Chroma Therapeutics Limited

Macrophage Pharma Limited

Stéphane Pintat

Stephen John Davies

David Festus Charles Moffat

Stephen H Davies

Carl Leslie North

David Charles Festus Moffat

David Charles Moffat

The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine.

Tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-YL]-3,5-difluorophenyl}ethyl]-L-alaninate or a salt, hydrate or solvate thereof

Tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl]-L-alaninate or a salt,hydrate or solvate thereof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein: ring A, R, R, n, X, V, W, Z, ring B, [Linker] and R areas defined herein. The compounds are useful as inhibitors of CSF-1R kinase. The compounds can thus be used in medicine. 

2-aminopyrazine derivatives as CSF-1R kinase inhibitors

Tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl]-L-alaninate or a salt, hydrate or solvate thereof

Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is &#x2014;N&#x2550; or &#x2014;CH&#x2550;; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; &#x2014;X-L-Y&#x2014; is a linker radical or bond; 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; and Rand Rare as defined in the claims. 

Inhibitors of P38 map kinase

Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is &#x2014;N&#x2550; or &#x2014;CH&#x2550;; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; Ris hydrogen or optionally substituted C-Calkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH)&#x2014;X-L-Y&#x2014;NH&#x2014;CHRRwherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L, and Xare as defined in the specification; 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; and Ris the side chain of a natural or non-natural alpha amino acid.

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Abingdon, United Kingdom

Stéphane Pintat