881209-27-4Relevant academic research and scientific papers
SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES
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, (2013/08/28)
The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia.
Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors
Elagawany, Mohamed,Ibrahim, Mohamed A.,Ali Ahmed, Hany Emary,El-Etrawy, A.Sh.,Ghiaty, Adel,Abdel-Samii, Zakaria K.,El-Feky, Said A.,Bajorath, Juergen
, p. 2007 - 2013 (2013/05/09)
The design and synthesis of pyridazinone and phthalazinone derivatives are described. Newly synthesized compounds were tested on a panel of four kinases in order to evaluate their activity and potential selectivity. In addition, the promising compounds were tested on four cancer cell lines to examine cytotoxic effects. The compounds inhibited DYRK1A and GSK3 with different activity. SAR analysis and docking calculations were carried out to aid in the interpretation of the results. Taken together, our findings suggest that pyridazinone and phthalazinone scaffolds are interesting starting points for design of potent GSK3 and DYRK1A inhibitors.
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT
Kettle, Jason G.,Brown, Simon,Crafter, Claire,Davies, Barry R.,Dudley, Phillippa,Fairley, Gary,Faulder, Paul,Fillery, Shaun,Greenwood, Hannah,Hawkins, Janet,James, Michael,Johnson, Keith,Lane, Clare D.,Pass, Martin,Pink, Jennifer H.,Plant, Helen,Cosulich, Sabina C.
experimental part, p. 1261 - 1273 (2012/04/10)
Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed predictable DMPK properties, and one such compound demonstrated pharmacodynamic knockdown of phosphorylation of AKT and downstream biomarkers in vivo and inhibition of tumor growth in a breast cancer xenograft model.
Fused heterocyclic compounds useful as kinase modulators
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Page/Page column 54-55, (2010/11/26)
Compounds having the formula (1), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are usefuil as kinase modulators, including MK2 modulation, wherein one of E and F is a nitrogen atom and the other of E and F is a carbon atom, Z is N or CR3, and R1, R2, R3, X and Y are as defined herein.
SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page/Page column 69, (2010/10/20)
The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic beta cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
