Methodology for the synthesis of xanthones
    51.
    发明授权
    Methodology for the synthesis of xanthones 有权
    合成呫吨酮的方法

    公开(公告)号:US09163002B2

    公开(公告)日:2015-10-20

    申请号:US14049809

    申请日:2013-10-09

    申请人: Qian Wang Jun Hu

    发明人: Qian Wang Jun Hu

    IPC分类号: C07D311/86

    CPC分类号: C07D311/86

    摘要: Methods are provided for forming a xanthone derivative via reacting a 2-substituted benzaldehyde with a phenol derivative to form the xanthone derivative.

    摘要翻译: 提供了通过2-取代的苯甲醛与酚衍生物反应形成呫吨酮衍生物以形成呫吨酮衍生物的方法。

    Bicyclo[2.2.1]hept-7-ylamine derivatives and their uses
    55.
    发明授权
    Bicyclo[2.2.1]hept-7-ylamine derivatives and their uses 失效
    双环[2.2.1]庚-7-基胺衍生物及其用途

    公开(公告)号:US07994211B2

    公开(公告)日:2011-08-09

    申请号:US12063212

    申请日:2006-08-08

    摘要: Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula (I) wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5—Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R4 is a group of formula (a), (b), (c) or (d); is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.

    摘要翻译: 式(I)化合物具有毒蕈碱M3受体调节活性; 式(I)其中A是氧原子或基团-N(R12) - ; (ⅰ)R 1是C 1 -C 6 - 烷基或氢原子; 并且R 2是氢原子或基团-R 5,-Z-Y-R 5 -Z-NR 9 R 10; -Z-CO-NR9R10; -Z-NR9-CO-R5; 或-Z-CO 2 H; 并且R 3是孤对的,或者是C 1 -C 6烷基,在这种情况下,与其连接的氮原子是季氮并携带正电荷; 或(ii)R 1和R 3与它们所连接的氮一起形成杂环烷基环,并且R 2是氢原子; 或基团-R5,-Z-Y-R5,-Z-NR9R10,-Z-CO-NR9R10,-Z-NR9-CO-R5或-Z-CO2H,其中, 附着是季氮并带正电荷; 或(iii)R 1和R 2与它们所连接的氮一起形成杂环烷基环,所述环被基团-Y-R 5,-Z-Y-R 5,-Z-NR 9 R 10取代; -Z-CO-NR9R10; -Z-NR9-CO-R5; 或-Z-CO 2 H,并且R 3是孤对的,或者C 1 -C 6 - 烷基,在这种情况下,与其连接的氮原子是季氮并带正电荷; R4是式(a),(b),(c)或(d)的基团; 是C 1 -C 6烷基,芳基,芳基稠合环烷基,芳基 - 稠合 - 杂环烷基,杂芳基,芳基(C 1 -C 8 - 烷基) - ,杂芳基(C 1 -C 8 - 烷基) - ,环烷基或杂环烷基, 剩余的变量如规范中所定义。

    Lipophilic electrophoretic probes
    58.
    发明授权
    Lipophilic electrophoretic probes 失效
    亲脂性电泳探针

    公开(公告)号:US07279585B2

    公开(公告)日:2007-10-09

    申请号:US10618956

    申请日:2003-07-14

    IPC分类号: C07D311/82

    CPC分类号: A61K31/66 C07D311/86

    摘要: Compounds, compositions, and methods for labeling membranes are disclosed. Compounds of formula G-L-E are described wherein G is a lipophilic group, L is a cleavable linkage and E is an electrophoretic group. The compounds become associated with membranes, and can be cleaved with a cleavage-inducing moiety thereby releasing the detectable electrophoretic group.

    摘要翻译: 公开了用于标记膜的化合物,组合物和方法。 描述式G-L-E的化合物,其中G是亲脂基团,L是可切割键,E是电泳基团。 化合物与膜结合,并且可以用切割诱导部分切割,从而释放可检测的电泳基团。

    7,8-dihydro-xanthenone-8-carboxylic acid derivative and novel microbe producing the same
    59.
    发明授权
    7,8-dihydro-xanthenone-8-carboxylic acid derivative and novel microbe producing the same 失效
    7,8-二氢呫吨酮-8-羧酸衍生物及其生产新颖的微生物

    公开(公告)号:US06770671B2

    公开(公告)日:2004-08-03

    申请号:US10220724

    申请日:2002-09-04

    IPC分类号: A61K3135

    CPC分类号: C12R1/66 C07D311/86 C12P17/06

    摘要: Disclosed are a novel compound represented by the following chemical formula (1), useful for the prophylaxis and treatment of angiogenic diseases, its production, and a novel microorganism producing the same. Aspergillus sp. Y80118 isolated from soil was found to produce 7,8-dihydro-1,7-dihydroxy-3-hydroxymethyl-xanthenone-8-carboxylic acid methylester which inhibits VEGF-induced proliferation of HUVEC, angiogenesis in CAM assay, and tumor growth. The novel compound can be effectively used for the medical treatment of anigiogenic diseases, including cancers, rheumatoid arthritis, and diabetic retinopathy.

    摘要翻译: 公开了由以下化学式(1)表示的新型化合物,其用于预防和治疗血管生成疾病及其生产,以及生产该新化合物的新型微生物。 曲霉菌 发现从土壤中分离的Y80118产生抑制VEGF诱导的HUVEC增殖,CAM测定中的血管发生和肿瘤生长的7,8-二氢-1,7-二羟基-3-羟甲基 - 呫吨酮-8-羧酸甲酯。 该新型化合物可有效地用于治疗致病性疾病,包括癌症,类风湿性关节炎和糖尿病性视网膜病变。