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US 2012/0122781 A1Published application
Peptide ligands of somatostatin receptors
AssigneeBcn Peptides, S.A.
InventorsAntonio Parente Duena, Berta Ponsati Obiols, Jimena Fernandez Carneado, Marc Gomez Caminals, Ribera Jordana I Lluch
Life of this patent
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Abstract
Peptide derivatives, their stereoisomers, mixtures thereof and/or their pharmaceutically acceptable salts, a method of obtaining them, pharmaceutical compositions containing them and the use thereof for the treatment, prevention and/or diagnosis of those conditions, disorders and/or pathologies in which the sstr1, sstr2, sstr3, sstr4 and/or sstr5 somatostatin receptors are expressed.
Claims23
A compound of general formula (I)
- their stereoisomers, mixtures thereof and/or their pharmaceutically acceptable salts, wherein:
- R1 is selected from the group consisting of H, a substituted or unsubstituted non-cyclic aliphatic group, a substituted or unsubstituted alicyclyl group, a substituted or unsubstituted heterocyclyl group, a substituted or unsubstituted heteroarylalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aralkyl group, a polyethylene glycol polymer, a chelating agent and R5—CO—;
- R2 is selected from the group consisting of —NR3R4, —OR3 and —SR3;
- R6 is selected from the group consisting of H, acetyl, trifluoroacetyl, isopropyl, palmitoyl, allyloxycarbonyl, 2-chlorobenzyl, formyl, N-[1-(4,4-dimethyl-2,6-dioxocyclohex-1-ylidene)ethyl] and benzyloxycarbonyl;
- R7, R8, R9, R10, R11, R12, R14, R15 and R16 are selected independently from one another from the group consisting of H and a non-cyclic aliphatic group;
- m is an integer selected from between 0 and 6 with the condition that when R7, R8 and R9 are H, then m is different from 0;
- n is an integer selected from between 0 and 6 with the condition that when R10, R11 and R12 are H, then n is different from 0;
- p is an integer selected from between 0 and 6 with the condition that when R14, R15 and R16 are H, then p is different from 0;
- R13 is selected from the group consisting of L-(3-quinolyl)methyl, D-(3-quinolyl)methyl, L-(3-indolyl)methyl and D-(3-indolyl)methyl;
- R17 is selected from the group consisting of —SS— and —CH═CH—;
- R3 and R4 are independently selected from the group consisting of H, a substituted or unsubstituted non-cyclic aliphatic group, a substituted or unsubstituted alicyclyl group, a substituted or unsubstituted heterocyclyl group, a substituted or unsubstituted heteroarylalkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aralkyl group and a polymer;
- R5 is selected from the group consisting of H, a substituted or unsubstituted non-cyclic aliphatic group, a substituted or unsubstituted alicyclyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted heterocyclyl group and a substituted or unsubstituted heteroarylalkyl group;
- and
- with the condition that when R6, R7, R8, R9, R10, R11, R12, R14, R15 and R16 are all equal to H, n, m and p are equal to 1 and R13 is equal to L-(3-indolyl)methyl or to D-(3-indolyl)methyl, R17 is not equal to —S—S—.
11 more elements
-19. (canceled)
Dependencies are inferred from the claim text.