CAS: 848942-61-0; 2-(4-((4-((3-Chloro-2-Fluorophenyl)Amino)-7-Methoxyquinazolin-6-yl)Oxy)Piperidin-1-yl)-N-Methylacetamide

上下游产品

N-(3-chloro-2-fluorophenyl)-7-methoxy-6-(piperidin-4-yloxy)quinazolin-4-amine chloroacetylmethylamide 2-[4-(5-cyano-4-{[(dimethylamino)methylene]amino}-2-methoxyphenoxy)piperidin-1-yl]-N-methylacetamide 3-chloro-2-fluoroaniline

📜2-氨基-4,5-二甲氧基苯甲酸乙酯置于吡啶,4-二甲氨基吡啶,甲烷磺酸,L-蛋氨酸,氨,Potassium Carbonate,Cesium Fluoride,N,N-二乙基苯胺,Potassium Iodide,Sodium Hydroxide,三氯氧磷体系中,用 甲醇,N,N-二甲基乙酰胺,水,异丙醇,乙腈 作为反应溶剂,化学反应 62.0H,反应生成 Az08931 2-(4-(4-(3-氯-2-氟苯基氨基)-7-甲氧基喹唑啉-6-基氧基)哌啶-1-基)-N-甲基乙酰胺
参考文献:The First Radiosynthesis Of [11 C]Azd8931 As A New Potential Pet Agent For Imaging Of Egfr,Her2 And Her3 Signaling
标题:The First Radiosynthesis Of [11 C]Azd8931 As A New Potential Pet Agent For Imaging Of Egfr,Her2 And Her3 Signaling
摘要:The Reference Standard Azd8931{2-(4-((4-((3-Chloro-2-Fluorophenyl) Amino)-7-Methoxyquinazolin-6-yl)Oxy) Piperidin-1-yl)-N-Methylacetamide} (11A) Was Synthesized From Methyl 4,5-Dimethoxy-2-Nitrobenzoate Or Ethyl 4,5-Dimethoxy-2-Nitrobenzoate And 2-Chloro-N-Methylacetamide In 11 Steps With 2-5% Overall Chemical Yield. The Precursor N-Desmethyl-Azd8931{2-(4-((4-((3-Chloro-2-Fluorophenyl)Amino)-7-Methoxyquinazolin-6-yl)Oxy)Piperidin-1-yl) Acetamide} (11B) Was Synthesized From Methyl 4,5-Dimethoxy-2-Nitrobenzoate Or Ethyl 4,5-Dimethoxy-2-Nitrobenzoate And 2-Bromoacetamide In 11 Steps With 2-4% Overall Chemical Yield. The Target Tracer [c-11] Azd8931 {2-(4-((4-((3-Chloro-2-Fluorophenyl) Amino)-7-Methoxyquinazolin-6-yl) Oxy) Piperidin-1-yl)-N-[c-11] Methylacetamide} ([c-11]11A) Was Prepared From N-Desmethyl-Azd8931 (11B) With [c-11]Ch3Otf Under Basic Condition (Nah) Through N-[11C] Methylation And Isolated By HPLC Combined With Solid-Phase Extraction (Spe) In 40-50% Radiochemical Yield Based On [c-11]Co2 And Decay Corrected To End Of Bombardment (Eob) With 370-1110 Gbq/mu Mol Specific Activity At Eob. (C) 2014 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2014.07.092

专利信息

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:US-2022396794-A1
优先权日:2019-06-04
标题:APTAMERS AGAINST TRANSFERRIN RECEPTOR (TfR)
发明人：HABIB NAGY; ROSSI JOHN; YOON SORAH; SWIDERSK PIOTR MAREK
权利人:APTERNA LTD; HOPE CITY
摘要:Methods of treating or preventing a disease or disorder are disclosed comprising administering to a subject in need thereof an effective amount of a nucleic acid compound comprising, or consisting of, a nucleic acid sequence capable of binding to a transferrin receptor (TfR) and an effective amount of an inhibitor of DNA synthesis. Also disclosed is a nucleic acid compound comprising, or consisting of, a nucleic acid sequence having at least 85% sequence identity to SEQ ID NO: 1, wherein said nucleic acid sequence is at least 30 nucleotides in length and at most 50 nucleotides in length, and wherein the nucleic acid sequence is capable of binding to a transferrin receptor (TfR).