Stabilized amorphous ticagrelor
    35.
    发明公开
    Stabilized amorphous ticagrelor 审中-公开
    Stabilisiertes amorphes Ticagrelor

    公开(公告)号:EP2813216A1

    公开(公告)日:2014-12-17

    申请号:EP13002963.0

    申请日:2013-06-10

    申请人: Zentiva, a.s.

    IPC分类号: A61K9/14 A61K9/16 A61K31/00

    摘要: Solid solution of ticagrelor molecularly dispersed within a polymer matrix formed by an ionic polymer in its solid state, characterized in that the ionic polymer is selected from hydroxypropyl methyl cellulose, polyvinylpyrrolidone or polyvinyl caprolactam-polyvinyl acetate-polyethyleneglycol.

    摘要翻译: 泰格列洛的固体溶液分散分散在由固体状态的离子聚合物形成的聚合物基质中,其特征在于离子聚合物选自羟丙基甲基纤维素,聚乙烯吡咯烷酮或聚乙烯基己内酰胺 - 聚乙酸乙烯酯 - 聚乙二醇。

    SALT OF OXALIC ACID WITH 5-[4-[2-(N-METHYL-N-(2-PYRIDYL)-AMINO)ETHOXY]BENZYL]THIAZOLIDIN-2,4-DIONE AND A METHOD OF ITS PREPARATION AND ITS USE
    38.
    发明授权
    SALT OF OXALIC ACID WITH 5-[4-[2-(N-METHYL-N-(2-PYRIDYL)-AMINO)ETHOXY]BENZYL]THIAZOLIDIN-2,4-DIONE AND A METHOD OF ITS PREPARATION AND ITS USE 有权
    用5- [4- [2-(N-甲基-N-(2-吡啶基)氨基)乙氧基]苄基]噻唑烷-2,4-二酮及其制备方法和使用方法制备草酸盐

    公开(公告)号:EP1771444B1

    公开(公告)日:2007-11-21

    申请号:EP05759059.8

    申请日:2005-07-20

    申请人: Zentiva, a.s.

    发明人: HALAMA, Ales

    CPC分类号: C07D417/12

    摘要: The salt of oxalic acid with 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)-ethoxy]-benzyl]-thiazolidin-2,4-dione of formula III including its tautomers and solvates. The method of preparation of the salt of oxalic acid with 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)-ethoxy]benzyl]thiazolidin-2,4-dione consists in a reaction of 5-[4-[2-(N-methyl-N-(2-pyridyl)-amino)ethoxy]benzyl]thiazolidin-2,4-dione of formula I with oxalic acid, the reaction being carried out in a solution in organic solvent or its mixture with water.

    摘要翻译: 草酸盐与式III的5- [4- [2-(N-甲基-N-(2-吡啶基)氨基] - 乙氧基] - 苄基] - 噻唑烷-2,4-二酮(包括其互变异构体和溶剂化物 。 用5- [4- [2-(N-甲基-N-(2-吡啶基)氨基] - 乙氧基]苄基]噻唑烷-2,4-二酮制备草酸盐的方法包括 式I的5- [4- [2-(N-甲基-N-(2-吡啶基) - 氨基)乙氧基]苄基]噻唑烷-2,4-二酮与草酸反应,该反应在 有机溶剂或其与水的混合物。

    pH-sensitive polymeric conjugates of an anthracycline cancerostatic drug for targeted therapy
    40.
    发明公开
    pH-sensitive polymeric conjugates of an anthracycline cancerostatic drug for targeted therapy 审中-公开
    pH敏感聚合物 - 魔芋螨蒽环类药物Kanzerostatikumsfürgezielte Therapie

    公开(公告)号:EP1782833A2

    公开(公告)日:2007-05-09

    申请号:EP06025316.8

    申请日:2002-12-20

    申请人: Zentiva, a.s.

    IPC分类号: A61K47/48

    CPC分类号: A61K47/6883 A61K47/65

    摘要: Conjugates consisting of a polymeric carrier constituted by 30 to 3,000 monomer units linked to form a polymeric chain, composed of
    a. 60 to 99 % of N -(2-hydroxypropyl)methacrylamide units
    b. 1 to 25 % of units of methacryloylated hydrazones of α-amino acids, ε-amino acids, aromatic amino acids, or oligopeptides terminated with a molecule of an anthracycline cancerostatic
    c. 0.5 to 15 % of units ofmethacryloylated α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides or their sodium salts, and optionally
    d. 0.5 to 10 % of units of methacryloylated hydrazides of α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides
    e. 0.5 to 5 % of methacryloylated α-amino acids, ε-amino acids or oligopeptides terminated by a molecule of immunoglobulin or of a specific monoclonal or polyclonal antibody,

    of the below given general formula, the individual structural units being disposed in a random manner in the chain and where x ranges from 20 to 3,000, a is from 1 to 750, b and c are each from 1 to 450, d ranges from 1 to 150, X is a residue of an amino acid or oligopeptide chosen from the following series: Gly, Ala, Leu, GlyGly, GlyLeuGly, GlyPheGly, GlyPheLeuGly, β-alanine, γ-amino butyric acid, ε-amino caproic acid (AKap), p-amino benzoic acid (AB), and S is an antibody selected from the following series: γ-globulin for i.v. administrations, autologous antibodies, antibodies anti-17-1A, anti-CA 15-3 and the like, linked to the polymeric chain by the marked structure.

    摘要翻译: 由聚合物载体组成的共轭体由30至3,000个连接形成聚合物链的单体单元构成,由a。 60-99%的N-(2-羟丙基)甲基丙烯酰胺单元b。 1-氨基酸,μ-氨基酸,芳香族氨基酸或用蒽环类抗癌药物c分子终止的寡肽的甲基丙烯酰化腙单位的1〜25%。 0.5至15%的甲基丙烯酰化±氨基酸,μ-氨基酸,芳族氨基酸或寡肽或其钠盐的单元,以及任选的d。 ±10-氨基酸,μ-氨基酸,芳香族氨基酸或寡肽的甲基丙烯酰化酰肼单位为0.5〜10% 0.5至5%的由下列给定通式的免疫球蛋白或特异性单克隆或多克隆抗体分子封端的甲基丙烯酰化的± - 氨基酸,μ-氨基酸或寡肽,各个结构单元以随机方式置于 链,其中x为20至3,000,a为1至750,b和c各自为1至450,d的范围为1至150,X为选自以下系列的氨基酸或寡肽的残基 :Gly,Ala,Leu,GlyGly,GlyLeuGly,GlyPheGly,GlyPheLeuGly,2-丙氨酸,3-氨基丁酸,μ-氨基己酸(AKap),对氨基苯甲酸(AB),S是选自 以下系列:³-球蛋白iv 给药,自体抗体,抗-17-1A抗体,抗CA15-3等抗体,通过标记结构与聚合物链连接。