[EN] MACROCYCLIC LIGANDS WITH PENDANT CHELATING MOIETIES AND COMPLEXES THEREOF<br/>[FR] LIGANDS MACROCYCLIQUES AYANT DES FRACTIONS CHÉLATANTES PENDANTES ET LEURS COMPLEXES
申请人:LUMIPHORE INC
公开号:WO2018045385A1
公开(公告)日:2018-03-08
The invention relates to chemical compounds and complexes that can be used in therapeutic and diagnostic applications.
Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.
DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
申请人:PIERRE FABRE MEDICAMENT
公开号:US20180222858A1
公开(公告)日:2018-08-09
The present invention concerns a compound of following formula (I): where: —R
1
is H or OH, —R
2
is a (C
1
-C
6
)alkyl, COOH, COO—((C
1
-C
6
)alkyl) or thiazolyl group, —R
3
is H or a (C
1
-C
6
)alkyl group, and —R
4
is: ▪a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR
5
R
6
, ▪—(CH
2
CH
2
X
1
)(CH
2
CH
2
X
2
)
a2
(CH
2
CH
2
X
3
)
a3
(CH
2
CH
2
X
4
)
a4
(CH
2
CH
2
X
5
)
a5
R
7
, ▪an aryl-(C
1
-C
8
)alkyl group substituted by one or more groups chosen from among OH and NR
9
R
10
groups, or ▪a heterocycle-(C
1
-C
8
)alkyl group optionally substituted by one or more groups chosen from among (C
1
-C
6
)alkyl, OH and NR
12
R
13
groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.