6-[3-(N-methyl-N-benzylamino)-2-hydroxypropoxy]carbostyril | 128667-13-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 6-[3-(N-methyl-N-benzylamino)-2-hydroxypropoxy]carbostyril
• 英文别名: 6-[3-[benzyl(methyl)amino]-2-hydroxypropoxy]-1H-quinolin-2-one
• CAS: 128667-13-0
• 化学式: C₂₀H₂₂N₂O₃
• 分子量: 338.406
• InChiKey: VINGRRUDLOWJBL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-(2,3-epoxypropoxy)-2(1H)-quinolinone 、 N-甲基苄胺 在 silica gel 、 甲醇 、 氯仿 、 乙醇 作用下， 以 甲醇 为溶剂， 反应 2.5h， 以to give 6-[3-(N-methyl-N-benzylamino)-2-hydroxypropoxy]carbostyril (5 g)的产率得到6-[3-(N-methyl-N-benzylamino)-2-hydroxypropoxy]carbostyril
  参考文献：
  名称：

  Cardiotonics

  摘要：

  使用公式为：##STR1## 的羧甲基苯基吡啶衍生物预防和治疗心脏疾病的方法，其中R.sup.1为H或CN，R.sup.2和R.sup.3分别为H、烷基，其上可选地取代为OH、环烷基、烯基、苯基、苯基烷基，其上可选地取代为烷氧烷氧基、卤素、烷氧基、NO.sub.2、烷基、CN、烷硫基或烷基磺酰基，其上可选地带有烷氧基取代的苯基環，苯基硫基烷基，苯基磺酰基烷基，其上可选地取代为卤素或烷氧基的苯基環，其上可选地取代为卤素或烷氧基的苯氧基烷基，其上可选地取代为卤素或烷氧基的吡啶基烷基，噻吩基烷基，苯甲酰基烷基，苯胺硫代氨基酰基，苯甲酰基，吡啶基，苯基烯基，或者为--A--NR.sup.4 R.sup.5（其中R.sup.4和R.sup.5分别为烷基或苯基，其上可选地取代为卤素或烷氧基的苯基環，A为可用O中断的烷基），以及其盐和新型羧甲基苯基吡啶衍生物，以及包含所述新型羧甲基苯基吡啶衍生物的预防和治疗心脏疾病的药物组成物。

  公开号：

  US05053514A1

文献信息

• Cardiotonics
  申请人：Otsuka Pharmaceutical Company, Limited

  公开号：US05198448A1

  公开（公告）日：1993-03-30

  Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

  本发明涉及使用公式为：##STR1##其中R.sup.1为H或CN，R.sup.2和R.sup.3分别为H，烷基（其上可选择性地取代为OH），环烷基，烯基，苯基，苯基烷基，其上可选择性地有取代基的烷氧基烷氧基，卤素，烷氧基，NO.sub.2，烷基，CN，烷硫基或烷基亚砜基，其在苯环上具有可选择性的OH取代基的烷基部分，苯基磺酰基烷基，其在苯环上具有可选择性的烷氧基取代基的苯基磺酰基烷基，苯基硫基烷基，苯基亚砜基烷基，其在苯环上具有可选择性的卤素或烷氧基取代基的苯基亚砜基烷基，苯氧基烷基，其在苯环上具有可选择性的卤素或烷氧基取代基的苯氧基烷基，吡啶基烷基，其在吡啶环上具有可选择性的卤素或烷氧基取代基，噻吩基烷基，苯甲酰基烷基，苯胺硫代氨基甲酰基，苯甲酰基，吡啶基，苯基烯基，或--A-NR.sup.4 R.sup.5（其中R.sup.4和R.sup.5分别为烷基或苯基，其在苯环上具有可选择性的卤素或烷氧基取代基，A为可用O中断的烷基），以及其盐的预防和治疗心脏疾病的方法，以及新的卡波斯蒂瑞尔衍生物和含有所述新的卡波斯蒂瑞尔衍生物的预防和治疗心脏疾病的药物组合物。
• Cardiotonic carbostyril agents for treating heart ailments
  申请人：Otsuka Pharmaceutical Company, Limited

  公开号：US05385914A1

  公开（公告）日：1995-01-31

  Method for prophylaxis and treatment of heart diseases using a carbostyril derivative-of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

  使用一种羧基苯基吡啶衍生物的方法预防和治疗心脏疾病，其化学式为：##STR1## 其中R.sup.1为H或CN，R.sup.2和R.sup.3分别为H，烷基（可选用OH取代），环烷基，烯基，苯基，苯基烷基，在苯环上可选地带有烷氧基烷氧基，卤素，烷氧基，NO.sub.2，烷基，CN，烷硫基或烷基磺酰基取代基，并在烷基部分上可选地带有OH取代基，苯基磺酰基烷基，在苯环上可选地带有烷氧基取代基，苯基硫基烷基，苯基磺酰基烷基，在苯环上可选地带有卤素或烷氧基取代基，苯氧基烷基，在苯环上可选地带有卤素或烷氧基取代基，吡啶基烷基，在吡啶环上可选地带有卤素或烷氧基取代基，噻吩基烷基，苯甲酰基烷基，苯胺基硫代羰基，苯甲酰基，吡啶基，苯基烯基，或--A--NR.sup.4 R.sup.5（其中R.sup.4和R.sup.5分别为烷基或苯基，苯环上可选地带有卤素或烷氧基取代基，A为可用O中断的烷基），及其盐，以及用于预防和治疗心脏疾病的新型羧基苯基吡啶衍生物和制药组合物。
• Method of treating congestive heart failure using carbostyril derivatives
  申请人：Otsuka Pharmaceutical Company Ltd.

  公开号：US05266577A1

  公开（公告）日：1993-11-30

  Method for the treatment of congestive heart failure or paroxymal frequent heart pulse using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of -A-NR.sup.4 R.sup.5 (R.sup.4 and R.sup.5 are each alkyl or phenyl having optionally substituents of halogen or alkoxy on phenyl ring, and A is alkylene which may be interrupted with O), and a salt thereof, and novel carbostyril derivatives, and pharmaceutical composition for prophylaxis and treatment of heart diseases containing said novel carbostyril derivative.

  使用公式式的carbostyril衍生物治疗充血性心力衰竭或阵发性频繁心跳的方法，其中公式为：##STR1##其中R.sup.1为H或CN，R.sup.2和R.sup.3分别为H，烷基，可选地被OH取代的环烷基，烯基，苯基，苯基烷基，其在苯环上具有可选的alkoxyalkoxy，卤素，alkoxy，NO.sub.2，烷基，CN，alkylthio或alkylsulfinyl取代基，并在烷基部分上具有可选的OH取代基，苯基磺酰基烷基，在苯环上具有可选的alkoxy取代基，苯基硫代烷基，苯基亚砜基烷基，在苯环上具有可选的卤素或alkoxy取代基，苯氧基烷基，在苯环上具有可选的卤素或alkoxy取代基，吡啶基烷基，在吡啶环上具有可选的卤素或alkoxy取代基，噻吩基烷基，苯甲酰基烷基，苯胺基硫代羰基，苯甲酰基，吡啶基，苯基烯基，或-A-NR.sup.4 R.sup.5（其中R.sup.4和R.sup.5分别为烷基或苯基，在苯环上具有可选的卤素或alkoxy取代基，A为可以被O中断的烷基），以及其盐，以及用于预防和治疗心脏疾病的新型carbostyril衍生物和制药组合物。
• Carbostyril derivatives as phosphodiesterase inhibitors
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP0647447A1

  公开（公告）日：1995-04-12

  A pharmaceutical preparation comprising at least one compound selected from the group consisting of carbostyril derivatives having the general formula: wherein R¹ is hydrogen or a lower alkyl group optionally having hydroxy group as a substituent; R² is a phenyl(lower alkyl) group optionally having 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom on the phenyl ring, pyridyl(lower alkyl) group, or a group of the formula -A-NR³R⁴ (wherein A is a lower alkylene group, R³ and R⁴ are the same or different and represent a lower alkyl group or phenyl group), and a salt thereof, which is useful as an agent for treating thrombosis, more particularly, as an agent for inhibiting platelet aggregation, an agent for platelet aggregate dissociation, an ameliorant of cerebral circulation and a phosphodiesterase inhibitor.

  一种药物制剂，包含至少一种选自具有通式的羧甲吡啶衍生物的化合物： 其中 R¹ 是氢或可选择具有羟基作为取代基的低级烷基；R² 是苯基（低级烷基）基团，可任选具有 1 至 3 个取代基，这些取代基可从苯基环上的低级烷氧基和卤原子、吡啶基（低级烷基）基团或式 -A-NR³R⁴ 的基团组成的组中选出（其中 A 是低级亚烷基、R³和R⁴相同或不同，代表低级烷基或苯基）及其盐，可用作治疗血栓的药物，特别是用作抑制血小板聚集的药物、血小板聚集解离剂、脑循环改善剂和磷酸二酯酶抑制剂。
• Carbostyril derivatives as anti-thrombotic agents
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP0531548B1

  公开（公告）日：1995-09-27