Bcr-Abl tyrosine kinase inhibitors: a patent review

被引:12
|
作者
Desogus, Andrea [1 ]
Schenone, Silvia [1 ]
Brullo, Chiara [1 ]
Tintori, Cristina [2 ]
Musumeci, Francesca [1 ]
机构
[1] Univ Genoa, Dipartimento Farm, I-16132 Genoa, Italy
[2] Univ Siena, Dipartimento Biotecnol Chim & Farm, I-53100 Siena, Italy
关键词
breakpoint cluster region Abl tyrosine kinase; chronic myeloid leukemia; inhibitors; mutation; T315I; tyrosine kinase; CHRONIC MYELOID-LEUKEMIA; AURORA KINASE; T315I MUTANT; IMATINIB; RESISTANCE; STRATEGIES; INSIGHTS; MUTATION; AP24534; POTENT;
D O I
10.1517/13543776.2015.1012155
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Introduction: Breakpoint cluster region Abelson (Bcr-Abl) tyrosine kinase (TK) is a constitutively activated cytoplasmic TK and is the underlying cause of chronic myeloid leukemia (CML). To date, imatinib represents the frontline treatment for CML therapy. The development of resistance has prompted the search for novel Bcr-Abl inhibitors. Areas covered: This review presents a short overview of drugs already approved for CML therapy and of the compounds that are in clinical trials. The body of the article deals with Bcr-Abl inhibitors patented since 2008, focusing on their chemical features. Expert opinion: The search for Bcr-Abl inhibitors is very active. We believe that a number of patented compounds could enter clinical trials and some could be approved for CML therapy in the next few years. Overall, Bcr-Abl inhibitors constitute a very appealing research field that can be expected to expand further.
引用
收藏
页码:397 / 412
页数:16
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