Patent EP0220957A2 successfully refreshed from Google Patents.
EP0220957A2
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EP
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Platelet binding inhibitors
Assignee: Scripps Research Institute
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Filing: 1986-10-27
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Granted: —
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Expires: 2006-10-27
Abstract
Abstract Peptides of the general formulaH₂N-(Ch)-Arg-Gly-Asp-(Cx)-Hand the derivatives thereof described herein, wherein (Cx) and (Ch) each contains 1 to 20 amino acid residues and (Ch) contains at least one Lys or Arg residue, or at least one of each, inhibit platelet-fibrinogen binding and platelet-platelet aggregation and are thus useful inhibitors of cell adhesion.
Inventors
- 👤 Theodore S. Zimmerman
- 👤 Zaverio M. Ruggeri
- 👤 Richard Houghten
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 07:40
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/745; C07K14/75; A; A61; A61P; A61P7/00; A61P7/02; A61K; A61K38/00
Claims Analysis
Total Claims: 36
Claim 1
Independent Claim
103 words
A peptide having one of the formulas H₂N-(Ch)-Arg-Gly-Asp-(Cx)-H (1a) [H₂N-(Ch)-NH] m -(CZ)-[C(O)-Arg-Gly-Asp-(Cx)-H] n (Ic) [H₂N-(Ch)-NH] m -(CZ)-[NH-(Cx)-Asp-Gly-Arg-NH₂] n (1d) wherein: (Ch) is a chain of 1 to 20 amino acid residues which contains at least 1 residue selected from the group consisting of Lys and Arg; m and n are each 1-10, and (m+n) is 3-20; (CZ) is a straight or branched alkyl group containing at least (m+n) carbon atoms and up to 20 carbon atoms; (Cx) is a chain of 1 to 20 amino acid residues or a chemical bond; and each amino acid residue is in the (L) or (D) configuration.
Claim 2
Dependent Claim
103 words
A peptide having one of the formulas H₂N-(Ch)-Arg-Gly-Asp-(Cx)-H (1a) [H₂N-(Ch)-NH] m -(CZ)-[C(O)-Arg-Gly-Asp-(Cx)-H] n (Ic) [H₂N-(Ch)-NH] m -(CZ)-[NH-(Cx)-Asp-Gly-Arg-NH₂] n (1d) wherein: (Ch) is a chain of 1 to 20 amino acid residues which contains at least 1 residue selected from the group consisting of Lys and Arg; m and n are each 1-10, and (m+n) is 3-20; (CZ) is a straight or branched alkyl group containing at least (m+n) carbon atoms and up to 20 carbon atoms; (Cx) is a chain of 1 to 20 amino acid residues or a chemical bond; and each amino acid residue is in the (L) or (D) configuration.
Claim 3
Dependent Claim
18 words
A peptide according to claim 1 wherein Ch contains at least one -Lys-Lys-, -Lys-Arg-, -Arg-Lys-, or -Arg-Arg- moiety.
Claim 4
Dependent Claim
57 words
A peptide of the formula H₂N-(His)₀ - ₂-(Y)₀ - ₁- (Gly)₀ - ₁-(X) n -(Gln)₀ - ₁-Arg-Gly-Asp-(Z)-H wherein: n is an integer from 1 to 20; X in each occurrence is independently Lys or Arg; Y is Leu or Ala; Z is Ser or Val; and each amino acid residue is in the (L) or (D) configuration.
Claim 5
Dependent Claim
57 words
A peptide of the formula H₂N-(His)₀ - ₂-(Y)₀ - ₁- (Gly)₀ - ₁-(X) n -(Gln)₀ - ₁-Arg-Gly-Asp-(Z)-H wherein: n is an integer from 1 to 20; X in each occurrence is independently Lys or Arg; Y is Leu or Ala; Z is Ser or Val; and each amino acid residue is in the (L) or (D) configuration.
Claim 6
Dependent Claim
48 words
A peptide according to claim 3 having the formula H₂N-(X) n -Arg-Gly-Asp-Val-H wherein n is an integer from 1 to 20; each of the amino acid residues X is independently Lys or Arg; and each amino acid residue in the peptide is in the (L) or (D) configuration.
Claim 7
Dependent Claim
13 words
A peptide according to claim 4 having the formula H₂N-(Arg ) n+1 -Gly-Asp-Val-H.
Claim 8
Dependent Claim
10 words
A peptide according to claim 5 wherein n is 8.
Claim 9
Dependent Claim
16 words
A peptide according to claim 6 wherein each amino acid residue is in the (L) configuration.
Claim 10
Dependent Claim
16 words
A peptide according to claim 6 wherein each amino acid residue is in the (D) configuration.
Claim 11
Dependent Claim
32 words
A peptide according to claim 4 having the formula H₂N-(X) n -Arg-Gly-Asp-Val-H wherein (X) n is -(Lys-Arg) i - or -(Arg-Lys) i - and i is an integer from 1 to 6.
Claim 12
Dependent Claim
10 words
A peptide according to claim 9 having the formula H₂N-Lys-Arg-Lys-Arg-Lys-Arg-Lys-Arg-Arg-Gly-Asp-Val-H.
Claim 13
Dependent Claim
16 words
A peptide according to claim 10 wherein each amino acid residue is in the (L) configuration.
Claim 14
Dependent Claim
16 words
A peptide according to claim 10 wherein each amino acid residue is in the (D) configuration.
Claim 15
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Asp-Val-H.
Claim 16
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-Lys-Lys-Lys-Lys-Lys-Lys-Arg-Gly-Asp-Val-H.
Claim 17
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-D-Ala-Arg-Lys-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 18
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-D-Ala-Gly-Gly-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 19
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-Lys-Arg-Lys-Arg-Lys-Arg-Arg-Gly-Asp-Ser-H.
Claim 20
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-Lys-Arg-Lys-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 21
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-Lys-Lys-Lys-Lys-Lys-Lys-Lys-Lys-Arg-Gly-Asp-Val-H.
Claim 22
Dependent Claim
11 words
A peptide according to claim 3 which has the formula H₂N-His-His-Leu-Arg-Lys-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 23
Dependent Claim
79 words
A peptide having the formula H₂N (Ch)-Arg-Gly-Asp-(Cx) p H wherein (Cx) is a chain of 1 to 20 amino acid residues; (Ch) is a chain of 1 to 20 amino acid residues which contains at least 1 residue selected from the group consisting of Lys and Arg; each amino acid residue is in the (L) or (D) configuration; and p is a value such that the peptide is soluble in an aqueous isotonic solution 0.15 M in sodium chloride.
Claim 24
Dependent Claim
79 words
A peptide having the formula H₂N (Ch)-Arg-Gly-Asp-(Cx) p H wherein (Cx) is a chain of 1 to 20 amino acid residues; (Ch) is a chain of 1 to 20 amino acid residues which contains at least 1 residue selected from the group consisting of Lys and Arg; each amino acid residue is in the (L) or (D) configuration; and p is a value such that the peptide is soluble in an aqueous isotonic solution 0.15 M in sodium chloride.
Claim 25
Dependent Claim
32 words
A method for inhibiting the binding of fibrinogen to platelets comprising contacting the platelets with a peptide according to claim 1 in an amount of said peptide effective to inhibit said binding.
Claim 26
Dependent Claim
32 words
A method for inhibiting the binding of fibrinogen to platelets comprising contacting the platelets with a peptide according to claim 4 in an amount of said peptide effective to inhibit said binding.
Claim 27
Dependent Claim
32 words
A method for inhibiting the binding of fibrinogen to platelets comprising contacting the platelets with a peptide according to claim 6 in an amount of said peptide effective to inhibit said binding.
Claim 28
Dependent Claim
32 words
A method for inhibiting the binding of fibrinogen to platelets comprising contacting the platelets with a peptide according to claim 10 in an amount of said peptide effective to inhibit said binding.
Claim 29
Dependent Claim
32 words
A method for inhibiting aggregation of cells to each other comprising contacting the cells with a peptide according to claim 1 in an amount of said peptide effective to inhibit said aggregation.
Claim 30
Dependent Claim
32 words
A method for inhibiting aggregation of platelets to each other comprising contacting the platelets with a peptide according to claim 1 in an amount of said peptide effective to inhibit said aggregation.
Claim 31
Dependent Claim
32 words
A method for inhibiting aggregation of cells to each other comprising contacting the cells with a peptide according to claim 4 in an amount of said peptide effective to inhibit said aggregation.
Claim 32
Dependent Claim
32 words
A method for inhibiting aggregation of platelets to each other comprising contacting the platelets with a peptide according to claim 4 in an amount of said peptide effective to inhibit said aggregation.
Claim 33
Dependent Claim
32 words
A method for inhibiting aggregation of cells to each other comprising contacting the cells with a peptide according to claim 6 in an amount of said peptide effective to inhibit said aggregation.
Claim 34
Dependent Claim
32 words
A method for inhibiting aggregation of platelets to each other comprising contacting the platelets with a peptide according to claim 6 in an amount of said peptide effective to inhibit said aggregation.
Claim 35
Dependent Claim
32 words
A method for inhibiting aggregation of cells to each other comprising contacting the cells with a peptide according to claim 10 in an amount of said peptide effective to inhibit said aggregation.
Claim 36
Dependent Claim
32 words
A method for inhibiting aggregation of platelets to each other comprising contacting the platelets with a peptide according to claim 10 in an amount of said peptide effective to inhibit said aggregation.
References Cited (Backward Citations)
No citation records indexed.
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