CAS: 1257628-77-5; 3-((1H-Pyrazolo[3,4-B]Pyridin-5-yl)Ethynyl)-4-Methyl-N-(4-((4-Methylpiperazin-1-yl)Methyl)-3-(Trifluoromethyl)Phenyl)Benzamide

上下游产品

3-iodo-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl) phenyl)benzamide 5-ethynyl-1H-pyrazolo[3,4-b]pyridine methyl 3-iodo-4-methylbenzoate 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylaniline3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide bismethanesulfonic acid

3-碘-4-甲基苯甲酸甲酯置于bis-Triphenylphosphine-Palladium(II) Chloride,Copper(L) Iodide,Potassium Tert-Butylate,三乙胺体系中,用 四氢呋喃,乙腈 用作溶剂,化学反应 23.0H,反应生成4-甲基-N-[4-[(4-甲基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-3-[2-(1H-吡唑并[3,4-B]吡啶-5-基)乙炔基]苯甲酰胺
参考文献:Identification Of Gzd824 As An Orally Bioavailable Inhibitor That Targets Phosphorylated And Nonphosphorylated Breakpoint Cluster Region-abelson (Bcr-Abl) Kinase And Overcomes Clinically Acquired Mutation-Induced Resistance Against Imatinib
标题:Identification Of Gzd824 As An Orally Bioavailable Inhibitor That Targets Phosphorylated And Nonphosphorylated Breakpoint Cluster Region-abelson (Bcr-Abl) Kinase And Overcomes Clinically Acquired Mutation-Induced Resistance Against Imatinib
摘要:Bcr-Abl(T315)I Mutation-Induced Imatinib Resistance Remains A Major Challenge For Clinical Management Of Chronic Myelogenous Leukemia (Cml). Herein,We Report Gzd824 (10A) As A Novel Orally Bioavailable Inhibitor Against A Broad Spectrum Of Bcr-Abl Mutants Including T315I. It Tightly Bound To Bcr-Abl(Wt) And Bcr-Abl(T315I) With K-D Values Of 0.32 And 0.71 Nm,Respectively,And Strongly Inhibited The Kinase Functions With Nanomolar Ic50 Values. The Compound Potently Suppressed Proliferation Of Bcr-Abl-Positive K562 And Ku812 Human Cml Cells With Ic50 Values Of 0.2 And 0.13 Nm,Respectively. It Also Displayed Good Oral Bioavailability (48.7%),A Reasonable Half-Life (10.6 H),And Promising In Vivo Antitumor Efficacy. It Induced Tumor Regression In Mouse Xenograft Tumor Models Driven By Bcr-Abl(Wt) Or The Mutants And Significantly Improved The Survival Of Mice Bearing An Allograft Leukemia Model With Ba/f3 Cells Harboring Bcr-Abl(T315I). Gzd824 Represents A Promising Lead Candidate For Development Of Bcr-Abl Inhibitors To Overcome Acquired Imatinib Resistance.
Doi:10.1021/jm301581Y

专利信息

专利号:US-11858953-B2
优先权日:2018-04-04
标 题:Compositions and methods for synthesis of phosphorylated molecules
发明人：CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT
权利人:UNIV CALIFORNIA
摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

专利号:US-2009306400-A1
优先权日:2006-03-27
标 题:Convergent process for the synthesis of taxane derivatives.
发明人：HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING
权利人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING
摘要:The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.

专利号:US-2025002518-A1
优先权日:2023-06-16
标 题 :Synthesis of heteroarynes and use thereof
发明人：MATTMILLER ROBERTS COURTNEY COLLEEN; HUMKE JENNA NICOLE; QUINLIVAN ANSEL ANNABEL; BELLI ROMAN GIANCARLO; KARGBO SALLU SO; PLASEK ERIN ELIZABETH
权利人:UNIV MINNESOTA
摘要:Disclosed herein are heterocyclic arynes and methods for preparing the same. Heteroarynes such as 5-membered O- or N-heterocyclic arynes have been considered inaccessible due to ring strain associated with the triple bond. The methods described herein demonstrate that these arynes can be successfully prepared through the utility of pi-backbonding from a transition metal. Synthetic utility of this method has been demonstrated by the facile synthesis and functionalization of heterocycles using these heteroaryne building blocks.

专利号:WO-9741109-A1
优先权日:1996-04-26
标 题 :Synthesis of (±) - calicheamicinone, precursors, intermediates and derivatives
发明人：CLIVE DERRICK L J; DAIGNEAULT SYLVAIN; BO YUNXIN; TAO YONG
权利人:UNIV ALBERTA; CLIVE DERRICK L J; DAIGNEAULT SYLVAIN; BO YUNXIN; TAO YONG
摘要:This invention relates to calicheamicinone and related compounds, and processes for the preparation of these compounds and derivatives or analogs thereof. Many of the products that can be synthesized using these compounds have antibiotic activity including, but not limited to, anticancer, antifungal or antimicrobial activity.

专利号:US-4897475-A
优先权日:1988-02-05
标 题:Process for synthesis of 5α-cholest-8(14)-en-3β-ol-15-one and other 15-oxygenated sterols
发明人：SCHROEPFER JR GEORGE J; WILSON WILLIAM K; WANG KER-SHI; KISIC ALEMKA
权利人:UNIV RICE WILLIAM M
摘要:A process for preparing 15-oxygenated sterols, such as 3β-hydroxy-5α-cholest-8(14)-ene-15 one, comprising converting 7-dehydrocholesterol to 3β-benzoyloxycholesta-5,7-diene, converting the 3β-benzoyloxycholesta-5,7-diene to a 3β-benzoyloxy-5-cholesta-7,14-diene, converting the 3β-benzoyloxy-5-cholesta-7,14-diene to a 3β-benzoyloxy-14α, 15α-epoxy-5-cholest-7-ene and converting the 3β-benzoyloxy-14α, 15α-epoxy-5-cholest-7-ene to a 15-oxygenated sterol. Preferably, the 3β-benzoyloxy-cholesta-5,7-diene is converted to a 3β-benzoyloxy-5-cholesta-7,14-diene by (i) contacting 3β-benzoyloxy-cholesta-5,7-diene, in a solvent at a temperature of at most about -55° C., with HCl at a concentration of at least about 2.0 M for a time sufficient to convert the 3β-benzoyloxycholesta-5,7-diene to a 3β-benzoyloxy-5-cholesta-7,14-diene; (ii) neutralizing the resultant reaction mixture with a base to prevent formation of a significant amount of 3β-benzoyloxy-5-cholesta-8,14-diene; and (iii) recovering the 3β-benzoyloxy-5-cholesta-7,14-diene.

专利号:US-2023303474-A1
优先权日:2020-07-30
标 题 :Total syntheses of specialized pro-resolving mediators (spms), structural isomers and structural analogs
发明人：MARETTE ANDRÉ; MALTAIS RENÉ; POIRIER DONALD; SANCÉAU JEAN-YVES
权利人:UNIV LAVAL
摘要:A method for the synthesis of specialized pro-resolving mediators, structural isomers thereof and analogs thereof is disclosed herein. The method comprises reacting a compound of the formula (I): n n n n n n n n n n n n wherein R 1 is alkyl (C≤12) , cycloalkyl (C≤12) , alkenyl (C≤12) , alkylidene (C≤12) , alkynyl (C≤12) , aryl, aralkyl, heteroaryl or heteroaralkyl; and X 1 , X 2 and X 3 are each independently hydroxy or OP, wherein P is a hydroxy protecting or hydroxy activating group; with a reducing agent under conditions sufficient to produce a compound of the formula (II): n n n n n n n n n n n n n n n n wherein: R 1 , X 1 , X 2 and X 3 are as defined above. n n n n n Novel protectins, more specifically novel structural isomers and analogs of PD1 and PDX are also disclosed.