1-(4-氟苯基)环丁胺 | 920501-69-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 1-(4-氟苯基)环丁胺
• 英文名称: 1-(4-fluorophenyl)cyclobutane-1-amine
• 英文别名: 1-(4-Fluorophenyl)cyclobutanamine；1-(4-fluorophenyl)cyclobutan-1-amine
• CAS: 920501-69-5
• 化学式: C₁₀H₁₂FN
• mdl: MFCD09904384
• 分子量: 165.21
• InChiKey: PAPAYUQUJVLXAF-UHFFFAOYSA-N

物化性质

• 沸点：
  229.0±33.0 °C(Predicted)
• 密度：
  1.136±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(4-氟苯基)环丁胺 、 在 benzotriazol-1-yloxy-tris(dimethylamino)-phosphonium chloride 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 生成 (1R,2R)-N-(1-(4-fluorophenyl)cyclobutyl)-2-(5-phenylisoxazol-3-yl)cyclopentanecarboxamide
  参考文献：
  名称：

  Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain

  摘要：

  A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na(v)1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement on Na(v)1.7 inhibitory activity. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.07.135

文献信息

• Amide Derivatives as Kinase Inhibitors
  申请人：Defert Olivier Raynald

  公开号：US20090118283A1

  公开（公告）日：2009-05-07

  The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar 1 , Ar 2 , R 1 , R 3 , p and n have the meaning defined in the claims In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.

  本发明涉及新的AGC激酶抑制剂，特别是公式（I）或（II）的化合物或其立体异构体、互变异构体、外消旋体、代谢物、前药或前药、盐、水合物或溶剂化物，其中Ar1、Ar2、R1、R3、p和n在权利要求中定义。特别地，本发明涉及更具体的AGC激酶抑制剂、包含这种抑制剂的组合物，特别是药物，以及在治疗和预防疾病中使用这种抑制剂的用途。
• Indazole and Pyrazolopyridine Compounds As CCR1 Receptor Antagonists
  申请人：Cook Brian Nicholas

  公开号：US20120270870A1

  公开（公告）日：2012-10-25

  Diclosed are CCR1 receptor antagonists of the formula (I) wherein Ar 1 , Ar 2 , R 1 , X and G are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).

  本发明公开了式(I)的CCR1受体拮抗剂，其中Ar1、Ar2、R1、X和G在此公开。还公开了式(I)化合物的组合物、制备方法和使用方法。
• CANNABINOID RECEPTOR MODULATORS
  申请人：Jones Robert M.

  公开号：US20120214766A1

  公开（公告）日：2012-08-23

  The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

  本发明涉及公式Ia的某些化合物及其制药组合物，其调节大麻素CB2受体的活性。本发明还涉及公式Ia的某些化合物及其制药组合物，其调节CB1受体和CB2受体的活性。本发明的化合物和制药组合物适用于治疗以下疾病的方法：疼痛，例如骨骼和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛，炎性疼痛，神经痛，由治疗副作用引起的疼痛和与骨关节炎相关的疼痛；过敏症；炎性过敏症；神经病性过敏症；急性疼痛感受；骨质疏松症；多发性硬化症相关痉挛；自身免疫疾病；过敏反应；中枢神经系统炎症；动脉粥样硬化；不良的免疫细胞活动和炎症；年龄相关的黄斑变性；咳嗽；白血病；淋巴瘤；中枢神经系统肿瘤；前列腺癌；阿尔茨海默病；中风引起的损伤；痴呆症；肌萎缩性侧索硬化症和帕金森病。
• 4-Piperidylbenzamides as 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
  申请人：NOVO NORDISK A/S

  公开号：EP1878721A1

  公开（公告）日：2008-01-16

  A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxy-steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

  本文描述了通式（I）的一类新型化合物、它们在治疗中的用途、包含这些化合物的药物组合物以及它们在制造药物中的用途。本化合物可调节 11β- 羟基类固醇脱氢酶 1 型（11βHSD1）的活性，因此可用于治疗这种调节有益的疾病，如代谢综合征。
• Cannabinoid receptor modulators
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US11214548B2

  公开（公告）日：2022-01-04

  The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

  本发明涉及某些调节大麻素 CB2 受体活性的式 Ia 化合物及其药物组合物。本发明还涉及某些能调节 CB1 受体和 CB2 受体活性的式 Ia 化合物及其药物组合物。本发明的化合物及其药物组合物用于治疗以下疾病的方法：疼痛，例如骨痛和关节痛、肌肉痛、牙痛、偏头痛和其他头痛、炎症性疼痛、神经性疼痛、作为治疗药物的不良反应出现的疼痛以及与骨关节炎相关的疼痛；痛觉减退；异动症；炎症性痛觉减退；神经性痛觉减退；急性痛觉；骨质疏松症；多发性硬化症相关的痉挛、自身免疫性疾病、过敏反应、中枢神经系统炎症、动脉粥样硬化、不想要的免疫细胞活性和炎症、老年性黄斑变性、咳嗽、白血病、淋巴瘤、中枢神经系统肿瘤、前列腺癌、阿尔茨海默病、中风引起的损伤、痴呆、肌萎缩性脊髓侧索硬化症和帕金森病。