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US 8,946,154 B2Granted
Peptide ligands of somatostatin receptors
AssigneeBcn Peptides, S.A.
InventorsAntonio Parente Dueña, Berta Ponsati Obiols, Jimena Fernández Carneado, Marc Gómez Caminals, Ribera Jordana I Lluch
Life of this patent
Estimating the term…
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.
Claims22
A compound of general formula (I)
- stereoisomers thereof, mixtures thereof or their pharmaceutically acceptable salts thereon, 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 from 0 to 6 with the condition that when R7, R8 and R9 are H, then m is different from 0;
- n is an integer from 0 to 6 with the condition that when R10, R11 and R12 are H, then n is different from 0;
- p is an integer from 0 to 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 —SS—;
- 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 and n, m and p are equal to 1, R13 is equal to L-(3-quinolyl)methyl or to D-(3-quinolyl)methyl.
11 more elements
A compound of general formula (I)
- their stereoisomers, mixtures thereof or their pharmaceutically acceptable salts, wherein:
- R1 is H;
- R2 is —OR3;
- R3 is H;
- R6 is H;
- R7, R8, and R9 are methyl and are in an ortho-, para-, or ortho-configuration;
- R10, R11, R12, R14, R15 and R16 are H;
- m is 1;
- n is 1;
- p is 1;
- R13 is D-(3-indolyl)methyl;
- and
- R17 is —SS—.
10 more elements
Dependencies are inferred from the claim text.