EP0353565A1
Expired / Lapsed
EP
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Immunostimulating peptides, a process for their preparation and pharmaceutical commpositions containing them
Assignee: Ellem Industria Farmaceutica SpA
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Filing: 1989-07-21
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Granted: —
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Expires: 2009-07-21
Abstract
Abstract The peptides of formula I A-x-Lys-y-B I in which: A is H, a tripeptide of formula Arg-Ala-Arg or an hexapeptide of formula Glu-Lys-Arg-Arg-Ala-Arg x and y, different one from the other, are an arginine (Arg) or a glutamic acid (Glu) residue; B is OH or a tripeptide Arg-Ala-Arg with the proviso that when A is hydrogen and x is Arg, B is different from OH comprising the steps of: a) binding the Boc-protected carboxyterminal aminoacid to a suitable resin; b) reacting the other Boc-protected aminoacids with the resin-bound carboxyterminal aminoacid in the desired sequence; c) removing the protecting groups and releasing the so obtained peptides from the resin, have valuable pharmacological properties as immunostimulating agents.
Inventors
- 👤 Brunetto Brunetti
- 👤 Marco Prada
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-09 03:38
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/04; C07K7/06; A; A61; A61P; A61P37/00; A61P37/02; A61P37/04; C07K14/00; C07K14/435; C07K14/575; C07K14/66; C07K14/662; C07K5/00; C07K5/04; C07K5/08; C07K5/0819; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
67 words
Peptides of formula I in which: A is H, a tripeptide of formula Arg-Ala-Arg or an hexapeptide of formula Glu-Lys-Arg-Arg-Ala-Arg x and y, different one from the other, are an arginine (Arg) or a glutamic acid (Glu) residue; B is OH or a tripeptide Arg-Ala-Arg with the proviso that when A is hydrogen and x is Arg, B is different from OH and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
67 words
Peptides of formula I in which: A is H, a tripeptide of formula Arg-Ala-Arg or an hexapeptide of formula Glu-Lys-Arg-Arg-Ala-Arg x and y, different one from the other, are an arginine (Arg) or a glutamic acid (Glu) residue; B is OH or a tripeptide Arg-Ala-Arg with the proviso that when A is hydrogen and x is Arg, B is different from OH and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
15 words
Peptides of formula I wherein the aminoacids are of the D-, L- or DL series.
Claim 4
Dependent Claim
15 words
Peptides of formula I wherein the aminoacids are of the D-, L- or DL series.
Claim 5
Dependent Claim
10 words
Acetate, trifluorocacetate, sulfate, hydrochloride salts of peptides of formula I.
Claim 6
Dependent Claim
10 words
Acetate, trifluorocacetate, sulfate, hydrochloride salts of peptides of formula I.
Claim 7
Dependent Claim
23 words
A peptide according to claim 1 or 2 selected in the group consisting of Arg-Lys-Glu-Arg-Ala-Arg, Arg-Lys-Glu-Arg-D-Ala-Arg, Arg-Ala-Arg-Arg-Lys-Glu, Arg-D-Ala-Arg-Arg-Lys-Glu, Arg-Ala-Arg-Arg-Lys-Glu-Arg-Ala-Arg, Glu-Lys-Arg, Arg-Ala-Arg-Glu-Lys-Arg, Glu-Lys-Arg-Arg-Ala-Arg, Glu-Lys-Arg-Arg-Ala-Arg-Glu-Lys-Arg.
Claim 8
Dependent Claim
22 words
A pharmaceutical composition having immunostimulating activity comprising as the active principle a peptide of claims 1-4 in admixture with an acceptable carrier.
Claim 9
Dependent Claim
24 words
Use of the peptides of claims 1-4 for the preparation of medicaments having immunostimulating activity for the treatment of primary and secondary immunode ficiencies.
Claim 10
Dependent Claim
12 words
A process for the preparation of peptides of formula I in which:
Claim 11
Dependent Claim
12 words
A process for the preparation of peptides of formula I in which:
Claim 12
Dependent Claim
107 words
A is H, a tripeptide of formula Arg-Ala-Arg or an hexapeptide of formula Glu-Lys-Arg-Arg-Ala-Arg x and y, different one from the other, are an arginine (Arg) or a glutamic acid (Glu) residue; B is OH or a tripeptide Arg-Ala-Arg with the proviso that when A is hydrogen and x is Arg, B is different from OH comprising the steps of: a) binding the Boc-protected carboxyterminal aminoacid to a suitable resin; b) reacting the other Boc-protected aminoacids with the resin-bound carboxyterminal aminoacid in the desired sequence; c) removing the protecting groups and releasing the so obtained peptides from the resin. Claims for the following Contracting States: ES, GR
Claim 13
Dependent Claim
111 words
A process for the preparation of peptides of formula I in which: A is H, a tripeptide of formula Arg-Ala-Arg or an hexapeptide of formula Glu-Lys-Arg-Arg-Ala-Arg x and y, different one from the other, are an arginine (Arg) or a glutamic acid (Glu) residue; B is OH or a tripeptide Arg-Ala-Arg with the proviso that when. A is hydrogen and x is Arg, B is different from OH comprising the steps of: a) binding the Boc-protected carboxyterminal aminoacid to a suitable resin; b) reacting the other Boc-protected aminoacids with the resin-bound carboxyterminal aminoacid in the desired sequence; c) removing the protecting groups and releasing the so obtained peptides from the resin.
Claim 14
Dependent Claim
111 words
A process for the preparation of peptides of formula I in which: A is H, a tripeptide of formula Arg-Ala-Arg or an hexapeptide of formula Glu-Lys-Arg-Arg-Ala-Arg x and y, different one from the other, are an arginine (Arg) or a glutamic acid (Glu) residue; B is OH or a tripeptide Arg-Ala-Arg with the proviso that when. A is hydrogen and x is Arg, B is different from OH comprising the steps of: a) binding the Boc-protected carboxyterminal aminoacid to a suitable resin; b) reacting the other Boc-protected aminoacids with the resin-bound carboxyterminal aminoacid in the desired sequence; c) removing the protecting groups and releasing the so obtained peptides from the resin.
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