2-(Morpholin-4-yl)ethane-1,1-diol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 2-(Morpholin-4-yl)ethane-1,1-diol
• 英文别名: 2-morpholin-4-ylethane-1,1-diol
• 化学式: C₆H₁₃NO₃
• 分子量: 147.17
• InChiKey: MHESXABHYGORSU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  52.9
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] BIS(DIAZIRINE) DERIVATIVES AS PHOTO-CROSSSLINKER FOR TREATING CORNEAL ECTATIC DISORDERS<br/>[FR] DÉRIVÉS DE BIS(DIAZIRINE) UTILISÉS EN TANT QU'AGENT DE PHOTO-RÉTICULATION POUR LE TRAITEMENT DE TROUBLES ECTASIQUES DE LA CORNÉE
  申请人：AVEDRO INC

  公开号：WO2020154673A1

  公开（公告）日：2020-07-30

  This disclosure features bis(diazirine) derivatives of the formulae (I) (l-a) or (l-b) that generate cross-linking in the cornea in response to exposure to an electromagnetic irradiation (e.g. UV-light). The compounds are useful, e.g. for treating a subject (e.g. a human) having a disease, disorder or condition in which abnormal shaping of the cornea (e.g. thinning of the cornea, e.g. bilateral thinning of the cornea, e.g. bilateral thinning of the central, paracentral, or peripheral cornea, or steepening (e.g., bulging) of the cornea) contributes to the pathology and/or symptoms, and/or progression of the disease, disorder or condition. Examples of such diseases, disorders or conditions include: (i) corneal ectatic disorders; (ii) vision conditions; and (iii) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular examples of such diseases, disorders or conditions include keratoconus, keratoglobus, pellucid marginal degeneration, corneal ectasia (e.g. postoperative ectasia, e.g. post-LASIK ectasia), Terrien's marginal degeneration, myopia, hyperopia, astigmatism, irregular astigmatism and presbyopia. In some embodiments, the claimed methods can be performed in the absence of added or supplemental oxygen levels, which can be advantageous in some applications. Preferred exemplary compounds are e.g. bis(diazirine) amino acid derivatives, such as e.g. example 1:

  这份披露涉及到式(I) (l-a)或(l-b)的双(重氮基)衍生物，当暴露于电磁辐射（例如紫外光）时，在角膜中产生交联作用。这些化合物可用于治疗患有疾病、疾病或病况的受试者（例如人类），其中角膜的异常形态（例如角膜变薄，例如角膜双侧变薄，例如角膜中央、副中央或周边变薄，或角膜变陡（例如突出））导致病理和/或症状的发生，以及/或疾病、疾病或病况的进展。此类疾病、疾病或病况的示例包括：(i) 角膜扩张性疾病；(ii) 视力状况；以及(iii) 与前述任何疾病、疾病或病况或本文所披露的任何内容相关的后遗症或共病。此类疾病、疾病或病况的更具体示例包括角膜锥状变性、角膜球状变性、边缘淡化变性、角膜扩张（例如术后扩张，例如术后LASIK扩张）、Terrien边缘变性、近视、远视、散光、不规则散光和老视。在某些实施例中，声称的方法可以在没有额外或补充氧气水平的情况下进行，这在某些应用中可能是有利的。优选的示例化合物包括双(重氮基)氨基酸衍生物，例如示例1：