1-(1,3-thiazol-2-yl)piperidine-4-carboxylic Acid | 874623-60-6

• 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: 1-(1,3-thiazol-2-yl)piperidine-4-carboxylic Acid
• CAS: 874623-60-6
• 化学式: C₉H₁₂N₂O₂S
• mdl: MFCD07692337
• 分子量: 212.27
• InChiKey: RBLAPOMCQIFXCT-UHFFFAOYSA-N

物化性质

• 沸点：
  400.3±55.0 °C(Predicted)
• 密度：
  1.355±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.555
• 拓扑面积：
  81.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] AMINOPYRIMIDINES AS SYK INHIBITORS<br/>[FR] AMINOPYRIMIDINES EN TANT QU'INHIBITEURS DE LA SYK
  申请人：MERCK SHARP & DOHME

  公开号：WO2011075560A1

  公开（公告）日：2011-06-23

  The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.

  本发明提供了式（I）的新型嘧啶胺化合物，它们是脾酪氨酸激酶的有效抑制剂，并可用于治疗和预防由该酶介导的疾病，如哮喘、慢性阻塞性肺病（COPD）和类风湿性关节炎。
• NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
  申请人：Zhu Hugh Y.

  公开号：US20120214823A1

  公开（公告）日：2012-08-23

  Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1.

  本发明公开了式1.0的ERK抑制剂：（式（A1）），以及其药学上可接受的盐，酯和溶剂化物。Q是一个可以有桥或融合环的哌啶环。所有其他取代基如本文所定义。本发明还公开了使用式A1化合物治疗癌症的方法。
• AMINOPYRIMIDINES AS SYK INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2512246A1

  公开（公告）日：2012-10-24
• US8658651B2
  申请人：——

  公开号：US8658651B2

  公开（公告）日：2014-02-25
• [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.