1-(Oxazolo[4,5-b]pyridin-2-yl)-1-oxo-decane | 288862-74-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶唑并吡啶类
• 英文名称: 1-(Oxazolo[4,5-b]pyridin-2-yl)-1-oxo-decane
• 英文别名: 1-[1,3]Oxazolo[4,5-b]pyridin-2-yldecan-1-one；1-([1,3]oxazolo[4,5-b]pyridin-2-yl)decan-1-one
• CAS: 288862-74-8
• 化学式: C₁₆H₂₂N₂O₂
• 分子量: 274.363
• InChiKey: ZISOEDFMAVZYAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  20
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  56
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Inhibitors of fatty acid amide hydrolase
  申请人：Boger L. Dale

  公开号：US20050239785A1

  公开（公告）日：2005-10-27

  Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K i 's below 200 pM and activities 10 2 -10 3 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an α-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other π-unsaturation corresponding to the arachidonyl Δ 8,9 /Δ 11,12 and/or oleyl Δ 9,10 positions. A preferred α-keto heterocylic head group is α-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).

  构建了具有Ki低于200 pM和比相应的三氟甲基酮活性高102-103倍的脂肪酸酰胺酶（FAAH）的有效抑制剂。这些有效的抑制剂结合了几个特征，即：1）α-酮杂环头基团；2）使用最佳C12-C8链长度的碳氢化合物连接单元；和3）与花生四烯酸Δ8,9/Δ11,12和/或油酸Δ9,10位置相对应的苯基或其他π-不饱和度。首选的α-酮杂环头基团是α-酮N4噁唑吡啶，并结合第二个弱碱性氮。脂肪酸酰胺酶是一种酶，负责降解油酰胺（一种内源性诱导睡眠的脂质）和阿那达胺（一种内源性的大麻素受体配体）。
• INHIBITORS OF FATTY ACID AMIDE HYDROLASE
  申请人：Boger Dale L.

  公开号：US20090270421A1

  公开（公告）日：2009-10-29

  Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K i 's below 200 pM and activities 10 2 -10 3 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an α-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other π-unsaturation corresponding to the arachidonyl Δ 8,9 /Δ 11,12 and/or oleyl Δ 9,10 positions. A preferred α-keto heterocylic head group is α-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).

  具有Ki值低于200 pM的脂肪酸酰胺水解酶（FAAH）的强效抑制剂被构建出来，其活性比相应的三氟甲基酮高102-103倍。这些强效抑制剂结合了几个特征，即：1）α-酮杂环头基团；2）使用最佳C12-C8链长的烃链连接单元；和3）与花生四烯酸Δ8,9/Δ11,12和/或油酸Δ9,10位置相对应的苯基或其他π-不饱和度。首选的α-酮杂环头基团是α-酮N4噁唑吡啶，并结合第二个弱碱性氮。脂肪酸酰胺水解酶是一种酶，负责降解油酰胺（一种内源性诱导睡眠的脂质）和阿那达胺（一种内源性的大麻素受体配体）。
• NEW INDOLE DERIVATIVES AS FACTOR XA INHIBITORS
  申请人：NAZARE Mark

  公开号：US20090069565A1

  公开（公告）日：2009-03-12

  The present invention relates to compounds of formula I, in which R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; R 5 ; R 6 ; R 7 ; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.

  本发明涉及式I的化合物，其中R0; R1; R2; R3; R4; R5; R6; R7; Q; V，G和M具有声明中指示的含义。式I的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓作用，例如适用于治疗和预防心血管疾病，如血栓栓塞性疾病或再狭窄。它们是血凝酶酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以应用于存在因子Xa和/或因子VIIa不良活性的情况，或者治疗或预防需要抑制因子Xa和/或因子VIIa的情况。此外，本发明还涉及制备式I化合物的方法，它们的用途，特别是作为治疗上述疾病的药物以及包含它们的制药制剂。
• US6462054B1
  申请人：——

  公开号：US6462054B1

  公开（公告）日：2002-10-08
• US6891043B2
  申请人：——

  公开号：US6891043B2

  公开（公告）日：2005-05-10