CAS: 1316214-52-4; 2-(Diphenylamino)-N-(7-(Hydroxyamino)-7-Oxoheptyl)Pyrimidine-5-Carboxamide

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CAS号1316216-07-5 7-({2-[(1-Methy... | CAS号89793-12-4 2-氯嘧啶-5-羧酸乙酯 | CAS号864172-93-0 5-Pyrimidinecar... | CAS号95928-49-7 2-羟基嘧啶-5-羧酸乙酯 | CAS号1316216-05-3 2-(二苯基氨基)嘧啶-5-羧酸乙酯 | CAS号1316216-06-4 2-(diphenylamin...

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    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-11666569-B2
    优先权日:2013-10-24
    标题 :Treatment of polycystic diseases with an HDAC6 inhibitor
    发明人:GRADILONE SERGIO A; LARUSSO NICHOLAS F
    权利人:MAYO FOUND MEDICAL EDUCATION & RES; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT
    摘要:An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.

    专利号:US-10144714-B2
    优先权日:2015-06-08
    标 题 :Methods of making protein deacetylase inhibitors
    发明人:SEYEDI FARZANEH; VAN DUZER JOHN H
    权利人:ACETYLON PHARMACEUTICALS INC
    摘要:The present invention relates to methods and intermediates useful for the synthesis of protein deacetylase inhibitors.

    专利号:US-11059815-B2
    优先权日:2018-07-23
    标 题:Synthesis of small molecule histone deacetylase 6 degraders, compounds formed thereby, and pharmaceutical compositions containing them
    发明人:TANG WEIPING; Yang Ka; WU HAO; ZHANG ZHONGRUI
    权利人:WISCONSIN ALUMNI RES FOUND
    摘要:Histone deacetylase (“HDACâ€?)-selective inhibitors covalently bonded to a linker covalently bonded to an E3 ubiquitin ligase ligand, and salts thereof; pharmaceutical compositions containing them; methods of using the composition to inhibit neoplastic cell growth in mammals, including humans.

    专利号:US-2018371021-A1
    优先权日:2017-05-11
    标 题 :Peptidomimetic macrocycles and uses thereof
    发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
    权利人:AILERON THERAPEUTICS INC
    摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

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    主要参考文献


    1: Amengual JE, Johannet P, Lombardo M, Zullo K, Hoehn D, Bhagat G, Scotto L, Jirau-Serrano X, Radeski D, Heinen J, Jiang H, Cremers S, Zhang Y, Jones S, O'Connor OA. Dual Targeting of Protein Degradation Pathways with the Selective HDAC6 Inhibitor ACY-1215 and Bortezomib Is Synergistic in Lymphoma. Clin Cancer Res. 2015 Oct 15;21(20):4663-75. doi: 10.1158/1078-0432.CCR-14-3068.
    2: Mishima Y, Santo L, Eda H, Cirstea D, Nemani N, Yee AJ, O'Donnell E, Selig MK, Quayle SN, Arastu-Kapur S, Kirk C, Boise LH, Jones SS, Raje N. Ricolinostat (ACY-1215) induced inhibition of aggresome formation accelerates carfilzomib-induced multiple myeloma cell death. Br J Haematol. 2015 May;169(3):423-34. doi: 10.1111/bjh.13315. doi: 10.1182/blood-2011-10-387365.
    4: Zhang L, Liu C, Wu J, Tao JJ, Sui XL, Yao ZG, Xu YF, Huang L, Zhu H, Sheng SL, Qin C. Tubastatin A/ACY-1215 improves cognition in Alzheimer's disease transgenic mice. J Alzheimers Dis. 2014;41(4):1193-205. doi: 10.3233/JAD-140066. doi: 10.3892/or.2016.5340. doi: 10.1016/j.jaci.2014.10.002.

    合成参考文献


    参考文献:10.1038/s41388-019-0855-x
    摘要:Saigi M, Alburquerque-Bejar JJ, Sanchez-Cespedes M. Determinants of immunological evasion and immunocheckpoint inhibition response in non-small cell lung cancer: the genetic front. Oncogene. 2019 Aug;38(31):5921–32. doi: 10.1038/s41388-019-0855-x.
    参考文献:10.1016/j.biopha.2019.109166
    摘要:Zhang WB, Yang F, Wang Y, Jiao FZ, Zhang HY, Wang LW, Gong ZJ. Inhibition of HDAC6 attenuates LPS-induced inflammation in macrophages by regulating oxidative stress and suppressing the TLR4-MAPK/NF-κB pathways. Biomed Pharmacother. 2019 Sep;117():109166. doi: 10.1016/j.biopha.2019.109166.
    参考文献:10.1007/s00296-020-04681-7
    摘要:Georgiev T. Multimodal approach to intraarticular drug delivery in knee osteoarthritis. Rheumatology International. 2020 Aug 16;40(11):1763–9. doi: 10.1007/s00296-020-04681-7.
    参考文献:10.1021/acs.jmedchem.9b01888
    摘要:Reßing N, Sönnichsen M, Osko JD, Schöler A, Schliehe-Diecks J, Skerhut A, Borkhardt A, Hauer J, Kassack MU, Christianson DW, Bhatia S, Hansen FK. Multicomponent Synthesis, Binding Mode, and Structure–Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups. J. Med. Chem. 2020 Aug 17;63(18):10339–51. doi: 10.1021/acs.jmedchem.9b01888.
    参考文献:10.1093/nar/gkab645
    摘要:Zhao T, Li Q, Zhou C, Lv X, Liu H, Tu T, Tang N, Cheng Y, Liu X, Liu C, Zhao J, Song Z, Wang H, Li J, Gu F. Small-molecule compounds boost genome-editing efficiency of cytosine base editor. Nucleic Acids Res. 2021 Sep 07;49(15):8974–86.
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