3,3-Difluorooxane-4-carboxylic acid | 1504681-05-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧唑烯
• 英文名称: 3,3-Difluorooxane-4-carboxylic acid
• CAS: 1504681-05-3
• 化学式: C₆H₈F₂O₃
• 分子量: 166.12
• InChiKey: GPLIATFXEYJWET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] CONDENSED SUBSTITUTED HYDROPYRROLES AS ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4<br/>[FR] HYDROPYRROLES SUBSTITUÉS CONDENSÉS EN TANT QU'ANTAGONISTES DU RÉCEPTEUR MUSCARINIQUE M4 DE L'ACÉTYLCHOLINE
  申请人：UNIV VANDERBILT

  公开号：WO2021216951A1

  公开（公告）日：2021-10-28

  Disclosed herein are substituted hexahydro-l//-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

  本文披露了一种替代的六氢-1H-环戊[ c ]吡咯化合物，可能作为肌碱乙酰胆碱受体M4（mAChR M4）的拮抗剂有用。本文还披露了制备这些化合物的方法、包含这些化合物的药物组合物以及使用这些化合物和组合物治疗疾病的方法。
• [EN] INDAZOLE DERIVATIVES AS ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4<br/>[FR] DÉRIVÉS D'INDAZOLE UTILISÉS EN TANT QU'ANTAGONISTES DU RÉCEPTEUR MUSCARINIQUE M4 DE L'ACÉTYLCHOLINE
  申请人：UNIV VANDERBILT

  公开号：WO2022212819A1

  公开（公告）日：2022-10-06

  Disclosed herein are (6-(2H-indazol-5-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5- amine compounds, useful as antagonists of the muscarinic acetylcholine receptor M4(mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

  本文揭示了(6-(2H-吲唑-5-基)吡啶并[3,4-d]嘧啶-3-基)八氢环戊[c]吡咯-5-胺类化合物，用作肌动蛋白乙酰胆碱受体M4(mAChR M4)的拮抗剂。本文还揭示了制备该化合物的方法、包含该化合物的制药组合物以及使用该化合物和组合物治疗疾病的方法。
• [EN] ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4<br/>[FR] ANTAGONISTES DU RÉCEPTEUR MUSCARINIQUE D'ACÉTYLCHOLINE M4
  申请人：[en]VANDERBILT UNIVERSITY

  公开号：WO2022140499A1

  公开（公告）日：2022-06-30

  Disclosed herein are compounds of formula (III) useful as antagonists of the muscarinic acetylcholine receptor M4(mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurodegenerative disorders using the compounds and compositions. (Formula (III))
• [EN] (4-(6-((2-OCTAHYDROCYCLOPENTA[C]PYRROL-5-YL)AMINO)PYRIDAZIN-3-YL)PHENYL)(IMINO)(METHYL)-LAMBDA6- SULFANONE DERIVATIVES AND SIMILAR COMPOUNDS AS MUSCARINIC ACETYLCHOLINE RECEPTOR M4 ANTAGONISTS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS<br/>[FR] DÉRIVÉS DE (4-(6-((2-OCTAHYDROCYCLOPENTA[C]PYRROL-5-YL)AMINO)PYRIDAZIN-3-YL)PHÉNYL)(IMINO)(MÉTHYL)-LAMBDA6-SULFANONE ET COMPOSÉS ANALOGUES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR MUSCARINIQUE M4 DE L'ACÉTYLCHOLINE POUR LE TRAITEMENT DE TROUBLES NEURODÉGÉNÉRATIFS
  申请人：[en]VANDERBILT UNIVERSITY

  公开号：WO2022261427A1

  公开（公告）日：2022-12-15

  Disclosed are compounds of formula (I) wherein G1is as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4) for use in the treatment of e.g. a neurodegenerative disorder, a movement disorder, or a brain disorder, such as e.g. Parkinson's disease, drug-induced Parkinsonism, dystonia, Tourette's syndrome, dyskinesias, schizophrenia, cognitive deficits associated with schizophrenia, excessive daytime sleepiness, attention deficit hyperactivity disorder (ADHD), Huntington's disease, chorea, cerebral palsy, and progressive supranuclear palsy. An exemplary compound is e.g. (2,5-difluoro-4-(6-(((3aR,5s,6aS)-2- ((tetrahydro-2H-pyran-4-yl)methyl)octahydrocyclopenta[c]pyrrol-5- yl)amino)pyridazin-3-yl)phenyl)(imino)(methyl)-A -sulfanone (e.g. example 12; compound no. 7) Pharmacological data on the activity of the compounds in an mAChR M4 cell-based assay are provided (e.g. table 2)