1H-Imidazo[4,5-g]quinazoline | 53974-23-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 1H-Imidazo[4,5-g]quinazoline
• CAS: 53974-23-5
• 化学式: C₉H₆N₄
• mdl: MFCD18808189
• 分子量: 170.17
• InChiKey: DMZDMJAFXVYQHZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (9ci)-1H-咪唑并[4,5-g]喹唑啉-8-胺 生成 1H-Imidazo[4,5-g]quinazoline
  参考文献：
  名称：

  LEONARD, NELSON J.;PETRIC, ANDREJ;RYKOWSKI, ANDRZEJ, J. ORG. CHEM., 53,(1988) N 16, C. 3873-3875

  摘要：

  DOI：

文献信息

• Quinazoline derivatives and therapeutic use thereof
  申请人：Lee B. Young

  公开号：US20050187231A1

  公开（公告）日：2005-08-25

  Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also described.

  描述了由一般式表示的喹唑啉衍生物及其药理学可接受的盐，以及含有这些化合物的组合物。还描述了使用这些化合物治疗过度增生性疾病的方法。
• [EN] COMPOUNDS USEFUL IN THERAPY<br/>[FR] COMPOSES UTILES EN THERAPIE
  申请人：PFIZER LTD

  公开号：WO2005068466A1

  公开（公告）日：2005-07-28

  Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein: X represents NR or O; R represents hydrogen, C1-8 alkyl or SO2[C,1-8 alkyl]; W represents N or CH; Y and Y' independently represent hydrogen, halogen, OH, CF3, OCF3, CN, NH2 C1-8 alkyl, C1-8 alkyloxy or C3-8cycloalkyl; Ring A represents a heterocyclic ring containing at least one nitrogen atom; Z represents a direct link, C1-8 alkyl or C3-8 cycloalkyl; R1 represents R2, OR2, OR 3-R4, N(R2)[C1-8 alkylene]aR4; NCOR2, or SR4; R2 and R4 independently represent hydrogen, C3-8 cycloalkyl, CF3, Ar or Het; R3 represents a direct link or C1-8 alkyl; is 0 or 1; Ar represents an aromatic ring, optionally fused to a heterocyclic ring, and/or optionally substituted with one or more groups as described below; Het represents a heterocyclic ring optionally substituted with one or more groups as described below, and/or optionally fused to an aromatic ring which is optionally substituted with one or more groups as described below; at each occurrence C1-8alkyl, C1-8alkylene and C3-8cycloalkyl may be independently optionally substituted with one or more groups as described below; substituent groups for Ar, Het, C1-8alkyl, C1-8alkylene and C3-8cycloalkyl referred to the above are independently selected from hydrogen, halogen, C1-8alkyl, C1-8alkyloxy, S[C1-8alkyl], CN, CF3, NH2 and OH; are useful for treating anxiety, cardiovascular disease (including angina, atherosclerosis, hypertension, heart failure, edema, hypernatremia), dysmenorrhoea (primary and secondary), endometriosis, emesis (including motion sickness), intrauterine growth retardation, inflammation (including rheumatoid arthritis), mittelschmerz, preclampsia, premature ejaculation, premature (preterm) labor and Raynaud's disease.

  式(I)的化合物，或其在药学上可接受的衍生物中，其中：X代表NR或O；R代表氢，C1-8烷基或SO2[C,1-8烷基]；W代表N或CH；Y和Y'独立地代表氢，卤素，羟基，三氟甲基，三氟甲氧基，氰基，NH2，C1-8烷基，C1-8烷氧基或C3-8环烷基；环A代表至少含有一个氮原子的杂环；Z代表直链，C1-8烷基或C3-8环烷基；R1代表R2，OR2，OR3-R4，N(R2)[C1-8烷基]aR4；NCOR2或SR4；R2和R4独立地代表氢，C3-8环烷基，三氟甲基，芳基或杂环基；R3代表直链或C1-8烷基；a为0或1；Ar代表芳香环，可选择与杂环环融合，并/或可选择使用下述一个或多个基团进行取代；Het代表杂环环，可选择使用下述一个或多个基团进行取代，并/或可选择与一个可选择使用下述一个或多个基团进行取代的芳香环融合；在每次出现时，C1-8烷基，C1-8烷基烯和C3-8环烷基可以独立地选择使用下述一个或多个基团进行取代；对于Ar，Het，C1-8烷基，C1-8烷基烯和C3-8环烷基的取代基团如上所述是独立选择自氢，卤素，C1-8烷基，C1-8烷氧基，S[C1-8烷基]，氰基，三氟甲基，NH2和羟基；适用于治疗焦虑症，心血管疾病（包括心绞痛，动脉粥样硬化，高血压，心力衰竭，水肿，高钠血症），月经疼痛（原发性和继发性），子宫内膜异位症，呕吐（包括晕动病），子宫内生长迟缓，炎症（包括类风湿关节炎），中期疼痛，子痫前症，早泄，早产（早产）和雷诺病。
• Quinazoline Derivatives and Therapeutic Use Thereof
  申请人：Lee Young B.

  公开号：US20090030021A1

  公开（公告）日：2009-01-29

  Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also disclosed.

  本发明涉及一般式所代表的喹唑啉衍生物，其药物学上可接受的盐以及含有这些化合物的组合物。还公开了使用这些化合物治疗过度增殖性疾病的方法。
• IMIDAZOQUINAZOLINE DERIVATIVE
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP0668280A1

  公开（公告）日：1995-08-23

  An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R1 andR2 may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R3 represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.

  一种由式(I)代表的咪唑喹唑啉衍生物或其药理学上可接受的盐，其中 R1 和 R2 可以相同或不同，各自代表氢、低级烷基、低级烯基、芳基等；R3 代表氢、低级烷基、环烷基、低级烯基、芳基等；X 代表 O 或 S。该化合物具有强效和选择性的 cCMP 特异性 PDE 抑制剂活性，可用于治疗或缓解心血管疾病，如血栓形成、心绞痛、高血压和动脉硬化、哮喘等。
• IMIDAZOQUINAZOLINE DERIVATIVES
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP0758653A1

  公开（公告）日：1997-02-19

  Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R1 represents hydrogen, optionally substituted lower alkyl, etc.; R2 and R3 are the same or different and each represents hydrogen, optionally substituted lower alkyl, optionally substituted aralkyl, optionally substituted aryl, etc., or R2 and R3 together form an optionally substituted nitrogenous heterocycle; R4 represents hydrogen or optionally substituted lower alkyl; X represents O or S; Y represents a single bond or O; and n is 0, 1, 2 or 3.

  由通式(I)代表的咪唑喹唑啉衍生物或其药理上可接受的盐，其中R1代表氢、任选取代的低级烷基等；R2和R3相同或不同，各自代表氢、任选取代的低级烷基、任选取代的芳烷基、任选取代的芳基等，或R2和R3一起形成任选取代的含氮杂环；R4代表氢或任选取代的低级烷基；X代表O或S；Y代表单键或O；n为0、1、2或3。