1-methyl-5-oxopyrrolidine-2-carboxamide | 3770-16-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-methyl-5-oxopyrrolidine-2-carboxamide
• CAS: 3770-16-9
• 化学式: C₆H₁₀N₂O₂
• mdl: MFCD19208267
• 分子量: 142.158
• InChiKey: KLBSBVDLPIOJRF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  63.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-methyl-5-oxopyrrolidine-2-carboxamide 、 5-bromo-7-(3-(trifluoromethyl)phenoxy)-2,3-dihydrobenzo[b][1,4]dioxine 在 caesium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 、 bis(dibenzylideneacetone)-palladium⁽⁰⁾ 作用下， 以 甲苯 为溶剂， 以0.0286 g的产率得到1-methyl-5-oxo-N-(7-(3-(trifluoromethyl)phenoxy)-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)pyrrolidine-2-carboxamide
  参考文献：
  名称：

  [EN] TEAD INHIBITORS
  [FR] INHIBITEURS DE TEAD

  摘要：

  The present invention relates to a compound of formula (I) wherein A, Z, L, R1, R2, R3, R4, R5and R33are as defined in claim 1, or a pharmaceutically acceptable salt thereof. The compounds of formula (I) possess utility as inhibitors of TEAD. The compounds are useful as medicaments in the treatment of diseases or conditions wherein inhibition of TEAD is desired, such as cancer and chronic pain.

  公开号：

  WO2022219246A1

文献信息

• 1-AMIDO-4-PHENYL-4-BENZYLOXYMETHYL-PIPERIDINE DERIVATIVES AND RELATED COMOUNDS AS NEUROKININ-1 (NK-1) ANTAGONSISTS FOR THE TREATMENT OF EMESIS, DEPRESSION, ANXIETY AND COUGH
  申请人：SCHERING CORPORATION

  公开号：EP1536797B1

  公开（公告）日：2007-04-04
• [EN] COMBINATIONS OF PROLINAMIDE P2X7 MODULATORS WITH FURTHER THERAPEUTIC AGENTS<br/>[FR] COMBINAISONS FORMÉES DE MODULATEURS AU PROLINAMIDE DU RÉCEPTEUR P2X7 ET D'AUTRES AGENTS THÉRAPEUTIQUES
  申请人：GLAXO GROUP LTD

  公开号：WO2009074518A1

  公开（公告）日：2009-06-18

  The invention provides a combination comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof: formula (I), together with a further therapeutic agent or agents; and the use of the combination in the treatment or prevention of pain, inflammation or a neurodegenerative disease. The compounds of formula (I) are thought to be P2X7 receptor antagonists. The compound of formula (I) is preferably N-[2-chloro-3-(trifluoromethyl)phenyl]methyl}- 1 -methyl-5-oxo-L-prolinamide. The further therapeutic agent can e.g. be methotrexate, an NSAID, a TNFα inhibitor, sulfasalazine, a statin, a glucocorticoid agent, an anti-IL-1 monoclonal antibody, or an anti-CD20 monoclonal antibody; e.g. for the treatment of rheumatoid arthritis. The further therapeutic agent can be capable of treating inflammatory or neuropathic pain, e.g. paracetamol, an opioid (e.g. morphine, fentanyl, oxycodone, or tramadol), pregabalin, gabapentin, gabapentin enacarbil, or carbamazepine.