rac-N-(2-amino-3-fluoro-2-methylpropyl)-8-[(2,6-difluorobenzyl)oxy]-2,6-dimethylimidazo[1,2-a]pyridine-3-carboxamide Formate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: rac-N-(2-amino-3-fluoro-2-methylpropyl)-8-[(2,6-difluorobenzyl)oxy]-2,6-dimethylimidazo[1,2-a]pyridine-3-carboxamide Formate
• 英文别名: N-(2-amino-3-fluoro-2-methylpropyl)-8-[(2,6-difluorophenyl)methoxy]-2,6-dimethylimidazo[1,2-a]pyridine-3-carboxamide;formic acid
• 化学式: C22H25F3N4O4
• 分子量: 466.5
• InChiKey: CEGWCSBNIDQYJA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.93
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  119
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  rac-Benzyl {1-[({8-[(2,6-difluorobenzyl)oxy]-2,6-dimethylimidazo[1,2-a]pyridin-3-yl}carbonyl)amino]-3-fluoro-2-methylpropan-2-yl}carbamate 在 氢氧化钯 氩 、 乙醇 、 acetonitrile-water 、 三氟乙酸 作用下， 以 乙醇 为溶剂， 反应 16.0h， 生成 rac-N-(2-amino-3-fluoro-2-methylpropyl)-8-[(2,6-difluorobenzyl)oxy]-2,6-dimethylimidazo[1,2-a]pyridine-3-carboxamide Formate
  参考文献：
  名称：

  AMINO-SUBSTITUTED IMIDAZO[1,2-A]PYRIDINECARBOXAMIDES AND THEIR USE

  摘要：

  本申请涉及新型取代的咪唑并[1,2-a]吡啶-3-羧酰胺，其制备方法，其单独或与其他药物联合用于治疗和/或预防疾病，以及其用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管疾病。

  公开号：

  US20150274719A1

文献信息

• Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20140179672A1

  公开（公告）日：2014-06-26

  The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

  本申请涉及新型取代的咪唑并[1,2-a]吡啶-3-羧酰胺，其制备过程，它们单独或与其他药物组合用于治疗和/或预防疾病，以及它们用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管疾病。
• THE USE OF SGC STIMULATORS AND SGC ACTIVATORS ALONE OR IN COMBINATION WITH PDE5 INHIBITORS FOR THE TREATMENT OF BONE DISORDERS INCLUDING OSTEOGENESIS IMPERFECTA (OI)
  申请人：Bayer AG

  公开号：EP3498298A1

  公开（公告）日：2019-06-19

  The present invention relates to sGC stimulators and sGC activators alone or in combination with PDE5 inhibitors or other combination partners for use in the treatment and/or prophylaxis of bone disorders, including osteogenesis imperfecta (OI).

  本发明涉及sGC刺激剂和sGC激活剂，可单独使用，也可与PDE5抑制剂或其他组合伙伴结合使用，用于治疗和/或预防骨质紊乱，包括成骨不全症（OI）。
• THE USE OF NON-STEROIDAL MINERALOCORTICOID RECEPTOR ANTAGONISTS ALONE OR IN COMBINATION FOR THE TREATMENT OF MUSCULAR OR NEUROMUSCULAR DISEASES
  申请人：Bayer Aktiengesellschaft

  公开号：EP3566704A1

  公开（公告）日：2019-11-13

  The present disclosure relates to non-steriodal mineralocorticoid receptor (MR) and the pharmacology of mineralocorticoid receptor antagonists (MR Antagonists, MRAs). In particular, the invention relates to MRAs alone (preferably finerenone), or preferably in combination with sGC stimulators and/or sGC activators (preferably BAY 41-2272), for use in the prevention and/or treatment of muscular or neuromuscular diseases, especially for the treatment of Duchenne Muscular Dystrophy (DMD).

  本公开涉及非甾体类矿物皮质激素受体（MR）和矿物皮质激素受体拮抗剂（MR 拮抗剂，MRAs）的药理学。特别是，本发明涉及单独使用（优选非格列酮）或优选与sGC刺激剂和/或sGC激活剂（优选BAY 41-2272）联合使用的MRAs，用于预防和/或治疗肌肉或神经肌肉疾病，特别是治疗杜氏肌肉萎缩症（DMD）。
• METHOD OF IDENTIFYING A SUBGROUP OF PATIENTS SUFFERING FROM DCSSC WHICH BENEFITS FROM A TREATMENT WITH SGC STIMULATORS AND SGC ACTIVATORS IN A HIGHER DEGREE THAN A CONTROL GROUP
  申请人：Adverio Pharma GmbH

  公开号：EP3574905A1

  公开（公告）日：2019-12-04

  The present invention relates to a method of identifying a subgroup of patients suffering from diffuse cutaneous systemic sclerosis (dcSSc) which subgroup of patients benefits from a treatment with at least one sGC stimulator and/or sGC activator in a higher degree than patients not belonging to this subgroup.

  本发明涉及一种确定弥漫性皮肤系统性硬化症（dcSSc）患者亚群的方法，该亚群患者从至少一种sGC刺激剂和/或sGC激活剂的治疗中获益的程度高于不属于该亚群的患者。
• Amino-substituted imidazo[1,2-A] pyridinecarboxamides and their use
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US10662185B2

  公开（公告）日：2020-05-26

  The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides of the general formula (I) to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

  本申请涉及通式 (I) 的新型取代咪唑并[1,2-a]吡啶-3-甲酰胺 它们的制备工艺，它们在治疗和/或预防疾病方面的单独用途或组合用途，以及它们在制备治疗和/或预防疾病（尤其是治疗和/或预防心血管疾病）的药物方面的用途。