CAS: 1399177-37-7; 4-(1-(4-Cyclobutyl-2-Methyl-5-(3-Methyl-1H-1,2,4-Triazol-5-yl)Benzoyl)Piperidin-4-yl)Benzonitrile

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    专利信息


    专利号:US-9994550-B2
    优先权日:2014-01-07
    标题 :Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
    发明人:WAGMAN ALLAN S; JOHNSON RUSSELL J; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREG; OHOL-GUPTA YAMINI; HEUER TIMOTHY; O'FARRELL MARIE
    权利人:3 V BIOSCIENCES INC
    摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds.

    专利号:US-2024400552-A1
    优先权日:2016-11-11
    标题 :Heterocyclic modulators of lipid synthesis
    发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
    权利人:SAGIMET BIOSCIENCES INC
    摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

    专利号:US-11622968-B2
    优先权日:2011-03-08
    标 题:Heterocyclic modulators of lipid synthesis
    发明人:BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
    权利人:SAGIMET BIOSCIENCES INC
    摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

    专利号:US-10189822-B2
    优先权日:2015-03-19
    标 题:Heterocyclic modulators of lipid synthesis
    发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; HEUER TIMOTHY SEAN; O'FARRELL MARIE
    权利人:3 V BIOSCIENCES INC
    摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.

    专利号:US-11034690-B2
    优先权日:2016-11-11
    标 题:Heterocyclic modulators of lipid synthesis
    发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
    权利人:SAGIMET BIOSCIENCES INC; SAGINIET BIOSCIENCES INC
    摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

    专利号:US-9809591-B2
    优先权日:2011-03-08
    标题 :Heterocyclic modulators of lipid synthesis
    发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W
    权利人:3-V BIOSCIENCES INC
    摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: O'Farrell M, Duke G, Crowley R, Buckley D, Martins EB, Bhattacharya D, Friedman SL, Kemble G. FASN inhibition targets multiple drivers of NASH by reducing steatosis, inflammation and fibrosis in preclinical models. Sci Rep. 2022 Sep 19;12(1):15661. doi: 10.1038/s41598-022-19459-z.
    2: Kelly W, Diaz Duque AE, Michalek J, Konkel B, Caflisch L, Chen Y, Pathuri SC, Madhusudanannair-Kunnuparampil V, Floyd J, Brenner A. Phase II Investigation of TVB-2640 (Denifanstat) with Bevacizumab in Patients with First Relapse High- Grade Astrocytoma. Clin Cancer Res. 2023 Jul 5;29(13):2419-2425. doi: 10.1158/1078-0432.CCR-22-2807.
    3: Hasan SMN, Lou JW, Keszei AFA, Dai DL, Mazhab-Jafari MT. Atomic model for core modifying region of human fatty acid synthase in complex with Denifanstat. Nat Commun. 2023 Jun 12;14(1):3460. doi: 10.1038/s41467-023-39266-y.

    合成参考文献


    参考文献:10.1038/s41523-024-00656-0
    摘要:Serhan HA, Bao L, Cheng X, Qin Z, Liu CJ, Heth JA, Udager AM, Soellner MB, Merajver SD, Morikawa A, Merrill NM. Targeting fatty acid synthase in preclinical models of TNBC brain metastases synergizes with SN-38 and impairs invasion. NPJ Breast Cancer. 2024 Jun 10;10(1):43.
    参考文献:10.1101/2024.05.30.596684
    摘要:Ward AV, Riley D, Cosper KE, Finlay-Schultz J, Brechbuhl HM, Libby AE, Hill KB, Varshney RR, Kabos P, Rudolph MC, Sartorius CA. Lipid metabolic reprogramming drives triglyceride storage and variable sensitivity to FASN inhibition in endocrine-resistant breast cancer cells. bioRxiv. 2024 Dec 19;().
    参考文献:10.1016/j.neo.2025.101143
    摘要:Steen TV, Espinoza I, Duran C, Casadevall G, Serrano-Hervás E, Cuyàs E, Verdura S, Kemble G, Kaufmann SH, McWilliams R, Osuna S, Billadeau DD, Menendez JA, Lupu R. Fatty acid synthase (FASN) inhibition cooperates with BH3 mimetic drugs to overcome resistance to mitochondrial apoptosis in pancreatic cancer. Neoplasia. 2025 Apr;62():101143.
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