2-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]oxy-1H-indole

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]oxy-1H-indole
• 化学式: C₁₅H₁₁F₃N₂O
• 分子量: 292.26
• InChiKey: FAFGPFOLXADZTK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  37.9
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] ANTIANGIOGENIC BICYCLIC DERIVATIVES<br/>[FR] DERIVES BICYCLIQUES ANTIANGIOGENIQUES
  申请人：ASTRAZENECA AB

  公开号：WO2002016348A1

  公开（公告）日：2002-02-28

  The invention relates to compounds of the formula I: wherein: ring C is a 5 or 6-membered heteroaromatic ring containing at least one nitrogen atom and optionally containing a further 1-2 heteroatoms, selected independently from O, S and N; either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are -CH-, or G1, G2, G3, G4, and G5 are all - CH-; Z is -O-, -NH-, -S-, CH2-, or a direct bond; Z is linked to any one of G1, G2, G3, and G4; n is an integer from 0 to 5; any of the substituents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 4, Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, oxo, hydroxy, halogeno, C¿1-4?alkyl, C1-4alkoxy, C1-4alkyxyC1-4alkyl, aminoC1-4alkyl, aminoC1-4alkyl, C1-3alkylaminoC1-4alkyl, di(C1-3alkyl)aminoC1-4alkyl, -C1-5alkyl(ring B) wherein ring B is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperzinyl, N-ethylpiperazinyl, morpholino and thiomorpholino; R?2¿ represents hydrogen, hydroxy, halogeno, cyano, nitro, trifuloromethyl, C ¿1-3?alkyl, C1-3alkoxy, C1-3alkylsulphanyl,-NR?3R4¿ /wherein R?3 and R4¿, which may be the same or different, each represents hydrogen or C¿1-3?alkyl), or R?5X1¿-(wherein R?5 and X1¿ are as defined herein) and salts thereof, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable slats thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.