Astrazeneca Ab

Janet Elizabeth Pease

Gloria Anne Breault

Roger John Butlin

Michael Howard Block

Thorsten Nowak

Jeremy Nicholas Burrows

Stewart R James

Robert Hugh Bradbury

Laurent Francois Andre Hennequin

Christopher Thomas Halsall

Benedicte Delouvrie

Craig Steven Harris

David Stephen Clarke

Philip John Jewsbury

Philip J Jewbury

Peter Mark Smith

A quinazoline derivative of the formula I: wherein: R, R, R, R, R, R, RR, R, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula I, are useful in the treatment of hyperproliferative disorders such as a cancer.

Quinazoline compounds for the treatment of hyperproliferative disorders

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

Amides as inhibitors for pyruvate dehydrogenase

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

A compound of formula (I) wherein: n is 1 or 2; R is chloro, fluoro, bromo, methyl or methoxy; R is as defined within; R is as defined within; and R is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Substituted N-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity

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 compounds

A compound of formula (I) wherein: R , R , R , R , R , R and R are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Chemical compounds

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Macclesfield, United Kingdom

Janet Elizabeth Pease