1436686-17-7Relevant articles and documents
MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS AND USES THEREOF
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, (2019/05/30)
The present disclosure describes novel TRK kinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such TRK kinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described.
Substituted heteroaryl compounds and compositions and uses thereof
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Paragraph 0745-0746; 0757-0758, (2017/12/02)
The invention discloses a substituted ceteroary compound as well as a composition and an application thereof. The compound is a compound shown in a formula (I) or a stereisomer, a tautomer, a nitric oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug of the compound shown in the formula (I). The invention further discloses a pharmaceutical composition including the compound. The compound and the pharmaceutical composition are capable of adjusting the activity of the AK kinase and can be used for preventing, processing, treating and relieving the JAK-mediated disease or disorder.
SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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Paragraph 385, (2015/06/03)
The present invention provides novel heterocyclic compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a JAK-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of JAK-mediated disease.
Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design
Wang, Xiaojing,Magnuson, Steven,Pastor, Rich,Fan, Eric,Hu, Huiyong,Tsui, Vickie,Deng, Wei,Murray, Jeremy,Steffek, Micah,Wallweber, Heidi,Moffat, John,Drummond, Jason,Chan, Grace,Harstad, Eric,Ebens, Allen J.
, p. 3149 - 3153 (2013/06/27)
Pim kinases are promising targets for the development of cancer therapeutics. Among the three Pim isoforms, Pim-2 is particularly important in multiple myeloma, yet is the most difficult to inhibit due to its high affinity for ATP. We identified compound 1 via high throughput screening. Using property-based drug design and co-crystal structures with Pim-1 kinase to guide analog design, we were able to improve potency against all three Pim isoforms including a significant 10,000-fold gain against Pim-2. Compound 17 is a novel lead with low picomolar potency on all three Pim kinase isoforms.