N-{3-[(3-{4-chloro-3-[2-methyl-8-(trifluoromethyl)quinazolin-4-yl]phenoxy}-phenyl)sulfonyl]propyl} methanesulfonamide | 1227674-09-0

• 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: N-{3-[(3-{4-chloro-3-[2-methyl-8-(trifluoromethyl)quinazolin-4-yl]phenoxy}-phenyl)sulfonyl]propyl} methanesulfonamide
• 英文别名: N-{3-[(3-{4-chloro-3-[2-methyl-8-(trifluoromethyl)quinazolin-4-yl]phenoxy}phenyl)-sulfonyl]propyl}methanesulfonamide；N-[3-[3-[4-chloro-3-[2-methyl-8-(trifluoromethyl)quinazolin-4-yl]phenoxy]phenyl]sulfonylpropyl]methanesulfonamide
• CAS: 1227674-09-0
• 化学式: C₂₆H₂₃ClF₃N₃O₅S₂
• 分子量: 614.066
• InChiKey: CYBNHYHQKMJYBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  40
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  132
• 氢给体数：
  1
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  3-(3-(4-chloro-3-(2-methyl-8-(trifluoromethyl)quinazolin-4-yl)phenoxy)-phenylsulfonyl)propan-1-amine 、 甲基磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 生成 N-{3-[(3-{4-chloro-3-[2-methyl-8-(trifluoromethyl)quinazolin-4-yl]phenoxy}-phenyl)sulfonyl]propyl} methanesulfonamide
  参考文献：
  名称：

  [EN] POLAR QUINAZOLINES AS LIVER X RECEPTORS ( LXRS ) MODULATORS
  [FR] QUINAZOLINES POLAIRES EN TANT QUE MODULATEURS DES RÉCEPTEURS HÉPATIQUES X (LXR)

  摘要：

  本文披露了基于极性喹唑啉的肝X受体（LXRs）调节剂及相关方法。这些调节剂包括式（I）的化合物：在规范中以书面形式显示的插入公式（I）中，其中，R1、R2、R3、R4、R5、R6、R22、R23、R24、R25、R26、R27、R28、R29、W、W1、W2、Ra、Rb、Rc、Rd、Re、Rf、Rg、Rh、Ri、Rj、Rm、Rn、Ro、Rp、Rq、Rr、Rs、Rt、Ru和n可以如本文任何地方定义的那样。一般来说，这些化合物可用于治疗或预防由LXRs介导的一种或多种疾病、疾病、疾病或症状。

  公开号：

  WO2010059627A1

文献信息

• Methods for the treatment of synucleinopathies
  申请人：Lansbury T. Peter

  公开号：US20050272722A1

  公开（公告）日：2005-12-08

  Methods are provided of treating synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease and Multiple System Atrophy, comprising administering to a synucleinopathic subject a farnesyl transferase inhibitor compound.

  提供了一种治疗突触核蛋白病的方法，例如帕金森病、弥漫性Lewy体病和多系统萎缩症，包括向突触核蛋白病患者施用一种法尼酰转移酶抑制剂化合物。
• Polar Quinazolines
  申请人：Travins Jeremy Mark

  公开号：US20100184786A1

  公开（公告）日：2010-07-22

  Disclosed are polar quinazoline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): in which, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 22 , R 23 , R 24 , R 25 , R 26 , R 27 , R 28 , R 29 , W, W 1 , W 2 , R a , R b , R c , R d , R e , R f , R g , R h , R i , R j , R m , R n , R o , R p , R q , R r , R s , R t , R u , and n can be as defined anywhere herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.

  本发明涉及极性喹嗪基的肝X受体（LXR）调节剂及其相关方法。这些调节剂包括式(I)的化合物：其中R1、R2、R3、R4、R5、R6、R22、R23、R24、R25、R26、R27、R28、R29、W、W1、W2、Ra、Rb、Rc、Rd、Re、Rf、Rg、Rh、Ri、Rj、Rm、Rn、Ro、Rp、Rq、Rr、Rs、Rt、Ru和n可以如本文中的任何地方所定义。一般来说，这些化合物可用于治疗或预防由LXR介导的一种或多种疾病、障碍、症状或病情。
• TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR
  申请人：Lansbury, JR. Peter T.

  公开号：US20110294794A1

  公开（公告）日：2011-12-01

  Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.

  本发明提供了一种低剂量法尼醇转移酶抑制剂及其制药组合物，用于治疗蛋白病。这些低剂量低于最初设计这些化合物用于肿瘤治疗所使用的剂量。治疗包括向需要治疗的受体中注射治疗有效量的法尼醇转移酶抑制剂，其中该量能够有效抑制参与自噬通路的非Ras FTase底物的法尼酰化，而不会对Ras或其他与肿瘤相关的底物的法尼酰化产生明显影响。按照本发明的治疗方法还可以包括乙酰胆碱酯酶抑制剂、神经营养因子受体激活剂、NMDA拮抗剂、淀粉样沉积抑制剂、抗精神病药物、抗抑郁药物、抗焦虑药物或抗氧化剂。
• Inhibitors of farnesyl protein transferase
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：EP1481975A1

  公开（公告）日：2004-12-01

  This invention relates to compounds that inhibit farnesyl-protein transferase and ras protein farnesylation, thereby making them useful as anti-cancer agents. The compounds are also useful in the treatment of diseases, other than cancer, associated with signal transduction pathways operating through ras and those associated with proteins other than ras that are also post-translationally modified by the enzyme farnesyl protein transferase. The compounds may also act as inhibitors of other prenyl transferases, and thus be effective in the treatment of diseases associated with other prenyl modifications of proteins.

  本发明涉及抑制法尼基蛋白转移酶和 ras 蛋白法尼基化，从而使其可用作抗癌剂的化合物。除癌症外，这些化合物还可用于治疗与通过 ras 运作的信号转导通路有关的疾病，以及与同样经法尼基蛋白转移酶翻译后修饰的 ras 以外的蛋白质有关的疾病。这些化合物还可以作为其他前炔基转移酶的抑制剂，从而有效治疗与蛋白质的其他前炔基化修饰有关的疾病。
• POLAR QUINAZOLINES AS LIVER X RECEPTORS ( LXRS ) MODULATORS
  申请人：Wyeth LLC

  公开号：EP2367801A1

  公开（公告）日：2011-09-28