288580-60-9Relevant academic research and scientific papers
TREATMENT OF CANCER BY STIMULATION OF IL-12 PRODUCTION
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Page/Page column 19, (2019/03/17)
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
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Page/Page column 14-15, (2014/05/07)
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
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Page/Page column 42, (2014/11/11)
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
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Page/Page column 20-21, (2009/06/27)
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
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Page/Page column 27, (2009/10/21)
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.
1- (1-CYCLOHEXYL-4-PIPERIDINYL) -1, 3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE
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Page/Page column 61-62, (2008/12/04)
Compounds of formula (I) or a salt thereof are provided, wherein R4, R5, R6, Q and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE ML RECEPTOR AND THEIR USE IN MEDICINE
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Page/Page column 56, (2008/12/04)
Compounds of formula I or a salt thereof are provided wherein R4, R5, R6, Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Page/Page column 59-60, (2010/11/26)
Compounds which have activity at M1 receptor and their uses in medicine Compounds of formula (I) and salts and solvates are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl
BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Page/Page column 44, (2010/11/28)
Compounds of formula (I), salts and solvates are provided, wherein Q, R, R4 - R6 are as def ined in the Claims. Uses of the Compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
Substituted bicyclic compounds
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, (2008/06/13)
The invention is directed to physiologically active compounds of formula (Ia): wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is alk
