2-[1-[3,5-Di(propan-2-yloxy)phenyl]-3-ethyl-7-methoxyisoquinolin-6-yl]oxyethanol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-[1-[3,5-Di(propan-2-yloxy)phenyl]-3-ethyl-7-methoxyisoquinolin-6-yl]oxyethanol
• 化学式: C₂₆H₃₃NO₅
• 分子量: 439.552
• InChiKey: NRJSHVPDELFHKB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  32
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  70
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-[1-[3,5-Di(propan-2-yloxy)phenyl]-3-ethyl-7-methoxyisoquinolin-6-yl]oxyethanol 在 4-二甲氨基吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 53.0h， 生成 carbonic acid 2-[1-(3,5-bis(1-methylethoxy)phenyl)-3-ethyl-7-methoxyisoquinolin-6-yloxy]ethyl ester 2-(5-hydroxy-4a,6a-dimethyl-2-oxo-8-propyl-2,4a,4b,5,6,6a,9a,10,10a,11,12-dodecahydro-7,9-dioxapentaleno[2,1-a]phenanthren-6b-yl)-2-oxo-ethyl ester
  参考文献：
  名称：

  Disease activated drugs: a new concept for the treatment of asthma

  摘要：

  Disease activated drugs (DAD) are pro-drugs of one active principle or combinations of two drugs. which have a proven efficacy for the treatment of the target disease. In opposition to pro-drugs, DAD are activated in inflamed but not normal tissues. Due to the disease specific activation, the amount of locally released drug(s) should be related directly to the severity of the inflammation. To test this concept in asthma a PDE4 inhibitor, an isoquinoline derivative, was chemically derivatized into prodrugs or combined with corticosteroids. These new compounds were more readily cleaved into active PDE4 inhibitor, in bronchoalveolar lavage fluid (BALF) from Brown-Norway rats with lung inflammation than in BALF from rats without airway inflammation. The DAD concept (local selective release and improved therapeutic window) was validated in vivo using the inhibition of methacholine induced bronchoconstriction in guinea pigs with or without ozone induced lung inflammation. An example of DAD hydrolysis (isoquinoline-dexamethasone) was also examined in BALF from asthmatics and healthy volunteers. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(01)00077-3

文献信息

• Isoquinolines
  申请人：SANDOZ LTD.

  公开号：EP0664289A2

  公开（公告）日：1995-07-26

  Compounds of formula I their physiologically-hydrolysable and -acceptable esters and salts thereof. Said compounds, esters and pharmaceutically acceptable acid addition salts are useful as pharmaceuticals, e.g. for asthma therapy.

  式 I 的化合物 它们的生理可水解和可接受的酯及其盐。上述化合物、酯类和药学上可接受的酸加成盐可用作药物，例如用于哮喘治疗。
• Pharmaceutical composition of a pde4 or a pde3/4 inhibitor and a histamine receptor antagonist
  申请人：Nycomed GmbH

  公开号：EP1849468A2

  公开（公告）日：2007-10-31

  The invention relates to the combined administration of PDE4 or PDE3/4 inhibitors and histamine receptor antagonists for the treatment of respiratory diseases.

  本发明涉及联合使用 PDE4 或 PDE3/4 抑制剂和组胺受体拮抗剂治疗呼吸系统疾病。
• Synergistic combination
  申请人：Nycomed GmbH

  公开号：EP2193808A1

  公开（公告）日：2010-06-09

  The invention relates to the combined administration of PDE inhibitors and β2 adrenoceptor agonists for the treatment of respiratory tract disorders.

  本发明涉及联合使用 PDE 抑制剂和 β2 肾上腺素受体激动剂治疗呼吸道疾病。
• JPH07188176A
  申请人：——

  公开号：JPH07188176A

  公开（公告）日：1995-07-25
• TREATMENT OF INFLAMMATORY DISEASE USING INGESTIBLE DEVICE TO RELEASE IMMUNE MODULATOR
  申请人：Progenity, Inc.

  公开号：US20200323772A1

  公开（公告）日：2020-10-15

  This disclosure features methods and compositions for treating inflammatory disorders or conditions that arise in a tissue originating from the endoderm using an immune modulator.