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    • 36. 发明授权
    • MAP4K4抑制剂
    • CN112585147B
    • 2023-12-05
    • CN201880071792.8
    • 2018-10-12
    • 帝国理工学院创新有限公司
    • 迈克尔·施奈德加里·牛顿凯蒂·查普曼特雷弗·佩里奥尔阿什利·贾维斯卡罗琳·洛里恩·阿基利马尔廷·费希尔梅拉妮·拜福德尼古拉斯·查普曼尼古拉斯·马尔廷蒂菲勒·赖辛格加布里埃·内戈伊塔·吉拉斯洛娜·R·费尔德勒
    • C07F9/09A61P9/00C07D487/04A61K31/519
    • 本发明涉及包含吡咯并嘧啶的化合物,这些化合物可用作丝裂原活化蛋白激酶激酶激酶激 (I)的化合物。酶4(MAP4K4)的抑制剂。本发明还涉及这些包含吡咯并嘧啶的化合物例如在治疗方法中的用途。还提供了用于产生本发明的化合物的方法以及这些化合物的使用方法。特别地,本发明涉及式(56)对比文件Mostafa M. Ghorab 等.Computer-BasedLigand Design and Synthesis of Some NewSulfonamides Bearing Pyrrole orPyrrolopyrimidine Moieties HavingPotential Antitumor and RadioprotectiveActivities《.Phosphorus, Sulfur, andSilicon》.2008,第183卷(第1期),90-104.Eva Altmann 等.N7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines Represent aVersatile Class of Potent Inhibitors ofthe Tyrosine Kinase c-Src《.Mini Reviewsin Medicinal Chemistry》.2002,第2卷(第3期),201-208.Andre Chow 等.Human InducedPluripotent Stem Cell-DerivedCardiomyocyte Encapsulating BioactiveHydrogels Improve Rat Heart Function PostMyocardial Infarction《.Stem CellReports》.2017,第9卷(第5期),1415-1422.Joseph V.Virbasius 等.Map4k4SignalingNodesin MetabolicandCardiovascular Diseases《.Trends inEndocrinology & Metabolism》.2016,第27卷484-492.Ghorab M M等.SYNTHESIS AND MOLECULARDOCKING OF SOME NOVEL ANTICANCERSULFONAMIDES CARRYING A BIOLOGICALLYACTIVE PYRROLE AND PYRROLOPYRIMIDINEMOIETIES《.Acta Poloniae Pharmaceutica-Drug Research》.2014,第71卷603-614.Chaitanya G. Dave 等.Synthesis of 5,7-Disubstituted 7H-Pyrrolo[2,3-d]Pyrimidin-4(3H)-ones and Their N-Alkylation’s under Phase TransferConditions《.Journal of HeterocyclicChemistry》.2014,第51卷943-947.Waleed M. Hussein等.Synthesis andKinetic Testing of Tetrahydropyrimidine-2-thione and Pyrrole Derivatives asInhibitors of the Metallo-beta-lactamasefrom Klebsiella pneumonia and Pseudomonasaeruginosa《.Chem Biol Drug Des》.2012,第80卷500-515.Mosaad S. Mohamed等.Synthesis andkinetic testing of new inhibitors for ametallo-beta-lactamase from Klebsiellapneumonia and Pseudomonas aeruginosa.《European Journal of MedicinalChemistry》.2011,第46卷6075-6082.Khairy Abdelhameed Mohsen EL-BAYOUKI等.SYNTHESIS OF NEW PYRROLE AND PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES OFPOTENTIAL ANTIOXIDANT ACTIVITY《.Collect.Czech. Chem. Commun.》.2010,第75卷813-834.Cristina Tintori.Docking, 3D-QSARstudies and in silico ADME prediction onc-Src tyrosine kinase inhibitors.《European Journal of MedicinalChemistry》.2008,第44卷990-1000.Saber M. Hassan 等.Heteroaromatization with SulfonamidoPhenyl Ethanone, Part I: Synthesis ofNovel Pyrrolo[2,3- D]Pyrimidine andPyrrolo[3,2- E][1,2,4]Triazolo[1,5- C]Pyrimidine Derivatives ContainingDimethylsulfonamide Moiety《.Phosphorus,Sulfur, and Silicon and the RelatedElements》.2009,第184卷291-308.Nirmal D. Desai.Synthesis of FusedTetrazolo[1,5‐c] pyrrolo[3,2‐e]pyrimidines and Their ReductiveConversion to New 4‐Aminopyrrolo[2,3‐d]pyrimidines《.Synthetic Communicat》.2006,第36卷2169-2182.Cicily Augustine等.syntheses of 1,3-disubstituted-5a-hydropyrrolo-[2,3-d]quinazolino[3,2-e]pyrimidin-6(5H)-ones:Acomparison of conventional and microwavetechnique《.Indian Journal of Chemistry》.2005,第44B卷1653-1658.Nirmal D. Desai.Synthesis andReaction of Fluoroaryl Substituted 2-Amino-3-cyanopyrroles and Pyrrolo[2,3-d]pyrimidines《.J. Heterocyclic Chem.》.1999,第36卷729-733. (续)