Chroma Therapeutics Limited

Michael Hugh Charlton

Stuart Thomas Onions

Stephen John Davies

Simon Christopher Hirst

Jonathan Gareth Williams

David Festus Charles Moffat

David Charles Festus Moffat

Jonathon Gareth Williams

Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein Ris hydrogen or optionally substituted (C-C)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L-Y&#x2014;(CH)&#x2014;, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) Ris a carboxylic acid group (&#x2014;COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; Ris hydrogen, or optionally substituted C-Calkyl, C-Ccycloalkyl, aryl or heteroaryl or &#x2014;(C&#x2550;O)R, &#x2014;(C&#x2550;O)OR, or &#x2014;(C&#x2550;O)NRwherein Ris hydrogen or optionally substituted (C-C)alkyl; Yis a bond, &#x2014;(C&#x2550;O)&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;C(&#x2550;O)O&#x2014;, &#x2014;OC(&#x2550;O)&#x2014;, &#x2014;(C&#x2550;O)NR&#x2014;, &#x2014;NR(C&#x2550;O)&#x2014;, &#x2014;S(O)NR&#x2014;, &#x2014;NRS(O)&#x2014;, or &#x2014;NR(C&#x2550;O)NR&#x2014;, wherein Rand Rare independently hydrogen or optionally substituted (C-C)alkyl, Lis a divalent linker radical of formula -(Alk)(Q)(Alk)- wherein m, n, p, Q, Alkand Alkare as defined in the claims.

Inhibitors of IKK-beta serine-threonine protein kinase

Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein Ris hydrogen or optionally substituted (C-C)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula RRCHNH&#x2014;Y-L-X&#x2014;(CH)&#x2014; wherein: z is 0 or 1; R1 is a carboxylic acid group (&#x2014;COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;P)2-, &#x2014;C(&#x2550;O)O&#x2014;, &#x2014;C(&#x2550;O)NR3-, &#x2014;C(&#x2550;S)&#x2014;NR, &#x2014;C(&#x2550;NH)&#x2014;NRor &#x2014;S(&#x2550;O)NR&#x2014; wherein Ris hydrogen or optionally substituted C-Calkyl; L is a divalent linker radical of formula -(Alk)(Q)(Alk)- wherein m, n, p, Q, AIkand AIkare as defined in the claims. 

IKK-beta serine-threonine protein kinase inhibitors

Growing community of inventors

Abingdon, United Kingdom

Michael Hugh Charlton