2-Amino-N-[4-fluoro-3-(trifluoromethyl)phenyl]benzamide | 269391-30-2

• 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: 2-Amino-N-[4-fluoro-3-(trifluoromethyl)phenyl]benzamide
• CAS: 269391-30-2
• 化学式: C₁₄H₁₀F₄N₂O
• 分子量: 298.24
• InChiKey: ALAWLLBUCUAXJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-Amino-N-[4-fluoro-3-(trifluoromethyl)phenyl]benzamide 、 6-甲氧基-3-吡啶甲醛 在 左旋樟脑磺酸 作用下， 以 甲苯 为溶剂， 反应 5.0h， 生成 3-(4-fluoro-3-trifluoromethyl-phenyl)-2-(6-methoxy-pyridin-3-yl)-2,3-dihydro-1H-quinazolin-4-one
  参考文献：
  名称：

  [EN] ANTHRANILIC ACID AMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE
  [FR] DERIVES D'AMIDE D'ACIDE ANTHRANILIQUE ET LEURS UTILISATIONS PHARMACEUTIQUES

  摘要：

  本发明涉及新的蒽酰胺衍生物，其制备方法，其在用于治疗人体或动物体的过程中的应用，以及其单独使用或与一个或多个其他药用活性化合物结合使用的用途。

  公开号：

  WO2004052884A1

文献信息

• N-aryl(thio)anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors
  申请人：——

  公开号：US20020019414A1

  公开（公告）日：2002-02-14

  1 Described are compounds of formula (I), wherein W is O or S; X is NR 8 ; Y is CR 9 R 10 -(CH 2 )n wherein R 9 and R 10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO 2 ; R 1 is aryl; R 2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R 2 cannot represent 2-phthalimidyl, and in case of Y═SO 2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R 3 , R 4 , R 5 and R 6 , independently of the other, is H or a substituent other than hydrogen; and R 7 and R 8 , independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

  描述的是化合物的结构式（I），其中W是O或S；X是NR8；Y是CR9R10-(CH2)n，其中R9和R10彼此独立地是氢或较低的烷基，n是从0到3的整数；或Y是SO2；R1是芳基；R2是一个含有一个或多个环氮原子的单环或双环杂环基团，但R2不能代表2-邻苯二甲酰胺，并且在Y为SO2的情况下不能代表2,1,3-苯并噻二唑-4-基；R3、R4、R5和R6中的任何一个，独立于其他，是H或除氢之外的取代基；R7和R8，彼此独立地是H或较低的烷基；或其N-氧化物或药用可接受的盐，用于制备用于治疗对VEGF受体酪氨酸激酶活性抑制产生反应的恶性疾病的药物产品。结构式（I）的化合物可用于治疗恶性疾病，如肿瘤疾病，视网膜病和老年性黄斑变性等。
• N-aryl (THIO) anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors
  申请人：——

  公开号：US20040198782A1

  公开（公告）日：2004-10-07

  1 Described are compunds of formula (I), wherein W is O or S; X is NR 8 ; Y is CR 9 R 10 —(CH 2 ) n wherein R 9 and R 10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO 2 ; R 2 is aryl; R 2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R 2 cannot represent 2-phthalimidyl, and in case of Y=SO 2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R 3 , R 4 , R 5 and R 6 , independently of the other, is H or a substituent other than hydrogen; and R 7 and R 8 , independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

  描述了化合物的公式(I)，其中W为O或S; X为NR8; Y为CR9R10—(CH2)n，其中R9和R10独立地为氢或低烷基，n为0至3的整数，包括0和3; 或Y为SO2; R2为芳基; R2为一种单环或双环杂环芳基，包括一个或多个环氮原子，但R2不能表示2-邻苯二甲酰亚胺基，且在Y = SO2的情况下不能表示2,1,3-苯并噻二唑-4-基; R3、R4、R5和R6中的任何一个，除了氢之外，都是取代基; R7和R8独立地为氢或低烷基; 或其N-氧化物或药学上可接受的盐，用于制备治疗对VEGF受体酪氨酸激酶活性抑制有反应的肿瘤疾病的制药产品。公式(I)的化合物可用于治疗肿瘤疾病，如肿瘤疾病，视网膜病和年龄相关性黄斑变性等。
• N-aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors
  申请人：——

  公开号：US20030064992A1

  公开（公告）日：2003-04-03

  1 Described are compunds of formula (I), wherein W is O or S; X is NR 8 ; Y is CR 9 R 10 —(CH 2 )n wherein R 9 and R 10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO 2 ; R 1 is aryl; R 2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R 2 cannot represent 2-phthalimidyl, and in case of Y=SO 2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R 3 , R 4 , R 5 and R 6 , independently of the other, is H or a substituent other than hydrogen; and R 7 and R 8 , independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

  本文描述了式(I)的化合物，其中W为O或S；X为NR8；Y为CR9R10—(CH2)n，其中R9和R10独立地为氢或低碳基，n为0至3的整数，或Y为SO2；R1为芳基；R2为一个单环或双环杂芳基，其中包含一个或多个环氮原子，但R2不能代表2-苯酰亚胺基，且在Y=SO2的情况下不能代表2,1,3-苯并噻二唑-4-基；R3、R4、R5和R6中的任意一个，独立于其他的，为H或除氢以外的取代基；且R7和R8独立地为H或低碳基；或其N-氧化物或药学上可接受的盐，用于制备治疗对VEGF受体酪氨酸激酶活性抑制有反应的肿瘤疾病的药物产品。式(I)的化合物可用于治疗肿瘤疾病，如肿瘤疾病、视网膜病变和老年性黄斑变性等。
• Anthranilic acid amide derivatives and their pharmaceutical use
  申请人：Bold Guido

  公开号：US20060128684A1

  公开（公告）日：2006-06-15

  The present invention relates to new anthranilic acid amide derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds.

  本发明涉及新的蒽酰胺衍生物，其制备方法，其在治疗人体或动物体的过程中的应用，以及其在单独使用或与一个或多个其他药物活性化合物结合使用的用途。
• ANTHRANILIC ACID AMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE
  申请人：Novartis AG

  公开号：EP1572686A1

  公开（公告）日：2005-09-14