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2-amino-3,4-dihydroquinazoline derivatives and their application as cathepsin D inhibitors
专利权人:
Merck Patent GmbH
发明人:
KLEIN, Markus,TSAKLAKIDIS, Christos
申请号:
ES14701470
公开号:
ES2612982T3
申请日:
2014.01.20
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Compounds of the formula I ** Formula ** in which I1, I2, I3 mean CR1 or CT, independently of each other, X means H or NH2, Y means a cyclic alkylaryl group, characterized in that in an unsubstituted cyclic alkyl or in one substituted once or twice by>; = S,>; = NR,>; = O, R, T, OR, NRR ', SOR, SO2R, SO2NRR', CN, COOR, CONRR ', NRCOR', NRCONR'R '' and / or NRSO2R ', with 5 or 6 C atoms, where one or two CH2 groups, independently of each other, can be replaced by O, S, SO, SO2, NR, -OCO-, -NRCONR'-, -NRCO-, -NRSO2R'-, -COO-, -CONR-, and / or 1-11 atoms of H by F and / or Cl, there are condensed 1 or 2 aromatic rings, Ar means a phenyl or a naphthyl not substituted or substituted once, twice, three or four times by R1, or a double-core aromatic heterocycle with 1 to 4 atoms of N, O and / or S which is unsubstituted or substituted once, twice or three times by R, >; = S,>; = NR 'and / or>; = O, Q means CH2, CR1R2 or C>; = O, T means an unsubstituted or substituted phenyl or naphthyl a a, two, three or four times by R1, or a saturated, unsaturated or aromatic double-nucleus heterocycle with 1 to 4 atoms of N, O and / or S that can be replaced once, twice or three times by R,>; = S,>; = NR 'and / or>; = O, R1, R2 means H, OR, Hal, C (Hal) 3, NRR', SOR, SO2R, SO2NRR ', CN, COOR, CONRR', NRCOR ', NR'CONR'R ', NRSO2R' independent of each other, a straight or branched chain alkyl unsubstituted or substituted once, twice or three times by>; = S,>; = NR,>; = O, Hal, C (Hal) 3, OR, NRR ', SO2R, SO2NRR', CN, CONRR ', NRCOR' and / or NRCONRR 'with 1-10 C atoms, in which one, two or three CH2 groups can independently replace each other with O , S, SO, SO2, NR, -OCO-, -NRCONR'-, -NRCO-, -NRSO2R'-, -COO-, -CONR-, -NRCO-, groups -CC- and / or by groups -CH >; = CH and / or also 1-20 H atoms by F and / or Cl, or a cyclic alkyl unsubstituted or substituted once, twice or three times by>; = S,>; = NR,>; = O, Hal, OR , NRR ', SO2R, SO2NRR', CN, CONRR ',
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