2-isoquinolin-3-yl-imidazo[1,2-a]pyridine-8-carboxamide | 1092689-70-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 2-isoquinolin-3-yl-imidazo[1,2-a]pyridine-8-carboxamide
• 英文别名: 2-Isoquinolin-3-ylimidazo[1,2-a]pyridine-8-carboxamide
• CAS: 1092689-70-7
• 化学式: C₁₇H₁₂N₄O
• 分子量: 288.308
• InChiKey: BLRBMMFBLVRXEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  73.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Heterocyclic compounds and their use as parp inhibitors
  申请人：——

  公开号：US20030134843A1

  公开（公告）日：2003-07-17

  The invention relates to compounds of formula (I), wherein; either A 1 or A 2 represents CONH 2 , and the other radical A 2 or A 1 represents hydrogen, chlorine, fluorine, bromine, iodine C 1 -C 6 alkyl, OH, nitro, CF 3 , CN, NR 11 R 12 , NH—CO—R 13 , O—C 1 -C 4 alkyl; X 1 can represent N and C—R 2 ; X 2 , independent of X 1 , can represent N and C—R 2 ; R 2 can represent hydrogen, C 1 -C 6 alkyl, C 1 -C 4 alkyl-phenyl, phenyl; B can represent an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 15 carbon atoms, an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 14 carbon atoms and 0 to 5 nitrogen atoms, 0 to 2 oxygen atoms or 0 to 2 sulfur atoms, which can each still be substituted with an R 4 and a maximum of 3 of the same or different radicals R 5 , and; R 1 , R 4 , R 5 , R 11 -R 13 have the meanings as cited in claim No. 1. The invention also relates to the tautomeric forms, and possible enantiomeric and diastereomeric forms of said compounds, to the prodrugs thereof and to their use as PARP inhibitors.

  本发明涉及化合物的公式（I），其中：A1或A2代表CONH2，而另一个基团A2或A1代表氢，氯，氟，溴，碘，C1-C6烷基，OH，硝基，CF3，CN，NR11R12，NH-CO-R13，O-C1-C4烷基；X1可以表示N和C-R2；独立于X1的X2可以表示N和C-R2；R2可以表示氢，C1-C6烷基，C1-C4烷基苯基，苯基；B可以表示最多具有15个碳原子的不饱和，饱和或部分不饱和的单环，双环或三环环，具有最多14个碳原子和0至5个氮原子，0至2个氧原子或0至2个硫原子的不饱和，饱和或部分不饱和的单环，双环或三环环，每个仍可用R4和最多3个相同或不同的基团R5取代；R1，R4，R5，R11-R13具有权利要求1所述的含义。本发明还涉及所述化合物的互变异构体形式，可能的对映异构体和顺反异构体形式，它们的前药和它们作为PARP抑制剂的用途。
• Pharmaceutical Compositions and Method for Treating, Reducing, Ameliorating, Alleviating, or Preventing Dry Eye
  申请人：Zhang Jinzhong

  公开号：US20080305994A1

  公开（公告）日：2008-12-11

  A composition for treating, reducing, ameliorating, alleviating, or preventing a dry eye condition or an opthalmologic disorder that has an etiology in inflammation comprises an inhibitor of activity of poly(ADP-ribose) polymerase (“PARP”). The composition can also include a modulator of pro-inflammatory gene expression.
• US7041675B2
  申请人：——

  公开号：US7041675B2

  公开（公告）日：2006-05-09
• [EN] PHARMACEUTICAL COMPOSITIONS AND METHOD FOR TREATING, REDUCING, AMELIORATING, ALLEVIATING, OR PREVENTING DRY EYE<br/>[FR] COMPOSITIONS PHARMACEUTIQUES ET PROCÉDÉ PERMETTANT DE TRAITER, RÉDUIRE, AMÉLIORER, ATTÉNUER, OU PRÉVENIR LA SÉCHERESSE OCULAIRE
  申请人：BAUSCH & LOMB

  公开号：WO2008154129A1

  公开（公告）日：2008-12-18

  [EN] A composition for treating, reducing, ameliorating, alleviating, or preventing a dry eye condition or an ophthalmologic disorder that has an etiology in inflammation comprises an inhibitor of activity of poly(ADP-ribose) polymerase ("PARP"). The composition can also include a modulator of pro-inflammatory gene expression.
  [FR] La présente invention concerne une composition permettant de traiter, réduire, améliorer, atténuer, ou prévenir un état de sécheresse oculaire ou un trouble ophtalmologique d'origine inflammatoire qui comprend un inhibiteur de l'activité de poly(ADP-ribose)-polymérase ('PARP'). La composition peut également inclure un modulateur de l'expression de gène pro-inflammatoire.