7-methyl-4-acetamidoindane | 1404051-76-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 7-methyl-4-acetamidoindane
• 英文别名: 7-methyl-4-acetamido-indan；N-(7-methyl-2,3-dihydro-1H-inden-4-yl)acetamide
• CAS: 1404051-76-8
• 化学式: C₁₂H₁₅NO
• 分子量: 189.257
• InChiKey: OFCJYWKALHUOCP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.44
• 重原子数：
  14.0
• 可旋转键数：
  1.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  29.1
• 氢给体数：
  1.0
• 氢受体数：
  1.0

反应信息

• 作为反应物：
  描述：

  7-methyl-4-acetamidoindane 在 盐酸 作用下， 以 水 为溶剂， 生成 7-methyl-4-amino-indan
  参考文献：
  名称：

  [EN] QUINAZOLINE COMPOUNDS FOR TREATMENT OF DISEASE
  [FR] COMPOSÉS DE QUINAZOLINE POUR LE TRAITEMENT D'UNE MALADIE

  摘要：

  Described herein are inhibitors of EGFR exon 20 insertion mutants and methods of treating cancer comprising the administration of said inhibitors.

  公开号：

  WO2023028054A1
• 作为产物：
  描述：

  N-(2,3-dihydro-1H-inden-4-yl)acetamide 在 四(三苯基膦)钯 、 溴 、 sodium carbonate 、 溶剂黄146 作用下， 以 1,4-二氧六环 为溶剂， 反应 10.33h， 生成 7-methyl-4-acetamidoindane
  参考文献：
  名称：

  Synthesis and Biological Evaluation of 2-Aryliminopyrrolidines as Selective Ligands for I₁ Imidazoline Receptors: Discovery of New Sympatho-Inhibitory Hypotensive Agents with Potential Beneficial Effects in Metabolic Syndrome

  摘要：

  New 2-aryliminopyrrolidines (1-18) were synthesized and tested for their binding properties on I-1 imidazoline receptors vs a2-adrenergic receptors and their blood pressure effects after both systemic and intracerebral administrations. The purposes of this study were: (i) to analyze structureactivity and affinity relationships on I-1 imdazoline receptors and (ii) to propose some leader compounds for the development of new sympatho-inhibitory drugs with potential applications in hypertension and/or metabolic syndrome, i.e., a cluster of cardiovascular (hypertension) and metabolic disorders. Our study highlights decisive arguments of SAR concerning both the affinity for I(1)Rs and the hypotensive activity of 2-aryliminopyrrolidines. Binding assays showed high affinity and selectivity of some compounds for I-1 imidazoline receptors over alpha(2)-adreergic receptors. Compound 13 (laboratory reference LNP599; K-i = 3.2 nM on I(1)imidazoline receptors) is the prototype for the development of new centrally acting agents targeting specifically I(1)imidazoline receptors to be used in the management of hypertension and/or metabolic syndrome.

  DOI：

  10.1021/jm501456p

文献信息

• NOVEL AMINO-PYRROLINE DERIVATIVES, AND USE THEREOF IN THE PREVENTION AND/OR TREATMENT OF METABOLIC SYNDROME
  申请人：Bousquet Pascal

  公开号：US20140045910A1

  公开（公告）日：2014-02-13

  Novel amino-pyrrolinic derivatives, their pharmacologically acceptable salts and use thereof in the prevention and/or treatment of metabolic syndrome.

  新型氨基吡咯烷衍生物，其药理学上可接受的盐和在预防和/或治疗代谢综合征中的应用。
• NOUVEAUX DERIVES AMINO-PYRROLINIQUES, LEUR UTILISATION DANS LA PREVENTION ET/OU LE TRAITEMENT DU SYNDROME METABOLIQUE
  申请人：Université de Strasbourg

  公开号：EP2699545A1

  公开（公告）日：2014-02-26
• US9303019B2
  申请人：——

  公开号：US9303019B2

  公开（公告）日：2016-04-05
• [EN] NOVEL AMINO-PYRROLINE DERIVATIVES, AND USE THEREOF IN THE PREVENTION AND/OR TREATMENT OF METABOLIC SYNDROME<br/>[FR] NOUVEAUX DERIVES AMINO-PYRROLINIQUES, LEUR UTILISATION DANS LA PREVENTION ET/OU LE TRAITEMENT DU SYNDROME METABOLIQUE
  申请人：UNIV STRASBOURG

  公开号：WO2012143660A1

  公开（公告）日：2012-10-26

  Nouveaux dérivés amino-pyrro Uniques, leurs sels pUarmacologiquement acceptables et leur utilisation dans la prévention et/ou le traitement du syndrome métabolique.
• [EN] QUINAZOLINE COMPOUNDS FOR TREATMENT OF DISEASE<br/>[FR] COMPOSÉS DE QUINAZOLINE POUR LE TRAITEMENT D'UNE MALADIE
  申请人：[en]ARTHROSI THERAPEUTICS, INC.

  公开号：WO2023028054A1

  公开（公告）日：2023-03-02

  Described herein are inhibitors of EGFR exon 20 insertion mutants and methods of treating cancer comprising the administration of said inhibitors.