2-imino-5-quinolin-6-ylmethylene-thiazolidin-4-one

• 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: 2-imino-5-quinolin-6-ylmethylene-thiazolidin-4-one
• 英文别名: (5Z)-2-amino-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4-one；(5Z)-2-imino-5-(quinolin-6-ylmethylidene)-1,3-thiazolidin-4-one
• 化学式: C₁₃H₉N₃OS
• 分子量: 255.3
• InChiKey: GWSGFSPSQGXVFI-XFFZJAGNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  93.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  喹啉-6-甲醛 在 氨 、 sodium acetate 、 溶剂黄146 、 N,N-二异丙基乙胺 作用下， 以 乙醇 、 乙腈 为溶剂， 反应 36.33h， 生成 2-imino-5-quinolin-6-ylmethylene-thiazolidin-4-one
  参考文献：
  名称：

  Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors

  摘要：

  A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase I (CDK1) inhibitors. Their synthesis and structure activity relationships (SAR) are described. Representative compounds from this class reversibly inhibit CDK1 activity in vitro, and block cell cycle progression in human tumor cell lines, suggesting a potential use as antitumor agents. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.01.081

文献信息

• [EN] AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES<br/>[FR] DERIVES DE BENZENE A FUSION AZOLIDINONE-VINYLE
  申请人：APPLIED RESEARCH SYSTEMS

  公开号：WO2004007491A1

  公开（公告）日：2004-01-22

  The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1 , R2 and n are as described in the description.

  本发明涉及式(I)的噁唑烷二酮-乙烯融合苯衍生物，用于治疗和/或预防自身免疫性疾病和/或炎症性疾病、心血管疾病、神经退行性疾病、细菌或病毒感染、肾脏疾病、血小板聚集、癌症、移植排斥或肺部损伤。式(I)中，A、X、Y、Z、R1、R2和n如描述中所述。
• [EN] USE OF COMPOUNDS FOR INCREASING SPERMATOZOA MOTILITY<br/>[FR] UTILISATION DE COMPOSES POUR ACCROITRE LA MOTILITE DES SPERMATOZOIDES
  申请人：APPLIED RESEARCH SYSTEMS

  公开号：WO2004006916A1

  公开（公告）日：2004-01-22

  The invention relates to a process for the improvement of spermatozoa fertilization activity, in particular for the increase of spermatozoa motility, by using a compound of formula (I). The invention further relates to uses and methods of compounds of formula (I) in infertility and assisted reproduction techniques (ART) as well as to a medium for storage and/or transportation of spermatozoa comprising said P13K inhibitors.

  本发明涉及一种通过使用式(I)化合物来改善精子受精活性，特别是增加精子运动能力的过程。本发明还涉及在不孕症和辅助生殖技术（ART）中使用式(I)化合物的方法，以及用于储存和/或运输精子的介质，其中包括所述P13K抑制剂。
• Azolidinone-vinyl fused-benzene derivatives
  申请人：Rueckle Thomas

  公开号：US20060122176A1

  公开（公告）日：2006-06-08

  The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R 1 , R 2 and n are as described in the description.

  本发明涉及公式（I）的噻唑烷二酮-乙烯基融合苯衍生物，用于治疗和/或预防自身免疫性疾病和/或炎症性疾病、心血管疾病、神经退行性疾病、细菌或病毒感染、肾脏疾病、血小板聚集、癌症、移植排斥或肺损伤。公式（I）中，A，X，Y，Z，R1，R2和n如说明书中所述。
• Use of compounds for increasing spermatozoa motility
  申请人：De Luca Giampiero

  公开号：US20050222225A1

  公开（公告）日：2005-10-06

  The invention relates to a process for the improvement of spermatozoa fertilization activity, in particular for the increase of spermatozoa motility, by using a compound of formula (I). The invention further relates to uses and methods of compounds of formula (I) in infertility and assisted reproduction techniques (ART) as well as to a medium for storage and/or transportation of spermatozoa comprising said P13K inhibitors.

  本发明涉及一种使用式(I)化合物改善精子受精活性的方法，特别是增加精子运动性的方法。本发明还涉及式(I)化合物在不孕症和辅助生殖技术（ART）中的用途和方法，以及一种包含所述P13K抑制剂的精子储存和/或运输介质。
• 2-Imino-4-(thio)oxo-5-poly cyclovinylazolines for use as p13 kinase ihibitors
  申请人：Rueckle Thomas

  公开号：US20070021447A1

  公开（公告）日：2007-01-25

  The present invention is related to 2-imino-azolinone-vinyl fused-benzene derivatives of Formula (1) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

  本发明涉及公式（1）的2-亚氨基-咪唑酮-乙烯基融合苯衍生物，特别用于治疗和/或预防自身免疫性疾病和/或炎症性疾病、心血管疾病、神经退行性疾病、肾脏疾病、血小板聚集、癌症、移植、移植排斥或肺损伤。