[5-(8-Hydroxy-1,4-dioxa-spiro[4.5]dec-8-yl)-thiazol-2-yl]-carbamic acid methyl ester | 708274-11-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: [5-(8-Hydroxy-1,4-dioxa-spiro[4.5]dec-8-yl)-thiazol-2-yl]-carbamic acid methyl ester
• 英文别名: Methyl [5-(8-Hydroxy-1,4-dioxaspiro[4.5]dec-8-yl)-1,3-thiazol-2-yl]carbamate；methyl N-[5-(8-hydroxy-1,4-dioxaspiro[4.5]decan-8-yl)-1,3-thiazol-2-yl]carbamate
• CAS: 708274-11-7
• 化学式: C₁₃H₁₈N₂O₅S
• 分子量: 314.362
• InChiKey: GATYSAHRFHMPJQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.69
• 拓扑面积：
  118
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  1,4-环己二酮单乙二醇缩酮 、 thiazole-2-ylcarbamic acid methyl ester 在 正丁基锂 、 氯化铵 作用下， 以 四氢呋喃 、 hexanes 为溶剂， 反应 0.5h， 生成 [5-(8-Hydroxy-1,4-dioxa-spiro[4.5]dec-8-yl)-thiazol-2-yl]-carbamic acid methyl ester
  参考文献：
  名称：

  4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANE ANTAGONISTS OF CCR2

  摘要：

  本发明包括式(I)的化合物。其中：X、R1、R2、R3和R4如规范中定义。该发明还包括一种预防、治疗或改善综合症、疾病或疾病的方法，其中所述综合症、疾病或疾病是2型糖尿病、肥胖和哮喘。该发明还包括通过给哺乳动物施用式(I)的至少一种化合物的治疗有效量来抑制CCR2活性的方法。

  公开号：

  US20100267688A1

文献信息

• 3-Aminopyrrolidine derivaties as modulators of chemokine receptors
  申请人：Xue Chu-Biao

  公开号：US20060252751A1

  公开（公告）日：2006-11-09

  The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

  本发明涉及式I的3-氨基吡咯烷衍生物（其中R1、R2、R3、R4、R5、R6、R7、R8、X、Y和X的定义如本文所述），它们可用作趋化因子受体活性调节剂。特别地，这些化合物可用作趋化因子受体的调节剂，更具体地作为CCR2和/或CCR5受体的调节剂。该发明的化合物和组合物可以结合趋化因子受体，例如CCR2和/或CCR5趋化因子受体，并用于治疗与趋化因子（例如CCR2和/或CCR5）活性相关的疾病，如动脉粥样硬化、再狭窄、狼疮、器官移植排斥和类风湿性关节炎。
• 3-Aminopyrrolidine Derivatives As Modulators Of Chemokine Receptors
  申请人：Xue Chu-Biao

  公开号：US20090247474A1

  公开（公告）日：2009-10-01

  The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

  本发明涉及公式I的3-氨基吡咯烷衍生物（其中R1、R2、R3、R4、R5、R6、R7、R8、X、Y和X如本文所定义），其可用作趋化因子受体活性调节剂。特别地，这些化合物可用作趋化因子受体的调节剂，更具体地作为CCR2和/或CCR5受体的调节剂。本发明的化合物和组合物可以结合趋化因子受体，例如CCR2和/或CCR5趋化因子受体，并且可用于治疗与趋化因子，例如CCR2和/或CCR5活性相关的疾病，例如动脉粥样硬化、再狭窄、狼疮、器官移植排斥和类风湿性关节炎。
• 4-azetidinyl-1-heteroaryl-cyclohexane antagonists of CCR2
  申请人：Janssen Pharmaceutica N.V.

  公开号：US08269015B2

  公开（公告）日：2012-09-18

  The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

  本发明涉及公式（I）的化合物，其中：X，R1，R2，R3和R4如规范中所定义。本发明还包括一种预防、治疗或改善综合症、疾病或疾病的方法，其中所述综合症、疾病或疾病是2型糖尿病、肥胖症和哮喘。本发明还包括一种通过给哺乳动物的C CR2活性抑制剂公式（I）的至少一种化合物治疗的方法。
• 3-aminopyrrolidine derivatives as modulators of chemokine receptors
  申请人：Incyte Corporation

  公开号：US07985730B2

  公开（公告）日：2011-07-26

  The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

  本发明涉及式I的3-氨基吡咯烷衍生物（其中R1、R2、R3、R4、R5、R6、R7、R8、X、Y和X如本文所定义），它们可用作趋化因子受体活性调节剂。特别地，这些化合物可用作趋化因子受体的调节剂，更具体地说，可用作CCR2和/或CCR5受体的调节剂。本发明的化合物和组合物可以结合趋化因子受体，例如CCR2和/或CCR5趋化因子受体，并且可用于治疗与趋化因子（例如CCR2和/或CCR5）活性相关的疾病，例如动脉粥样硬化、再狭窄、狼疮、器官移植排斥和类风湿性关节炎。
• 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS
  申请人：Xue Chu-Biao

  公开号：US20110251168A1

  公开（公告）日：2011-10-13

  The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

  本发明涉及式I的3-氨基吡咯烷衍生物（其中R1、R2、R3、R4、R5、R6、R7、R8、X、Y和X如本文所定义），其可用作趋化因子受体活性调节剂。特别地，这些化合物可用作趋化因子受体的调节剂，更具体地，可用作CCR2和/或CCR5受体的调节剂。本发明的化合物和组合物可结合趋化因子受体，例如CCR2和/或CCR5趋化因子受体，并且可用于治疗与趋化因子（例如CCR2和/或CCR5）活性相关的疾病，例如动脉粥样硬化、再狭窄、狼疮、器官移植排斥和类风湿性关节炎。