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Carboxylic acid derivatives substituted as aggrecanase aggregates for the treatment of osteoarthritis
专利权人:
Merck Patent GmbH
发明人:
KLEIN, Markus,LINDEMANN, Sven
申请号:
ES14701909
公开号:
ES2627281T3
申请日:
2014.01.16
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Compounds of formula I, ** Formula ** where X is CHR1 or CR1R2, where optionally R1 and R2 with the C atom to which they are attached form a cycloalkyl or heterocyclyl containing from 3 to 7 C atoms where optionally from 1 to 3 CH2 groups are substituted by -O-, -S-, -SO-, -SO2-, -NR-, -OCO-, -NRCONR'-, -NRCO-, -NRSO2R'-, -COO-, -CONR - or -CH>; = CH- and where optionally 1 to 11 H atoms are substituted by F or Cl, D -EGK or -L, E, K are independently of each other a saturated, unsaturated or aromatic hydrocarbon cycle that does not is substituted or substituted 1 to 4 times by R1 or R2, or a monocyclic saturated, unsaturated or aromatic heterocycle with 1 to 4 heteroatoms selected from N, O and S that is not substituted or is mono-, di- or trisubstituted by R1, R2,>; = S,>; = NR1 or>; = O, G is a single bond, L is -EGK, where E and K, in addition to the single bond G, are linked through an additional alkyl linker that contains 1 to 3 atoms of C, where optionally a CH2 group is substituted by -CR1R2-, -O-, -S-, -SO-, -SO2-, -NR1-, -OCO-, -NR1CONR2-, -NR1CO-, -NR1SO2R2- , -COO-, -CONR1- or -CH>; = CH-, Y is H, R1 or a saturated, unsaturated or aromatic hydrocarbon cycle that is not substituted or is substituted 1 to 4 times by R1 or a saturated heterocycle, unsaturated or monocyclic aromatic with 1 to 4 heteroatoms selected from N, O and S that is not substituted or mono-, di- or trisubstituted by R1,>; = S,>; = NR1 or>; = O, Q is a bond single or a linear, branched or mono- or bicyclic alkyl linker containing 1 to 10 C atoms where optionally 1 to 5 CH2 groups are substituted by -CR3R4-, -S-, -SO-, -SO2-, - NR3-, -OCO-, -NR3CONR4-, -NR3CO-, -NR3SO2R4-, -COO- or -CONR3- and where optionally 1 to 20 atoms of H are substituted by F or Cl, where R3 and R4 with atoms to which they are attached optionally form a cycloalkyl or heterocyclyl containing from 3 to 7 atoms C where optionally 1 to 3 CH2 groups are substituted by -O-, -S-, -SO-, -SO2-, -NR-, -OCO-,
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