1454848-24-8Relevant articles and documents
Synthesis method of glatianide intermediate
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, (2021/08/25)
The invention provides a synthesis method of a strain facitinib intermediate, which takes acetone oxalate as a starting raw material in a simple and easy manner and is cyclized in sequence. The bromo, propionamide, bromination, amidation, deprotection and dehydration 7 steps give (4 - bromo -5 - cyano -1 - methyl - 1H - pyraz -3 -yl) methyl tert-butyl carbamate. The synthesis method of the Litinib intermediate disclosed by the invention has the characteristics of easily available raw materials, simple operation, low cost, short steps and high yield.
Benzoxadiazepine tetradecene derivative and application thereof
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, (2020/07/15)
The invention discloses a benzoxadiazepine tetradecene derivative and application thereof, belonging to the field of medicines. The benzoxadiazepine tetradecene derivative with a structure as shown ina general formula (I) has excellent anaplastic lymphoma enzyme (ALK) inhibition activity and excellent pharmacodynamic performance, and can obviously prolong the large metabolic half-life period of adrug; the derivative can be safely and effectively used for treating anaplastic lymphoma kinase positive (ALK+) metastatic (advanced) non-small cell lung cancer (NSCLC) and the like, thereby providing a new means for treating cancers, metabolic and immune diseases, cardiovascular diseases, neurological diseases and the like.
Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners
Elleraas, Jeff,Ewanicki, Jason,Johnson, Ted W.,Sach, Neal W.,Collins, Michael R.,Richardson, Paul F.
, p. 3590 - 3595 (2016/03/25)
Lorlatinib (PF-06463922) is an ALK/ROS1 inhibitor and is in clinical trials for the treatment of ALK positive or ROS1 positive NSCLC (i.e. specific subsets of NSCLC). One of the laboratory objectives for this molecule indicated that it would be desirable