Astrazeneca Ab

Imperial Chemical Industries Limited

Zeneca Limited

Jeffrey James Morris

John Preston

Jethro L Longridge

Anthony L Cooper

Steven P Brown

Zbigniew Stanley Matusiak

Richard William Arthur Luke

Andrew Leach

Paul David Johnson

David R Brittain

Linda Slater

Gloria Anne Breault

Elizabeth Janet Pease

Andrew Peter Thomas

Robert Hugh Bradbury

Maurice Raymond Verschoyle Finlay

Kurt G Pike

Dearg Sutherland Brown

Emma Jane Williams

Linda Salter

Kurt Gordon Pike

Richard William Luke

The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z, Z, R, R, Rand n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).

Protein kinase B inhibitors

A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.

Compounds-943

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

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

Aniline derivatives

The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Acetamide derivatives

The invention concerns novel phenoxy- and phenylthio-acetyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Amidobenzene derivatives, compositions and use

The invention concerns novel (oxamido- and ureido-phenylsulfonyl)nitromethane derivatives and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Urea derivatives, compositions and use

The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.

Phenylsulfonyl nitromethanes as aldose reductase inhibitors

Growing community of inventors

Macclesfield, United Kingdom

Jeffrey James Morris