Aminoacid Derivatives Containing a Disulfanyl Group in the form of Mixed Disulfanyl and Aminopeptidase N Inhibitors
    23.
    发明申请
    Aminoacid Derivatives Containing a Disulfanyl Group in the form of Mixed Disulfanyl and Aminopeptidase N Inhibitors 有权
    含二硫烷基和氨基肽酶N抑制剂形式的二硫烷基的氨基酸衍生物

    公开(公告)号:US20090131509A1

    公开(公告)日:2009-05-21

    申请号:US12084091

    申请日:2006-10-24

    CPC分类号: C07C323/60 C07D333/24

    摘要: The invention relates to novel compounds of formula (I): H2N—CH(R1)—CH2—S—S—CH2—CH(R2)—COONH—R5, wherein R1 is a hydrocarbon chain, phenyl or benzyl radical, methylene radical substituted by a 5 or 6 atom heterocycle; R2 is a phenyl or benzyl radical, a 5 or 6 atom aromatic heterocycle, methylene group substituted by a 5 or 6 atom heterocycle; R5 is a CH(R3)—COOR4 radical, wherein R3 is hydrogen, an OH or OR group, a saturated hydrocarbon group, a phenyl or benzyl radical and OR4 is hydrophile ester, or 5 or 6 membered heterocycle comprising several heteroatoms selected from a group consisting of nitrogen, sulphur and oxygen, with at least two nitrogene atoms, wherein said heterocycle is substitutable by an alkyl C1-C6, phenyl or benzyl radical. The use of the inventive compounds in the form of drugs, a pharmaceutical composition comprising said compounds, a pharmaceutically acceptable excipient, the use in conjunction of at least one type of cannabinoid derivative for potentiating the analgesic and antidepressant effect of the novel compounds of formula (I) and/or morphine or the derivatives thereof are also disclosed.

    摘要翻译: 本发明涉及新的式(I)化合物:H 2 N-CH(R 1)-CH 2 -S-CH 2 -CH(R 2)-COONH-R 5,其中R 1是烃链,苯基或苄基,被 5或6原子杂环; R2是苯基或苄基,5或6个芳族杂环,被5或6个原子杂环取代的亚甲基; R 5是CH(R 3)-COOR 4基团,其中R 3是氢,OH或OR基团,饱和烃基,苯基或苄基,OR 4是亲水酯,或包含若干个杂原子的5或6元杂环, 由氮,硫和氧组成的组,具有至少两个氮原子,其中所述杂环可被C 1 -C 6烷基,苯基或苄基取代。 药物形式的本发明化合物的使用,包含所述化合物的药物组合物,药学上可接受的赋形剂,联合至少一种类型的大麻素衍生物的用途,用于增强新型式(III)化合物的镇痛作用和抗抑郁作用 I)和/或吗啡或其衍生物也被公开。

    5-Thioxylopyranose Compounds
    24.
    发明申请
    5-Thioxylopyranose Compounds 有权
    5-噻吩基吡喃糖化合物

    公开(公告)号:US20090118325A1

    公开(公告)日:2009-05-07

    申请号:US12352382

    申请日:2009-01-12

    CPC分类号: C07H1/00 C07H17/00

    摘要: 5-thioxylose compounds, especially 5-thioxylopyranose compounds, a process for their preparation, and their use for treating and/or inhibiting thromboses, especially venous thromboses. The compounds correspond to formula I: in which the pentapyranosyl group represents a free or substituted 5-thio-β-D-xylopyranosyl group; R′, R″ and R′″ each independently represent a hydrogen atom, a C2-C6 acyl group, or two adjacent ones of them form a 1-methylethylidene bridge; X1 and X2 each represent carbon or nitrogen; Y1 and Y2 each independently represent carbon, nitrogen, sulfur or oxygen, with the proviso that if Y2 represents oxygen or sulfur, then Y1 represents carbon or nitrogen; R1, R2, R3, R4 and R5 each independently represent hydrogen, a COOR6 group where R6 represents hydrogen or a C1-C4 alkyl group optionally substituted by a phenyl ring, a halogen atom or a —COOR6 group; a C1-C4 alkoxy group; a C1-C6 acyl group; a benzoyl group or a phenyl ring; and the addition salts and/or active metabolites of such compounds.

    摘要翻译: 5-硫代羟基化合物,特别是5-羟基吡喃糖化合物,其制备方法及其用于治疗和/或抑制血栓形成,特别是静脉血栓形成的用途。 化合物对应于式I:其中五草酰基代表游离或取代的5-硫代-β-D-吡喃木糖基; R',R“和R”'各自独立地表示氢原子,C 2 -C 6酰基或其两个相邻的一个形成1-甲基亚乙基桥; X1和X2各自表示碳或氮; Y1和Y2各自独立地表示碳,氮,硫或氧,条件是如果Y2表示氧或硫,则Y1表示碳或氮; R 1,R 2,R 3,R 4和R 5各自独立地表示氢,COOR 6基团,其中R 6表示氢或任选被苯环,卤素原子或-COOR 6基团取代的C 1 -C 4烷基; C1-C4烷氧基; C1-C6酰基; 苯甲酰基或苯环; 和这些化合物的加成盐和/或活性代谢物。

    MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENT AND ORGANIC ELECTROLUMINESCENT ELEMENT EMPLOYING THE SAME
    27.
    发明申请
    MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENT AND ORGANIC ELECTROLUMINESCENT ELEMENT EMPLOYING THE SAME 有权
    有机电致发光元件和有机电致发光元件的材料

    公开(公告)号:US20090030202A1

    公开(公告)日:2009-01-29

    申请号:US11775593

    申请日:2007-07-10

    摘要: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.

    摘要翻译: 描述了用于与至少一种磷光金属络合物组合使用的主体材料的有机电致发光器件的材料,其包含具有特定杂环结构的化合物。 还描述了具有阳极,阴极和具有一层或多层的有机薄膜层的有机电致发光器件。 有机薄膜层介于阳极和阴极之间,并且具有包含与至少一种磷光金属络合物组合的主体材料的发光层。 至少一层有机薄膜层含有有机电致发光器件的材料。 有机电致发光元件用材料提供了发光效率高,产生少量像素缺陷,耐热性优异,使用寿命长的有机电致发光器件。