Astrazeneca Ab

Zeneca Limited

Imperial Chemical Industries Limited

Ici Pharma S.a.

Gloria Anne Breault

Howard Tucker

Peter Warner

John Oldfield

Janet Elizabeth Pease

Robert Hugh Bradbury

Elizabeth Janet Pease

Andrew Peter Thomas

Jeffrey James Morris

Michael John Betts

Stewart R James

Nicholas John Newcombe

Emma Jane Williams

Philip John Jewsbury

John Franklin Beattie

Phillip John Jewsbury

Philip J Jewbury

A pyrimidine derivative of formula (I) wherein, for example, Ris hydrogen, (1&#x2013;6C)alkyl, (3&#x2013;5C)alkenyl or (3&#x2013;5C)alkynyl; Qand Qare independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Qand Qbears on any available carbon atom one substituent of formula (Ia) [provided that when present in Qthe substituent of formula (Ia) is not adjacent to the &#x2014;NH&#x2014; link]; wherein, for example, X is CH, O, S or NH; Y is H or as defined for Z; Z is OH, SH, NH, (1&#x2013;4C)alkoxy, (1&#x2013;4C)alkylthio, &#x2014;NH(1&#x2013;C)alkyl, &#x2014;N[(1&#x2013;4C)alkyl]or &#x2014;NH&#x2014;(3&#x2013;8C)cycloalkyl; n is 1, 2 or 3; m is 1, 2 or 3; and Qand Qmay optionally bear other substituents selected, for example, from halogeno, (1&#x2013;6C)alkyl, cyano and (2&#x2013;4C)alkenyl; or a pharmaceutically-acceptable salt or in-vivo-hydrolyzable ester thereof; are useful as anti-cancer agents; and processes for heir manufacture and pharmaceutical compositions containing them are described 

2,4-diamino pyrimidine compounds having anti-cell proliferative activity

Pyrimidine derivatives of formula (I) wherein: Qhand Qare independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Qand Qor both Qand Qis substituted on a ring carbon by one group selected from sulphamoyl, N&#x2014;(Calkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(Calkyl)sulphamoyl (optionally substituted by halo or hydroxy), Calkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia'): wherein Q, Q, G, R, Y, Z, Q, 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 

Pyrimidine compounds

Compounds of the formula (I): wherein R, R, R, R, R, R, 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.

Imidazolo-5-YL-2-anilino-pyrimidines as agents for the inhibition of the cell proliferation

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 Ccycloalkyl 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&#x2266;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.

Imidazo[1,2-A]pyridine and pyrazolo[2,3-A]pyridine derivatives

Substituted aryl and heteroaryl compounds as E-type prostaglandin antagonists

A pyrimidine derivative of formula (I) or (I&prime;): wherein: R is a substituent as defined within; Q is optionally substituted phenyl, and Q bears a substituent of formula (Ia) wherein: X, Y , Y , Z, n, and m are as defined within; &mdash;NQ 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.

2,4-diamino-pyrimidine deprivatives having anti-cell proliferative activity

Pyrimidine derivatives of the formula (I) wherein: one of Q and Q or both of Q and Q is substituted on a ring carbon by one substituent of the formula (Ia) &lsqb;provided that when present in Q the substituent of formula (Ia) is not adjacent to the &mdash;NH&mdash; link&rsqb;; wherein Q , Q , G, R , X, Y , Y , Z, n and m are as described within; and pharmaceutically acceptable salts and in vivo hydrolyzable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.

A pyrimidine derivative of formula (I) wherein V is O or S, Q and Q are independently selected from phenyl, naphthyl, a 5- or 6-membered monocyclic moiety and a 9- or 10-membered bicyclic heterocyclic moiety; and Q is substituted by one substituent of formula (Ia), and Q may optionally bear further substituents of formula (Ia) wherein X is CH &mdash;, O&mdash;, NH&mdash;, NR &mdash; or &mdash;S&mdash;&lsqb;wherein R is as defined within&rsqb;; Y is H, C alkyl or as defined for Z; Y is H or C alkyl; Z is R O&mdash;, R R N&mdash;, R S&mdash;, R R NNR &mdash;, a nitrogen linked heteroaryl or a nitrogen linked heterocycle, wherein R , R , R , R , R , R and R are as defined within; n is 1, 2 or 3; m is 1, 2 or 3; and Q and Q may optionally be 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 with pharmaceutical activity

Pyrimidine derivatives of the formula (I), wherein: Q and Q are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one or both Q and Q are substituted on a ring carbon by one substituent of the formula (Ia) or (Ia&prime;), wherein: Y, Z, n, m Q , G, R , are as defined within; and pharmaceutically acceptable salts and in in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.

2,4-di(hetero-)arylamino (oxy)-5-substituted pyrimidines as antineoplastic agents

Aromatic compounds and pharmaceutical compositions containing them

Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a &mdash;CH(R,)N(R,)B&mdash;R,and &mdash;OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R,is positioned on B in a 1,3 or 1,4 relationship with the &mdash;CH(R,)N(R,)B- linking group. R,, R,and R,and D can be a number of different organic or halogen moieties. N-oxides of &mdash;NR,and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.

Aromatic amine compounds that antagnoize the pain enhancing effects of prostaglandins

Aromatic amine compounds that antagonize the pain enhancing effects of

Compounds of the formula, ##STR1## and pharmaceutically-acceptable salts thereof, which are useful as antagonists of the pain-enhancing effects of E-type prostaglandins, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for treating pain comprising the administration of such compounds.

Growing community of inventors

Macclesfield, United Kingdom

Gloria Anne Breault