7-[(R)-(四氢呋喃-3-基)氧基]-N-(3-氯-4-氟苯基)-6-[(二乙氧基磷酰基)-乙酰氨基]-4-氨基喹唑啉 | 618061-77-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 7-[(R)-(四氢呋喃-3-基)氧基]-N-(3-氯-4-氟苯基)-6-[(二乙氧基磷酰基)-乙酰氨基]-4-氨基喹唑啉
• 中文别名: 阿法替尼TM8对映体Ｒ型
• 英文名称: 4-[(3-chloro-4-fluoro-phenyl)amino]-6-[(diethoxy-phosphoryl)-acetylamino]-7-[(R)-(tetrahydrofuran-3-yl)oxy]-quinazoline
• 英文别名: (R)-diethyl 2-(4-(3-chloro-4-fluorophenylaMino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-ylaMino)-2-oxo；N-[4-(3-chloro-4-fluoroanilino)-7-[(3R)-oxolan-3-yl]oxyquinazolin-6-yl]-2-diethoxyphosphorylacetamide
• CAS: 618061-77-1
• 化学式: C₂₄H₂₇ClFN₄O₆P
• 分子量: 552.927
• InChiKey: FNGRCLBEXKFSST-MRXNPFEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  37
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  121
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
  申请人：Himmelsbach Frank

  公开号：US20050107358A1

  公开（公告）日：2005-05-19

  The present invention relates to bicyclic heterocycles of general formula wherein R a , R b , R c , R d , R e and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.

  本发明涉及一般式的双环杂环化合物 其中 R a ，R b ，R c ，R d ，R e 和X的定义如权利要求书中所述， 其互变异构体、立体异构体、它们的混合物及其盐，特别是其与无机或有机酸形成的生理上可接受的盐，具有有价值的药理特性，特别是对酪氨酸激酶介导的信号传导具有抑制作用，其用于治疗疾病，特别是肿瘤性疾病和良性前列腺增生（BPH），肺部和呼吸道疾病，以及其制备。
• Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
  申请人：Himmelsbach Frank

  公开号：US20050159436A1

  公开（公告）日：2005-07-21

  The present invention relates to bicyclic heterocycles of general formula wherein R a , R b , R c , A, B, C, D, E and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.

  本发明涉及一般式为的双环杂环化合物， 其中Ra，Rb，Rc，A，B，C，D，E和X如权利要求1所定义，其互变异构体、立体异构体、混合物及其与无机或有机酸形成的生理上可接受的盐，具有有价值的药理学特性，特别是对酪氨酸激酶介导的信号转导具有抑制作用，其用于治疗疾病，特别是肿瘤性疾病、良性前列腺增生（BPH）、肺和呼吸道疾病，以及其制备方法。
• BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR THE PREPARATION THEREOF
  申请人：Himmelsbach Frank

  公开号：US20080103161A1

  公开（公告）日：2008-05-01

  The present invention relates to bicyclic heterocycles of general formula wherein R a , R b , R c , A, B, C, D, E and X are defined as in claim 1 , the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.

  本发明涉及一般式为的双环杂环化合物 其中Ra，Rb，Rc，A，B，C，D，E和X如权利要求1中所定义，其互变异构体，立体异构体，混合物和盐，特别是其与无机或有机酸的生理上可接受的盐，具有有价值的药理特性，特别是对由酪氨酸激酶介导的信号转导具有抑制作用，其用于治疗疾病，特别是肿瘤性疾病，以及良性前列腺增生症（BPH），肺和呼吸道疾病，以及其制备方法。
• Bicyclic heterocylces, pharmaceutical compositions containing these compounds, their use and processes for preparing them
  申请人：HIMMELSBACH Frank

  公开号：US20070185081A1

  公开（公告）日：2007-08-09

  The present invention relates to bicyclic heterocycles of general formula wherein R a , R b , R c , R d , R e and X are defined as in claim 1 , the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
• US7223749B2
  申请人：——

  公开号：US7223749B2

  公开（公告）日：2007-05-29