PEPTIDES AND PEPTIDE DERIVATIVES AS WELL AS PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

• US 20080039388A1
• Filed: 02/23/2007
• Published: 02/14/2008
• Est. Priority Date: 02/23/2006
• Status: Active Grant

• Current Assignee: Fibrex Medical Research & Development GmbH
• Original Assignee: Fibrex Medical Research & Development GmbH
• Inventors: Henning, Rainer, Reingruber, Sonja, Petzelbauer, Peter
• Granted Patent: US 7,799,758 B2
• Time in Patent Office: Days
• US Class Current: 514/12
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07K 14/75 Fibrinogen
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Peptides and peptide derivatives of the following general Formula I:

H₂H-GHRPX₁X₂X₃X₄X₅X₆X₇X₈X₉X₁₀-(I)X₁₁PX₁₂PPPX₁₃X₁₄X₁₅X₁₆GYR-X₁₇,wherein:

• X₁-X₁₆ denote one of the 20 genetically encoded amino acids,
• X₁₇ denotes OR₁, with R₁=hydrogen or (C₁-C₁₀-alkyl), or NR₂R₃, R₂ and R₃ being identical or different and denoting hydrogen, (C₁-C₁₀)-alkyl, or a residue -PEG_5-60K, wherein the PEG-residue is linked to the N atom via a spacer, or
  • a residue NH—Y-Z-PEG_5-60K, wherein Y denotes a chemical bond or a genetically coded amino acid from among the group of S, C, K or R, and Z denotes a spacer by way of which a polyethylene glycol (PEG)-residue may be linked, as well as the physiologically acceptable salts thereof, or wherein:
• X₁₅ or X₁₆ denotes an amino acid from the group of C or K, which is linked to a residue Z-PEG_5-60K via the heteroatom in the side chain, and wherein
• X₁₇ denotes OR₁, with R₁=hydrogen or (C₁-C₁₀-alkyl), or NR₂R₃, R₂ and R₃ being identical or different and denoting hydrogen or (C₁-C₁₀)-alkyl, as well as the physiologically acceptable salts thereof.

Claims

1. Peptides and peptide derivatives of the following general Formula I:

2. Peptides and peptide derivatives of the general Formula I, wherein:

X₁, X₉, X₁₀, X₁₄ denote L, I, S, M or A,

X₂, X₆, X₇ denote E or D,

X₃, X₄, X₅, X₁₁ denote R or K

X₈, X₁₂ denote A, G, S, or L

X₁₃ denotes I, L or V and wherein

X₁₅, X₁₆ and X₁₇ have the same meaning as in claim 1,

as well as the physiologically acceptable salts thereof.

3. Peptides and peptide derivatives of Formula II,

7. A pharmaceutical drug composition, containing a peptide or peptide derivative according to any of claims 1 to 6.

4. Peptides and peptide derivatives of Formula (II),

wherein:

X₁₇ denotes NR₂R₃, R₂ and R₃ being identical or different and being hydrogen or (C₁-C₁₀)-alkyl, or a residue

C(NR₂R₃)—

(S-succinimido)-(PEG_5-40K), the succinimide residue being linked to the sulfur atom of the cysteine residue via C-atom 3,

as well as the physiologically acceptable salts thereof.

5. Peptide derivatives of Formula (III),

6. Peptide derivative of Formula (III),