403793-46-4Relevant academic research and scientific papers
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors
Anderson, Malcolm,Andrews, David M.,Barker, Andy J.,Brassington, Claire A.,Breed, Jason,Byth, Kate F.,Culshaw, Janet D.,Finlay, M. Raymond V.,Fisher, Eric,McMiken, Helen H.J.,Green, Clive P.,Heaton, Dave W.,Nash, Ian A.,Newcombe, Nicholas J.,Oakes, Sandra E.,Pauptit, Richard A.,Roberts, Andrew,Stanway, Judith J.,Thomas, Andrew P.,Tucker, Julie A.,Walker, Mike,Weir, Hazel M.
scheme or table, p. 5487 - 5492 (2009/05/30)
An imidazole series of cyclin-dependent kinase (CDK) inhibitors has been developed. Protein inhibitor structure determination has provided an understanding of the emerging structure activity trends for the imidazole series. The introduction of a methyl sulfone at the aniline terminus led to a more orally bioavailable CDK inhibitor that was progressed into clinical development.
Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors
Jones, Clifford D.,Andrews, David M.,Barker, Andrew J.,Blades, Kevin,Byth, Kate F.,Finlay, M. Raymond V.,Geh, Catherine,Green, Clive P.,Johannsen, Marie,Walker, Mike,Weir, Hazel M.
scheme or table, p. 6486 - 6489 (2009/10/01)
The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. The series was found to have much improved CDK2 inhibition and potent in vitro anti-proliferative effects against cancer cell lines. Control of overall lipophilicity was important to achieve good in vitro potency along with acceptable physiochemical properties and margins against inhibition of both CYP isoforms and the hERG potassium ion channel. A compound with an attractive overall balance of properties was profiled in vivo and possessed suitable physiochemical and pharmacokinetic profiles for oral dosing.
USE OF PYRIMIDINE DERIVATIVES IN THE MANUFACTURE OF A MEDICAMENT FOR PREVENTION AND/OR TREATMENT OF ALZHEIMER’S DISEASE
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Page/Page column 38-39, (2008/06/13)
The present invention relates to a new use of pyrimidine derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof in the manufacture of a medicament in the treatment and/or prophylaxis of Alzheimer's Disease:
DERIVATIVES OF 4- (IMIDAZOL-5-YL)-2-(4-SULFOANILINO) PYRIMIDINE WITH CDK INHIBITORY ACTIVITY
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Page/Page column 53, (2008/06/13)
Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
4- IMIDAZOLYL SUBSTUITED PYRIMIDINE DERIVATIVES WITH CDK INHIBITIORY ACTIVITY
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Page/Page column 55, (2010/02/07)
Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes
