4-(benzothiazol-6-ylamino)-6-[(1H-indazol-6-yl)-methylamino]-[1,3, 5] triazin-2-ol | 677710-85-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-(benzothiazol-6-ylamino)-6-[(1H-indazol-6-yl)-methylamino]-[1,3, 5] triazin-2-ol
• 英文别名: 6-(1,3-benzothiazol-6-ylamino)-4-[1H-indazol-6-yl(methyl)amino]-1H-1,3,5-triazin-2-one
• CAS: 677710-85-9
• 化学式: C₁₈H₁₄N₈OS
• 分子量: 390.428
• InChiKey: OEXNQFKQXZHSHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  139
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• [EN] 4,6-DIAMINOSUBSTITUTED-2-[OXY OR AMINOXY]-[1,3,5]TRIAZINES AS PROTEIN TYROSINE KINASE INHIBITORS<br/>[FR] 4,6-DIAMINOSUBSTITUES-2-[OXY OR AMINOXY]-[1,3,5]TRIAZINES UTILISES EN TANT QU'INHIBITEURS DE LA PROTEINE TYROSINE KINASE
  申请人：DIMENSIONAL PHARM INC

  公开号：WO2004031184A1

  公开（公告）日：2004-04-15

  The invention is directed to compounds of Formulae (I, II, III) or (IV): wherein R, R1, R2, R3, A1 and A2 are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially VEGFR-2 (KDR), c-fms, c-met and tie-2 kinases. The invention is also directed toward methods of preparation of the compounds of Formulae (I, II, III) and (IV).

  该发明涉及具有以下化学式（I，II，III）或（IV）的化合物：其中R，R1，R2，R3，A1和A2如规范中所述，以及它们的溶剂化合物、水合物、互变异构体或药用可接受的盐，这些化合物抑制蛋白酪氨酸激酶，特别是VEGFR-2（KDR），c-fms，c-met和tie-2激酶。该发明还涉及制备具有化学式（I，II，III）和（IV）的化合物的方法。
• [EN] 7-ARYL-3,9-DIAZABICYCLO(3.3.1)NON-6-ENE DERIVATIVES AND THEIR USE AS RENIN INHIBITORS IN THE TREATMENT OF HYPERTENSION, CARDIOVASCULAR OR RENAL DISEASES<br/>[FR] DERIVES DE 7-ARYL-3,9-DIAZABICYCLO(3.3.1)NON-6-ENE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE RENINE DANS LE TRAITEMENT DE L'HYPERTENSION, DE MALADIES CARDIOVASCULAIRES OU RENALES
  申请人：ACTELION PHARMACEUTICALS LTD

  公开号：WO2003093267A1

  公开（公告）日：2003-11-13

  The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors or renin.

  该发明涉及新型3,9-二氮杂双环[3.3.1]壬烯衍生物（I）及相关化合物，以及它们作为药物组合物中活性成分的用途。该发明还涉及相关方面，包括制备这些化合物的过程、含有这些化合物中的一个或多个的药物组合物，尤其是它们作为肾素抑制剂的用途。
• 4,6-Diaminosubstituted-2-[oxy or aminoxy]-[1,3,5]triazines as protein tyrosine kinase inhibitors
  申请人：——

  公开号：US20040110758A1

  公开（公告）日：2004-06-10

  The invention is directed to compounds of Formulae I, II, III or IV: 1 wherein R, R 1 , R 2 , R 3 , A 1 and A 2 are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially VEGFR-2 (KDR), c-fms, c-met and tie-2 kinases. The invention is also directed toward methods of preparation of the compounds of Formulae I, II, III and IV.

  本发明涉及公式I、II、III或IV的化合物：1其中R、R1、R2、R3、A1和A2如规范中所述，以及其溶剂化物、水合物、互变异构体或药学上可接受的盐，其抑制蛋白酪氨酸激酶，特别是VEGFR-2（KDR）、c-fms、c-met和tie-2激酶。本发明还涉及制备公式I、II、III和IV的化合物的方法。
• 7-ARYL-3,9-DIAZABICYCLO[3.3.1]NON-6-ENE DERIVATIVES AND THEIR USE AS RENIN INHIBITORS IN THE TREATMENT OF HYPERTENSION, CARDIOVASCULAR OR RENAL DISEASES
  申请人：Actelion Pharmaceuticals Ltd.

  公开号：EP1501830A1

  公开（公告）日：2005-02-02
• 4,6-DIAMINOSUBSTITUTED-2-[OXY OR AMINOXY]-[1,3,5]TRIAZINES AS PROTEIN TYROSINE KINASE INHIBITORS
  申请人：Johnson & Johnson Pharmaceutical Research & Development, Inc.

  公开号：EP1549645A1

  公开（公告）日：2005-07-06