HISTONE DEMETHYLASE 5 INHIBITORS AND USES THEREOF

    公开(公告)号:WO2020033377A1

    公开(公告)日:2020-02-13

    申请号:PCT/US2019/045259

    申请日:2019-08-06

    Abstract: Provided herein are compounds of Formulae (I) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds or compositions disclosed herein for treating and/or preventing proliferative diseases, cancers, carcinoma lung cancer, breast cancer, liver cancer, pancreatic cancer, gastric cancer, ovarian cancer, colon cancer, colorectal cancer, leukemia, sarcoma and/or cardiovascular diseases in a subject in need thereof. In certain embodiments, the sarcoma is Ewing's sarcoma. Provided are methods of inhibiting a histone demethylase in a subject and/or in a cell, tissue, or biological sample. In certain embodiments, the histone demethylase is a KDM. In certain embodiments, the KDM is KDM5. In certain embodiments, the biological sample is a cell. In certain embodiments, the biological sample is a tissue.

    METHOD FOR NOX REDUCTION
    4.
    发明申请
    METHOD FOR NOX REDUCTION 审中-公开
    减少NOX的方法

    公开(公告)号:WO2004020808A1

    公开(公告)日:2004-03-11

    申请号:PCT/US2003/027365

    申请日:2003-08-28

    Abstract: A method for reducing NO x in a gas stream by sequentially exposing the gas stream to a first and a second catalyst. The first catalyst converts at least a portion of the gas stream to a reducing gas, it reduces at least a portion of the NO x in a first temperature range, and it absorbs at least a portion of the NO x in the temperature range. The second catalyst reduces at least a portion of the NO x in a second temperature range utilizing the reducing gas produced by the second catalyst. The reducing gas produced by the first catalyst is typically a partially oxidized hydrocarbon, preferably an aldehyde, and more preferably acetaldehyde or formaldehyde. In addition to the first and second catalysts, the gas stream may be exposed to a plasma. Preferably, the first catalyst is selected as a zeolite, and more preferably a zeolite impregnated with a cation. The cation is preferably selected from the group consisting of an alkaline cation, an alkaline earth cation, and combinations thereof and preferably exhibits pores sizes of greater than 4 angstroms, and more preferably exhibits pores sizes of greater than 7 angstroms. The second catalyst is preferably γ-alumina catalyst, and more preferably a γ-alumina catalyst impregnated with transition metals, including, but not limited to, Ag, In and Sn.

    Abstract translation: 一种通过将气流顺序地暴露于第一和第二催化剂来还原气流中的NOx的方法。 第一催化剂将至少一部分气流转化为还原气体,其在第一温度范围内减少NOx的至少一部分,并且其在该温度范围内吸收至少一部分NOx。 第二催化剂利用由第二催化剂产生的还原气体在第二温度范围内还原NOx的至少一部分。 由第一催化剂产生的还原气体通常是部分氧化的烃,优选醛,更优选乙醛或甲醛。 除了第一和第二催化剂之外,气流可以暴露于等离子体。 优选地,选择第一催化剂作为沸石,更优选选择用阳离子浸渍的沸石。 阳离子优选选自碱性阳离子,碱土金属阳离子及其组合,并且优选显示大于4埃的孔径,更优选地具有大于7埃的孔径。 第二催化剂优选是γ-氧化铝催化剂,更优选浸渍有过渡金属的γ-氧化铝催化剂,包括但不限于Ag,In和Sn。

    METHOD FOR TESTING ACTIVE COMPOUNDS
    6.
    发明申请
    METHOD FOR TESTING ACTIVE COMPOUNDS 审中-公开
    测试活性化合物的方法

    公开(公告)号:WO2008028500A1

    公开(公告)日:2008-03-13

    申请号:PCT/EP2006/008645

    申请日:2006-09-05

    Abstract: In one aspect the invention relates to a method for testing a chemical entity for its capability to modulate a (poly)peptide that is malfunctioning by means of an interaction of said chemical entity and said (poly)peptide, the method using single- molecule force spectroscopy. In another aspect the invention relates to a method for testing a chemical or physical entity for its capability to interact with a G protein-coupled receptor (GPCR) in its natural membrane environment, the method using single-molecule force spectroscopy.

    Abstract translation: 一方面,本发明涉及一种用于测试化学实体的能力,以通过所述化学实体和所述(多)肽的相互作用来调节(多)肽失活的能力的方法,该方法使用单分子力 光谱。 在另一方面,本发明涉及一种用于测试化学或物理实体在其天然膜环境中与G蛋白偶联受体(GPCR)相互作用的能力的方法,该方法使用单分子力谱。

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