An updated patent review of histone deacetylase (HDAC) inhibitors in cancer (2020 – present)

References

• Singh T, Kaur P, Singh P, et al. Differential molecular mechanistic behavior of HDACs in cancer progression. Med Oncol. 2022;39:171.
   PubMed Web of Science ®Google Scholar
• Yamagishi M. The role of epigenetics in T-cell lymphoma. Int J Hematol. 2022;116(6):828–836.
   PubMed Web of Science ®Google Scholar
• Yang F, Zhao N, Ge D, et al. Next-generation of selective histone deacetylase inhibitors. RSC Adv. 2019;9(34):19571–19583. DOI:10.1039/C9RA02985K
   PubMed Web of Science ®Google Scholar
• Hai R, Yang D, Zheng F, et al. The emerging roles of HDACs and their therapeutic implications in cancer. Eur J Pharmacol. 2022;931:175216.
   PubMed Web of Science ®Google Scholar
• Shanghai Bioray Biotechnology Co Ltd, East China Normal University. IDO/HDAC double-target compound and synthetic method and application thereof. CN110668992A; 2020
   Google Scholar
• Institute of Chemical Industry of Forest Products of CAF. Synthesis method of novel urushiol-based hydroxamic acid derivatives having HDAC (Histone deacetylase) inhibition and antitumor activity. CN111440138A; 2020
   Google Scholar
• Shenzhen Technology University. Targeted HDAC inhibitor and application thereof in antitumor therapeutic drugs. CN111617085A; 2021
   Google Scholar
• Cheshmazar N, Hamzhe-Mivehroud M, Nozad Charoudeh H, et al. Current trends in development of HDAC-based chemotherapeutics. Life Sci. 2022;308:120946.
   PubMed Web of Science ®Google Scholar
• TCS H, Chan AHY, Ganesan A. Thirty years of HDAC inhibitors: 2020 insight and hindsight. J Med Chem. 2020;63(21):12460–12484. DOI:10.1021/acs.jmedchem.0c00830
   PubMed Web of Science ®Google Scholar
• Anhui University of Traditional Chinese Medicine AHUTCM. mTOR/HDAC dual inhibitor and application thereof. CN111848629A; 2021
   Google Scholar
• Beijing Xinkaiyuan Pharmaceuticals Co Ltd. Compound with HDAC (Histone deacetylase) inhibitory activity, preparation method, composition and application. CN112225737A; 2021
   Google Scholar
• Beijing Huashi Jingheng Pharmaceutical Technology Co ltd. Pharmaceutical composition with HDAC (Histone deacetylase) inhibitory activity, preparation method and application thereof. CN112516142A; 2021
   Google Scholar
• Changzhou Vocational Institute of Engineering. HDAC and JAK dual-targeting inhibitor, preparation method and application. CN113429351A; 2021
   Google Scholar
• Sarkar R, Banerjee S, Amin SA, et al. Histone deacetylase 3 (HDAC3) inhibitors as anticancer agents: a review. Eur J Med Chem. 2020;192:112171.
   PubMed Web of Science ®Google Scholar
• Shandong University. HDAC, JAK and BET three-target inhibitor and preparation method and application thereof. CN113754591A;2021
   Google Scholar
• Xinxiang Medical University. 2-aryl isonicotinic acid amide LSD1/HDAC double-target inhibitor, and preparation method and application thereof. CN113444038A; 2022
   Google Scholar
• Xinxiang Medical University. 2-aryl-4- (1H-pyrazol-3-yl) pyridine LSD1/HDAC double-target inhibitor. CN113444069A; 2022
   Google Scholar
• Xinxiang Medical University. 5-aryl nicotinamide LSD1/HDAC double-target inhibitor, preparation method and application thereof. CN113527195A; 2022
   Google Scholar
• Hangzhou Normal University. HDAC/MAO-B dual inhibitor and preparation and application thereof. CN113956182A; 2022
   Google Scholar
• Shenyang Pharmaceutical University. HDAC inhibitor and preparation method and application thereof. CN114524799A; 2022
   Google Scholar
• Hangzhou Innogate Pharma Co Ltd. Heterocyclic compound as CDK-HDAC double-channel inhibitor. WO2020108661A1; 2022
   Google Scholar
• Hangzhou Innogate Pharma Co Ltd. Heterocyclic compound as CDK-HDAC dual pathway inhibitor. WO2020114519A1; 2020
   Google Scholar
• Hitgen INC. HDAC inhibitor, preparation method therefor and use thereof. WO2020216298A1; 2020
   Google Scholar
• West China Hospital, Sichuan University. Double-target inhibitor targeting fgfr and HDAC, preparation method therefor and application thereof, pharmaceutical composition and medicament. WO2022037365A1; 2022
   Google Scholar
• University of Pittsburgh-of the commonwealth system of higher education. HDAC inhibitors. WO2022120048A1; 2022
   Google Scholar
• Hangzhou Normal University. Histone deacetylase inhibitor, preparation thereof and application thereof in preparation of anti-cancer drugs. CN115417877A; 2022
   Google Scholar
• Huaqiao University. Biphenyl compound containing hydroxamic acid structure and application thereof. CN115368277A; 2022
   Google Scholar
• Shandong University. Diphenylaminopyrimidine-containing compound, preparation and application thereof as HDACs enzyme inhibitor. CN115286583A; 2022
   Google Scholar
• Anhui University of Traditional Chinese Medicine AHUTCM. HDAC (Histone deacetylase) inhibitor containing tetrahydroisoquinoline structure, composition and application thereof. CN115368306A; 2022
   Google Scholar
• Nantong University. 2-((4-morpholinyl phenyl) amino) pyrimidine amino acid derivative and preparation method and application thereof. CN115304551A; 2022
   Google Scholar
• Nantong University. Piperazine phenyl amino substituted pyrimidine amino acid derivative, preparation method and application. CN115304550A; 2022
   Google Scholar
• Nantong University. 2,4,5-trisubstituted pyrimidine hydroxylamine acyl derivative and preparation method and application thereof. CN115141150A; 2022
   Google Scholar
• The Reagents of the University of California. Carborane-based histone deacetylase (HDAC) inhibitors. WO2020117976A1; 2020
   Google Scholar
• Guangdong Medical University. Dasatinib derivative with HDAC (Histone deacetylase) inhibitory activity and application thereof. CN111039890A; 2020
   Google Scholar
• Beijing Xinkaiyuan Pharmaceuticals Co Ltd. Compounds having HDAC inhibitory activity, methods of making, compositions, and uses thereof. CN114605348A; 2022
   Google Scholar
• Southeast University. HDAC inhibitor containing ras/raf protein interfering group , and preparation method therefor. WO2022110958A1; 2022
   Google Scholar
• Moffat D, Patel S, Day F, et al. Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J Med Chem. 2010;53(24):8663–8678. DOI:10.1021/jm101177s
   PubMed Web of Science ®Google Scholar
• Viracta Therapeutics, INC. HDAC inhibitor solid state forms. WO2021113694A1; 2021
   Google Scholar
• Viracta Subsidiary, INC. HDAC inhibitor solid state forms. WO2022094122A1; 2022
   Google Scholar
• Kim YD, Park SM, Ha HC, et al. HDAC inhibitor, CG-745, enhances the anti-cancer effect of anti-PD-1 immune checkpoint inhibitor by modulation of the immune microenvironment. J Cancer. 2020;11(14):4059–4072. DOI:10.7150/jca.44622
   PubMed Web of Science ®Google Scholar
• CrystalGenomics Inc. Pharmaceutical composition comprising HDAC inhibitor and anti-pd1 antibody or anti pd-l1 antibody. EP4026544A1; 2022
   Google Scholar
• Yaokang Zhongtuo (Jiangsu) Pharmaceutical Technology Co.,Ltd. IDO/HDAC dual inhibitor and pharmaceutical composition and application thereof. CN111909107A; 2020
   Google Scholar
• Beijing Xinkaiyuan Pharmaceuticals Co Ltd. HDAC inhibitor, preparation method, pharmaceutical composition and application thereof. CN111116469A; 2020
   Google Scholar
• Beijing Huashi Xinhuake Biotechnology Co ltd. Aniline compounds with HDAC (HDAC) inhibitory activity, preparation method, composition and application. CN113461602A; 2022
   Google Scholar
• DANA-FARBER cancer institute, INC. Selective histone deacetylase (HDAC) degraders and methods of use thereof. WO2021092174A1; 2021
   Google Scholar
• University of Leicester. HDAC degrader. WO2021148811A1; 2021
   Google Scholar
• Smalley JP, Adams GE, Millard CJ, et al. PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes. Chem Commun. 2020;56(32):4476–4479. DOI:10.1039/D0CC01485K
   PubMed Web of Science ®Google Scholar
• Baker IM, Smalley JP, Sabat KA, et al. Comprehensive transcriptomic analysis of novel class I HDAC proteolysis targeting chimeras (PROTACs). Biochemistry. 2023;62(3):645–656. DOI:10.1021/acs.biochem.2c00288
   PubMed Web of Science ®Google Scholar
• University of Florida Research Foundation. Benzoylhydrazide-derived HDAC degraders as therapeutics for treating cancer and other human diseases. WO2021236491A1; 2021
   Google Scholar
• Xiao Y, Wang J, Zhao LY, et al. Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs. Chem Commun. 2020;56(68):9866–9869. DOI:10.1039/D0CC03243C
   PubMed Web of Science ®Google Scholar
• DANA-FARBER cancer institute, INC. Class IIa histone deacetylase (HDAC) degrader ligands and methods of use thereof. WO2022235565A1; 2022
   Google Scholar
• Xidian University. Phosphoric acid compound with HDAC (Histone deacetylase) inhibitory activity as well as preparation method and application thereof. CN111116647A; 2021
   Google Scholar
• Lightox Limited. Protected HDAC (histone deacetylase) inhibitors. WO2022157499A1; 2022
   Google Scholar
• Tongji Medical College of Huazhong University of Science and Technology. SUlfonium salt stabilization based HDAC (HDAC) -targeted polypeptide drug conjugate and application thereof. CN114146186A; 2022
   Google Scholar
• The Reagents of the University of California. Compositions comprising HDAC inhibitors and retinoids. WO2020232399A1; 2020
   Google Scholar
• Jiangsu Province Hospital First Affiliated Hospital With Nanjing Medical University. Application of novel HDAC inhibitor LAQ824 in medicine for treating diffuse large B cell lymphoma. CN111973590A; 2020
   Google Scholar
• Wang L, Wu Z, Xia Y, et al. Single-cell profiling-guided combination therapy of c-Fos and histone deacetylase inhibitors in diffuse large B-cell lymphoma. Clin Transl Med. 2022;12(5):e798. DOI:10.1002/ctm2.798
   PubMedGoogle Scholar
• Yu J, Qiu S, Ge Q, et al. A novel SAHA-bendamustine hybrid induces apoptosis of leukemia cells. Oncotarget. 2015;6(24):20121–20131. DOI:10.18632/oncotarget.4041
   PubMedGoogle Scholar
• People’s Hospital Affiliated To Ningbo University. Compositions of Bcl-2 inhibitors and HDAC inhibitors and uses thereof. CN114588269A; 2022
   Google Scholar
• Xunuo Pharmaceutical Nanjing Co ltd. Combination containing Pan-HDAC and immune checkpoint inhibitor and application. CN114146181A; 2022
   Google Scholar
• Viracta Therapeutics INC Dosages for HDAC treatment with reduced side effects. WO2021071809A1; 2021
   Google Scholar
• Anhui Provincial Hospital First Affiliated Hospital of USTC. Application of IIa HDAC inhibitor TMP269 in ARID 1A-deficient liver cancer. CN114601929A; 2022
   Google Scholar
• Ito R, Miyanishi K, Kubo T, et al. Synergistic antitumor effect of histone deacetylase class IIa inhibitor with lenvatinib in hepatocellular carcinoma. Hepatol Int. 2023. doi:10.1007/s12072-023-10484-2.
   Web of Science ®Google Scholar
• 4SC AG. Combination comprising HDAC inhibitor, CTLA-4 inhibitor and a PD-1 inhibitor or PD-L1 inhibitor for cancer treatment. WO2021064188A1; 2021
   Google Scholar
• HUYA Bioscience International, LLC. Triplet therapies of HDAC inhibitors, PD-L1 and/or PD-1 inhibitors, and CTLA-4 inhibitors. WO2020247830A1; 2020
   Google Scholar
• Clinical trial, https://clinicaltrials.gov/ct2/home ( last access 02/23/2023)
   Google Scholar
• H. Lee Moffitt Cancer Center and Research Institute INC. Immune checkpoint inhibitor and HDAC inhibitor combination therapy strategy. WO2022251827A1; 2022
   Google Scholar
• Italfarmaco SPA A combination comprising a specific HDAC6 inhibitor and at least one CTLA4 checkpoint inhibitor. WO2022223543A1; 2022
   Google Scholar
• Karus Therapeutics, LTD. HDAC inhibitors for use in the therapy of biliary tract cancers. WO2021001651A1; 2021
   Google Scholar
• Shenyang Pharmaceutical University. Application of HDAC6 inhibitor in preparation of medicine for treating DNMT3A gene deletion cancer. CN115192714A; 2022
   Google Scholar
• Centre D’etude des Cellules, Institut national de la SaNte et de la recherche medicale, universite Paris-Est Creteil val de Marne. Combination of a HDAC inhibitor and VX molecules, and its use for the treatment of cystic fibrosis. WO2021130381A1; 2021
   Google Scholar
• Korfei M, Mahavadi P, Guenther A. Targeting histone deacetylases in idiopathic pulmonary fibrosis: a future therapeutic option. Cells. 2022;11:1626.
   PubMed Web of Science ®Google Scholar
• Kumar V, Kundu S, Singh A, et al. Understanding the role of histone deacetylase and their inhibitors in neurodegenerative disorders: current targets and future perspective. Curr Neuropharmacol. 2022;20(1):158–178. DOI:10.2174/1570159X19666210609160017
   PubMed Web of Science ®Google Scholar
• Regenacy Pharmaceuticals, LLC. Pyrimidine and pyrazine HDAC1, 2 inhibitors. WO2020076951A1; 2020
   Google Scholar
• Kaur N, Fang YC, Lee HY, et al. Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment. Eur J Med Chem. 2020;187:111915.
   PubMed Web of Science ®Google Scholar