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Compounds comprising short amino alcohol chains and metal complexes for medical imaging
专利权人:
GUERBET
发明人:
PORT, MARC
申请号:
DK06807100
公开号:
DK1931673T3
申请日:
2006.10.09
申请国别(地区):
DK
年份:
2012
代理人:
摘要:
Polyaza compounds (I) and their isomers, enantiomers and/or diastereomers and salts, are new. Polyaza compounds (I) of formula (IIa), (IIb) and (VIa) or linear polyaza compounds (Vb) of formula (R 5-CH(X 5)-N(CHX 4R 4)-CH(K 16)-CH(K 15)-N(CH(R 3)(X 3))-CH(K 14)-CH(K 13)-N(CHX 2R 2)-CH(R 1)-X 1), and their isomers, enantiomers and/or diastereomers and salts of (VIa) and (VIb), are new. R 1-R 5COOH, P(O)(OH) 2or R 6-P(O)-OH, preferably COOH; R 6H or 1-3C alkyl; X 1-X 5L-Y 1; L : 1-3C alkyl, preferably (CH 2) n; n : 1-3; Y 1-CONH 2, CO-NR 7R 8or NR 7-CO-R 8; R 7, R 7H or 1-6C (hydroxy)alkyl, preferably -CH 2-CH 2-OH, CHOH-CH 2OH, -CH-(CH 2OH) 2, -(CH 2) m-(CHOH) p-CH 2OH or -C(CH 2OH) 3; m : 1-3; p : 1-4; D, E, F 1CH or N; either K 1-K 20H, -(CH 2) j-CH 3or -(CH 2) i-OH, preferably H; or K 3K 5, K 4K 5, K 3K 6, K 4K 6, K 7K 9, K 7K 10, K 8K 9, K 8K 10, K 13K 14, K 15K 16, K 17K 18, K 19K 203-6C ring; j : 0-3; and i : 1-3. Provided that the sum of m and p is 2-5. Independent claims are included for: (1) a multimer, preferably dimer or trimer, of (II) or (VI); (2) vectorized compound comprising (II) or (VI) coupled to a biovector by an intermediate optionally of a bridging group; (3) a complex compound or multimer or a vectorized compound having a metal ion (M); (4) lipidic pharmaceutical composition comprising the compound, multimer, vectorized product or complex bound to a lipidic nanoparticule; (5) diagnostic composition for magnetic resonance imaging comprising the compound, multimer, vectorized product or complex; and (6) preparation of the metal complex of (IIa) comprising reacting an ester compound of formula (R aOOC-CHQ-(CH 2) n-COOR a) with a fused macrocycle of formula (IV) to obtain a hexaacid of formula (V), optionally hydrolyzing or hydrogenating the ester groups of (V) to obtain the hexaacid of formula (Va), reacting a salt or an oxide of the metal to be complexed with (Va), to obtain the complex or its base salts and reacting amino alcohol groups of formul
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