DOUBLE-STRANDED LIPID-MODIFIED RNA HAVING HIGH RNA INTERFERENCE EFFECT
    101.
    发明公开
    DOUBLE-STRANDED LIPID-MODIFIED RNA HAVING HIGH RNA INTERFERENCE EFFECT 有权
    DOPPELSTRÄNGIGE脂质变性RNA麻醉HOHEM RNA-INTERFERENZEFFEKT

    公开(公告)号:EP2264167A1

    公开(公告)日:2010-12-22

    申请号:EP09729165.2

    申请日:2009-03-31

    摘要: An object of the present invention is to provide a novel double-stranded RNA that has high resistance to nuclease and cellular uptake efficiency and that can produce an excellent RNA interference effect. The present invention provides a double-stranded lipid-modified RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence in a target gene, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of suppressing the expression of the target gene, and the sense strand having a double-stranded lipid bound directly or via a linker to at least one of the first to sixth nucleotides from the 5' end.

    摘要翻译: 本发明的目的是提供对核酸酶和细胞摄取效率具有高抗性并且可以产生优异的RNA干扰效果的新型双链RNA。 本发明提供了包含具有与靶基因中的靶序列互补的核苷酸序列的有义链和具有与有义链互补的核苷酸序列的反义链的双链脂质修饰的RNA,所述双链RNA为 能够抑制靶基因的表达,并且具有直链或经由连接体结合至5'末端的至少一个第一至第六个核苷酸的双链脂质的有义链。

    Amine salt of carbostyril derivative
    104.
    发明公开
    Amine salt of carbostyril derivative 有权
    喹诺酮衍生物的胺盐

    公开(公告)号:EP2253619A1

    公开(公告)日:2010-11-24

    申请号:EP10174397.9

    申请日:2005-01-20

    IPC分类号: C07D215/227

    CPC分类号: C07D215/227

    摘要: The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects.

    摘要翻译: 本发明提供由式(1)代表的喹诺酮衍生物形成的喹诺酮衍生物的胺盐[其中R是卤素原子; 侧链的取代位置是喹诺酮骨架中的3-或4-位; 并且喹诺酮骨架的3-和4-位之间的键是单键或双键]和胺; 并且由于优异的水溶性和优异的药理作用,本发明作为用于治疗各种疾病的药物是有用的,特别是作为含水制剂。

    Tetomilast polymorphs
    108.
    发明公开
    Tetomilast polymorphs 有权
    替莫司特多晶型

    公开(公告)号:EP2206711A2

    公开(公告)日:2010-07-14

    申请号:EP10160007.0

    申请日:2007-03-15

    CPC分类号: A61K31/4436 C07D417/04

    摘要: The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a powder X-ray diffraction spectrum having characteristic peaks at 2θ = 10.6°, 12.9°, 21.1°, 22.3° and 25.0°; (2) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum having characteristic peaks at 2θ = 4.2°, 8.2°, 12.0°, 16.4°, 24.7° and 25.9°; (3) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum having characteristic peaks at 2θ = 3.6°, 7.1°, 10.6°, 14.2° and 24.8°. These crystals are stable towards heat and moisture, and are also excellent in terms of the disintegration property and dissolution property of tablets. Accordingly, these crystals are preferably used as pharmaceutical compositions.

    摘要翻译: 本发明提供工业上易于大量生产的替托司特晶体。 (1)具有在2θ= 10.6°,12.9°,21.1°,22.3°和25.0°具有特征峰的粉末X射线衍射光谱的替托司他水合物晶体; (2)具有在2θ= 4.2°,8.2°,12.0°,16.4°,24.7°和25.9°处具有特征峰的粉末X射线衍射光谱的无水替托司特C型晶体; (3)具有在2θ= 3.6°,7.1°,10.6°,14.2°和24.8°处具有特征峰的粉末X射线衍射光谱的替托司特乙腈溶剂合物晶体。 这些晶体对于热和水分是稳定的,并且在片剂的崩解性和溶解性方面也是优异的。 因此,这些晶体优选用作药物组合物。

    METERED DOSE INHALER
    109.
    发明公开
    METERED DOSE INHALER 审中-公开
    定量吸入器

    公开(公告)号:EP2196234A1

    公开(公告)日:2010-06-16

    申请号:EP08834311.6

    申请日:2008-09-26

    IPC分类号: A61M15/00

    摘要: The present invention provides an improved metered dose inhaler utilizing the property of the aerosol canister. The metered dose inhaler includes: a housing body (2); an aerosol canister (3) including a canister body (3a), a valve stem (3b), and a spring urging the valve stem, wherein the valve stem (3b) is held at a fixed position inside the housing body (2), and wherein the canister body (3a) is supported inside the housing body (2) to be depressible against a spring force of the spring; a dose counter (10) including display members (12) and (13) rotatably supported inside the housing body (2), and a control lever (14) swingably supported inside the housing body (2) to rotate the display member (13); and a control cap (20) including a junction member rotatably joined to the control lever (14), and a cap portion (20b) which sheaths the canister body (3a) from a bottom side of the canister body (3a), wherein the control cap (20) causes the control lever (14) to swing.