Purine Derivatives as A3 and A1 Adenosine Receptor Agonists
    1.
    发明申请
    Purine Derivatives as A3 and A1 Adenosine Receptor Agonists 失效
    嘌呤衍生物作为A3和A1腺苷受体激动剂

    公开(公告)号:US20070232626A1

    公开(公告)日:2007-10-04

    申请号:US11574779

    申请日:2005-09-02

    IPC分类号: A61K31/52 C07D473/26

    CPC分类号: C07D473/00

    摘要: Disclosed are (N)-methanocarba adenine nucleosides of the formula: [Formula] as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.

    摘要翻译: 公开了具有下式的(N) - 甲烷卡巴腺嘌呤核苷:作为高效A 3 N 3腺苷受体激动剂,包含这种核苷的药物组合物,以及这些核苷的使用方法,其中R < SUB> 1 6 如说明书中所定义。 这些核苷被考虑用于治疗许多疾病,例如炎症,心脏缺血,中风,哮喘,糖尿病和心律失常。 本发明还提供了用于心脏保护的作为Aβ1 N和A 3 N 3腺苷受体的激动剂的化合物。

    Alpha-morpholino ribonucleoside derivatives and polymers thereof
    3.
    发明授权
    Alpha-morpholino ribonucleoside derivatives and polymers thereof 失效
    α-吗啉代核糖核苷衍生物及其聚合物

    公开(公告)号:US5378841A

    公开(公告)日:1995-01-03

    申请号:US74120

    申请日:1993-06-08

    摘要: Alpha-morpholino subunits and polymer compositions composed of alpha-morpholino subunits are disclosed. These subunits can be linked together by uncharged linkages, one to three atoms in length, joining the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide. The polymers of the instant invention can be used in place of standard RNA or DNA oligomers. For example, the target-specific polymers of the invention can be used in a variety of diagnostic assays for detection of RNA or DNA having a given target sequence. Further, the polymers of the invention also have potential use as therapeutic agents.

    摘要翻译: 公开了α-吗啉代亚基和由α-吗啉代亚基组成的聚合物组合物。 这些亚基可以通过不带电荷的键连接在一起,长度为1-3个原子,将一个亚基的吗啉代氮连接到相邻亚基的5'环外碳上。 每个亚基含有通过氢键与靶多核苷酸中的特定碱基或碱基对有效结合的嘌呤或嘧啶碱基配对部分。 本发明的聚合物可以用于代替标准的RNA或DNA寡聚体。 例如,本发明的靶标特异性聚合物可用于各种用于检测具有给定靶序列的RNA或DNA的诊断测定。 此外,本发明的聚合物也具有潜在的用途作为治疗剂。

    Derivatives of 9-(2-hydroxyethoxymethyl) guanine
    9.
    发明授权
    Derivatives of 9-(2-hydroxyethoxymethyl) guanine 失效
    9-(2-羟基乙氧基甲基)鸟嘌呤的衍生物

    公开(公告)号:US4548819A

    公开(公告)日:1985-10-22

    申请号:US507712

    申请日:1983-06-23

    CPC分类号: C07D473/00 Y10S514/931

    摘要: Compounds of the general formula ##STR1## (wherein X represents an oxygen or sulphur atom, R.sup.1 represents a hydroxy or amino group, R.sup.2 represents a hydrogen atom or a group of formula --CH.sub.2 OR.sup.3.sub.a and R.sup.3 and R.sup.3.sub.a which may be the same or different, each represents an amino acid acyl radical) and physiologically acceptable salts thereof are useful for the treatment of viral infections and have been found to have a surprisingly high water-solubility which renders them of value in the formulation of aqueous pharmaceutical preparations. Processes for preparing the compounds are described.

    摘要翻译: 通式(I)的化合物(其中X表示氧或硫原子,R1表示羟基或氨基,R2表示氢原子或式-CH2OR3a基团,R3和R3a可以相同) 或不同的,各自表示氨基酸酰基)及其生理上可接受的盐可用于治疗病毒感染,并且已经发现具有惊人的高水溶性,这使得它们在水性药物制剂的制剂中具有价值。 描述了制备化合物的方法。