914604-52-7Relevant academic research and scientific papers
INHIBITORS OF HSP90
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Page/Page column 50, (2010/04/30)
The invention provides a compound which is (a) a pyrrolopyrimidine derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: Formula (I) wherein R1, R2, R3/
P38 MAP KINASE INHIBITORS
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Page/Page column 32-33, (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.
HDAC INHIBITORS
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Page/Page column 32, (2008/06/13)
Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent =C- or =N-; W is a divalent radical -CH=CH- or CH2CH2-; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER
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Page/Page column 25-26, (2008/12/05)
Compounds of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful, inter alia, in the treatment of proliferative diseases: wherein R1 is hydrogen, or a (C1C6)alkyl, (C2-C6)alkenyl, (
HYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 30; 32-33, (2008/12/05)
Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: wherein Q, V and W independently represent -N= or -C=; B is
INHIBITORS OF P38 MITOGEN-ACTIVATED PROTEIN KINASE
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Page/Page column 27-28, (2008/12/05)
Compounds of formula (I) are inhibitors of p38 MAP kinase activity, and are useful in the treatment of, inter alia, inflammatory and autoimmune disease formula (I): wherein R3, R4, R5 and R6 are each independently hydrogen or halogen; M and P are independently -N= or -CH=; Z is (a) a radical of formula R1R2CHNH-Y-L1-X1-(CH2)Z-, wherein R1R2CHNH- is an N-linked amino acid or amino acid ester group as defined in the description, and -Y-L1-X1-(CH2)Z- is a linker radical as defined in the description.
IKK-β SERINE-THREONINE PROTEIN KINASE INHIBITORS
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Page/Page column 28; 31, (2008/12/05)
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 R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH-Y-L1-X1-(CH2)Z- wherein: z is 0 or 1; 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; R2 is the side chain of a natural or non- natural alpha amino acid; Y is a bond, -C(=O)-, -S(=O)2-, -C(=O)O-, -C(=O)NR3-, - C(=S)-NR3, -C(=NH)-NR3 or -S(=O)2NR3- wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
p38 MAP KINASE INHIBITORS
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Page/Page column 56; 59, (2008/06/13)
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: (I), wherein: G is -N= or -CH=; D is an optionally substituted divale
THIAZOLE DERIVATIVES AS INHIBITORS OF P13 KINASE
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Page/Page column 31, (2008/06/13)
Compounds of formula (I) are inhibitors of P13 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases: wherein: s is 0 or 1; U is hydrogen or halogen; X is -(C=O), an optionally substituted divalent ph
