Sarakalim | 148430-28-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: Sarakalim
• 英文别名: 6-trifluoromethyl-2,2-dimethyl-3-(N-hydroxyacetamido)methyl-4-(2-oxo-1,2-dihydropyridin-1-yl)-2H-1-benzopyran；N-[[2,2-dimethyl-4-(2-oxopyridin-1-yl)-6-(trifluoromethyl)chromen-3-yl]methyl]-N-hydroxyacetamide
• CAS: 148430-28-8
• 化学式: C₂₀H₁₉F₃N₂O₄
• 分子量: 408.377
• InChiKey: FXRJKZVWFJSKGI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  70.1
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  6-trifluoromethyl-2,2-dimethyl-3-(hydroxyamino)methyl-4-(2-oxo-1,2-dihydropyridin-1-yl)-2H-1-benzopyran 、 乙酰氯 在 三乙胺 作用下， 以 二氯甲烷 、 水 为溶剂， 生成 Sarakalim
  参考文献：
  名称：

  Novel benzopyran derivatives

  摘要：

  式中的化合物：##STR1## 其中：R.sup.1-7 如规范中所定义。这些化合物和盐表现出有用的药理特性，包括钾通道激活特性和5-脂氧合酶抑制特性，特别是作为平滑肌松弛剂和支气管扩张剂时非常有用。

  公开号：

  US05447943A1

文献信息

• Benzopyran derivatives
  申请人：Syntex (U.S.A.) Inc.

  公开号：US05250547A1

  公开（公告）日：1993-10-05

  Compounds of the Formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl of 3 to 8 carbon atoms; R.sup.3 is fluoro lower alkyl; cyano; or nitro; R.sup.4 is ##STR2## R.sup.5 and R.sup.6 are independently hydrogen or lower alkyl; and R.sup.7 is --NR.sup.8 R.sup.9 ; wherein: R.sup.8 is hydrogen; lower alkyl; lower alkoxy; hydroxy; or hydroxy lower alkyl; and R.sup.9 is hydrogen; lower alkyl; hydroxy lower alkyl; --SO.sub.2 R.sup.10 ; --CO.sub.2 R.sup.10 ; --C(O)NR.sup.11 R.sup.12 ; --C(S)NR.sup.11 R.sup.12 ; or --C(O)R.sup.12 ; wherein R.sup.10 is lower alkyl; R.sup.11 is hydrogen or lower alkyl; and R.sup.12 is hydrogen, lower alkyl, or fluoro lower alkyl; with the proviso that R.sup.8 and R.sup.9 cannot both be hydrogen; and the pharmaceutically acceptable salts thereof. The compounds and salts exhibit useful pharmacological properties, including potassium channel activating properties and 5-lipoxygenase inhibiting properties, and in particular are useful as smooth muscle relaxants and bronchodilators.

  式的化合物：##STR1##其中：R.sup.1和R.sup.2分别是氢或较低的烷基，或者与它们连接的碳一起取为3到8个碳原子的环烷基；R.sup.3是氟烷基；氰基；或硝基；R.sup.4是##STR2##R.sup.5和R.sup.6分别是氢或较低的烷基；而R.sup.7是--NR.sup.8 R.sup.9；其中：R.sup.8是氢；较低的烷基；较低的烷氧基；羟基；或羟基较低的烷基；而R.sup.9是氢；较低的烷基；羟基较低的烷基；--SO.sub.2 R.sup.10；--CO.sub.2 R.sup.10；--C(O)NR.sup.11 R.sup.12；--C(S)NR.sup.11 R.sup.12；或--C(O)R.sup.12；其中R.sup.10是较低的烷基；R.sup.11是氢或较低的烷基；而R.sup.12是氢，较低的烷基，或氟烷基；但R.sup.8和R.sup.9不能同时为氢；以及其药学上可接受的盐。这些化合物和盐表现出有用的药理特性，包括钾通道激活特性和5-脂氧酶抑制特性，特别是作为平滑肌松弛剂和支气管扩张剂时非常有用。
• Benzopyran derivatives as potassium channel activators and 5-lipoxygenase inhibitors
  申请人：SYNTEX (U.S.A.) INC.

  公开号：EP0529654A1

  公开（公告）日：1993-03-03

  Compounds of the Formula: wherein: R¹ and R² areindependently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl of 3 to 8 carbon atoms; R³ ishydrogen, halo, fluoro lower alkyl, cyano, or nitro; R⁴ is R⁵ and R⁶ areindependently hydrogen or lower alkyl; and R⁷ is-NR⁸R⁹; wherein: R⁸ ishydrogen; lower alkyl; lower alkoxy; hydroxy; or hydroxy lower alkyl; and R⁹ ishydrogen; lower alkyl; hydroxy lower alkyl; -SO₂R¹⁰; -CO₂R¹⁰; -C(O)NR¹¹R¹²; -C(S)NR¹¹R¹²; or -C(O)R¹²; wherein R¹⁰ islower alkyl; R¹¹ ishydrogen or lower alkyl; and R¹² ishydrogen, lower alkyl, or fluoro lower alkyl; with the proviso that R⁸ and R⁹ cannot both be hydrogen; and the pharmaceutically acceptable salts thereof. The compounds and salts exhibit useful pharmacological properties, including potassium channel activating properties and 5-lipoxygenase inhibiting properties, and in particular are useful as smooth muscle relaxants and bronchodilators.

  式的化合物： 其中 R¹ 和 R² 分别为氢或低级烷基，或与所连接的碳一起为 3 至 8 个碳原子的环烷基； R³ 是氢、卤素、氟低级烷基、氰基或硝基； R⁴ 是 R⁵ 和 R⁶ 分别是氢或低级烷基；以及 R⁷ 是-NR⁸R⁹；其中 R⁸ 是氢；低级烷基；低级烷氧基；羟基；或羟基低级烷基；和 R𠞙 是氢；低级烷基；羟基低级烷基；-SO₂R¹⁰；-CO₂R¹⁰；-C(O)NR¹R¹²；-C(S)NR¹R¹²；或 -C(O)R¹²；其中 R¹⁰ 是低级烷基； R¹¹ 是氢或低级烷基；以及 R¹² 是氢、低级烷基或氟低级烷基； 但 R⁸ 和 R𠞙 不能都是氢；及其药学上可接受的盐。这些化合物和盐具有有用的药理特性，包括钾通道激活特性和 5-脂氧合酶抑制特性，特别是可用作平滑肌松弛剂和支气管扩张剂。
• PHARMACEUTICAL FORMULATIONS FOR AEROSOLS WITH TWO OR MORE ACTIVE SUBSTANCES
  申请人：BOEHRINGER INGELHEIM PHARMACEUTICALS INC.

  公开号：EP1087750A1

  公开（公告）日：2001-04-04
• PHARMAZEUTISCHE FORMULIERUNG FÜR AEROSOLE MIT ZWEI ODER MEHR WIRKSTOFFEN UND MINDESTENS EINER OBERFLÄCHENAKTIVEN SUBSTANZ
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：EP1988874A2

  公开（公告）日：2008-11-12
• Intranasal administration of modulators of hypothalamic ATP-sensitive potassium channels
  申请人：Herlands Louis

  公开号：US20070026079A1

  公开（公告）日：2007-02-01

  Provided are methods of increasing K ATP channel activity in the hypothalamus of a mammal, methods of reducing glucose production in a mammal, methods of reducing peripheral glucose levels in a mammal, methods of reducing triglyceride levels in a mammal, methods of reducing very low density lipoprotein (VLDL) levels in a mammal, methods of methods of reducing gluconeogenesis in the liver of a mammal, methods of treating metabolic disorders such as diabetes, hyperglycemia, insulin resistance, glucose intolerance, metabolic syndrome and/or obesity, and methods of increasing glucose production and peripheral glucose levels in a mammal. Also provided are methods of treating heart failure, ischemia, coronary heart disease, familial lipoprotein lipase deficiency, hypopituitarism, hyperlipidemia, hypertriglyceridemia, hyperVLDLemia, atherosclerosis, hypercholesterolemia, hypertension, polycystic ovary syndrome, gonadotropin deficiency and/or amenorrhea.