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NF-KB factor inhibitors
专利权人:
INC.;PROFECTUS BIOSCIENCES
发明人:
ZHANG, JIE,SLISKOVIC, D. ROBERT,DUCKER, CHARLES E.
申请号:
ES10724601
公开号:
ES2540351T3
申请日:
2010.03.25
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula (1) or of formula (2): ** Formula ** or a pharmaceutical salt thereof, in which: HET is a saturated or unsaturated, mono- or multi-ring carbocycle, in which one or more carbon atoms in the ring are replaced (n) by N, S, P or O; each R1 is independently hydrogen; CF3; phenyl optionally substituted with cyano; halo; nitro; hydroxyl; (C1.C6) alkyl; (C1-C6) alkyl-OH; (C1-C6) alkoxy; COR3; NR4R5 or NHCO (C1-C6) alkyl; cyano; halo; nitrohydroxy; (C1-C6) alkyl; (C1-C6) alkyl-OH; (C1-C6) alkoxy; (C1-C6) thioalkoxy; phenoxy; COR3; NR4R5; NHCO (C1-C6) alkyl; SO2 (C1-C6) alkyl; or SO2NR4R5; R2 is H, R6, COR6. CONHR6, CH2OCOR6, P (O) (OH) 2, P (O) (O (C1-C6) alkyl) 2, P (O) (OCH2OCO (C1-C6) alkyl) 2, P (O) (OH) (OCH2OCO (C1-C6) alkyl), P (O) (OH) (O (C1-C6) alkyl), P (O) (OH) (C1-C6) alkyl, glycosyl or an inorganic salt of P (O ) (OH) 2, P (O) (O (C1-C6) alkyl, P (O) (OCH2OCO (C1-C6) alkyl) 2, P (O) (OH) (OCH2OCO (C1-C6) alkyl) , P (O) (OH) (OC1-C6) alkyl, or P (O) (OH) (C1-C6) alkyl; R6 is C1-C6 alkyl, trifluoromethyl, (C3-C6) cycloalkyl, cyclohexylmethyl or phenyl, wherein the phenyl is substituted with 0 to 4 groups selected from the group consisting of fluorine, chlorine, bromine, hydroxyl, trifluoromethyl, (C1-C4) alkyl, (C1-C4) alkoxy and phenylmethyl, in which the phenylmethyl Phenyl ring is substituted with 0-4 groups selected from the group consisting of fluorine, chlorine, bromine, hydroxyl, trifluoromethyl, (C1-C4) alkyl, (C1-C4) alkoxy, 2-pyridinyl, 3-pyridinyl, 4 -pyridinyl, 2-pyrimidinyl, 4-pyrimidinyl and 5-pyrimidinyl, R3 is independently hydroxy, (C1-C6) alkoxy, phenoxy or -NR4R5; each of R4 and R5 are independently Tooth hydrogen, (C1-C6) alkyl or (C3-C6) cycloalkyl, and n is 0-3, in which on HET, there is an ortho relationship between the OR2 group and the amide portion.Un compuesto de fórmula (1) o de fórmula (2): **Fórmula** o una sal farmacéutica del mismo, en el que: HET es un carbociclo saturado o insaturado, mono- o multi-anillo, e
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