4-amino-3-ethoxyphenylacetic acid ethyl ester | 594844-43-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 4-amino-3-ethoxyphenylacetic acid ethyl ester
• 英文别名: ethyl 4-amino-3-ethoxyphenylacetate；Ethyl 2-(4-amino-3-ethoxyphenyl)acetate
• CAS: 594844-43-6
• 化学式: C₁₂H₁₇NO₃
• 分子量: 223.272
• InChiKey: VNJULQOLWZRPST-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  16
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  61.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-amino-3-ethoxyphenylacetic acid ethyl ester 、 4'-trifluoromethylbiphenyl-2-carbonyl chloride 生成 Ethyl 2-[3-ethoxy-4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]phenyl]acetate
  参考文献：
  名称：

  EP1669345

  摘要：

  公开号：

文献信息

• ESTER COMPOUND AND MEDICINAL USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：EP1479666A1

  公开（公告）日：2004-11-24

  A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1") (wherein    R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.;    X is -COO- or -CON(R10)-;    R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.;    R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.;    R8 and R9 are each independently hydrogen atom, C1-C6 alkyl, -CON(R18)(R19) or -COO(R20), etc.;    ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.;    Alk1 and Alk2 are each independently alkanediyl, etc.;    l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

  一种治疗高脂血症的新型药物，其为酯化合物，由式(1")表示（其中：R1和R2均为氢原子或可选择取代的芳基等；X为-COO-或-CON(R10)-；R3和R4均为氢原子、C1-C6烷基或C1-C6烷氧基等；R5、R6和R7均为氢原子、C1-C6烷基或C1-C6烷氧基等；R8和R9各自独立地为氢原子、C1-C6烷基、-CON(R18)(R19)或-COO(R20)等；环A、环B和环C各自独立地为芳基或杂环残基等；Alk1和Alk2各自独立地为脂肪二亚基等；l和m均为0或1至3的整数），或其前药，或其药学上可接受的盐。该治疗剂能够选择性地抑制小肠中的MTP，因此不会引起脂肪肝等副作用。
• Ester derivatives and medical use thereof
  申请人：Hagiwara Atsushi

  公开号：US20060205726A1

  公开（公告）日：2006-09-14

  A therapeutic agent for hyperlipidemia which has no side effects on the liver unlike conventional MTP inhibitors and has excellent MTP inhibitory activity. Also, provided is an ester compound represented by the general formula (1): or a pharmaceutically acceptable salt thereof.

  一种治疗高血脂症的药物，与传统的MTP抑制剂不同，没有对肝脏产生副作用，并具有优秀的MTP抑制活性。同时，提供了一种由通式（1）表示的酯化合物，或其药学上可接受的盐。
• Ester compound and medicinal use thereof
  申请人：Hagiwara Atsushi

  公开号：US20050075367A1

  公开（公告）日：2005-04-07

  A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1″) (wherein R 1 and R 2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R 10 )—; R 3 and R 4 are each hydrogen atom, C 1 -C 6 alkyl or C 1 -C 6 alkoxy, etc.; R 5 , R 6 and R 7 are each hydrogen atom, C 1 -C 6 alkyl or C 1 -C 6 alkoxy, etc.; R 8 and R 9 are each independently hydrogen atom, C 1 -C 6 alkyl, —CON(R 18 )(R 19 ) or —COO(R 20 ), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk 1 and Alk 2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

  一种治疗高脂血症的新型药物，其为酯化合物，由式（1”）所表示（其中，R1和R2分别为氢原子或可选取代的芳基等；X为—COO—或—CON(R10)—；R3和R4分别为氢原子、C1-C6烷基或C1-C6烷氧基等；R5、R6和R7分别为氢原子、C1-C6烷基或C1-C6烷氧基等；R8和R9分别独立地为氢原子、C1-C6烷基、—CON(R18)(R19)或—COO(R20)等；环A、环B和环C分别独立地为芳基或杂环残基等；Alk1和Alk2分别独立地为脂肪二亚基等；l和m分别为0或1至3的整数），或其前药，或其药学上可接受的盐。该治疗剂能够选择性地抑制小肠中的MTP，从而不会引起脂肪肝等副作用。
• ESTER COMPOUND AND MEDICAL USE THEREOF
  申请人：Hagiwara Atsushi

  公开号：US20100158996A1

  公开（公告）日：2010-06-24

  A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1″) (wherein R 1 and R 2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R 10 )—; R 3 and R 4 are each hydrogen atom, C 1 -C 6 alkyl or C 1 -C 6 alkoxy, etc.; R 5 , R 6 and R 7 are each hydrogen atom, C 1 -C 6 alkyl or C 1 -C 6 alkoxy, etc.; R 9 and R 9 are each independently hydrogen atom, C 1 -C 6 alkyl, —CON(R 18 ) (R 19 ) or —COO(R 20 ), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk 1 and Alk 2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

  一种治疗高脂血症的新型药物，其为酯化合物，由式（1″）所表示（其中R1和R2分别为氢原子或可选择取代的芳基等；X为—COO—或—CON(R10)—；R3和R4分别为氢原子、C1-C6烷基或C1-C6烷氧基等；R5、R6和R7分别为氢原子、C1-C6烷基或C1-C6烷氧基等；R8和R9分别独立地为氢原子、C1-C6烷基、—CON(R18)(R19)或—COO(R20)等；环A、环B和环C分别独立地为芳基或杂环残基等；Alk1和Alk2分别独立地为脂肪二亚基等；l和m分别为0或1至3的整数），或其前药，或其药学上可接受的盐。该治疗剂选择性地抑制小肠中的MTP，从而不会引起脂肪肝等副作用。
• ESTER DERIVATIVE AND MEDICINAL USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：EP1669345A1

  公开（公告）日：2006-06-14

  A therapeutic agent for hyperlipidemia which has no side effects on the liver unlike conventional MTP inhibitors and has excellent MTP inhibitory activity. Also, provided is an ester compound represented by the general formula (1): or a pharmaceutically acceptable salt thereof.

  一种治疗高脂血症的药物，它与传统的 MTP 抑制剂不同，对肝脏没有副作用，并且具有优异的 MTP 抑制活性。此外，还提供了一种由通式（1）代表的酯类化合物： 或其药学上可接受的盐。