2-{N-[4-(2-pyridylcarbonylamino)butyl]}aminomethyl-2,3-dihydrobenzo[b]furan | 175902-86-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-{N-[4-(2-pyridylcarbonylamino)butyl]}aminomethyl-2,3-dihydrobenzo[b]furan
• 英文别名: N-[4-(2,3-dihydro-1-benzofuran-2-ylmethylamino)butyl]pyridine-2-carboxamide
• CAS: 175902-86-0
• 化学式: C₁₉H₂₃N₃O₂
• 分子量: 325.411
• InChiKey: SFJXJKBPLPDWST-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  63.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• NOVEL 2,3-DIHYDROBENZOFURAN DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE THEREOF
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0769496A1

  公开（公告）日：1997-04-23

  Disclosed are a 2,3-dihydrobenzofuran derivative represented by formula (1) or a salt thereof, a method for producing the same, and use thereof:    wherein R1 represents a hydrogen atom or a lower alkyl group; R2 represents a naphthyl group, a pyridyl group, a furyl group or a thienyl group; n is an integer of from 2 to 6; A represents a carbonyl group or a sulfonyl group; and * represents an asymmetric carbon atom. The 2,3-dihydrobenzofuran derivatives of the present invention and the non-toxic salts thereof have a strong affinity for serotonin 1A receptors. Therefore, are useful as pharmaceutical composition containing the 2,3-dihydrobenzofuran derivatives and the non-toxic salts thereof are especially useful for treating a serotonergic neuron-related disease, such as anxiety, depression, eating disorder, high blood pressure, emesis (including emesis induced by motion sickness, space sickness, dizziness and drug, etc.) and the like.

  本发明公开了式(1)代表的2,3-二氢苯并呋喃衍生物或其盐、生产方法及其用途： 其中 R1 代表氢原子或低级烷基；R2 代表萘基、吡啶基、呋喃基或噻吩基；n 为 2 至 6 的整数；A 代表羰基或磺酰基；* 代表不对称碳原子。 本发明的 2,3-二氢苯并呋喃衍生物及其无毒盐对血清素 1A 受体有很强的亲和力。因此，作为含有 2,3-二氢苯并呋喃衍生物及其无毒盐的药物组合物，特别适用于治疗与血清素能神经元有关的疾病，如焦虑、抑郁、饮食失调、高血压、呕吐（包括晕车、晕船、晕眩和药物等引起的呕吐）等。
• COMBINATION THERAPY EMPLOYING ILEAL BILE ACID TRANSPORT INHIBITING BENZOTHIEPINES AND HMG Co-A REDUCTASE INHIBITORS
  申请人：G.D. SEARLE & CO.

  公开号：EP0971744A2

  公开（公告）日：2000-01-19
• US5798382A
  申请人：——

  公开号：US5798382A

  公开（公告）日：1998-08-25
• [EN] COMBINATION THERAPY EMPLOYING ILEAL BILE ACID TRANSPORT INHIBITING BENZOTHIEPINES AND HMG Co-A REDUCTASE INHIBITORS<br/>[FR] TRAITEMENT ASSOCIE UTILISANT DES BENZOTHIEPINES INHIBITRICES DU TRANSPORT ILEAL DE L'ACIDE BILIAIRE ET DES INHIBITEURS DE LA HMG Co-A REDUCTASE
  申请人：——

  公开号：WO1998040375A2

  公开（公告）日：1998-09-17

  [EN] Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
  [FR] La présente invention concerne des benzothiépines, certains de leurs dérivés et de leurs analogues. L'invention concerne également des compositions contenant ces benzothiépines, dérivés et analogues. L'invention concerne enfin des procédés permettant d'utiliser ces composés et compositions dans des médicaments, en particulier pour la prophylaxie et le traitement d'états hyperlipidémiques tels que ceux qui sont liés chez les mammifères à l'athérosclérose ou l'hypercholestérolémie. L'invention concerne en outre des compositions et des procédés applicables dans un traitement associé utilisant des benzothiépines inhibitrices du transport iléal de l'acide biliaire et des inhibiteurs de la HMG Co-A réductase pour le traitement d'états hyperlipidémique.