EP0540969A2
Expired / Lapsed
EP
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Derivatives of structurally modified VIP and pharmaceutical compositions containing them
Assignee: Ramot at Tel Aviv University Ltd
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Filing: 1992-10-26
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Granted: —
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Expires: 2012-10-26
Abstract
Abstract There are provided novel compounds for the treatment of male impotence. The compounds are derived from vasoactive intestinal peptide (VIP) and VIP₇₋₂₈ and VIP₁₆₋₂₈ fragments in which the natural amino acid sequence is modified by replacement of any of the 5, 17 and 19 amino acid residues by other natural or non-natural amino acids, and they bear at least one terminal lipophilic group. The modified VIP sequences and fragments are prepared by conventional peptide chain assembling methods. The novel compounds and compositions containing them are suitable for transdermal application.
Inventors
- 👤 Illana Gozes
- 👤 Matityahu Fridkin
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 03:51
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/57563; A; A61; A61K; A61K8/00; A61K8/18; A61K8/30; A61K8/33; A61K8/34; A61K8/345; A61K8/35; A61K8/46; A61K8/466; A61P; A61P13/00; A61P13/02; A61P13/08; A61P15/00; A61P15/10; A61Q; A61Q19/00; A61Q19/04; A61K38/00
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
143 words
A conjugate of a modified vasoactive intestinal peptides (VIP) having the sequence of formula I or of a modified VIP₇₋₂₈ or VIP₁₆₋₂₈ fragment of the sequence of formula I, in which formula I R¹ and R² are the same or different and each is hydrogen, a saturated or unsaturated lipophilic group or 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 are the same or different and each is -CH₂-or -CO-, or is a bond in case the associated R¹ or R² is hydrogen; and X¹, X², and X³ are the same or different and each is a residue of a natural or non-natural amino acid, provided that when both X¹ and X³ are valine X² may not be methionine; and a functional derivative of any such conjugate.
Claim 2
Dependent Claim
10 words
A conjugate according to claim 1, wherein X² is norleucine.
Claim 3
Dependent Claim
15 words
A conjugate according to claim 1 or 2, wherein X¹ and X³ are each valine.
Claim 4
Dependent Claim
16 words
A conjugate according to any one of claims 1 to 3, wherein R¹ is a C₁₇alkyl.
Claim 5
Dependent Claim
26 words
A conjugate according to any one of claims 1 to 4, wherein either of Y¹ and Y² is -CO-and either of R¹-Y¹ and R²-Y² is hydrogen.
Claim 6
Dependent Claim
14 words
A conjugate according to claim 5, wherein both of Y¹ and Y² are -CO-.
Claim 7
Dependent Claim
25 words
A conjugate according to any one of claims 1 to 5, wherein either of Y¹ and Y² is -CH₂-and either of R¹-Y¹-and R²-Y² is hydrogen.
Claim 8
Dependent Claim
14 words
A conjugate according to claim 7, wherein both of Y¹ and Y² are -CH₂-.
Claim 9
Dependent Claim
29 words
A conjugate according to any one of claims 2 to 8, wherein at least one of the amino acid residues in position 2 to 27 bears a functional group.
Claim 10
Dependent Claim
1 words
Stearoyl-norleucine¹⁷-VIP.
Claim 11
Dependent Claim
15 words
A conjugate according to claim 1, being a conjugate of modified VIP₇₋₂₈ or VIP₁₆₋₂₈ fragment.
Claim 12
Dependent Claim
30 words
A pharmaceutical composition for transdermal application containing as an active ingredient a conjugate according to any one of claims 1 to 10, optionally in combination with a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
37 words
A pharmaceutical composition according to claim 11, wherein said pharmaceutically acceptable carrier is selected from the group of glycerine, lubricants, nitroglycerine, glyceryl monocaprylate, propylene glycol didecanoate, propylene glycol dicaprylate, glyceryl tricaprylate and sorbitan monocaprylate, and mixtures thereof.
Claim 14
Dependent Claim
23 words
A pharmaceutical composition according to claim 12 or 13, wherein said active ingredient is stearoyl-norleucine¹⁷-VIP and said pharmaceutically acceptable carrier is glyceryl monocaprylate.
Claim 15
Dependent Claim
26 words
Use of a conjugate according to any one of claims 1 to 10 for the preparation of a pharmaceutical composition for the treatment of male impotence.
Claim 16
Dependent Claim
26 words
A sustained-release transdermal dispenser comprising an applicator adapted for application to the skin, loaded with a conjugate according to any one of claims 1 to 11.
Claim 17
Dependent Claim
24 words
A dispenser according to claim 15, wherein said conjugate is in form of a composition according to any one of claims 12 to 14.
References Cited (Backward Citations)
No citation records indexed.
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