(+/-) 3-(4-fluorophenyl)-1,3-dihydro-7-hydroxy-6-methylfurop-[3,4-c] pyridine | 96788-34-0

• 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: (+/-) 3-(4-fluorophenyl)-1,3-dihydro-7-hydroxy-6-methylfurop-[3,4-c] pyridine
• 英文别名: 1,3-dihydro-3-p-fluorophenyl-6-methyl-7-hydroxy-furo-(3,4-c)-pyridine；3-(4-Fluorophenyl)-6-methyl-1,3-dihydrofuro[3,4-c]pyridin-7-ol
• CAS: 96788-34-0
• 化学式: C₁₄H₁₂FNO₂
• 分子量: 245.253
• InChiKey: ANEYGXYUZGDDGH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  42.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (+/-) 3-(4-fluorophenyl)-1,3-dihydro-7-hydroxy-6-methylfurop-[3,4-c] pyridine 以47%的产率得到1,3-dihydro-3-p-fluorophenyl-6-methyl-7-carboxymethoxy-furo-(3,4-c)-pyridine
  参考文献：
  名称：

  Diuretic, antihypertensive and antihistaminic

  摘要：

  本发明涉及一种新的1,3-二氢-6-甲基呋喃-(3,4-c)-吡啶衍生物，其一般式为：##STR1## 其中，A.sub.1和A.sub.2各自代表不同的碳氢基团，以及它们的药学上可接受的盐，以及从相应的6-羟基化合物经乙酰溴酸乙酯处理然后水解制备上述衍生物的方法。本发明还提供了制药组合物，其中上述衍生物被用作活性成分。该化合物可用作利尿剂，降低血压和抗组胺药。

  公开号：

  US04569938A1

文献信息

• USE OF CICLETANINE AND OTHER FUROPYRIDINES FOR TREATMENT OF HYPERTENSION
  申请人：Navitas Pharma, Inc.

  公开号：EP1951264A2

  公开（公告）日：2008-08-06
• EP1951264A4
  申请人：——

  公开号：EP1951264A4

  公开（公告）日：2009-03-25
• COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS
  申请人：Gilead Sciences, Inc.

  公开号：EP2167082A1

  公开（公告）日：2010-03-31
• Use of cicletanine and other furopyridines for treatment of systolic-predominant hypertension, isolated systolic hypertension, elevated pulse pressure, and general hypertension
  申请人：Page Jim

  公开号：US20070105817A1

  公开（公告）日：2007-05-10

  This invention provides therapeutic compositions of cicletanine and other furopyridines for the treatment of, elevated pulse pressure or isolated systolic hypertension, as well as general hypertension, in monotherapy and in combined therapy with other anti-hypertensive agents (such as organic and inorganic nitrogen donors, calcium channel blockers, diuretics, beta blockers, angiotensin receptor blockers, ACE inhibitors, aldosterone antagonists, renin inhibitors and centrally-acting antihypertensives) cardiovascular agents (such as medications to treat heart failure) and oral antidiabetic agents (such as biguanides and glitazones). Such compositions include enantiomerically pure (positive or negative) embodiments, as well as enantiomeric mixtures other than a racemic mixture, and include daily dosages of less than 50 mg. Further provided are methods of treatment of general or systolic hypertension, wherein patients are administered the inventive compositions, either a monotherapeutic furopyridine composition, or a combination therapy, which includes a second agent in addition to the furopyridine, for treatment of general hypertension or systolic hypertension, and hypertension-associated complications.
• Enantiomeric compositions of cicletanine, in combination with other agents, for the treatment of hypertension
  申请人：Cornett V. Glenn

  公开号：US20070141174A1

  公开（公告）日：2007-06-21

  The invention provides formulations and methods of use of furopyridine-based compositions alone and in combination with one or more various second therapeutic agents for the treatment of human disease. The furopyridine composition may include one or more furopyridine species, of which cicletanine is an example. The furopyridines may take various enantiomeric forms, ranging from pure (−) through (−)-dominant, racemic and (+)-dominant to pure (+). Second agents may be any drug useful in combination with a furopyridine in the treatment of diseases such as, cardiovascular disease (hypertension, restenosis, etc.), diabetes, diabetes complications, and polycystic ovarian syndrome. Some of these diseases are associated with endothelial dysfunction and imbalances of prostacyclin or of reactive oxygen species (ROS) or reactive nitrogen species (RNS).