5-(2-amino-1-hydroxy-ethyl)-8-hydroxy-3,4-dihydro-1H-quinolin-2-one | 57275-96-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 5-(2-amino-1-hydroxy-ethyl)-8-hydroxy-3,4-dihydro-1H-quinolin-2-one
• 英文别名: 5-(1-Hydroxy-2-amino)ethyl-8-hydroxy-3,4-dihydrocarbostyril；5-(2-Amino-1-hydroxyethyl)-8-hydroxy-3,4-dihydroquinolin-2(1H)-one；5-(2-amino-1-hydroxyethyl)-8-hydroxy-3,4-dihydro-1H-quinolin-2-one
• CAS: 57275-96-4
• 化学式: C₁₁H₁₄N₂O₃
• 分子量: 222.244
• InChiKey: ZYEHKADBQAOYSD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  95.6
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-(2-amino-1-hydroxy-ethyl)-8-hydroxy-3,4-dihydro-1H-quinolin-2-one 生成 5-(1-Hydroxy-2-amino)ethyl-8-hydroxycarbostyril
  参考文献：
  名称：

  JOSIDZAKI, SIRO

  摘要：

  DOI：

文献信息

• [EN] NITROGEN CONTAINING HETEROCYCLIC COMPOUNDS USEFUL AS BIFUNCTIONAL MODULATORS OF M3 RECEPTORS AND BETA-2 RECEPTORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES CONTENANT DE L'AZOTE UTILES COMME MODULATEURS BIFONCTIONNELS DES RÉCEPTEURS M3 ET DES RÉCEPTEURS BÊTA-2
  申请人：ARGENTA DISCOVERY LTD

  公开号：WO2010015792A1

  公开（公告）日：2010-02-11

  The present invention relates to named compounds of the formula (I) having both M3 receptor antagonist and β2 agonist activity; compositions comprising such compounds; the use of such compounds in therapy (such as respiratory tract disorders); and a method of treating a patient with such compounds.

  本发明涉及具有M3受体拮抗剂和β2激动剂活性的式（I）的化合物；包含这种化合物的组合物；在治疗中使用这种化合物（如呼吸道疾病）；以及使用这种化合物治疗患者的方法。
• Biphenyl derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
  申请人：——

  公开号：US20040209860A1

  公开（公告）日：2004-10-21

  This invention provides biphenyl derivatives containing (i) a (biphenyl-2-yl)oxycarbonylamino- or (biphenyl-2-yl)aminocarbonylamino-substituted (2-7C)azacycloalkyl or (5-10C)azabicycloalkyl group; (ii) a substituted 2-(4-hydroxyphenyl)-2-hydroxyethylamino group; and a divalent hydrocarbon group, where each group is further defined and optionally substituted as described in the specification. The biphenyl derivatives of the invention possess both &bgr; 2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

  该发明提供了含有以下结构的联苯衍生物：(i)一个(biphenyl-2-yl)oxycarbonylamino-或(biphenyl-2-yl)aminocarbonylamino取代的(2-7C)氮杂环烷基或(5-10C)氮杂双环烷基；(ii)一个取代的2-(4-羟基苯基)-2-羟乙基氨基基团；以及一个二价碳氢基团，其中每个基团进一步在说明书中描述并可选地取代。该发明的联苯衍生物具有β2肾上腺素受体激动剂和毒蕈碱受体拮抗剂活性，因此，这种联苯衍生物对于治疗肺部疾病，如慢性阻塞性肺疾病和哮喘，是有用的。
• BIPHENYL DERIVATIVES HAVING &bgr; sb 2 /sb ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY
  申请人：Theravance Inc

  公开号：EP1592685A1

  公开（公告）日：2005-11-09
• US3994901A
  申请人：——

  公开号：US3994901A

  公开（公告）日：1976-11-30
• [EN] BIPHENYL DERIVATIVES HAVING beta2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY<br/>[FR] DERIVES BIPHENYLES PRESENTANT UNE ACTIVITE AGONISTE DU RECEPTEUR DE BETA 2 ADRENERGIQUE ET ANTAGONISTE DE RECEPTEUR MUSCARINIQUE
  申请人：THERAVANCE INC

  公开号：WO2004074276A1

  公开（公告）日：2004-09-02

  This invention provides biphenyl derivatives containing (i) a (biphenyl-2-yl)oxycarbonylamino- or (biphenyl-2-yl)aminocarbonylamino-substituted (2-7C)azacycloalkyl or (5-10C)azabicycloalkyl group; (ii) a substituted 2-(4-hydroxyphenyl)-2-hydroxyethylamino group; and a divalent hydrocarbon group, where each group is further defined and optionally substituted as described in the specification. The biphenyl derivatives of the invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.