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DERIVATIVES OF PIRAZOLONA AS INHIBITORS OF PDE4.
专利权人:
NYCOMED GMBH
发明人:
SCHMIDT, BEATE,SCHEUFLER, CHRISTIAN,VOLZ, JUERGEN,FETH, MARTIN P.,HUMMEL, ROLF-PETER,HATZELMANN, ARMIN,ZITT, CHRISTOF,WOHLSEN, ANDREA,MARX, DEGENHARD,KLEY, HANS-PETER,OCKERT, DEBORAH,HEUSER, ANKE,CHRI
申请号:
ES08759563
公开号:
ES2374337T3
申请日:
2008.05.14
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula 1 in which R1 represents a f enyl derivative of formulas (a) or (b) R2 is selected from the group consisting of C1-2 alkoxy and C1-2 alkoxy which is completely or predominantly substituted with fluorine ; R3 is selected from the group consisting of C1-2 alkoxy, C3-5 cycloalkoxy, C3-5 cycloalkyl and C1-2 alkoxy which is completely or predominantly substituted with fluorine; R4 is selected from the group consisting of C1-2 alkoxy and C1-2 alkoxy that is completely or predominantly substituted with fluorine; R5 is C1-2 alkyl, and R6 is selected from the group consisting of hydrogen and C1-2 alkyl; or R5 and R6, together, and including the two carbon atoms to which they are attached, form a 5 or 6-membered spiro bonded hydrocarbon ring; R7 is C1-3 alkyl, and R8 is C1-3 alkyl, or R7 and R8, together with the carbon atom to which they are attached, form a 3, 4, 5 or 6-membered spiro-linked hydrocarbon ring, R9 is -N (R11) R12, in which R11 and R12, together, and including the nitrogen atom to which they are attached, form a heterocyclic ring selected from the group consisting of a pyrrolidin-2,5-dion-1 ring -yl, isoindol-1,3-dion-2-yl, 2-oxo-2,3-dihydro-1H-indole-1-yl, pyrrolidin-2-on-1-yl, piperidin-2,6-dion -1-yl, morpholin-3,5-dion-4-yl, thiomorpholin-3,5-dion-4-yl, thiomorpholin-1-oxide-3,5-dion-4-yl and thiomorpholin-1,1 -3,5-dion-4-yl dioxide; and n is 1 or 2; or a stereoisomer of the compound.Un compuesto de fórmula 1 en la que R1 representa un derivado f enílico de fórmulas (a) o (b) R2 se selecciona del grupo que consiste en alcoxi de C1-2 y alcoxi de C1-2 que está completa o predominantemente sustituido con flúor; R3 se selecciona del grupo que consiste en alcoxi de C1-2, cicloalcoxi de C3-5, cicloalquil C3-5-metoxi y alcoxi de C1-2 que está completa o predominantemente sustituido con flúor; R4 se selecciona del grupo que consiste en alcoxi de C1-2 y alcoxi de C1-2 que está completa o predominantemente sustituido con flúor; R5 es alquilo de
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