115204-74-5Relevant articles and documents
HYPOXANTHINE COMPOUND
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Paragraph 0066, (2021/05/13)
The present invention aims to provide a novel compound which has prolyl hydroxylases (PHDs) inhibitory effect and which is useful for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. The present invention relates to hypoxanthine compound or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have prolyl hydroxylase inhibitory effect and are useful as agents for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. In an embodiment, the present invention relates to a method for treating an inflammatory bowel disease, comprising administering a necessary amount of a pharmaceutical composition containing hypoxanthine compound or a pharmaceutically acceptable salt thereof, and pharmaceutical additive to a patient.
EGFR INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 42; 43, (2020/07/31)
Provided are compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or inf
Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1
Malínková, Veronika,?ezní?ková, Eva,Jorda, Radek,Gucky, Tomá?,Kry?tof, Vladimír
, p. 6523 - 6535 (2017/11/03)
Inhibition of protein kinases is a validated concept for pharmacological intervention in cancers. Many kinase inhibitors have been approved for clinical use, but their practical application is often limited. Here, we describe a collection of 23 novel 2,6,9-trisubstituted purine derivatives with nanomolar inhibitory activities against PDGFRα, a receptor tyrosine kinase often found constitutively activated in various tumours. The compounds demonstrated strong and selective cytotoxicity in the human eosinophilic leukemia cell line EOL-1, whereas several other cell lines were substantially less sensitive. The cytotoxicity in EOL-1, which is known to express the FIP1L1‐PDGFRA fusion gene encoding an oncogenic kinase, correlated significantly with PDGFRα inhibition. EOL-1 cells treated with the compounds also exhibited dose-dependent inhibition of PDGFRα autophosphorylation and suppression of its downstream signaling pathways with concomitant G1 phase arrest, confirming the proposed mechanism of action. Our results show that substituted purines can be used as platforms for preparing tyrosine kinase inhibitors with specific activity towards eosinophilic leukemia.