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US 2019/0100508 A1Published application
Novel derivatives and their use as selective inhibitors of caspase-2
AssigneesInstitut National De La Sante Et De La Recherche Medicale (Inserm), Universite Paris Diderot—Paris 7
InventorEtienne JACOTOT
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Abstract
The present invention relates to a compound of formula (I) wherein P1, P3, P4 and P5 are amino acid residues. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.
Claims15
A compound of formula (I):
- wherein:
- Z1 is a (C1-C6)alkyl group;
- P5 is selected from the following amino acid residues
- P1 and P4, identical or different, are selected from the following amino acid residues
- in which Z2 and Z3, identical or different, are selected from a hydrogen atom and a (C1-C6)alkyl group;
- P3 is selected from the following amino acids residues
- R1 is selected from
- and
- R2 is selected from
- in which
- m is 0, 1 or 2;
- p is 1, 2, 3 or 4;
- Z4 is a halogen atom;
- q is 0 or 1;
- Z5 is selected from a (C1-C6)alkyl and a phenyl group, said phenyl group being substituted or not by an amino group;
- Z6, Z7 and Z10, identical or different, are selected from a hydrogen atom, a (C1-C4)alkyl, a tetrahydroquinolynyl and a —(CH2)i-aryl group with i being 0, 1 or 2, said aryl group being substituted or not by one, two, three, or four halogen atom(s) or one (C1-C4) alkyl group;
- and
- Z8 and Z9, identical or different, are selected from a halogen atom and a (C1-C6)alkyl group;
- or one of its salts;
- said compound of formula (I) being in all the possible racemic, enantiomeric and diastereoisomeric isomer forms.
17 more elements
Dependencies are inferred from the claim text.