7-methyl-4-amino-indan

• 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-amino-indan
• 化学式: C₁₀H₁₃N
• 分子量: 147.22
• InChiKey: STLTVJMFLJYPIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.07
• 重原子数：
  11.0
• 可旋转键数：
  0.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  26.02
• 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-amino-indan 、 6-乙酰氧基-4-氯-7-甲氧基喹唑啉 以 异丙醇 为溶剂， 生成 [7-methoxy-4-[(7-methyl-2,3-dihydro-1H-inden-4-yl)amino]quinazolin-6-yl] acetate
  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 盐酸 、 四(三苯基膦)钯 、 溴 、 sodium carbonate 、 溶剂黄146 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 12.33h， 生成 7-methyl-4-amino-indan
  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。
• PYRROLOPYRIDINE DERIVATIVE AND USE THEREOF IN PREVENTION AND TREATMENT OF PROTEIN KINASE-RELATED DISEASE
  申请人：Voronoi Co., Ltd.

  公开号：EP3915985A1

  公开（公告）日：2021-12-01

  The present invention relates to a pyrrolopyridine derivative and a pharmaceutical composition comprising the same as an active ingredient for prevention or treatment of a protein kinase-related disease. The pyrrolopyridine derivative has excellent inhibitory activity against various protein kinases including LRRK2, DYRK1, and CLK1 and exhibits an excellent suppressive effect on the growth of triple-negative breast cancer cells. A pharmaceutical composition comprising the same as an active ingredient can be advantageously used for treating or preventing protein kinase-related diseases, inter alia, cancers, degenerative brain diseases, and inflammatory diseases, and specifically for treating triple-negative breast cancer.

  本发明涉及一种吡咯并吡啶衍生物和一种以其为活性成分的药物组合物，用于预防或治疗蛋白激酶相关疾病。该吡咯并吡啶衍生物对包括 LRRK2、DYRK1 和 CLK1 在内的多种蛋白激酶具有极佳的抑制活性，并对三阴性乳腺癌细胞的生长具有极佳的抑制作用。由其作为活性成分的药物组合物可以很好地用于治疗或预防蛋白激酶相关疾病，尤其是癌症、脑退化性疾病和炎症性疾病，特别是用于治疗三阴性乳腺癌。
• [EN] STEROID COMPOUND, AND PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF<br/>[FR] COMPOSÉ STÉROÏDE, COMPOSITION PHARMACEUTIQUE ET UTILISATION ASSOCIÉES<br/>[ZH] 甾体类化合物、其药物组合物及其应用
  申请人：[en]JIANGSU SIMCERE PHARMACEUTICAL CO., LTD.;[zh]江苏先声药业有限公司

  公开号：WO2022268176A1

  公开（公告）日：2022-12-29

  一种式(I)所示化合物或其药学上可接受的盐、药物组合物及其制备方法，以及其在治疗肿瘤、炎性疾病或自身免疫性疾病中的用途。
• US9303019B2
  申请人：——

  公开号：US9303019B2

  公开（公告）日：2016-04-05
• [EN] AHR INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS D'AHR ET LEURS UTILISATIONS
  申请人：KYN THERAPEUTICS

  公开号：WO2019036657A1

  公开（公告）日：2019-02-21

  The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.