methyl 2{(benzofuran-5-yl)methylene}-3-oxobutyrate | 179482-27-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: methyl 2{(benzofuran-5-yl)methylene}-3-oxobutyrate
• 英文别名: Methyl 2-{(benzofuran-5-yl)methylene}-3-oxobutyrate；methyl 2-(1-benzofuran-5-ylmethylidene)-3-oxobutanoate
• CAS: 179482-27-0
• 化学式: C₁₄H₁₂O₄
• 分子量: 244.247
• InChiKey: UVXGISRXCYOGPN-UHFFFAOYSA-N

物化性质

• 沸点：
  373.3±27.0 °C(Predicted)
• 密度：
  1.238±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  56.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  methyl 2{(benzofuran-5-yl)methylene}-3-oxobutyrate 、 O-甲基异脲 半硫酸盐 在 碳酸氢钠 作用下， 以 正己烷 、 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 以43%的产率得到Methyl 4-(2,1,3-benzoxadiazol-5-yl)-2-methoxy-6-methyl-1,4-dihydropyrimidine-5-carboxylate
  参考文献：
  名称：

  5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines

  摘要：

  这项发明涉及选择性拮抗人类α1C受体的二氢嘧啶化合物，其结构为：##STR1##其中A为芳基；R.sub.1、R.sub.2和R.sub.3为烷基或杂原子烷基；R.sub.4为杂环烷基；X为S、O或NR.sub.3。该发明还涉及利用这些化合物治疗良性前列腺增生和其他需要拮抗人类α1C受体的疾病。该发明还提供包含该化合物的治疗有效量和药用可接受载体的药物组合物。

  公开号：

  US05942517A1
• 作为产物：
  描述：

  哌啶 、 乙酰乙酸甲酯 、 2,1,3-苯并二唑-5-甲醛 在 溶剂黄146 作用下， 以 乙酸乙酯 、 苯 为溶剂， 以98.3%的产率得到methyl 2{(benzofuran-5-yl)methylene}-3-oxobutyrate
  参考文献：
  名称：

  5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines

  摘要：

  这项发明涉及选择性拮抗人类α1C受体的二氢嘧啶化合物，其结构为：##STR1##其中A为芳基；R.sub.1、R.sub.2和R.sub.3为烷基或杂原子烷基；R.sub.4为杂环烷基；X为S、O或NR.sub.3。该发明还涉及利用这些化合物治疗良性前列腺增生和其他需要拮抗人类α1C受体的疾病。该发明还提供包含该化合物的治疗有效量和药用可接受载体的药物组合物。

  公开号：

  US05942517A1

文献信息

• Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
  申请人：——

  公开号：US20030069261A1

  公开（公告）日：2003-04-10

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

  本发明涉及一种选择性拮抗黑色素浓缩激素-1（MCH1）受体的化合物。该发明提供了一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供了一种通过组合本发明化合物的治疗有效量和药学上可接受的载体制备药物组合物的方法。本发明还提供了一种制备药物组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。本发明还提供了一种改变受试者进食行为的方法，包括向受试者投药一种有效减少受试者进食的本发明化合物。本发明还提供了一种治疗受试者进食障碍的方法，包括向受试者投药一种有效减少受试者进食的本发明化合物。在本发明的实施例中，进食障碍是贪食症、神经性贪食症或肥胖症。
• Dihydropyrimidines and uses thereof
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US20020010186A1

  公开（公告）日：2002-01-24

  This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr; 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr; 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

  这项发明涉及二氢嘧啶化合物，它们是人类α1A受体的选择性拮抗剂。此发明还涉及使用这些化合物降低眼压、抑制胆固醇合成、放松下尿路组织、治疗良性前列腺增生、阳痿、心律失常和治疗任何需要拮抗α1A受体的疾病。该发明还提供一种制药组合物，包括上述定义化合物的治疗有效量和药学可接受的载体。
• DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof
  申请人：——

  公开号：US20030077701A1

  公开（公告）日：2003-04-24

  This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention provides a method of modifying the feeding behavior of a subject which comprises administering to the subject an amount of an MCH1 antagonist effective to decrease the body mass of the subject and/or decrease the consumption of food by the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's depression and/or anxiety.

  本发明提供了编码人MCH1受体的分离核酸、纯化的人MCH1受体、包含编码人MCH1受体的分离核酸的载体、包含这种载体的细胞、针对人MCH1受体的抗体、用于检测编码人MCH1受体的核酸探针、互补于编码人MCH1受体独特序列的反义寡核苷酸、表达正常或突变人MCH1受体DNA的转基因非人类动物、分离人MCH1受体的方法、治疗与人MCH1受体活性相关的异常的方法，以及确定化合物与哺乳动物MCH1受体结合的方法。本发明提供了一种修改受试者进食行为的方法，该方法包括向受试者施用足以减少受试者体重和/或减少受试者食物摄入量的MCH1拮抗剂。本发明还提供了一种治疗患有抑郁和/或焦虑的受试者的方法，该方法包括向受试者施用足以治疗受试者抑郁和/或焦虑的MCH1拮抗剂。
• 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US05942517A1

  公开（公告）日：1999-08-24

  This invention is directed to dihydropyrimidine compounds which are selective antagonists for human .alpha..sub.1C receptors and which have the structure: ##STR1## wherein A is aryl; R.sub.1, R.sub.2 and R.sub.3 are alkyl or heteroalkyl; R.sub.4 is heterocyclic alkyl; and X is S, O or NR.sub.3. This invention also relates to use of these compounds for the treatment of benign prostatic hyperplasia and other diseases where antagonism of the human .alpha..sub.1C receptor is useful. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of such a compound and a pharmaceutically acceptable carrier.

  这项发明涉及选择性拮抗人类α1C受体的二氢嘧啶化合物，其结构为：##STR1##其中A为芳基；R.sub.1、R.sub.2和R.sub.3为烷基或杂原子烷基；R.sub.4为杂环烷基；X为S、O或NR.sub.3。该发明还涉及利用这些化合物治疗良性前列腺增生和其他需要拮抗人类α1C受体的疾病。该发明还提供包含该化合物的治疗有效量和药用可接受载体的药物组合物。