632) As A Development Candidate And Confirmed Its Binding Mode By Cocrystal Structure With Braf. Accommodation Of The 7-Cyano Group Into The Braf-Selectivity Pocket And The 3-(Trifluoromethyl)Phenyl Acetamide Moiety Into The Hydrophobic Back Pocket Of Braf In The Dfg-Out Conformation Contributed To Enhanced Raf Potency And Selectivity Vs Vegfr2. Reflecting Its Potent Pan-Raf Inhibition And Slow Off-Rate Profile,8B Demonstrated Significant Cellular Activity Against Mutated Braf Or Mutated Nras Cancer Cell Lines. Furthermore,In Both A375 (Braf(V600E))And Hmvii (Nras(Q61K)) Xenograft Models In Rats,8B Demonstrated Regressive Antitumor Efficacy By Twice Daily,14-Day Repetitive Administration Without Significant Body Weight Loss.
Doi:10.1021/jm400778D

专利信息

专利号:US-2005043376-A1
优先权日:1996-12-03
标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof
发明人：DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A
摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

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-6965034-B2
优先权日:1996-12-03
标题:Synthesis of epothilones, intermediates thereto and analogues thereof
发明人：DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A; KUDUK SCOTT; HARRIS CHRISTINA; ZHANG XIU-GUO; BERTINO JOSEPH R
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

专利号:US-2008227851-A1
优先权日:2007-03-12
标题 :Laulimalide and laulimalide analogs
发明人：WENDER PAUL A
权利人:WENDER PAUL A
摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.

专利号:RU-2739034-C2
优先权日:2015-05-07
标 题 :Macrocyclisation reaction and intermediate compound and other fragments, useful in synthesis of macrolides of halichondrins

专利号:EP-3292130-B1
优先权日:2015-05-07
标题:Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides