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    GLUTAMINASE INHIBITOR DISCOVERY AND NANOPARTICLE-ENHANCED DELIVERY FOR CANCER THERAPY
    3.
    发明申请
    GLUTAMINASE INHIBITOR DISCOVERY AND NANOPARTICLE-ENHANCED DELIVERY FOR CANCER THERAPY 有权

    公开(公告)号：US20220370371A1

    公开(公告)日：2022-11-24

    申请号：US17543450

    申请日：2021-12-06

    Applicant: The Johns Hopkins University

    Inventor： Justin Hanes ,  Barbara S. Slusher ,  Anne Le ,  Jie Fu ,  Qingguo Xu ,  Takashi Tsukamoto

    IPC: A61K9/51 ,  A61K9/00 ,  A61K31/433 ,  A61K45/06 ,  A61K31/337 ,  C07D417/12 ,  C07D417/14 ,  C07D285/135

    Abstract: Currently available glutaminase inhibitors are generally poorly soluble, metabolically unstable, and/or require high doses, which together reduce their efficacy and therapeutic index. These can be formulated into nanoparticles and delivered safely and effectively for treatment of pancreatic cancer and other glutamine addicted cancers. Studies demonstrate that nanoparticle delivery of BPTES, relative to use of BPTES alone, can be safely administered and provides dramatically improved tumor drug exposure, resulting in greater efficacy. GLS inhibitors can be administered in higher concentrations with sub-100 nm nanoparticles, since the nanoparticles package the drug into “soluble” colloidal nanoparticles, and the nanoparticles deliver higher drug exposure selectively to the tumors due to the enhanced permeability and retention (EPR) effect. These factors result in sustained drug levels above the IC50 within the tumors for days, providing significantly enhanced efficacy compared to unencapsulated drug.

    NOVEL INHIBITORS
    5.
    发明申请
    NOVEL INHIBITORS 有权

    公开(公告)号：US20220274977A1

    公开(公告)日：2022-09-01

    申请号：US17737602

    申请日：2022-05-05

    Applicant: VIVORYON THERAPEUTICS N.V.

    Inventor： Ulrich HEISER ,  Torsten HOFFMANN ,  Ingeborg LUES ,  Antje MEYER

    IPC: C07D417/12 ,  C07D235/08 ,  C07D249/14 ,  C07D277/40 ,  C07D285/135 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/04

    Abstract: The invention relates to a compound of formula (1): A-B-D-E  (1) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (1) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

    Glutaminase inhibitors
    10.
    发明授权
    Glutaminase inhibitors 有权

    公开(公告)号：US11013724B2

    公开(公告)日：2021-05-25

    申请号：US16268133

    申请日：2019-02-05

    Applicant: University of Pittsburgh—Of the Commonwealth System of Higher Education ,  Cornell University

    Inventor： Lee A. McDermott ,  Prema C. Iyer ,  Richard A. Cerione ,  William P. Katt

    IPC: C07D417/14 ,  A61K31/433 ,  C07D285/135 ,  C07D401/14 ,  C07D417/12 ,  A61K31/4535

    Abstract: A compound, or a pharmaceutically acceptable salt thereof, having a structure of: wherein A is a ring; Y1 and Y2 are each independently N or C with the proper valency; X1 and X2 are each independently —NH—, —O—, —CH2—O—, —NH—CH2—, or —N(CH3)—CH2—, provided that when at least one of X1 and X2 is —CH2—O—, —NH—CH2—, or —N(CH3)—CH2— then the —CH2— is directly connected to A; a and b are each independently 0 or 1; c and d are each independently 0 or 1; Z1 and Z2 are each independently a heterocyclic; and R1 and R2 are each independently optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, amino, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; provided that if Y1 and Y2 are each C, then a is 1 and b is 1; provided that if Y1 and Y2 are each N, then a is 0 and b is 0; provided that if Y1 is N and Y2 is C, then a=0 and b=1; provided that if Y1 is C and Y2 is N, then a=1 and b=0; provided that if c=0 and d=0, then R1 and R2 are both amino; provided that if c is 1 and d is 1, then both R1 and R2 are not amino; provided that if c is 0 and d is 1, then R′ is amino and R2 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; and provided that if c is 1 and d is 0, then R2 is amino and R1 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl.

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