2-Amino-3-hydroxy-1-phenyl-7-[(pyridin-2-yl)oxy]heptan-4-one | 235763-33-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-Amino-3-hydroxy-1-phenyl-7-[(pyridin-2-yl)oxy]heptan-4-one
• 英文别名: 2-amino-3-hydroxy-1-phenyl-7-pyridin-2-yloxyheptan-4-one
• CAS: 235763-33-4
• 化学式: C₁₈H₂₂N₂O₃
• 分子量: 314.4
• InChiKey: RGAQHFURJIAYJC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  23
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  85.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• NOVEL ACETAMIDE DERIVATIVES AND PROTEASE INHIBITORS
  申请人：NIPPON KAYAKU KABUSHIKI KAISHA

  公开号：EP0936216A1

  公开（公告）日：1999-08-18

  The present invention relates to novel acetamide derivatives having a substituted heterocyclic group and consecutive dicarbonyl structures, for example 1-pyrimidinylacetamide compounds, 1-pyrazinylacetamide compounds, 1-triazinylacetamide compounds etc., and these compounds have inhibitory activity on chymotrypsin type proteases and are useful as inhibitors for said enzymes, particularly as chymase inhibitors. The novel acetamide derivatives of the present invention are shown in formula (I) below: wherein R0 is substituted or unsubstituted phenyl; R1 is aryl, heteroaryl or aliphatic lower alkyl which may be substituted or unsubstituted; R2 is substituted or unsustituted alkyl, arylalkyl, or heteroarylalkyl; R3 is hydrogen; acyl group; sulfonyl group; isocyanate group; thiourea; or hydrogen, a lower alkyl or a substituted lower alkyl; aryl (1-7C) alkyl, heteroaryl (1-7C) alkyl, aryl and heteroaryl; X and Y independently represent a nitrogen atom or a carbon atom; and Z is a polymethylene group wherein a hydrogen atom in the polymethylene may be replaced.

  本发明涉及具有取代杂环基团和连续二羰基结构的新型乙酰胺衍生物，例如1-嘧啶基乙酰胺化合物、1-吡嗪基乙酰胺化合物、1-三嗪基乙酰胺化合物等，这些化合物对糜蛋白酶型蛋白酶具有抑制活性，可用作上述酶的抑制剂，特别是糜蛋白酶抑制剂。本发明的新型乙酰胺衍生物如下式(I)所示： 其中 R0 是取代或未取代的苯基；R1 是芳基、杂芳基或可取代或未取代的脂肪族低级烷基；R2 是取代或未取代的烷基、芳烷基或杂芳基；R3 是氢；酰基；磺酰基；异氰酸酯基；硫脲；或氢、低级烷基或取代的低级烷基；芳基（1-7C）烷基、杂芳基（1-7C）烷基、芳基和杂芳基； X 和 Y 独立地代表一个氮原子或一个碳原子；Z 是一个聚亚甲基，其中聚亚甲基中的一个氢原子可被取代。
• NOVEL ACETAMIDE DERIVATIVE AND USE THEREOF
  申请人：Nippon Kayaku Kabushiki Kaisha

  公开号：EP1055683A1

  公开（公告）日：2000-11-29

  The present Invention relates to a novel acetamide derivative represented by the following Formula 1, which has an inhibition activity for chymotrypsin type proteases and is usefull as an inhibitor for the above enzyme, especially as an inhibitor for chymase, and the use thereof as a medicine, for example, an antiasthma drug or a drug for curing vascular injuries complicated with angiogenesis and atheroma.    wherein R0 represents a substituted or unsubstituted phenyl group, R1 represents an aryl group, a heteroaryl or an aliphatic lower alkyl group with or without substituents, R2 represents a substituted or unsubstituted alkyl, an aryl alkyl, a heteroaryl alkyl, and a heteroaryloxy alkyl or the like, J represents a carbonyl group, or a methylene group or the like, L represents a methoxy, hydroxyl or acetyloxy group or the like, X and Y independently represents a nitrogen atom or a carbon atom, Z represents a methylene group or a polyethylene group optionally having a substituent.

  本发明涉及一种由下式 1 表示的新型乙酰胺衍生物，该衍生物对糜蛋白酶型蛋白酶具有抑制活性，可用作上述酶的抑制剂，特别是糜蛋白酶的抑制剂，并可将其用作药物，例如抗哮喘药物或治疗并发血管生成和动脉粥样硬化的血管损伤的药物。 其中 R0 代表取代或未取代的苯基，R1 代表芳基、杂芳基或带或不带取代基的脂族低级烷基，R2 代表取代或未取代的烷基、芳基烷基、杂芳基烷基和杂芳基氧基烷基或类似物、J 代表羰基或亚甲基或类似基团，L 代表甲氧基、羟基或乙酰氧基或类似基团，X 和 Y 独立地代表氮原子或碳原子，Z 代表亚甲基或可选具有取代基的聚乙烯基团。
• US6271238B1
  申请人：——

  公开号：US6271238B1

  公开（公告）日：2001-08-07
• US6300337B1
  申请人：——

  公开号：US6300337B1

  公开（公告）日：2001-10-09