1151805-64-9

Upstream product

• 1151805-63-8 2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl acetate 
• 1151805-62-7 2-(4-{[1-amino-3-(2,4-difluorophenyl)-3-oxoprop-1-en-1-yl]amino}-3,5-difluoro-phenyl)ethyl acetate 
• 1151805-51-4 2-(3,5-difluoro-4-nitrophenyl)ethanol 
• 932373-91-6 (3,5-difluoro-4-nitrophenyl)acetic acid 
• 19064-24-5 2,6-difluoro-1-nitrobenzene 
• 288580-60-9 tert-butyl (3,5-difluoro-4-nitrophenyl)acetate 
• 1151805-32-1 2-(4-amino-3,5-difluorophenyl)ethanol 
• 1602492-14-7 2-(4-{[3-(2,4-difluorophenyl)-3-oxopropanimidoyl]amino}-3,5-difluorophenyl)ethyl acetate 

Downstream Products

• 1151805-34-3 {4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}acetaldehyde 

Relevant academic research and scientific papers

TREATMENT OF CANCER BY STIMULATION OF IL-12 PRODUCTION

The present invention relates to a compound and composition for use in the stimulation of IL-12 production and IFN-γ production, which compound is selected from: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5- difluorophenyl}ethyl)-L-alaninate, or a pharmaceutically acceptable salt, hydrate or solvate thereof; and 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

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.

COMBINATION OF P38 INHIBITORS AND ANOTHER ANTICANCER AGENTS

The present invention provides an amino acid ester of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, for use in combination with a cytotoxic agent: (Formula (I)). The combination is useful in the treatment of cancer.

P38 MAP KINASE INHIBITORS

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: formula (I) wherein: G is -N= or -CH=; 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 C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z-X1-L1 -Y-NH-CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5 - 13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.

INHIBITORS OF P38 MAP KINASE

Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is -N= or -CH=; 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; -X1-L1-Y- is a linker radical or bond; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 are as defined in the claims.