1060815-90-8Relevant articles and documents
Pyrrolo[2,3-b]pyridine-3-one derivatives as novel fibroblast growth factor receptor 4 inhibitors for the treatment of hepatocellular carcinoma
Jin, Qiaomei,Zhang, Dongjian,Gao, Meng,Jiang, Cuihua,Zhang, Jian
, (2021)
Aberrant signaling of the FGF/FGFR pathway occurs frequently in cancers and is an oncogenic driver in many solid tumors, especially liver cancer. With the resurgence of interest in irreversible inhibitors, efforts have been directed to the discovery of ir
The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain
Skerratt, Sarah E.,Andrews, Mark,Bagal, Sharan K.,Bilsland, James,Brown, David,Bungay, Peter J.,Cole, Susan,Gibson, Karl R.,Jones, Russell,Morao, Inaki,Nedderman, Angus,Omoto, Kiyoyuki,Robinson, Colin,Ryckmans, Thomas,Skinner, Kimberly,Stupple, Paul,Waldron, Gareth
supporting information, p. 10084 - 10099 (2016/12/07)
The neurotrophin family of growth factors, comprised of nerve growth factor (NGF), brain derived neurotrophic factor (BDNF), neurotrophin 3 (NT3), and neurotrophin 4 (NT4), is implicated in the physiology of chronic pain. Given the clinical efficacy of anti-NGF monoclonal antibody (mAb) therapies, there is significant interest in the development of small molecule modulators of neurotrophin activity. Neurotrophins signal through the tropomyosin related kinase (Trk) family of tyrosine kinase receptors, hence Trk kinase inhibition represents a potentially druggable point of intervention. To deliver the safety profile required for chronic, nonlife threatening pain indications, highly kinase-selective Trk inhibitors with minimal brain availability are sought. Herein we describe how the use of SBDD, 2D QSAR models, and matched molecular pair data in compound design enabled the delivery of the highly potent, kinase-selective, and peripherally restricted clinical candidate PF-06273340.
NEW CHEMICAL COMPOUNDS
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Page/Page column 91-92, (2010/04/03)
The present invention encompasses compounds of general formula (1) while the groups R4 to R7 and the units W, L, Qa and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.