Smithkline Beecham Corporation

Pfizer Corporation

Glaxo Wellcome Inc.

Glaxosmithkline LLC

Other

Novartis Ag

George Stuart Cockerill

Karen Elizabeth Lackey

Malcolm Clive Carter

Stephen Barry Guntrip

Kathryn Jane Smith

James Good

Edward Cochrane

Robert J Blade

Alan T Hudson

Karl Witold Franzmann

Paul Barraclough

Robert J Peek

Sadie Vile

Martin John Page

Matthew Barrett

Craig Alex Avery

Andrew Joseph Warner

Stephen Carl McKeown

Benzodiazepine derivatives of formula (I): (I) wherein: each of Rand Ris independently H or halo; Ris H, C-Calkyl or —NHR; either (i), a, c and c are all bonds, with, b, d and f absent; or b, d, and f are all bonds, with a, c, and c absent; Ris H or a group selected from C-Calkyl, C-Ccycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; Ris H or halo; Ris —OR, —NRRor —R; Ris H or halo; each of Rand Ris independently H or a group selected from C-Calkyl, C-Ccycloalkyl and 4- to 10-membered heterocyclyl, the group being unsubstituted or substituted; n is 1 or 2; and one of V, W and X is N or CH and the other two are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Pharmaceutical compounds

Benzodiazepine derivatives of formula (I): (I) wherein: each of Rand Ris independently H or halo; either (i) T is N, Z is C,andare bonds, andandare absent; or (ii) T is C, Z is N,andare bonds, andandare absent; each of Rand Ris independently halo, —OR, —NRR, —COR, —C(O)OR, —CON(R)or —R; Ris H or halo; each of Rand Ris independently H or a group selected from C-Calkyl, C-Ccycloalkyl, C-Caryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; Ris H or C-Calkyl, each Rbeing the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Benzodiazepine derivatives of formula (I): (I) wherein: each of Rand Ris independently H or halo; either (i) T is N, Z is C, -a- and -c- are bonds, and -b- and -d- are absent; or (ii) T is C, Z is N, -b- and -d- are bonds, and -a- and -c- are absent; each of Rand Ris independently halo, &#x2014;OR, &#x2014;NRR&#x2014;COR, &#x2014;C(O)OR, &#x2014;CON(R)or &#x2014;R; Ris H or halo; each of Rand Ris independently H or a group selected from C-Calkyl, C-Ccycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; Ris H or C-Calkyl, each Rbeing the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

A pharmaceutical formulation comprising the compound of formula 

Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

A process for the preparation of a compound of formula (I) comprising the steps:(a) reacting a compound of formula (II) wherein L and L' are suitable leaving groups,with a compound of formula (III)UNH&#x2003;&#x2003;(III)to prepare a compound of formula (IV) and subsequently (b) substituting the group Rby replacement of the leaving group L&#x2032;.

Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.

Heterocyclic compounds

Anilinoquinazaolines as protein tyrosine kianse inhibitors

A process for the preparation of a compound of formula (I) comprising the steps:  

Anilinoquinazaolines as protein tyrosine kinase inhibitors

Anilinoquinazolines as protein tyrosine kinase inhibitors

Substituted heteroaromatic compounds, and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.

Substituted heteroaromatic compounds of formula (I), wherein X is N or CH; Y is CR and V is N; or Y is N and V is CR ; or Y is CR and V is CR ; or Y is CR and V is CR ; R represents a group CH SO CH CH NHCH &mdash;Ar&mdash;, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C alkyl or C alkoxy groups; R is selected from the group comprising hydrogen, halo, hydroxy, C alkyl, C alkoxy, C alkylamino and di&lsqb;C alkyl&rsqb;amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R group and optionally substituted by at least one independently selected R group; R is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl, or R represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R represents a group of formula (a) wherein each R is independently selected from halogen, C alkyl, C alkoxy; and n is 0 to 3; each R is independently hydroxy, halogen, C alkyl, C alkenyl, C alkynyl, C alkoxy, amino, C alkylamino, di&lsqb;C alkyl&rsqb;amino, C alkylthio, C alkylsulphinyl, C alkylsulphonyl, C alkylcarbonyl, carboxy, carbamoyl, C alkoxycarbonyl, C alkanoylamino, N-(C alkyl)carbamoyl, N,N-di(C alkyl)carbamoyl, cyano, nitro and trifluoromethyl; and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O) , wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O) atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O) , wherein m is 0,1 or 2 and wherein the ring system is substituted by at least one independently selected R group and is optionally substituted by at least one independently selected R group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.

Growing community of inventors

Maulden, United Kingdom

George Stuart Cockerill