403793-48-6Relevant academic research and scientific papers
Concise, flexible syntheses of 4-(4-imidazolyl)pyrimidine cyclin-dependent kinase 2 (CDK2) inhibitors
Toumi, Mathieu,Barbazanges, Marion,Kroll, Sebastian H.B.,Patel, Hetal,Ali, Simak,Coombes, R. Charles,Barrett, Anthony G.M.
supporting information; experimental part, p. 6126 - 6128 (2010/12/24)
A flexible six-step synthesis of potential cyclin-dependent kinase 2 (CDK2) inhibitors is reported. The synthesis involves the condensation between 3-chloro-4,4-dimethoxy-2-butanone and amidines, which provides acetyl-imidazoles and late stage palladium-catalyzed N-arylation to give the target pyrimidine derivatives.
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.
METHOD FOR PRODUCING 1-SUBSTITUTED-5-ACYLIMIDAZOLE COMPOUND
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Page/Page column 8; 9, (2008/12/05)
An industrially advantageous process for preparing 1-substituted 5-acylimidazole compounds can be performed by reacting an N-substituted amidine compound or a salt thereof with a ketone compound in the presence of a base.
(IMIDAZOLO-5-YL)-2-ANILO-PYRIMIDINES AS AGENTS FOR THE INHIBITION OF CELL PROLIFERATION
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Page/Page column 74-75, (2008/06/13)
Compounds of the formula (I): wherein variable groups 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.
Imidazolo-5-YL-2anilino-pyrimidines as agents for the inhibition of the cell proliffration
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Page/Page column 39, (2010/02/05)
Compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, p, q, and n 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.
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.
