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    METHODS OF TREATMENT USING MODULATORS OF SIRT2
    2.
    发明申请
    METHODS OF TREATMENT USING MODULATORS OF SIRT2 有权
    使用SIRT2调节剂治疗的方法

    公开(公告)号：US20160279091A1

    公开(公告)日：2016-09-29

    申请号：US15172756

    申请日：2016-06-03

    Applicant: CORNELL UNIVERSITY

    Inventor： Hening Lin ,  Bin HE

    IPC: A61K31/27

    CPC classification number: A61K31/27 ,  A61K31/16 ,  C07C327/42

    Abstract: The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method.

    Abstract translation: 本申请描述了使用本文提供的根据式（1）和（2）的结构调节（特别是抑制）Sirt2的新型化合物。 本发明还涉及其药物组合物，通过施用调节化合物的治疗方法（即癌症和神经变性疾病），用于发现Sirt2调节剂的测定方法和用于实施测定方法的试剂盒。

    Methods of treatment using modulators of SIRT2
    6.
    发明授权
    Methods of treatment using modulators of SIRT2 有权
    使用SIRT2调节剂治疗的方法

    公开(公告)号：US09359293B2

    公开(公告)日：2016-06-07

    申请号：US14349140

    申请日：2012-10-05

    Applicant: CORNELL UNIVERSITY

    Inventor： Hening Lin ,  Bin He

    IPC: C07C327/42 ,  A61K31/16

    CPC classification number: A61K31/27 ,  A61K31/16 ,  C07C327/42

    Abstract: The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2 , with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2 , and kits for practicing the assay method.

    Abstract translation: 本申请描述了使用本文提供的根据式（1）和（2）的结构调节（特别是抑制）Sirt2的新型化合物。 本发明还涉及其药物组合物，通过施用调节化合物的治疗方法（即癌症和神经变性疾病），用于发现Sirt2调节剂的测定方法和用于实施测定方法的试剂盒。

    APT1 and APT2 Inhibitors and Uses Thereof
    7.
    发明申请
    APT1 and APT2 Inhibitors and Uses Thereof 有权

    公开(公告)号：US20250092067A1

    公开(公告)日：2025-03-20

    申请号：US18562243

    申请日：2022-05-19

    Applicant: Cornell University

    Inventor： Hening Lin ,  Kevin Wielenberg ,  Min Yang

    IPC: C07F5/02 ,  A61K31/496 ,  A61K31/675 ,  A61K31/69 ,  C07D409/06 ,  C07D495/04 ,  C07F9/6509 ,  C07F9/6558

    Abstract: Compounds, compositions including one or more of the compound(s), and methods of using the compounds and the compositions. The compounds comprise an (I) group. In various examples, a compound is an Acyl Protein Thioesterase 1 inhibitor (APT1 inhibitor) and/or an Acyl Protein Thioesterase 2 inhibitor (APT2 inhibitor). Compound(s) or composition(s), which may be pharmaceutical composition(s), can be used in methods of treating diseases or disorders, such as, for example, autoimmune disorders, neurodegenerative disorders, inflammatory disorders, and immune-mediated cancer diseases.

    HIGH-THROUGHPUT ENZYME ASSAY FOR SCREENING ACTIVITY OF ACYLTRANSFERASES
    8.
    发明申请
    HIGH-THROUGHPUT ENZYME ASSAY FOR SCREENING ACTIVITY OF ACYLTRANSFERASES 有权

    公开(公告)号：US20220403443A1

    公开(公告)日：2022-12-22

    申请号：US17840140

    申请日：2022-06-14

    Applicant: CORNELL UNIVERSITY

    Inventor： Hening Lin ,  Maurine E. Linder ,  Jun Young Hong

    IPC: C12Q1/48

    Abstract: A method for determining activity of an acyl transferase enzyme, the method comprising: (i) preparing a reaction mixture comprising: (a) an acyl transferase enzyme, (b) a peptide substrate bound to a fluorophore, wherein the substrate is a cysteine-containing oligopeptide of 5-25 amino acids in length, (c) an acyl-CoA, and (d) a detergent comprising micelles, wherein the acyl transferase enzyme mediates acylation on a cysteine of said peptide substrate to result in association of the peptide with micelles of the detergent with resultant increase in fluorescence polarization; and (ii) measuring fluorescent signal of the reaction mixture; wherein an increase in fluorescence polarization of the reaction mixture compared to fluorescence polarization of a control reaction indicates acyl transferase activity of the acyl transferase enzyme. The above assay method may also be used for screening compounds for their ability to act as inhibitors of an acyl transferase enzyme.

    Thiourea compounds and their use as inhibitors of Sirt2 or Sirt5
    9.
    发明授权
    Thiourea compounds and their use as inhibitors of Sirt2 or Sirt5 有权

    公开(公告)号：US10556878B2

    公开(公告)日：2020-02-11

    申请号：US14896057

    申请日：2014-06-06

    Applicant: CORNELL UNIVERSITY

    Inventor： Hening Lin

    IPC: C07D335/06 ,  C07C335/08

    Abstract: A compound useful as a Sirt2 or Sirt5 inhibitor having the formula (1) wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —O—, —S—, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is —(CH2)n—; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, biological groups, and protecting groups. Also described are pharmaceutical compositions of the inhibiting compounds, and methods of treatment by administration of the inhibiting compounds.

    Methods of treatment using modulators of SIRT2
    10.
    发明授权
    Methods of treatment using modulators of SIRT2 有权
    使用SIRT2调节剂治疗的方法

    公开(公告)号：US09572789B2

    公开(公告)日：2017-02-21

    申请号：US15172756

    申请日：2016-06-03

    Applicant: CORNELL UNIVERSITY

    Inventor： Hening Lin ,  Bin He

    IPC: A61K31/27

    CPC classification number: A61K31/27 ,  A61K31/16 ,  C07C327/42

    Abstract: The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method.

    Abstract translation: 本申请描述了使用本文提供的根据式（1）和（2）的结构调节（特别是抑制）Sirt2的新型化合物。 本发明还涉及其药物组合物，通过施用调节化合物的治疗方法（即癌症和神经变性疾病），用于发现Sirt2调节剂的测定方法和用于实施测定方法的试剂盒。

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