New 5,6-dihydro-4H-pyrrolo- [1,2-a] [1,4] benzodiazepines and 6H-pyrrolo [1,2-a] [1,4] antifungal benzodiazepines substituted with heterocyclic derivatives
MEERPOEL, LIEVEN,MAES, LOUIS JULES ROGER MARIE,DE WIT, KELLY,AUGUSTYNS, KOEN JAN LUDOVICUS
申请号：
ES12717780
公开号：
ES2542900T3
申请日:
2012.05.03
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound of formula (I) ** Formula ** or a stereoisomeric form thereof, wherein, R 1 is hydrogen, halo, C 1-4 alkyl or C 1-4 alkyloxy； R2 is hydrogen, halo, C1-10 alkyl or C1-4 alkyloxy； R3 and R4 are hydrogen； or R3 and R4 taken together form a bond； Het is a monocyclic or bicyclic radical chosen from (d-1) and (d-2) are attached to the rest of the molecule with a bond in position a, b or c； (d-4), (d-6), (d-7), (d-10) and (d-12) are attached to the rest of the molecule with a bond in position a or b； X1 is O, S or NH； X2 is O or S； X3, X4 and X5 are each independently CH or N； with the proviso that exactly two of X3, X4 and X5 are N, the other being CH； X6, X7, X8 and X9 are each independently CH or N； with the proviso that one or two of X6, X7, X8 and X9 are N, the other being CH； X10, X11, X12 and X13 are each independently CH or N； with the proviso that at most one of X10, X11, X12 and X13 is N, the other being CH； X14 is CH or N； X15 is NH, O or S； X16 is CH or N； X17 is CH or N； X18 is NH, S or O； X19 is CH or N； X20 is NH or S； R5 and R6 taken together form a bivalent radical -R5-R635 -, with the formula: - (CH2) mO- (CH2) nm- (a), - (CH2) nmO- (CH2) m (b), - ( CH2) s- (c), or -CH>； = CH-CH>； = CH- (d)； wherein the bivalent radical -R5-R6- may be, when possible, substituted with one or more substituents chosen from the group consisting of halo, C1-4 alkyl, hydroxyl, C1-4 alkyloxy and oxo； m represents 0, 1 or 2； n represents 2, 3 or 4； s represents 3, 4 or 5； wherein the radicals (d-1) - (d-11) may be substituted with one or more substituents each independently selected from the group consisting of C1-4 alkyloxy, halo, C1-4 alkylcarbonyl, C1- alkylthio 4, C1-4 alkylsulfonyl, C1-4 alkylsulfinyl and C1-4 alkyl optionally substituted with one or more halo substituents； with the proviso that the radicals (d-1) - (d-11) are not substituted in the positions - to the bonding carbon atom； or a pharmaceutically acceptable addition salt or solvate thereof； with
