3-(3,4-dichlorophenyl)-2-oxo-N-[4-(2-pyridinyl)-1,3-thiazol-2-yl]-1-oxa-3,8-diazaspiro[4.5]decane-8-carboxamide | 1044574-06-2

• 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: 3-(3,4-dichlorophenyl)-2-oxo-N-[4-(2-pyridinyl)-1,3-thiazol-2-yl]-1-oxa-3,8-diazaspiro[4.5]decane-8-carboxamide
• 英文别名: 3-(3,4-Dichlorophenyl)-2-oxo-N-[4-(2-pyridinyl)-1,3-thiazol-2-yl]-1-oxa-3,8-diazaspiro-[4.5]decane-8-carboxamide；3-(3,4-dichlorophenyl)-2-oxo-N-(4-pyridin-2-yl-1,3-thiazol-2-yl)-1-oxa-3,8-diazaspiro[4.5]decane-8-carboxamide
• CAS: 1044574-06-2
• 化学式: C₂₂H₁₉Cl₂N₅O₃S
• 分子量: 504.397
• InChiKey: ZJSGMPSVLHPTDX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  33
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  116
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  苯基[4-(2-吡啶基)-1,3-噻唑-2-基]氨基甲酸酯 、 3-(3,4-dichlorophenyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one 在 N,N-二异丙基乙胺 作用下， 以 乙腈 为溶剂， 反应 2.5h， 以87%的产率得到3-(3,4-dichlorophenyl)-2-oxo-N-[4-(2-pyridinyl)-1,3-thiazol-2-yl]-1-oxa-3,8-diazaspiro[4.5]decane-8-carboxamide
  参考文献：
  名称：

  WO2008/92887

  摘要：

  公开号：

文献信息

• I-OXA-3-Azaspiro (4.5) Decan-2-One And 1-OXA-3, 8-Diazaspiro (4.5) Decan-2-One Derivatives For The Treatment of Eating Disorders
  申请人：Bentley Jonathan

  公开号：US20100197699A1

  公开（公告）日：2010-08-05

  The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; W is —CZ 1 or nitrogen; Z 1 is hydrogen, C1-C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is —CZ 1 , compounds of formula (I) have a trans stereochemistry; 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.

  本发明涉及式（I）的新化合物，或其药学上可接受的盐或溶剂，其中R是芳基或杂环芳基；可以被一个或多个卤素，C1-C4烷基，C1-C4烷氧基，C1-C4卤代烷基，C1-C4卤代烷氧基，氰基取代；W是—CZ1或氮；Z1是氢，C1-C4烷基；A是5元杂环芳基，吡嗪，嘧啶或喹啉或喹嗪，可以被一个或多个卤素，C1-C4烷基，C1-C4烷氧基，C1-C4卤代烷基，C1-C4卤代烷氧基，氰基取代；B是氢或一个5-10元芳基或杂环芳基，可以被一个或多个卤素，C1-C4烷基，C1-C4烷氧基，C1-C4卤代烷基，C1-C4卤代烷氧基，氰基取代；A和B通过任何原子连接；但当W是—CZ1时，式（I）的化合物具有反式立体化学；其制备方法，用于这些方法的中间体，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/或预防暴食障碍的药物代理的用途。
• I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS
  申请人：Glaxo Group Limited

  公开号：EP2121673A1

  公开（公告）日：2009-11-25
• [EN] I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS<br/>[FR] DÉRIVÉS 1-OXA-3-AZASPIRO [4,5] DÉCANE-2-ONE ET 1-OXA-3,8-DIAZASPIRO [4,5] DÉCANE-2-ONE POUR LE TRAITEMENT DE TROUBLES DE L'ALIMENTATION
  申请人：GLAXO GROUP LTD

  公开号：WO2008092887A1

  公开（公告）日：2008-08-07

  [EN] The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1 -C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; W is -CZ₁ or nitrogen; Z₁ is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C₄ alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ₁, compounds of formula (I) have a trans stereochemistry; 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.
  [FR] L'invention concerne de nouveaux composés de formule (I) ou un sel ou un solvate pharmaceutiquement acceptable de ceux-ci, R étant aryle ou hétéroaryle; pouvant être substitué par : halogène, C1-C4-alkyle, C1-C4-alcoxy, C1-C4-haloalkyle, C1-C4-haloalcoxy et/ou cyano; W étant -CZ₁ ou azote; Z₁ étant hydrogène ou C1-C4-alkyle; A étant hétéroaryle, pyrazine, pyrimidine, quinoléine ou quinazoline à 5 éléments, pouvant être substitué par halogène, C1-C4-alkyle, C1-C4-alkoxy, C1-C4-haloalkyle, C1-C4-haloalkoxy et/ou cyano; B étant hydrogène ou un aryle ou hétéroaryle à 5 éléments pouvant être substitué par : halogène, C1-C4-alkyle, C1-C4-alcoxy, C1-C4-haloalkyle, C1-C4-haloalcoxy et/ou cyano; A et B étant liés par n'importe quel atome; à la condition que lorsque W est -CZ₁, les composés de formule (I) ont une stéréochimie trans. L'invention concerne également des procédés de fabrication de ces composés, des intermédiaires employés dans ces procédés, des compositions pharmaceutiques contenant ces composés et leur utilisation en thérapie, en tant qu'antagonistes du récepteur de NPY Y5, et en tant qu'agents pour le traitement et/ou la prophylaxie de troubles de l'alimentation tels que la frénésie alimentaire.
• WO2008/92887
  申请人：——

  公开号：——

  公开（公告）日：——