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EP0620008A1
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EP
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Use of vip, analogues and fragments thereof for the treatment of neurodegenerative diseases
Assignee: Ramot at Tel Aviv University Ltd
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Filing: 1994-03-08
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Granted: —
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Expires: 2014-03-08
Abstract
Abstract Use of a peptide selected from the group consisting of: (i) vasoactive intestinal peptide (VIP); (ii) analogues of vasoactive intestinal peptide (VIP) in which one or more amino acids has been replaced, added or deleted without substantially altering the biological properties of the parent peptide (iii) a conjugate being a peptide according to either of (i) and (ii) coupled to a lipophilic moiety; (iv) a physiologically active fragment of (i), (ii) and (iii); and (v) a functional derivative of any of (i), (ii), (iii) and (iv) for the preparation of a medicament for the treatment of neurodegenerative disease.
Inventors
- 👤 Illana Gozes
- 👤 Matityahu Fridkin
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 12:12
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/16; C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/57563; A61P; A61P25/00; A61P25/28; C07K19/00; C07K7/00; C07K7/04; C07K7/06
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
98 words
Use of a peptide selected from the group consisting of: (i) vasoactive intestinal peptide (VIP); (ii) analogues of vasoactive intestinal peptide (VIP) in which one or more amino acids has been replaced, added or deleted without substantially altering the biological properties of the parent peptide; (iii) a conjugate being a peptide according to either of (i) and (ii) coupled to a lipophilic moiety; (iv) a physiologically active fragment of (i), (ii) and (iii); and (v) a functional derivative of any of (i), (ii), (iii) and (iv) for the preparation of a medicament for the treatment of neurodegenerative disease.
Claim 2
Dependent Claim
45 words
Use according to Claim 1 in which the active ingredient is an analogue of VIP having the sequence of Formula I wherein X¹, X² and X³ may be the same or different and each is a residue of a natural or non-natural lipophilic amino acid.
Claim 3
Dependent Claim
39 words
Use according to Claim 2, wherein X¹, X² and X³ are the same or different and each is selected from the group consisting of leucine, isoleucine, norleucine, valine, tryptophan, phenylalanine, methionine, octahydroindole-2-carboxylic acid (oic), cyclo-hexylglycine (chg) and cyclopentylglycine (cpg).
Claim 4
Dependent Claim
56 words
Use according to Claim 1, wherein the peptide is a conjugate of VIP or of an analogue, functional derivative or fragment thereof coupled to a lipophilic moiety at either or both of the N-terminus and C-terminus, wherein said lipophilic moiety is a saturated or unsaturated hydrocarbyl or carboxylic acyl radical having at least 5 carbon atoms.
Claim 5
Dependent Claim
175 words
Use according to Claim 1, wherein the peptide has the sequence of Formula II wherein R¹ and R² may be the same or different and each is hydrogen, a lipophilic moiety being a saturated or unsaturated hydrocarbyl or carboxylic acyl hving at least 5 carbon atoms, or R¹ and R² may be the same or different and each is a C₁-C₄ hydrocarbyl or carboxylic acyl with the proviso that at least one of R¹ and R² is a C₁-C₄ hydrocarbyl or carboxylic acyl with the proviso that at least one of R¹ and R² is a lipophilic group; Y¹ and Y² may be the same or different and each is -CH₂ or is a bond in case the associated R¹ or R² is hydrogen and Y¹ may further be -CO-; and X¹, X² and X³ may be the same or different and each is a residue of a natural or non-natural lipophilic amino acid; or a physiologically active fragment thereof; and functional derivatives of said peptide of Formula II or of physiologically active fragments thereof.
Claim 6
Dependent Claim
39 words
Use according to Claim 5, wherein X¹, X² and X³ are the same or different and each is selected from the group consisting of leucine, isoleucine, norleucine, valine, tryptophan, phenylalanine, methionine, octahydroindole-2-carboxylic acid (oic), cyclo-hexylglycine (chg) and cyclopentylglycine (cpg).
Claim 7
Dependent Claim
18 words
Use according to Claim 3 or 6, wherein X² is leucine or norleucine X¹ and X³ are valine.
Claim 8
Dependent Claim
26 words
Use according to Claim 5, wherein X² is neuroleucine, X¹ and X² are valine, Y¹ is -CO-, R¹ is a lipophilic group and R²-Y² is hydrogen.
Claim 9
Dependent Claim
11 words
Use according to Claim 8, wherein R¹ is a C₁₇ alkyl.
Claim 10
Dependent Claim
33 words
Use according to Claim 1, wherein at least one of the amino acid residues in position 2 to 27 of a peptide of any of groups (i) to (iv) bears a functional group.
Claim 11
Dependent Claim
30 words
Use according to Claim 1, wherein the physiologically active fragment has amino acids in posiiton 7 to 28 or 16 to 28 of VIP or of an analogue of VIP.
Claim 12
Dependent Claim
10 words
Use according to Claim 1, wherein the peptide is stearoylnorleucine¹⁷-VIP.
Claim 13
Dependent Claim
10 words
Use according to Claim 1, wherein the peptide is caproylnorleucine¹⁷-VIP.
Claim 14
Dependent Claim
10 words
Use according to Claim 1 for the treatment of dementia.
Claim 15
Dependent Claim
12 words
Use according to Claim 14 for the treatment of Alzheimer caused dementia.
References Cited (Backward Citations)
WO1992011026A1
Cited
EP0540969A2
Cited
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