Formylamino-5-chinolin | 42464-79-9

• 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: Formylamino-5-chinolin
• 英文别名: N-quinolin-5-yl-formamide；N-quinolin-5-ylformamide
• CAS: 42464-79-9
• 化学式: C₁₀H₈N₂O
• 分子量: 172.186
• InChiKey: MODGIVWBSKCBPL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Metastin derivatives and use thereof
  申请人：Asami Taiji

  公开号：US20090215700A1

  公开（公告）日：2009-08-27

  The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids, the metastin derivatives of the present invention achieve more improved blood stability, solubility, etc., reduced gelation tendency, improved pharmacokinetics, as well as exhibit an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity. The metastin derivatives of the present invention also have a gonadotropic hormone secretion suppressing activity, sex hormone secretion suppressing activity, etc.

  本发明提供了稳定的metastin衍生物，具有优异的生物活性（癌转移抑制活性、癌症生长抑制活性、促性腺激素分泌活性、性激素分泌刺激活性等）。通过用特定的氨基酸替换metastin的组成氨基酸，本发明的metastin衍生物实现了更好的血液稳定性、溶解度等，减少了凝胶化倾向，改善了药代动力学，并表现出优异的癌转移抑制活性或癌症生长抑制活性。本发明的metastin衍生物还具有抑制促性腺激素分泌活性、性激素分泌抑制活性等。
• [EN] SYNTHESIS OF QUINOLINE 5-CARBOXAMIDES USEFUL FOR THE PREPARATION OF PDE IV INHIBITORS<br/>[FR] SYNTHESE DE QUINOLINE 5-CARBOXAMIDES UTILES POUR LA PREPARATION D'INHIBITEURS DE PDE IV
  申请人：SCHERING CORP

  公开号：WO2005028471A1

  公开（公告）日：2005-03-31

  In one embodiment, the present application discloses a process for making the compound of the formula:

  在一种实施例中，本申请公开了制备化合物的方法，其化学式为：
• Synthesis of quinoline 5-carboxamides useful for the preparation of PDE IV inhibitors
  申请人：Andrews R. David

  公开号：US20050124655A1

  公开（公告）日：2005-06-09

  In one embodiment, the present application discloses a process for making the compound of the formula:

  在一种实施例中，本申请公开了一种制备化合物的方法，该化合物的化学式为：
• METASTIN DERIVATIVES AND USE THEREOF
  申请人：Kitada Chieko

  公开号：US20090318365A1

  公开（公告）日：2009-12-24

  The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivatives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action.

  本发明提供了一种metastin衍生物，其中包含metastin的氨基酸被替代化学基团修饰，从而产生了metastin衍生物，具有出色的血液稳定性，并表现出抑制癌症转移或抑制癌症生长的作用。
• Metastin Derivatives and Use Thereof
  申请人：Kitada Chieko

  公开号：US20080312155A1

  公开（公告）日：2008-12-18

  The invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, etc.). By modifying the constituent amino acids of metastin with specific modifying groups, metastin derivatives having more improved blood stability, etc. than native metastin and showing excellent cancer metastasis suppressing activity or cancer growth suppressing activity have been found. Furthermore, it has been found that these metastin derivatives exhibit effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc., which are wholly different from the effects heretofore known.

  该发明提供了稳定的metastin衍生物，具有优异的生物活性（抑制癌细胞转移的活性，抑制癌细胞生长的活性等）。通过用特定的修饰基团修饰metastin的组成氨基酸，发现比天然的metastin具有更好的血液稳定性等，同时表现出优异的抑制癌细胞转移或抑制癌细胞生长的活性。此外，发现这些metastin衍生物表现出抑制性腺激素分泌、抑制性激素分泌等完全不同于以往所知的效应。