3endo-(2,2-di-[2]thienyl-vinyl)-N,N-dimethyl-nortropanium; bromide | 102924-25-4

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: 3endo-(2,2-di-[2]thienyl-vinyl)-N,N-dimethyl-nortropanium; bromide
• 英文别名: (3-endo)-3-(2,2-di-2-thienylethenyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide；3-endo-(2,2-di-2-thienylethenyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide
• CAS: 102924-25-4
• 化学式: Br*C₁₉H₂₄NS₂
• 分子量: 410.442
• InChiKey: BWOXSKDDWQTJRH-ZIGIEQIVSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  2.26
• 重原子数：
  23.0
• 可旋转键数：
  3.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  0.0
• 氢给体数：
  0.0
• 氢受体数：
  2.0

反应信息

• 作为产物：
  描述：

  溴甲烷 、 3endo-(2,2-di-[2]thienyl-vinyl)-tropane 以 丙酮 为溶剂， 反应 12.0h， 生成 3endo-(2,2-di-[2]thienyl-vinyl)-N,N-dimethyl-nortropanium; bromide
  参考文献：
  名称：

  Design, Synthesis, and Structure−Activity Relationship of Tropane Muscarinic Acetylcholine Receptor Antagonists

  摘要：

  Novel tropane derivatives were characterized as muscarinic acetylcholine receptor antagonists (mAChRs). Through optimization of the structure-activity relationship around the tropane scaffold, the quaternary ammonium salt 34 was identified as a very Potent M(3) mAChR antagonist. The compound was functionally active and displayed greater than 24 It duration of action in a mouse model of bronchoconstriction.

  DOI：

  10.1021/jm900736e

文献信息

• 5-Lipoxygenase-Activating Protein Inhibitor
  申请人：SCHAAB Kevin Murray

  公开号：US20090291981A1

  公开（公告）日：2009-11-26

  Described herein is the FLAP inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, including solvates, and polymorphs thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

  描述了一种FLAP抑制剂：3-[3-叔丁基硫基-1-[4-(6-乙氧基-吡啶-3-基)-苄基]-5-(5-甲基-吡啶-2-基甲氧基)-1H-吲哚-2-基]-2,2-二甲基丙酸，或其药用可接受盐。还描述了制备该FLAP抑制剂的方法，或其药用可接受盐，包括水合物和其多晶型。还描述了适合给予哺乳动物的药物组合物，包括FLAP抑制剂，或其药用可接受盐，以及使用此类药物组合物治疗呼吸系统疾病或疾病的方法，以及治疗其他白三烯依赖性或白三烯介导的条件或疾病的方法。
• [EN] PYRAZOLE COMPOUNDS ACTING AGAINST ALLERGIC, INFLAMMATORY AND IMMUNE DISORDERS<br/>[FR] COMPOSÉS DE PYRAZOLE AGISSANT CONTRE DES TROUBLES ALLERGIQUES, INFLAMMATOIRES ET IMMUNITAIRES
  申请人：GLAXO GROUP LTD

  公开号：WO2012052459A1

  公开（公告）日：2012-04-26

  The present invention relates to pyrazole amide derivatives pharmaceutical compositions containing these compounds and to their use in therapy.

  本发明涉及吡唑酰胺衍生物、含有这些化合物的药物组合物以及它们在治疗中的用途。
• [EN] PYRAZOLE COMPOUNDS ACTING AGAINST ALLERGIC, IMMUNE AND INFLAMMATORY CONDITIONS<br/>[FR] COMPOSÉS PYRAZOLE AGISSANT CONTRE DES ÉTATS ALLERGIQUES, IMMUNITAIRES ET INFLAMMATOIRES
  申请人：GLAXO GROUP LTD

  公开号：WO2012052458A1

  公开（公告）日：2012-04-26

  The present invention relates to a pyrazole amide derivative, pharmaceutical compositions containing this compound and to its use in therapy.

  本发明涉及一种吡唑酰胺衍生物，含有该化合物的药物组合物及其在治疗中的应用。
• [EN] PYRIDINE-3-SULFONAMIDE COMPOUNDS AS PI3-KINASE INHIBITORS<br/>[FR] COMPOSÉS DE PYRIDINE-3-SULFONAMIDE UTILISÉS EN TANT QU'INHIBITEURS DE PI3-KINASE
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2019020657A1

  公开（公告）日：2019-01-31

  The invention is directed to compounds of formula (I) and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity.

  这项发明涉及式(I)的化合物及其盐。这些化合物是激酶活性抑制剂，特别是PI3激酶活性抑制剂。
• PYRIDO[3,4-B]PYRAZINE DERIVATIVES AS SYK INHIBITORS
  申请人：Atkinson Francis Louis

  公开号：US20140005188A1

  公开（公告）日：2014-01-02

  A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.

  化合物的化学式（I）：或其盐；它是脾酪氨酸激酶（Syk）的抑制剂，因此可能用于治疗由于肥大细胞、巨噬细胞和B细胞不适当活化引起的疾病，例如炎症性疾病和/或过敏性疾病，以及癌症治疗，特别是血液恶性肿瘤和自身免疫症状。