Ucb Pharma, S.a.

Celltech R&d Limited

Rachel Jane Cubbon

Daniel Christopher Brookings

Barry John Langham

Jeremy Martin Davis

Richard Jeremy Franklin

Manisha Naik

A series of 5-6 fused ring bicyclic heteroaromatic derivatives, based in particular on the 5-oxo-4,5-dihydro-1H-pyrrolo[3,2-b]pyridine ring system, being inhibitors of p38 kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.

Bicyclic heteroaromatic compounds as kinase inhibitors

Compounds of formula (1) are described in which Rand Ris each independently a hydrogen atom or a group R, or Rand Rtogether form an oxo (&#x2550;O) or thio (&#x2550;S) group; X is a N atom or an optionally substituted CH group: Y is a &#x2014;O&#x2014; or &#x2014;S&#x2014; atom or &#x2014;SO&#x2014; or &#x2014;SO&#x2014; group or an optionally substituted &#x2014;CH&#x2014; or &#x2014;NH&#x2014; group with the proviso that when Rand Rtogether form an oxo (&#x2550;O) or thio (&#x2550;S) group Y is an optionally substituted &#x2014;CH&#x2014; or &#x2014;NH-group; Lis a covalent bond or a linker atom or group; p is zero or the integer 1; Alkis an optionally substituted Caliphatic or Cheteroaliphatic chain; n is zero the integer 1, 2 or 3 with the proviso that when n is zero Y is an optionally substituted &#x2014;CH&#x2014; group; Ar is an optionally substituted Caromatic or Cheteroaromatic group; m is zero or the integer 1, 2 or 3; q is zero or the integer 1 or 2; R, Rand Rare hydrogen atoms or the substituents described in the patent specification; and the salts, solvates, hydrates and N-oxides thereof. The compounds are potent and selective inhibitors of p38 kinase and are useful in the treatment of immune or inflammatory disorders.

Pyridine and pyrimidine derivatives

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Slough, United Kingdom

Rachel Jane Cubbon