Methods for treating glioma
    4.
    发明授权
    Methods for treating glioma 失效
    治疗胶质瘤的方法

    公开(公告)号:US08748445B2

    公开(公告)日:2014-06-10

    申请号:US11791588

    申请日:2005-10-27

    摘要: The present disclosure provides for method of treatment and/or prevention of disease states that require cystine for maintenance or progression of the disease state. In addition, methods for screening and identifying novel therapeutic agents useful in the treatment of such disease states are described. In one embodiment, the disease state is a cancer, such as, but not limited to, glioma. In this embodiment, methods for the treatment and prevention of glioma by inhibiting cystine uptake or decreasing intracellular cystine concentrations are provided. The present disclosure teaches that glioma cells are dependent on system Xc for cystine uptake. Pharmacological inhibition of system Xc causes a rapid depletion of intracellular glutathione, resulting in decreased cell growth. In contrast, non-malignant astrocytes and cortical neurons remain viable in the presence of Xc inhibitors and continue to take up cystine via alternate amino acid transporters.

    摘要翻译: 本公开提供了治疗和/或预防需要胱氨酸以维持或发展疾病状态的疾病状态的方法。 此外,描述了筛选和鉴定用于治疗这种疾病状态的新型治疗剂的方法。 在一个实施方案中,疾病状态是癌症,例如但不限于神经胶质瘤。 在该实施方案中,提供了通过抑制胱氨酸摄取或减少细胞内胱氨酸浓度来治疗和预防神经胶质瘤的方法。 本公开内容教导了神经胶质瘤细胞依赖于系统Xc用于胱氨酸摄取。 系统Xc的药理学抑制导致细胞内谷胱甘肽的快速消耗,导致细胞生长减少。 相比之下,非恶性星形胶质细胞和皮层神经元在Xc抑制剂存在下保持存活,并通过替代氨基酸转运体继续摄取胱氨酸。

    Oligomeric derivatives of spirobifluorene, their preparation and use
    6.
    发明授权
    Oligomeric derivatives of spirobifluorene, their preparation and use 有权
    螺二芴的低聚衍生物,其制备和用途

    公开(公告)号:US08614357B2

    公开(公告)日:2013-12-24

    申请号:US11632337

    申请日:2005-07-15

    摘要: SBF derivatives, represented with the following formula: SBF-X wherein: with m=0, 1, 2 or 3; p=positive integer,; n=positive integer; L: is the same or different and independently represents C, PR, AsR, SbR, BiR, S, Se, Te, S═Y, Se═Y or Te═Y; Y: is the same or different and independently represents O, S, Se or Te; K: is the same or different and independently represents a chemical bond or a group selected from O, S, BR(2−p), N, NR(2−p), R(2−p)P═O, B3O3, (PR)3N3, CR(3−p), CR(3−p)(C6H4)(p+1), SiR(3−p)(C6H4)(p+1) alkyne, substituted alkyne, alkyne, substituted alkyne, aromatic or R substituted aromatic, heteroaromatic-or a combination of two, three or four of the above mentioned groups; SBF: spiro-compound of formula (I): R, A, B, C, D: is the same or different and independently represents H, deuterium, F, Cl, Br, I, CN, a linear, branched or cyclic alkyl, alkoxy or thioalkoxy chain, or a combination from two, three or four of these systems; two or more substituents R can form a further monocyclic or polycyclic aliphatic or aromatic ring system with each other.

    摘要翻译: SBF衍生物,用下式表示:SBF-X其中:m = 0,1,2或3; p =正整数 n =正整数; L:相同或不同,独立地表示C,PR,AsR,SbR,BiR,S,Se,Te,S = Y,Se = Y或Te = Y; Y:相同或不同,独立地表示O,S,Se或Te; K:相同或不同,独立地表示化学键或选自O,S,BR(2-p),N,NR(2-p),R(2-p)P = O, (PR)3N3,CR(3-p),CR(3-p)(C6H4)(p + 1),SiR(3-p)(C6H4)(p + 1)炔,取代炔,炔,取代炔 ,芳族或R取代的芳族,杂芳族或两个,三个或四个上述基团的组合; SBF:式(I)的螺 - 化合物:R,A,B,C,D:相同或不同,独立地表示H,氘,F,Cl,Br,I,CN,直链,支链或环状烷基 ,烷氧基或硫代烷氧基链,或这些系统中的两个,三个或四个的组合; 两个或更多个取代基R可以彼此形成另外的单环或多环脂族或芳环体系。

    Method for producing 3-mercaptoaniline compound
    8.
    发明授权
    Method for producing 3-mercaptoaniline compound 有权
    3-巯基苯胺化合物的制备方法

    公开(公告)号:US08334410B2

    公开(公告)日:2012-12-18

    申请号:US12743389

    申请日:2008-11-28

    申请人: Kentaro Kawazoe

    发明人: Kentaro Kawazoe

    摘要: A method for producing a 3-mercaptoaniline compound, which is a known intermediate for a 3-(1H-1,2,4-triazol-1-yl)phenylsulfide derivative, useful as a pesticide, and a method for producing a compound which can be used as a starting material in producing the 3-mercaptoaniline compound are disclosed. In one embodiment the nitro group and the chlorosulfonyl group of a 3-nitrobenzenesulfonyl chloride compound represented by general formula (1): are reduced in the presence of an acid catalyst to produce a compound of general formula (2): In the above general formulas (1) and (2), R represents an alkyl group or a cyclic alkyl group, and X represents a halogen atom.

    摘要翻译: 作为可用作农药的3-(1H-1,2,4-三唑-1-基)苯硫醚衍生物的已知中间体的3-巯基苯胺化合物的制造方法及其制造方法 可以用作生产3-巯基苯胺化合物的原料。 在一个实施方案中,通式(1)表示的3-硝基苯磺酰氯化合物的硝基和氯磺酰基在酸催化剂的存在下还原,得到通式(2)的化合物:在上述通式 (1)和(2)中,R表示烷基或环状烷基,X表示卤素原子。