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A patent review of MAPK inhibitors (2018-present)
被引:7
|作者:
Wydra, Valentin R.
[1
]
Ditzinger, Raphael B.
[1
]
Seidler, Nico J.
[1
]
Hacker, Frederik W.
[1
]
Laufer, Stefan A.
[1
,2
,3
,4
]
机构:
[1] Eberhard Karls Univ Tubingen, Dept Pharmaceut & Med Chem, Tubingen, Germany
[2] Eberhard Karls Univ Tubingen, Cluster Excellence iFIT EXC2180 Image Guided & Fun, Tubingen, Germany
[3] Tubingen Ctr Acad Drug Discovery & Dev Tucad2, Tubingen, Germany
[4] Eberhard Karls Univ Tubinge, Pharmazeut Inst, Pharmazeut Chem, Morgenstelle 8, D-72076 Tubingen, Germany
关键词:
C-Jun N-terminal kinase;
deuteration;
downstream target selectivity;
extracellular signal-regulated kinase;
isoform selectivity;
P38 MAP kinase;
mitogen-activated protein kinase;
protacs;
ACTIVATED PROTEIN-KINASE;
N-TERMINAL KINASES;
CELL-PROLIFERATION;
BIOLOGICAL EVALUATION;
ERK5;
POTENT;
DERIVATIVES;
DISCOVERY;
JNK3;
DIFFERENTIATION;
D O I:
10.1080/13543776.2023.2242584
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
IntroductionThe mitogen-activated protein kinase (MAPK) family consist of p38 MAP kinases, c-Jun N-terminal kinases (JNKs) and extracellular signal-regulated kinases (ERKs). They are involved in a multitude of diseases, including inflammatory, autoimmune, neurodegenerative, and metabolic diseases as well as cancer. In recent years, further developments in the field of MAPK-inhibitors have been reported, including an isoform or downstream target selective inhibition of MAPKs as well as target protein degradation approaches.Areas coveredThis review summarizes newly patented MAPK-inhibitors that were claimed between 2018 and early 2023. Presented are the patents as well as their corresponding publications, the storyline of development, and clinical trials involving these compounds. This article elaborates a total of 27 patents, which were identified using established search engines.Expert opinionAlthough industrial research on MAPK-inhibitors has been ongoing for more than 20 years, novel clinical trials of MAPK-inhibitors as potential drug candidates are still being conducted in the period under review. Recently reported inhibitors show an excellent selectivity profile and are even achieving selectivity between closely related isoforms. This progression offers the possibility to eliminate unwanted side effects and may finally lead to the approval of the first MAPK-inhibitor.
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页码:421 / 444
页数:24
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