1-[(benzofuran-2-yl)(4'-cyanophenyl)methyl]-1H-1,2,4-triazole | 207288-29-7

• 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: 1-[(benzofuran-2-yl)(4'-cyanophenyl)methyl]-1H-1,2,4-triazole
• 英文别名: 4-(2-benzofuranyl-1H-1,2,4-triazol-1-ylmethyl)benzonitrile；4-[1-benzofuran-2-yl(1,2,4-triazol-1-yl)methyl]benzonitrile
• CAS: 207288-29-7；328404-65-5
• 化学式: C₁₈H₁₂N₄O
• 分子量: 300.319
• InChiKey: JMVXKKZHONWLEN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  67.6
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Methods and compositions for the treatment of estrogen-dependent hyperproliferative uterine disorders
  申请人：Wang Changjin

  公开号：US20100087402A1

  公开（公告）日：2010-04-08

  The present invention relates to the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor, an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estrogen levels. This results in enhanced clinical efficacy and reduced side effects.

  本发明涉及治疗依赖雌激素的子宫过度增生性疾病，包括子宫内膜异位症、子宫肌瘤、子宫内膜增生、子宫癌及其相关症状，通过阴道给药至少两种活性药物，所选药物包括芳香化酶抑制剂、抗炎药和子宫选择性雌激素受体拮抗剂。这种联合疗法降低了局部雌激素产生，阻断了局部雌激素作用，并在局部抑制了炎症，导致对依赖雌激素的疾病组织的饥饿，缓解相关症状，延缓疾病进展。阴道给药最大限度地抑制了局部雌激素产生，而不显著影响全身循环雌激素水平。这导致增强的临床疗效和减少的副作用。
• Method of using a COX-2 inhibitor and an aromatase inhibitor as a combination therapy
  申请人：Pharmacia Corporation

  公开号：US20040053900A1

  公开（公告）日：2004-03-18

  The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia, a neoplasia-related disorder or osteoporosis in a mammal using a combination of a COX-2 inhibitor and an aromatase inhibitor.

  本发明提供了一种使用COX-2抑制剂和芳香化酶抑制剂的组合物和方法，用于治疗、预防或抑制哺乳动物中的肿瘤、肿瘤相关疾病或骨质疏松症。
• THERAPEUTIC COMBINATION OF A COX-2 INHIBITOR AND AN AROMATASE INHIBITOR
  申请人：Pharmacia Corporation

  公开号：EP1653940A1

  公开（公告）日：2006-05-10
• Methods and Compositions for the Treatment of Estrogen-Dependent Hyperproliferative Uterine Disorders
  申请人：Vivus, Inc.

  公开号：US20140080794A1

  公开（公告）日：2014-03-20

  The present invention relates to the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor, an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estrogen levels. This results in enhanced clinical efficacy and reduced side effects.
• [EN] HETEROCYCLIC FURAN COMPOUNDS, THEIR PREPARATION AND USE AS AROMATASE INHIBITORS<br/>[FR] COMPOSES DE FURANE HETEROCYCLIQUES, PREPARATION DE CES COMPOSES ET UTILISATION DE CES COMPOSES COMME INHIBITEURS D'AROMATASE
  申请人：——

  公开号：WO1998018791A1

  公开（公告）日：1998-05-07

  [EN] Described herein are furan compounds having formula (I), their preparation and their use as aromatase inhibitors.
  [FR] Composés de furane représentés par la formule (I), leur préparation et leur utilisation en tant qu'inhibiteurs d'aromatase.