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Review

A patent review of MAT2a inhibitors (2018–2021)

Pages 1043-1053 | Received 03 Feb 2022, Accepted 26 Aug 2022, Published online: 01 Sep 2022

References

  • Lu SC, Mato JM. S-adenosylmethionine in liver health, injury, and cancer. Physiol Rev. 2012;92(4):1515–1542.
  • Ramani K, Mato JM, Lu SC. Role of methionine adenosyltransferase genes in hepatocarcinogenesis. Cancers (Basel). 2011;3(2):1480–1497.
  • McDonald ER, de Weck A, Schlabach MR, et al. Project DRIVE: a compendium of cancer dependencies and synthetic lethal relationships uncovered by large-scale, deep RNAi screening. Cell. 2017;170(3):577–592.
  • Kryukov Gregory V, Wilson Frederick H, Ruth Jason R, et al. MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells. Science. 2016;351(6278):1214–1218.
  • Marjon K, Cameron Michael J, Quang P, et al. MTAP deletions in cancer create vulnerability to targeting of the MAT2A/PRMT5/RIOK1 axis. Cell Rep. 2016;15(3):574–587.
  • Zhang H, Chen Z-H, Savarese TM. Codeletion of the genes for p16INK4, methylthioadenosine phosphorylase, interferon-α1, interferon-β1, and other 9p21 markers in human malignant cell lines. Cancer Genet Cytogenet. 1996;86(1):22–28.
  • Albers E. Metabolic characteristics and importance of the universal methionine salvage pathway recycling methionine from 5′-methylthioadenosine. IUBMB Life. 2009;61(12):1132–1142.
  • Quinlan CL, Kaiser SE, Bolaños B, et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017;13(7):785–792.
  • Murray B, Antonyuk SV, Marina A, et al. Structure and function study of the complex that synthesizes S-adenosylmethionine. IUCrJ. 2014;1(4):240–249.
  • Hester JB, Rudzik AD, Von Voigtlander PF. 1-(Aminoalkyl)-6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. J Med Chem. 1980;23(4):392–402.
  • Travins JM, Konteatis ZD, Sui Z, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Preparation of pyrazolo[1,5-a]pyrimidin-7(4H)-ones as methionine adenosyltransferase 2A inhibitors for treatment of cancer patent WO2018039972. 2018.
  • Konteatis ZD, Sui Z, Travins JM, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Preparation of pyrazolo[1,5-a]pyrimidin-7(4H)-ones as methionine adenosyltransferase 2A inhibitors for treatment of cancer patent WO2018045071. 2018.
  • Kalev P, Hyer ML, Gross S, et al. MAT2A inhibition blocks the growth of MTAP-deleted cancer cells by reducing PRMT5-dependent mRNA splicing and inducing DNA damage. Cancer Cell. 2021;39(2):209–224.
  • Konteatis Z, Travins J, Gross S, et al. Discovery of AG-270, a first-in-class oral MAT2A inhibitor for the treatment of tumors with homozygous MTAP deletion. J Med Chem. 2021;64(8):4430–4449.
  • Hyer ML, Kalev P, Marjon K, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Combination of 3-(cyclohex-1-en-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(pyridine-3-ylamino)pyrzolo[1,5-a]pyrimidin-7(4H)-one and other chemotherapeutic agents for treatment of cancer patent WO2020168032. 2020.
  • Kruger RG, Laraio J, Mohammad H, inventors; Glaxosmithkline Intellectual Property Development Limited, assignee. Combination of a Type I protein arginine methyltransferase (type I PRMT) inhibitor and a methionine adenosyltransferase II alpha (MAT2A) inhibitor for treating cancer patent WO2021023609. 2021.
  • Konteatis ZD, Li M, Liu P, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Preparation of heterobicyclic compounds as inhibitors of MAT2A and methods of use for treating cancer patent WO2019191470. 2019.
  • Konteatis ZD, Li M, Reznik SK, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Preparation of azaheterobicyclic inhibitors of MAT2A and methods of use for treating cancer patent WO2020139991. 2020.
  • Konteatis ZD, Li M, Reznik SK, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Preparation of azaheterobicyclic inhibitors of MAT2A and methods of use for treating cancer patent WO2020139992. 2020.
  • Konteatis ZD, Li M, Reznik SK, et al., inventors; Agios Pharmaceuticals, Inc., assignee. Preparation of heterobicyclic inhibitors of MAT2A and methods of use for treating cancer patent WO2020243376. 2020.
  • Hayes S, Chubukov V, Roddy TP, et al., inventors; Agios Pharmaceuticals, Inc., The Royal Institution for the Advancement of Learning/Mcgill University, assignee. Methods of treating autoimmune or inflammatory diseases or disorders patent WO2021158792. 2021.
  • Alam M, Cleary L, Fleury M, et al., inventors; Ideaya Biosciences, Inc., assignee. 2-Oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors and their preparation patent WO2020123395. 2020.
  • De Fusco C, Schimpl M, Börjesson U, et al. Fragment-based design of a potent MAT2a inhibitor and in vivo evaluation in an MTAP null xenograft model. J Med Chem. 2021;64(10):6814–6826.
  • Knox JE, Cleary L, Fleury M, et al., inventors; IDEAYA Biosciences, Inc., assignee. Preparation of heteroaryl alkylene substituted 2-oxoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors patent WO2021252678. 2021.
  • Steel R, Fleury M, Barsanti PA, inventors; IDEAYA Biosciences, Inc., assignee. Preparation of aminoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors for treatment of cancer patent WO2021252679. 2021.
  • Cleary L, Fleury M, Pei Z, et al., inventors; IDEAYA Biosciences, Inc., assignee. Preparation of 4-arylquinazoline derivatives as methionine adenosyltransferase 2a inhibitors for treatment of cancer patent WO2021252680. 2021.
  • Cleary L, Fleury M, Pei Z, inventors; IDEAYA Biosciences, Inc., assignee. Preparation of quinolinone derivatives as methionine adenosyltransferase 2a inhibitors for treatment of cancer patent WO2021252681. 2021.
  • Li Z, Tang F, Zhao C, et al., inventors; Jiangsu Simcere Pharmaceutical Co., Ltd., assignee. Pyrimidinopyridone compound, its preparation method and application patent WO2021139775. 2021.
  • Li Z, Tang F, Zhao C, et al., inventors; Jiangsu Simcere Pharmaceutical Co., Ltd., assignee. Preparation of bicyclic heteroaryl compounds as MAT2A inhibitors patent WO2021254529. 2021.
  • Bobinski TP, Marx MA, inventors; Mirati Therapeutics, Inc., assignee. Preparation of substituted N-(imidazol-2-yl) benzamides as MAT2A inhibitors patent WO2020167952. 2020.
  • Bell AS, Besnard J, Bradley AR, et al., inventors; F. Hoffmann-La Roche, AG Hoffmann-La Roche Inc., assignee. Preparation of sulfone derivatives as inhibitors of the human methionine adenosyltransferase 2A (Mat2A) for use in the treatment of cancer patent WO2021259831. 2021.
  • Bell AS, Besnard J, Bradley AR, et al., inventors; F. Hoffmann-La Roche, AG Hoffmann-La Roche Inc., assignee. Preparation of aminopyrimidone derivatives as inhibitors of the human methionine adenosyltransferase 2A (Mat2A) for use in the treatment of cancer patent WO2021259815. 2021.

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