MRNA CAP ANALOGS
    22.
    发明公开

    公开(公告)号:EP2297175A2

    公开(公告)日:2011-03-23

    申请号:EP09759412.1

    申请日:2009-06-04

    IPC分类号: C07H21/00 C07H21/02

    摘要: Dinucleotide cap analogs are disclosed, modified at different phosphate positions with a boranophosphate group or a phosphoroselenoate group. The analogs are useful as reagents in the preparation of capped mRNAs and have increased stability both
    in vitro and
    in vivo . They may be used as inhibitors of cap-dependent translation. Optionally, the boranophosphate or phosphoroselenoate group has a 2'-O or 3'-O-alkyl group, preferably a methyl group, producing analogs called BH
    3 -ARCAs or Se-ARCAs. ARCAs may be modified with α-, β-, or γ-boranophosphate or phosphoroselenoate groups.

    摘要翻译: 公开了二核苷酸帽类似物,其在不同的磷酸位置用硼烷磷酸酯基团或磷酸硒代酸酯基团进行修饰。 该类似物可用作制备加帽mRNA的试剂,并且在体外和体内都具有增加的稳定性。 它们可以用作帽依赖性翻译的抑制剂。 任选地,硼烷磷酸酯或磷酸硒化酯基团具有2'-O或3'-O-烷基,优选甲基,产生称为BH 3 -ARA或Se-ARCA的类似物。 可以用α-,β-或γ-硼烷磷酸酯或磷酸硒酸酯基团修饰ARCAs。

    USE OF NITRITE SALTS IN CHRONIC ISCHEMIA
    23.
    发明公开
    USE OF NITRITE SALTS IN CHRONIC ISCHEMIA 审中-公开
    VERWENDUNG VON NITRITSALZEN BEI CHRONISCHERISCHÄMIE

    公开(公告)号:EP2219657A2

    公开(公告)日:2010-08-25

    申请号:EP08849380.4

    申请日:2008-11-17

    IPC分类号: A61K33/14 A61K33/06 A61P7/06

    CPC分类号: A61K33/06 A61K33/00 A61K45/06

    摘要: Methods of treating a subject who has chronic tissue ischemia are disclosed. The methods can include administering to the subject a pharmaceutical composition comprising inorganic nitrite or a pharmaceutically acceptable salt thereof, for a time and in an amount sufficient to result in blood vessel growth in the ischemic tissue. The subject can be diagnosed as having a medical condition that results in persistent or recurring restriction of blood supply to a tissue, for example, peripheral artery disease, diabetes, atherosclerotic cardiovascular disease or defective wound healing. The methods can include the step of identifying a suitable subject.

    摘要翻译: 公开了治疗患有慢性组织缺血的受试者的方法。 所述方法可以包括向受试者施用包含无机亚硝酸盐或其药学上可接受的盐的药物组合物,其时间和量足以导致缺血组织中的血管生长。 该受试者可以被诊断为具有导致对组织的血液供应的持续或重复限制的医学病症,例如外周动脉疾病,糖尿病,动脉粥样硬化心血管疾病或有缺陷的伤口愈合。 所述方法可以包括鉴定合适的受试者的步骤。

    A NOVEL PEPTIDE INVOLVED IN ENERGY HOMEOSTASIS
    25.
    发明公开
    A NOVEL PEPTIDE INVOLVED IN ENERGY HOMEOSTASIS 审中-公开
    新的有关能量平衡肽

    公开(公告)号:EP1928487A2

    公开(公告)日:2008-06-11

    申请号:EP06800865.5

    申请日:2006-08-07

    IPC分类号: A61K38/17 C07K14/705

    摘要: The expression of a mRNA encoding a putative 76 amino acid, secreted protein ('Swirl') was found to negatively correlate with fasting triglyceride and cholesterol levels. A recombinant adenovirus was used to increase the expression of Swirl mRNA in two mouse models of obesity, KK-Ay and Lepob/Lepob mice. Over-expression of Swirl by adenovirus injection significantly, and reproducibly, reduced fasting triglyceride and cholesterol levels in both models. In addition, transgenic mice strains were made that over express Swirl protein. The expression of a key gene involved in lipogenesis (fatty acid synthase) and FAS protein levels were reduced by SWIRl adenoviral treatment in Lepob/Lepob mice. Full-length SWIRl peptide, or peptide derivatives, homologues, analogues, or mimetics thereof, delivered by oral intake, injection, subcutaneous patch, or intranasal routes, could be used as therapeutic or diagnostic agents for hypercholesterolemia, hypertriglyceridemia, insulin resistance, obesity, diabetes, and/or energy imbalance.

    MODULATION OF PERIPHERAL CLOCKS IN ADIPOSE TISSUE
    26.
    发明公开
    MODULATION OF PERIPHERAL CLOCKS IN ADIPOSE TISSUE 审中-公开
    外设周期对肥胖织物调制

    公开(公告)号:EP1888102A2

    公开(公告)日:2008-02-20

    申请号:EP06784696.4

    申请日:2006-06-09

    IPC分类号: A61K38/17

    摘要: Genes encoding the transcription factors controlling the core circadian oscillator (BMAL, Clock, NPAS, Per) and their regulatory targets (Rev-erba, Rev-erb) have been found in adipose tissue. The circadian pattern of these genes was entrained using restricted feeding. The circadian gene expression profiles were examined in mice and in undifferentiated and adipocyte-differentiated human adipose stem cells following exposure to nuclear hormone receptor ligands (dexamethasone or thiazolidinedione) or 30% fetal bovine serum. All three agents induced the initiation of a cyclic expression profile in representative circadian genes in the human adipose stem cells. The circadian genes studied displayed an oscillatory expression profile, characterized by both a zenith and nadir within a 24-28 hr phase. The circadian gene pattern has been lengthened with use of an inhibitor of glycogen synthase kinase 3 beta. Modulation of the circadian pattern to lengthen or shorten can be used to affect weight gain or loss, respectively.