260045-39-4Relevant academic research and scientific papers
5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase
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Page/Page column 34, (2010/11/26)
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R101 and R200 are described in the specification.
2,4-DIAMINO PYRIMIDINE COMPOUNDS HAVING ANTI-CELL PROLIFERATIVE ACTIVITY
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Page/Page column 22; 23, (2010/02/11)
A pyrimidine derivative of formula (I) wherein, for example, R1 is hydrogen, (1-6C)alkyl, (3-5C)alkenyl or (3-5C)alkynyl; Q1 and Q2 are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Q1 and Q2 bear
Imidazo[1,2-a]pyridines: A potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation
Anderson, Malcolm,Beattie, John F.,Breault, Gloria A.,Breed, Jason,Byth, Kate F.,Culshaw, Janet D.,Ellston, Rebecca P. A.,Green, Stephen,Minshull, Claire A.,Norman, Richard A.,Pauptit, Richard A.,Stanway, Judith,Thomas, Andrew P.,Jewsbury, Philip J.
, p. 3021 - 3026 (2007/10/03)
High-throughput screening identified the imidazo[1,2-a]pyridine and bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase CDK4. Comparison of their experimentally-determined binding modes and emerging structure-activity trends led to th
Pyrimidine compounds
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Page/Page column 46, (2010/01/31)
A pyrimidine derivative of formula (I) wherein, for example, R1is-(1-6C)alkyl or (3-5C)alkenyl [optionally substituted by a phenyl substituent]; Q1and Q2are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4
IMIDAZO[1,2-A]PYRIDINE AND PYRAZOLO[2,3-A]PYRIDINE DERIVATIVES
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Page/Page column 34, (2010/02/04)
A compound of formula (I) wherein Ring A is imidazol[1,2a]pyrid-3-yl or pyrazolo[2,3a]pyrid-3-yl; Ris as defined within; m is 0-5; wherein the values of Rmay be the same or different; Ris as defined within; n is 0 to 2, wherein the values of Rmay be the same or different; Ring B is phenyl or phenyl fused to a C5-7cycloalkyl ring; Ris as defined within; p is 0-4; wherein the values of Rmay be the same or different; Ris as defined within; q is 0-2; wherein the values of Rmay be the same or different; and wherein p+q=5; or a pharmaceutically acceptable salt or an in vivo hydrolyzable ester thereof is described. The use of compounds of formula (I) in the inhibition of cell cycle kinases CDK2, CDK4, and CDK6 are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
Pyrimidine compounds with pharmaceutical activity
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Page column 30, (2010/02/05)
A pyrimidine derivative of formula (I) wherein V is O or S, Q1and Q2are independently selected from phenyl, naphthyl, a 5- or 6-membered monocyclic moiety and a 9- or 10-membered bicyclic heterocyclic moiety; and Q1is subs
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: Identification and optimisation of substituted 2,4-bis anilino pyrimidines
Breault, Gloria A.,Ellston, Rebecca P. A.,Green, Stephen,James, S. Russell,Jewsbury, Philip J.,Midgley, Catherine J.,Pauptit, Richard A.,Minshull, Claire A.,Tucker, Julie A.,Pease, J. Elizabeth
, p. 2961 - 2966 (2007/10/03)
Through chemical modification and X-ray crystallography we identified the 2,4-bis anilino pyrimidines as potent inhibitors of CDK4. Herein, we describe the optimisation of this series.
Pyrimidine compounds
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, (2008/06/13)
Pyrimidine derivatives of formula (I) wherein: Q1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 is substituted on a ring carbon by one group selected from sulphamoyl, N—(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), C1-4alkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia′): wherein Q1, Q2, G, R1, Y, Z, Q3, n and m are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) inhibitors are also described.
2,4-diamino pyrimidine compounds having anti-cell proliferative activity
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, (2008/06/13)
A pyrimidine derivative of formula (I): wherein: R1is an optional substituent as defined within; Rxis selected from halo, hydroxy, nitro, amino, cyano, mercapto, carboxy, sulphamoyl, formamido, ureido or carbamoyl or a group of formula (Ib): A—B—C— as defined within; Q1and Q2are independently selected from aryl, a 5- or 6-membered monocyclic moiety; and a 9- or 10-membered bicyclic heterocyclic moiety; and one or both of Q1and Q2bears on any available carbon atom one substituent of formula (Ia) as defined within; and Q1and Q2are optionally further substituted; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof; are useful as anti-cancer agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
PYRIMIDINE COMPOUNDS
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, (2008/06/13)
A pyrimidine derivative of formula (I) or (I'): wherein: Ris a substituent as defined within; Q1 is optionally substituted phenyl, and Q1 bears a substituent of formula (Ia) wherein: X, Y, Y, Z, n, and m are as defined within; -NQ2 is an optionally substituted heterocyclic moiety containing one hydrogen heteroatom and optionally containing a further heteroatom; or a pharmaceutically acceptable salt in vivo hydrolysable ester thereof; are useful as anti-cancer agents. Processes for their manufacture and pharmaceutical compositions containing them are described.
