6-methoxy-N-phenylquinazolin-4-amine

• 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: 6-methoxy-N-phenylquinazolin-4-amine
• 化学式: C₁₅H₁₃N₃O
• 分子量: 251.28
• InChiKey: GKRKTKNUATZSTP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  47
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• QUINAZOLINE DERIVATIVES AS VEGF INHIBITORS
  申请人：Thomas Andrew Peter

  公开号：US20110065736A1

  公开（公告）日：2011-03-17

  The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R 1 represents halogeno or C 1-3 alkyl; X 1 represents —O—; R 2 is selected from one of the following three groups: 1) C 1 -5alkylR 3 (wherein R 3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C 1-4 alkyl, C 1-4 hydroxyalkyl and C 1-4 alkoxy; 2) C 2-5 alkenylR 3 (wherein R 3 is as defined hereinbefore); 3) C 2-5 alkynylR 3 (wherein R 3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

  本发明涉及式（I）的喹唑啉衍生物，其中m是1到3的整数；R1代表卤素或C1-3烷基；X1代表—O—；R2从以下三个群组中选择：1）C1-5烷基R3（其中R3是哌啶基-4-基，可能带有一个或两个取自羟基、卤素、C1-4烷基、C1-4羟基烷基和C1-4烷氧基的取代基）；2）C2-5烯基R3（其中R3如上定义）；3）C2-5炔基R3（其中R3如上定义）；其中任何烷基、烯基或炔基可能带有一个或多个取自羟基、卤素和氨基的取代基；以及它们的盐；制备它们的方法，含有式（I）的化合物或其药学上可接受的盐作为活性成分的制药组合物。式（I）化合物和其药学上可接受的盐抑制VEGF的作用，这是在治疗包括癌症和类风湿性关节炎在内的多种疾病状态中具有价值的属性。
• QUINAZOLINE DERIVATIVES HAVING TYROSINE KINASE INHIBITORY ACTIVITY
  申请人：KUME Masaharu

  公开号：US20120123114A1

  公开（公告）日：2012-05-17

  A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided. A compound represented by the general formula (I): wherein R X is a group represented by the formula: wherein R 1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R 10 )—, etc.; R 10 is a hydrogen atom, alkyl, etc.; R 2 is a hydrogen atom, optionally substituted alkyl, etc.; R 18 is a hydrogen atom, optionally substituted alkyl, etc.; R 19 is optionally substituted alkyl, etc.; W 1 is an optionally substituted non-aromatic nitrogen-containing group; R 17 is a hydrogen atom, optionally substituted alkyl, etc.; R 3 and R 4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R 12 )—, etc.; R 12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.

  提供了一种同时抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶的化合物。该化合物的普遍式表示为（I）：其中，RX是由以下式表示的基团：其中，R1是氢原子，可选地取代的烷基等；Z为—O—，—N(R10)—等；R10为氢原子，烷基等；R2为氢原子，可选地取代的烷基等；R18为氢原子，可选地取代的烷基等；R19为可选地取代的烷基等；W1为可选地取代的非芳香族含氮基团；R17为氢原子，可选地取代的烷基等；R3和R4分别为氢原子，可选地取代的烷基等；X为—O—，—S—或—N(R12)—等；R12为氢原子，烷基等；A为苯基，可选地具有取代基等，其药学上可接受的盐或其溶剂化物。
• Quinazoline Derivatives as VEGF Inhibitors
  申请人：AstraZeneca AB

  公开号：US20140121228A1

  公开（公告）日：2014-05-01

  The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R 1 represents halogeno or C 1-3 alkyl; X 1 represents —O—; R 2 is selected from one of the following three groups: 1) C 1-5 alkylR 3 , wherein R 3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C 1-4 alkyl, C 1-4 hydroxyalkyl and C 1-4 alkoxy; 2) C 2-5 alkenylR 3 , wherein R 3 is as defined herein; 3) C 2-5 alkynylR 3 , wherein R 3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

  本发明涉及公式（I）的喹唑啉衍生物，其中m是1至3的整数；R1代表卤素或C1-3烷基；X1代表—O—；R2从以下三个组中选择一个：1）C1-5烷基R3，其中R3是哌啶基-4-基，可以带有一个或两个取自羟基、卤素、C1-4烷基、C1-4羟基烷基和C1-4烷氧基的取代基；2）C2-5烯基R3，其中R3如上定义；3）C2-5炔基R3，其中R3如上定义；其中任何烷基、烯基或炔基可以带有一个或多个取自羟基、卤素和氨基的取代基；以及它们的盐；制备它们的方法；含有公式（I）的化合物或其药学上可接受的盐作为活性成分的制药组合物。
• US8349857B2
  申请人：——

  公开号：US8349857B2

  公开（公告）日：2013-01-08
• US8642608B2
  申请人：——

  公开号：US8642608B2

  公开（公告）日：2014-02-04