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DERIVATIVES OF HETEROCICLILALQUILO AS NEW INHIBITORS OF HISTONA DEACETILASA.
专利权人:
JANSSEN PHARMACEUTICA; N.V.
发明人:
ROUX, BRUNO,ANGIBAUD, PATRICK RENE
申请号:
ES07703885
公开号:
ES2376121T3
申请日:
2007.01.16
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula (I) ** Formula ** its N-oxide forms, its pharmaceutically acceptable addition salts and its stereochemically isomeric forms, in which: R 1 is hydroxyl or a radical of the formula (a-1) ** Formula ** in which: R2 is hydroxyl or amino; R3 is hydrogen, thienyl, furanyl or phenyl and each thienyl, furanyl or phenyl may be optionally substituted with one or two halo, amino, nitro, cyano, hydroxyl, phenyl, C1-6 alkyl, (C1-6 dialkyl) amino, alkyl C1-6-oxy, phenyl-C1-6-oxy alkyl, hydroxy C1-6 alkyl, alkoxy C1-6-carbonyl, hydroxycarbonyl, C1-6 alkylcarbonyl, polyhaloalkyl C1-6-oxy, polyhaloalkyl C1-6, alkyl C1-6-sulfonyl, hydroxycarbonylalkyl C1-6, alkyl C1-6-carbonylamino, aminosulfonyl, aminosulfonylalkyl C1-6, isoxazolyl, aminocarbonyl, phenylalkyl C2-6, phenylalkyl C3-6 or pyridinylalkyl C3-6; R4, R5 and R6 are each independently, amino, nitro, furanyl, halo, C1-6 alkyl, C1-6-oxy alkyl, trifluoromethyl, thienyl, phenyl, C1-6 alkylcarbonylamino, C1-6 aminocarbonylalkyl or -CC -CH2-R7; wherein R 7 is hydrogen, C 1-6 alkyl, hydroxy, amino or C 1-6 alkyl-oxy; X is N or CH; Y is O, N, NH, CH or CH2 and when Y is N or CH then the substituent is attached to the Y atom of the ring structure; T is O or NR8 in which R8 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl, C1-6 hydroxyalkyl, C1-6 cyanoalkyl, C1-6 alkyl C1-6 oxyalkyl, C1-6 hydroxyaminocarbonylalkyl, C1 alkyl -6-sulfonylC 1-6 alkylcarbonyl, C 1-6 alkylcarbonyl or mono- or di- (C 1-6 alkyl) aminosulfonyl; n is 0 or 1 and when n is 0 it means a direct link; m is 1 or 2; p is 0 or 1 provided that when p is 0 then n is 0, - (CH2) n- (T) p- is a direct link and Y is N; A is a radical selected from: ** Formula ** in which R9 is hydrogen, C1-6 alkyl, C3-7 cycloalkyl or C3-7 cycloalkyl-C1-6 alkyl; and R 10 is hydrogen, hydroxy, amino, halo, C 1-6 alkyl, C 1-6 polyhaloalkyl, C 1-6 alkyl oxycarbonyl, hydroxycarbonyl, C 1-6 alkylcarbonylamino, C 1-6 alkyl oxy, or mono- or di - (C1-6 alkyl) amino.Un compuesto de fórmul
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