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    • 7. 发明申请
    • METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS
    • 合成取代的嘌呤化合物的方法
    • WO2014152566A2
    • 2014-09-25
    • PCT/US2014/027481
    • 2014-03-14
    • EPIZYME, INC.
    • OLHAVA, Edward, James
    • A61K31/7076
    • C07H19/16A61K31/4184A61K31/7076C07B2200/13C07D235/12C07H1/06C07H19/06C07H19/067C07H19/167Y02A50/401Y02A50/409Y02A50/411
    • The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H- benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofiiran-3,4-diol and hydrates thereof and methods for treating disorders in which DOTl -mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)- 5 -(((( 1 r,3 S)-3 -(2-(5 -(tert-butyl)- 1 H-benzo[d] imidazol-2- yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
    • 本发明提供了合成(2R,3R,4S,5R)-2-(6-氨基-9H-嘌呤-9-基)-5 - ((((1r,3S)-3- (2-(5-(叔丁基)-1H-苯并[d]咪唑-2-基)乙基)环丁基)(异丙基)氨基)甲基)四氢呋喃-3,4-二醇及其水合物和治疗疾病的方法 通过将这些化合物和药物组合物施用于有需要的受试者,其中DOT1介导的蛋白质甲基化部分起作用,例如癌症和神经障碍。 本发明还提供了(2R,3R,4S,5R)-2-(6-氨基-9H-嘌呤-9-基)-5 - ((((1R,3S) (2-(5-(叔丁基)-1H-苯并[d]咪唑-2-基)乙基)环丁基)(异丙基)氨基)甲基)四氢呋喃-3,4-二醇及其水合物(形式A, 形式B和形式C),其特征在于独特的X射线衍射图和差示扫描量热法,以及独特的晶体结构。
    • 8. 发明申请
    • INJECTABLE FORMULATIONS FOR TREATING CANCER
    • 用于治疗癌症的注意事项
    • WO2014152562A1
    • 2014-09-25
    • PCT/US2014/027477
    • 2014-03-14
    • EPIZYME, INC.
    • OLHAVA, Edward, James
    • A61K31/7076
    • A61K31/7076A61K9/0019A61K9/08A61K47/40Y02A50/401Y02A50/409Y02A50/411
    • The present invention provides injectable formulations of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H- benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders. Disease-associated chromatin-modifying enzymes (e.g., DOT1L) play a role in diseases such as proliferative disorders, metabolic disorders, and blood disorders. The formulations further include a solubilizer such as cyclodextrins; pH adjustment reagent such as citric acid; and isotonic reagent such as dextrose or sodium chloride.
    • 本发明提供(2R,3R,4S,5R)-2-(6-氨基-9H-嘌呤-9-基)-5 - ((((1r,3S)-3-(2-( (叔丁基)-1H-苯并[d]咪唑-2-基)乙基)环丁基)(异丙基)氨基)甲基)四氢呋喃-3,4-二醇及其水合物以及其中DOT1- 介导的蛋白质甲基化发挥作用,如癌症和神经系统疾病。 与疾病相关的染色质修饰酶(例如,DOT1L)在增殖性疾病,代谢紊乱和血液病症等疾病中发挥作用。 制剂还包括增溶剂如环糊精; pH调节试剂如柠檬酸; 和等渗试剂如葡萄糖或氯化钠。