CAS: 1802220-02-5; (7S,13R)-11-Fluoro-6,7,13,14-Tetrahydro-7,13-Dimethyl-1,15-Etheno-1H-Pyrazolo[4,3-F][1,4,8,10]Benzoxatriazacyclotridecin-4(5H)-One

2,5-二氟苯腈置于盐酸,1,2-Bis((2R,5R)-2,5-Dimethylphospholano)Benzene(Cyclooctadiene)Rhodium(I)Tetrafluoroborate,五氟苯基二苯基磷酸酯,水,氢气,双(三甲基硅烷基)氨基钾,三乙胺,N,N-二异丙基乙胺,Lithium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,N,N-二甲基甲酰胺,正丁醇 用作溶剂,-78.0~120.0 °C,620.54 Kpa 条件下,反应 60.0H,反应生成洛普替尼
参考文献: Diaryl Macrocycle Polymorph[fr] Polymorphe De Macrocycle De Diaryle
标题: Diaryl Macrocycle Polymorph[fr] Polymorphe De Macrocycle De Diaryle
摘要:这项披露涉及对(7S,13R)-11-氟-7,13-二甲基-6,7,13,14-四氢-1,15-乙烯吡唑并[4,3-F][1,4,8,10]苯并氧三唑环三十四(5H)-酮的多型体,这些多型体在哺乳动物中治疗疾病(如癌症)方面是有用的.这项披露还涉及包括这些多型体的组合物,以及在哺乳动物中(尤其是人类)治疗疾病(如癌症)中使用这些组合物的方法.

专利信息

专利号:US-2011124634-A1
优先权日:2008-05-13
标 题:Bioactive compounds for treatment of cancer and neurodegenerative diseases
发明人：SUN CONNIE L; LI XIAOYUAN
权利人:PONIARD PHARMACEUTICALS INC
摘要:The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.