ethyl 1-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-4-piperidinecarboxylate | 1207618-18-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: ethyl 1-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-4-piperidinecarboxylate
• 英文别名: Ethyl 1-[4-(2-hydroxyphenyl)-2-thiazolyl]-4-piperidinecarboxylate；ethyl 1-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]piperidine-4-carboxylate
• CAS: 1207618-18-5
• 化学式: C₁₇H₂₀N₂O₃S
• 分子量: 332.423
• InChiKey: ZQNIJEBQFVWJQB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  90.9
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  ethyl 1-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-4-piperidinecarboxylate 在 N-氯代丁二酰亚胺 作用下， 以 乙腈 为溶剂， 反应 16.0h， 以55%的产率得到ethyl 1-[5-chloro-4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-4-piperidinecarboxylate
  参考文献：
  名称：

  [EN] THIAZOLE COMPOUNDS AS MEDICAMENTS FOR THE TREATMENT OF (INTER ALIA) CARDIOVASCULAR DISEASES
  [FR] COMPOSÉS THIAZOLE UTILISÉS COMME ACTIVATEURS DE LA GUANYLATE CYCLASE SOLUBLE

  摘要：

  公开号：

  WO2010015652A3
• 作为产物：
  描述：

  ethyl 1-(4-bromothiazol-2-yl)piperidine-4-carboxylate 、 2-羟基苯硼酸 在 四(三苯基膦)钯 caesium carbonate 作用下， 以 乙二醇二甲醚 、 水 为溶剂， 以75%的产率得到ethyl 1-[4-(2-hydroxyphenyl)-1,3-thiazol-2-yl]-4-piperidinecarboxylate
  参考文献：
  名称：

  [EN] THIAZOLE COMPOUNDS AS MEDICAMENTS FOR THE TREATMENT OF (INTER ALIA) CARDIOVASCULAR DISEASES
  [FR] COMPOSÉS THIAZOLE UTILISÉS COMME ACTIVATEURS DE LA GUANYLATE CYCLASE SOLUBLE

  摘要：

  公开号：

  WO2010015652A3

文献信息

• [EN] SOLUBLE GUANYLATE CYCLASE ACTIVATORS<br/>[FR] ACTIVATEURS DE GUANYLATE CYCLASE SOLUBLE
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2013025425A1

  公开（公告）日：2013-02-21

  The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein R1 - R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本发明涉及式（I）的化合物及其药用盐，其中R1 - R5和n如本文所定义。该发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和紊乱的方法，制备这些化合物的方法以及在这些过程中有用的中间体。
• SOLUBLE GUANYLATE CYCLASE ACTIVATORS
  申请人：BOSANAC Todd

  公开号：US20130203729A1

  公开（公告）日：2013-08-08

  The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 -R 5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本发明涉及式（I）的化合物及其药学上可接受的盐，其中R1-R5和n的定义如本文所述。本发明还涉及包括这些化合物的制药组合物，在治疗各种疾病和障碍中使用这些化合物的方法，制备这些化合物的过程以及这些过程中有用的中间体。
• US8815857B2
  申请人：——

  公开号：US8815857B2

  公开（公告）日：2014-08-26
• [EN] THIAZOLE COMPOUNDS AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE<br/>[FR] COMPOSÉS THIAZOLE UTILISÉS COMME ACTIVATEURS DE LA GUANYLATE CYCLASE SOLUBLE
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2010015652A2

  公开（公告）日：2010-02-11

  Disclosed are compounds of formula (I) wherein R1 and R2 are independently selected from hydrogen, halo, C1-4alkyl, C1-4alkoxy, CF3 and OCF3; -Y- represents formula (IA) R3 represents hydrogen, fluoro, chloro or C1-4alkyl; R4a and R4b each independently represent hydrogen, C1-4alkyl, C1-4alkoxy, CF3 or halo; and R5 represents a group Z-X; wherein Z is absent or represents (CH2)2 or O; and X represents formula (IB) wherein: J and L both represent CH, or one of J and L represents CH and the other represents N; when both J and L represent CH, R6 represents hydrogen, halo, CF3, C1-4alkyl or C1-4alkoxy in a meta or ortho position relative to the R7 substituent and R7 represents hydrogen, halo, CF3, OCF3, C1-4alkyl, C1-4alkoxy, CH2OH, CN, CONR8R9 or CO2H; or when one of J or L represents N, R6 represents hydrogen or halo in a meta or ortho position relative to the R7 substituent and R7 represents hydrogen, halo, CF3, C1-4alkyl, C1-4alkoxy, CH2OH, CN, CONR8R9 or CO2H; and R8 and R9 are independently selected from hydrogen and C1-4alkyl; or salts thereof which activate soluble guanylate cyclase (sGC), pharmaceutical compositions containing them, their use in medicine, and processes for their preparation.