(cis)-3-phenyl-8-({[4-(2-pyridinyl)-1,3-thiazol-2-yl]amino}methyl)-1-oxa-3-azaspiro[4.5]-decan-2-one | 1044267-94-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: (cis)-3-phenyl-8-({[4-(2-pyridinyl)-1,3-thiazol-2-yl]amino}methyl)-1-oxa-3-azaspiro[4.5]-decan-2-one
• 英文别名: (cis)-3-phenyl-8-({[4-(2-pyridyl)-1,3-thiazol-2-yl]amino}methyl)-1-oxa-3-azaspiro[4.5]-decan-2-one
• CAS: 1044267-94-8
• 化学式: C₂₃H₂₄N₄O₂S
• 分子量: 420.535
• InChiKey: YMYLSDPBBPCICV-LBEPJEHYSA-N

反应信息

• 作为产物：
  描述：

  在 三乙酰氧基硼氢化钠 、 溶剂黄146 作用下， 以 二氯甲烷 为溶剂， 生成 (cis)-3-phenyl-8-({[4-(2-pyridinyl)-1,3-thiazol-2-yl]amino}methyl)-1-oxa-3-azaspiro[4.5]-decan-2-one
  参考文献：
  名称：

  Discovery and structure–activity relationship of a novel spirocarbamate series of NPY Y5 antagonists

  摘要：

  A novel series of trans-8-aminomethyl-1-oxa-3-azaspiro[4.5] decan-2-one derivatives was identified with potent NPY Y5 antagonist activity. Optimization of the original lead furnished compounds 23p and 23u, which combine sub-nanomolar Y5 activity with metabolic stability, oral bioavailability, brain penetration and strong preclinical profile for development. Both compounds significantly inhibited the food intake induced by a Y5 selective agonist with minimal effective doses of 3 mg/kg po. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.08.041

文献信息

• Chemical Compounds
  申请人：Bentley Jonathan

  公开号：US20090042897A1

  公开（公告）日：2009-02-12

  The present invention relates to novel compounds or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of: (trans)-8-([1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(2-fluoro-3-pyridinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-([1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(3-pyridazinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-([1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(1-methyl-1H-pyrazol-3-yl)-1-oxa-3-azaspiro[4.5]decan-2-one; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.

  本发明涉及一组新化合物或其药学上可接受的盐或溶剂，所述化合物从以下组中选择：（顺式）-8-（[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（2-氟-3-吡啶基）-1-氧杂-3-氮杂螺[4.5]癸烷-2-酮；（顺式）-8-（[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（3-吡嗪基）-1-氧杂-3-氮杂螺[4.5]癸烷-2-酮；（顺式）-8-（[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（1-甲基-1H-吡唑-3-基）-1-氧杂-3-氮杂螺[4.5]癸烷-2-酮；以及用于它们的制备的中间体，包含它们的药物组合物以及它们作为NPY Y5受体拮抗剂和治疗和/或预防暴食障碍等进食障碍的药物的用途。