CAS: 1214265-56-1; N-(3-((5-Chloro-2-((4-(4-Methylpiperazin-1-yl)Phenyl)Amino)Pyrimidin-4-yl)Oxy)Phenyl)Acrylamide

上下游产品

5-chloro-N-(4-(4-methylpiperazin-1-yl)phenyl)-4-(3-nitrophenoxy)pyrimidin-2-amine 4-(3-aminophenoxy)-5-chloro-N-(4-(4-methylpiperazin-1-yl)phenyl)pyrimidin-2-amine acryloyl chloride 2,5-dichloro-4-(3-nitrophenoxy)pyrimidine

📜4-(4-甲基哌嗪)苯胺置于platinum(Iv) Oxide,氢气,N,N-二异丙基乙胺,三氟乙酸体系中,用 甲醇,二氯甲烷,仲丁醇 用作溶剂,化学反应生成N-[3-[[5-氯-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-4-嘧啶基]氧基]苯基]-2-丙烯酰胺
参考文献:Discovery Of Selective Irreversible Inhibitors For Egfr-T790M
标题:Discovery Of Selective Irreversible Inhibitors For Egfr-T790M
摘要:Targeting The Epidermal Growth Factor Receptor Kinase (Egfr) With Atp-Competitive Kinase Inhibitors Results In Dramatic But Short-Lived Responses In Patients With Egfr Mutant Non Small Cell Lung Cancer. A Series Of Novel Covalent Egfr Kinase Inhibitors With Selectivity For The Clinically Relevant T790M 'Gatekeeper' Resistance Mutation Relative To Wild-Type Egfr Were Discovered By Library Screening. A Representative Compound 3I Was Obtained Through A Systematic Sar Study Guided By Mutant Egfr-Dependent Cellular Proliferation Assays. (C) 2010 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2010.12.036

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-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).