METHOD OF SCREENING COMPOUND SAFE TO GASTRIC MUCOSA
    1.
    发明公开
    METHOD OF SCREENING COMPOUND SAFE TO GASTRIC MUCOSA 审中-公开
    筛选方法,安全连接胃黏膜

    公开(公告)号:EP1710574A4

    公开(公告)日:2008-09-17

    申请号:EP04807081

    申请日:2004-12-15

    摘要: A screening method for selecting a compound being safe to gastric mucosa and having less side effect of gastrointestinal tract lesion or a salt thereof, especially a nonsteroidal antiinflammatory compound or a salt thereof. There is provided a method of screening a compound safe to gastric mucosa, especially a nonsteroidal antiinflammatory compound, characterized in that using a liposome having a fluorescent dye, especially calcein, sealed therein and having a cell membrane model constituted of a phospholipid, such as phosphatidylcholine, phosphatidylglycerol, phosphatidylserine or phosphatidylinositol, the liposome is reacted with a test compound and thereafter the degree of leakage of fluorescent dye from the liposome is estimated.

    OPTICALLY ACTIVE FORM OF MEPENZOLATE, AND AMELIORATING AGENT FOR CHRONIC OBSTRUCTIVE PULMONARY DISEASE WHICH CONTAINS SAME AS ACTIVE INGREDIENT
    4.
    发明公开
    OPTICALLY ACTIVE FORM OF MEPENZOLATE, AND AMELIORATING AGENT FOR CHRONIC OBSTRUCTIVE PULMONARY DISEASE WHICH CONTAINS SAME AS ACTIVE INGREDIENT 审中-公开
    OPTISCH AKTIVE FORM VON MEPENZOLAT UND LINDERUNGSMITTELFÜRCHRONISCH-OBSTRUKTIVE LUNGENERKRANKUNG DAMIT ALS WIRKSTOFF

    公开(公告)号:EP3109232A4

    公开(公告)日:2017-06-28

    申请号:EP14882606

    申请日:2014-06-16

    发明人: MIZUSHIMA TORU

    CPC分类号: C07D211/42 A61K31/452

    摘要: An optically active form of mepenzolate bromide is provided. An agent for ameliorating chronic obstructive pulmonary disease that contains the optically active form as an active ingredient and is based on a bronchodilator effect and an anti-inflammatory effect is also provided. (3R)- or (3S)-3-[(hydroxy)(diphenyl)acetoxy]-1,1-dimethylpiperidinium bromide (hereinafter referred to as "(R)- or (S)-mepenzolate bromide") is provided. An agent for ameliorating chronic obstructive pulmonary disease that contains the (R)- or (S)-mepenzolate bromide as an active ingredient is provided. Furthermore, an agent for ameliorating chronic obstructive pulmonary disease whose mode of administration is airway administration or inhalation administration is provided.

    摘要翻译: 提供了一种光学活性形式的甲苯溴化物。 还提供了一种用于改善慢性阻塞性肺病的药剂,其含有光学活性形式作为活性成分并基于支气管扩张作用和抗炎作用。 (3R) - 或(3S)-3 - [(羟基)(二苯基)乙酰氧基] -1,1-二甲基哌啶鎓溴化物(以下称为“(R) - 或(S) 本发明提供了含有(R) - 或(S) - 溴苯佐辛溴化物作为活性成分的缓解慢性阻塞性肺病的药剂。 此外,提供了一种改善慢性阻塞性肺病的药物,其给药方式为气道给药或吸入给药。

    NANOPARTICLE CONTAINING PROSTAGLANDIN I2 DERIVATIVE
    5.
    发明公开
    NANOPARTICLE CONTAINING PROSTAGLANDIN I2 DERIVATIVE 有权
    NANOPARTIKELHALTIGES PROSTAGLANDIN-I2-DERIVAT

    公开(公告)号:EP2679227A4

    公开(公告)日:2016-06-08

    申请号:EP12746685

    申请日:2012-02-13

    摘要: There is provided a beraprost sodium-containing nanoparticle that contains beraprost sodium among other prostaglandin I 2 (prostacyclin) derivatives, which are therapeutic agents for pulmonary hypertension. The beraprost sodium-containing nanoparticle is obtained by making beraprost sodium hydrophobic using a metal ion and allowing the hydrophobic beraprost sodium to react with poly-L-lactic acid or a poly(L-lactic acid/glycolic acid) copolymer, and a poly-DL- or L-lactic acid-polyethylene glycol block copolymer or a poly(DL- or L-lactic acid/glycolic acid)-polyethylene glycol block copolymer. The beraprost sodium-containing nanoparticle excels in sustained release of an active ingredient, reduces a side effect, and furthermore, has an excellent drug retention in the blood. Therefore, the beraprost sodium-containing nanoparticle is quite outstanding particularly regarding the sustainability of the medicinal effect.

    Ameliorating agent for chronic obstructive pulmonary disease
    6.
    发明公开
    Ameliorating agent for chronic obstructive pulmonary disease 有权
    LINDERUNGSMITTELFÜRCHRONISCH-OBSTRUKTIVE LUNGENERKRANKUNG

    公开(公告)号:EP2407176A4

    公开(公告)日:2012-11-28

    申请号:EP10750713

    申请日:2010-03-02

    发明人: MIZUSHIMA TORU

    摘要: An ameliorating agent for chronic obstructive pulmonary disease (COPD) containing as an active ingredient a lecithinized superoxide dismutase represented by the following general formula (I): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒSOD'(Q-B) m €ƒ€ƒ€ƒ€ƒ€ƒ(I) (in the formula SOD' represents a residue of the superoxide dismutase; Q represents a chemical crosslinking; B represents a residue without a hydrogen atom of a hydroxyl group of lysolecithin having the hydroxyl group at the 2-position of glycerol; m is the average number of bonds of lysolecithin to one molecule of superoxide dismutase and represents an integer of 1 or more). The ameliorating agent for COPD is intravenously administered or inhalation-administrated.

    摘要翻译: 一种慢性阻塞性肺疾病(COPD)改善剂,其含有以下述通式(I)表示的卵磷脂化超氧化物歧化酶作为有效成分:SOD(QB) (I)(式中,SOD'表示超氧化物歧化酶的残基; Q表示化学交联; B表示没有溶血卵磷脂的羟基的氢原子的残基,其具有 羟基在甘油的2位; m是溶血卵磷脂对1分子超氧化物歧化酶的平均键数,表示1以上的整数。 COPD改善剂静脉给药或吸入给药。

    AMELIORATING AGENT FOR CHRONIC OBSTRUCTIVE PULMONARY DISEASE
    8.
    发明公开
    AMELIORATING AGENT FOR CHRONIC OBSTRUCTIVE PULMONARY DISEASE 审中-公开
    治疗慢性阻塞性肺疾病的药物

    公开(公告)号:EP2826479A4

    公开(公告)日:2015-11-11

    申请号:EP13761185

    申请日:2013-02-28

    IPC分类号: A61K31/452 A61K9/72 A61P11/00

    摘要: This invention provides a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect. The agent for ameliorating chronic obstructive pulmonary disease contains mepenzolate bromide as an active ingredient. More preferably the mode of administration of the agent for ameliorating chronic obstructive pulmonary disease is airway administration or inhalation administration, and furthermore the mode of administration thereof is oral administration or rectal administration. This invention is a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect of mepenzolate bromide.