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    • 2. 发明授权
    • Fungicidally active compounds
    • 杀真菌活性化合物
    • US5672492A
    • 1997-09-30
    • US427015
    • 1995-04-24
    • Ruby Illum NielsenFrank Winther Rasmussen
    • Ruby Illum NielsenFrank Winther Rasmussen
    • A01N43/16A61K31/352C07D311/86C12P17/16C12P17/06C12N1/14
    • A01N43/16A61K31/352C07D311/86C12P17/162C12R1/645Y10S435/911
    • Novel compounds of formula I ##STR1## wherein R.sup.1 is independently hydrogen, hydroxy, alkyl with 1 to 6 carbon atoms, acyloxy groups with 1 to 6 carbon atoms, alkyloxy with 1 to 6 carbon atoms or from 1 to 5 sugar moieties; and R.sup.2 is independently hydrogen, or alkyl with 1 to 6 carbon atoms. The compounds are producible by aerobic cultivation on suitable nutrient media under suitable conditions of a strain of the fungus Ascochyta sp., subsequent recovery of the active component from the fermentation medium, and optionally modifying the active compound to obtain a compound of the desired formula I. Disclosed is also microorganisms capable of producing said compounds, compositions containing said compounds, and the use of such compositions for controlling fungi in valuable crops, animals, including birds and mammals, and in the preservation of wood, paints and edible products.
    • 式I的新型化合物其中R 1独立地是氢,羟基,具有1至6个碳原子的烷基,具有1至6个碳原子的酰氧基,1至6个碳原子的烷氧基或1至5个糖部分 ; 并且R 2独立地是氢或具有1至6个碳原子的烷基。 这些化合物可以通过在合适的营养培养基上在真菌Ascochyta sp。菌株的合适条件下进行需氧培养来生产,随后从发酵培养基中回收活性成分,并任选地改性活性化合物以获得所需式I化合物 还公开了能够产生所述化合物的微生物,含有所述化合物的组合物,以及这些组合物用于控制有价值作物,动物,包括鸟类和哺乳动物中的真菌以及保护木材,油漆和可食用产品的用途。
    • 5. 发明授权
    • Potent LNA oligonucleotides for the inhibition of HIF-1a expression
    • 用于抑制HIF-1a表达的强大的LNA寡核苷酸
    • US07939507B2
    • 2011-05-10
    • US12477261
    • 2009-06-03
    • Majken WestergaardCharlotte Albaek ThrueFrank Winther RasmussenHenrik Frydenlund Hansen
    • Majken WestergaardCharlotte Albaek ThrueFrank Winther RasmussenHenrik Frydenlund Hansen
    • A01N43/04C12Q1/68C12N15/63C07H21/02C07H21/04
    • C12N15/113C12N2310/11C12N2310/315C12N2310/3231C12N2310/3341C12N2310/341C12N2310/345C12N2310/346
    • The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-(Tx)GxGxcsasasgscsastscscsTxGxT-3′ and 5′-(Gx)TxTxascstsgscscststscsTxTxA-3′, wherein capital letters designate a beta-D-oxy-LNA nucleotide analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighbouring nucleotides/LNA nucleotide analogues, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighbouring nucleotides/LNA nucleotide analogues, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.
    • 本公开内容涉及由选自5' - (Tx)GxGxcsasasgscsastscscsTxGxT-3'和5' - (Gx)TxTxascstsgscscststscscTTTXA-3'的序列组成的LNA寡核苷酸,其中大写字母表示β-D-氧基 -LNA核苷酸类似物,小写字母表示2-脱氧核苷酸,下划线表示β-D-氧-LNA核苷酸类似物或2-脱氧核苷酸,下标“s”表示相邻核苷酸/ LNA核苷酸类似物之间的硫代磷酸酯连接,下标 “x”表示相邻核苷酸/ LNA核苷酸类似物之间的硫代磷酸酯连接或磷酸二酯连接,并且其中该序列任选地延伸多达五个2-脱氧核苷酸单元。 LNA寡核苷酸可用于调节缺氧诱导因子-1a(HIF-1a)的表达,例如, 在治疗癌症疾病,抑制血管发生,诱导细胞凋亡,预防细胞增殖或治疗血管生成疾病,例如, 糖尿病性视网膜病变,黄斑变性(ARMD),牛皮癣,类风湿性关节炎等炎症性疾病。
    • 10. 发明授权
    • Potent LNA oligonucleotides for the inhibition of HIF-1A expression
    • 用于抑制HIF-1A表达的强效LNA寡核苷酸
    • US08410071B2
    • 2013-04-02
    • US13079525
    • 2011-04-04
    • Majken WestergaardCharlotte Albaek ThrueFrank Winther RasmussenHenrik Frydenlund Hansen
    • Majken WestergaardCharlotte Albaek ThrueFrank Winther RasmussenHenrik Frydenlund Hansen
    • C12Q1/68C12P19/34C12N15/63A01N43/04C07H21/04
    • C12N15/113C12N2310/11C12N2310/315C12N2310/3231C12N2310/3341C12N2310/341C12N2310/345C12N2310/346
    • The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-(Tx)GxGxcsasasgscsastscscsTxGxT-3′ and 5′-(Gx)TxTxascstsgscscststscsTxTxA-3′, wherein capital letters designate a beta-D-oxy-LNA nucleotide analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighboring nucleotides/LNA nucleotide analogues, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighboring nucleotides/LNA nucleotide analogues, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.
    • 本公开内容涉及由选自5' - (Tx)GxGxcsasasgscsastscscsTxGxT-3'和5' - (Gx)TxTxascstsgscscststscscTTTXA-3'的序列组成的LNA寡核苷酸,其中大写字母表示β-D-氧基 -LNA核苷酸类似物,小写字母表示2-脱氧核苷酸,下划线表示β-D-氧-LNA核苷酸类似物或2-脱氧核苷酸,下标s表示相邻核苷酸/ LNA核苷酸类似物之间的硫代磷酸酯连接,下标x表示 在相邻核苷酸/ LNA核苷酸类似物之间是硫代磷酸酯连接或磷酸二酯连接,并且其中所述序列任选地延伸多达五个2-脱氧核苷酸单元。 LNA寡核苷酸可用于调节缺氧诱导因子-1a(HIF-1a)的表达,例如, 在治疗癌症疾病,抑制血管发生,诱导细胞凋亡,预防细胞增殖或治疗血管生成疾病,例如, 糖尿病性视网膜病变,黄斑变性(ARMD),牛皮癣,类风湿性关节炎等炎症性疾病。