(R)-2-(1-amino-1-oxobutan-2-ylamino)-4-(2,3-dihydrobenzo[b][1,4]dioxin-6-ylamino)-6-oxo-1,6-dihydropyrimidine-5-carboxamide | 1374159-59-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并二恶烷
• 英文名称: (R)-2-(1-amino-1-oxobutan-2-ylamino)-4-(2,3-dihydrobenzo[b][1,4]dioxin-6-ylamino)-6-oxo-1,6-dihydropyrimidine-5-carboxamide
• 英文别名: 2-[[(2R)-1-amino-1-oxobutan-2-yl]amino]-4-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-6-oxo-1H-pyrimidine-5-carboxamide
• CAS: 1374159-59-7
• 化学式: C₁₇H₂₀N₆O₅
• 分子量: 388.383
• InChiKey: CFISUHIEEARLOO-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  170
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• [EN] OXYPYRIMIDINES AS SYK MODULATORS<br/>[FR] OXYPYRIMIDINES EN TANT QUE MODULATEURS DE SYK
  申请人：PORTOLA PHARM INC

  公开号：WO2012061415A1

  公开（公告）日：2012-05-10

  The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

  本发明涉及式(I)的化合物及其互变异构体或药用可接受的盐、酯和前药，其为Syk激酶的抑制剂。本发明还涉及用于制备这种化合物的中间体，该化合物的制备，含有该化合物的药物组合物，抑制Syk激酶活性的方法，抑制血小板聚集的方法，以及预防或治疗至少部分由Syk激酶活性介导的多种疾病的方法，如不良血栓形成和非霍奇金淋巴瘤。