6-{[1-(1H-Imidazol-1-ylmethyl)pentyl]oxy}-5-[(phenylsulfonyl)methyl]3,4-dihydro-1(2H)-naphthalenone | 368884-24-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 6-{[1-(1H-Imidazol-1-ylmethyl)pentyl]oxy}-5-[(phenylsulfonyl)methyl]3,4-dihydro-1(2H)-naphthalenone
• 英文别名: 6-{[1-(1H-imidazol-1-ylmethyl)pentyl]oxy}-5-[(phenylsulfonyl)methyl]-3,4-dihydro-1(2H)-naphthalenone；5-(benzenesulfonylmethyl)-6-(1-imidazol-1-ylhexan-2-yloxy)-3,4-dihydro-2H-naphthalen-1-one
• CAS: 368884-24-6
• 化学式: C₂₆H₃₀N₂O₄S
• 分子量: 466.601
• InChiKey: UZGDRWOYWNIAMC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  33
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  86.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  偶氮二甲酸二乙酯 、 6-hydroxy-5-[(phenylsulfonyl)methyl]-3,4-dihydro-1(2H)-naphthalenone 、 1-(1H-Imidazol-1-yl)-2-hexanol 、 三苯基膦 在 氮气 、 SiO2 、 Isopropanol methylene chloride 作用下， 以 四氢呋喃 为溶剂， 反应 120.17h， 以to give 6-{[1-(1H-imidazol-1-ylmethyl)pentyl]oxy}-5-[(phenylsulfonyl)methyl]-3,4-dihydro-1(2H)-naphthalenone as a colorless foam, 283 mg, 62% yield的产率得到6-{[1-(1H-Imidazol-1-ylmethyl)pentyl]oxy}-5-[(phenylsulfonyl)methyl]3,4-dihydro-1(2H)-naphthalenone
  参考文献：
  名称：

  5-substituted tetralones as inhibitors of ras farnesyl transferase

  摘要：

  本发明提供了式I、II、III和IV的新型5-取代四酮及其药学上可接受的盐、酯、酰胺和前药，用于治疗和预防组织的不受控制或异常增殖，如癌症、动脉粥样硬化、再狭窄和银屑病。具体来说，本发明涉及抑制法尼酰转移酶酶的化合物。

  公开号：

  US06943183B2

文献信息

• 5- substituted tetralones as inhibitors of ras farnesyl trransferase
  申请人：——

  公开号：US20040044057A1

  公开（公告）日：2004-03-04

  The present invention provides novel 5-substituted tetralones of Formulas (I), (II), (III) and (IV) and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme. 1

  本发明提供了式(I)、(II)、(III)和(IV)的新型5-取代四酮及其药学上可接受的盐、酯、酰胺和前药，用于治疗和预防组织的不受控制或异常增殖，如癌症、动脉粥样硬化、再狭窄和银屑病。具体而言，本发明涉及抑制法尼基转移酶酶的化合物。
• 5-SUBSTITUTED TETRALONES AS INHIBITORS OF RAS FARNESYL TRANSFERASE
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP1276725A2

  公开（公告）日：2003-01-22
• US6943183B2
  申请人：——

  公开号：US6943183B2

  公开（公告）日：2005-09-13
• [EN] 5-SUBSTITUTED TETRALONES AS INHIBITORS OF RAS FARNESYL TRANSFERASE<br/>[FR] TETRALONES 5-SUBSTITUEES EN TANT QU'INHIBITEURS DE RAS FARNESYL TRANSFERASE
  申请人：WARNER LAMBERT CO

  公开号：WO2001079180A2

  公开（公告）日：2001-10-25

  The present invention provides novel 5-substituted tetralones of Formulas (I), (II), (III) and (IV) and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme.
• 5-substituted tetralones as inhibitors of ras farnesyl transferase
  申请人：Denny William Alexander

  公开号：US06943183B2

  公开（公告）日：2005-09-13

  The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme

  本发明提供了式I、II、III和IV的新型5-取代四酮及其药学上可接受的盐、酯、酰胺和前药，用于治疗和预防组织的不受控制或异常增殖，如癌症、动脉粥样硬化、再狭窄和银屑病。具体来说，本发明涉及抑制法尼酰转移酶酶的化合物。