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INHIBITORS OF THE IKK-BETA SERINA-TREONINA PROTEIN QUINASA.
专利权人:
CHROMA THERAPEUTICS LIMITED
发明人:
MOFFAT, DAVID,DAVIES, STEPHEN,CHARLTON, MICHAEL,HIRST, SIMON,ONIONS, STUART,WILLIAMS, JONATHON
申请号:
ES07824358
公开号:
ES2372707T3
申请日:
2007.10.29
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula (IA) or (IB), or its salt, N-oxide, hydrate or solvate: wherein: R7 is an optionally substituted hydrogen or (C1-C6) alkyl; Ring A is an aryl or heteroaryl ring optionally substituted with 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH-Y-L 1 -X 1 - (CH2) z-, in which: R1 is an ester group that can be hydrolyzed by one or more intracellular esterase enzymes to produce a carboxylic acid group; R2 is the side chain of a natural or unnatural alpha-amino acid; Y is a link, -C (= O) -, -S (= O) 2-, -C (= O) O-, -C (= O) NR3-, -C (= S) -NR3, - C (= NH) -NR3 or -S (= O) 2NR3-, in which R3 is hydrogen or optionally substituted (C1-C6) alkyl; L 1 is a divalent radical of the formula - (Alq 1) m (Q) n (Alq 2) p-, in which m, n and p are independently 0 or 1; Q is (i) a divalent mono- or bicyclic carbocyclic or heterocyclic radical optionally substituted with 5-13 ring members, or (ii) in the case where p is 0, a divalent radical of formula -Q 1 -X 2 - , wherein X 2 is -O-, - S- or NR A -, in which RA is optionally substituted hydrogen or (C1-C3) alkyl, and Q 1 is an optionally divalent mono- or bicyclic carbocyclic or heterocyclic radical optionally substituted with 5-13 ring members, Alq 1 and Alq 2 independently represent optionally substituted divalent cycloalkyl (C3-C7) radicals, or linear (C1-C6) alkylene, C2-C6) alkenylene or C2-C6 alkenylene radicals or optionally substituted branched which may optionally contain or terminate in an ether (-O-), thioether (-S-) or amino (-NR A -) bond, wherein RA is hydrogen or optionally substituted (C1-C3) alkyl ; X 1 is a link, -C (= O) -; or -S (= O) 2-; -NR4C (= O) -, -C (= O) NR4-, -NR4C (= O) -NR5-, -NR4S (= O) 2-, or -S (= O) 2NR4-, in which R4 and R5 are independently hydrogen or optionally substituted (C1-C6) alkyl; and z is 0 or 1.Un compuesto de fórmula (IA) o (IB), o su sal, N-óxido, hidrato o solvato: en la que: R7 es un hidrógeno o alquilo(C1-C6) opcionalmente sustituido; el anillo A es un an
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