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Patent US4683291A successfully refreshed from Google Patents.
US4683291A
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Platelet binding inhibitors
Assignee: Scripps Research Institute
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Filing: 1985-10-28
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Granted: 1987-07-28
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Expires: 2005-10-28
Abstract
Abstract Peptides of the general formula H2N-(Ch)-Arg-Gly-Asp-(Cx)-H and 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
US
Data Source
google_patents
Last Synchronized
2026-10-24 20:05
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
111 words
A peptide having one of the formulas ##STR4## 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 contained 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 with the proviso that (Cx) in formula (1a) does not include the amino acid residues, Cys, Thr or Ser; and each amino acid residue is in the (L) or (D) configuration.
Claim 2
Dependent Claim
111 words
A peptide having one of the formulas ##STR4## 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 contained 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 with the proviso that (Cx) in formula (1a) does not include the amino acid residues, Cys, Thr or Ser; and each amino acid residue is in the (L) or (D) configuration.
Claim 3
Dependent Claim
17 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
41 words
A peptide of the formula ##STR5## wherein: n is a integer from 1 to 20; X in each occurrence is independently Lys or Arg; Y is Leu or Ala; and each amino acid residue is in the (L) or (D) configuration.
Claim 5
Dependent Claim
41 words
A peptide of the formula ##STR5## wherein: n is a integer from 1 to 20; X in each occurrence is independently Lys or Arg; Y is Leu or Ala; and each amino acid residue is in the (L) or (D) configuration.
Claim 6
Dependent Claim
50 words
A peptide according to claim 3 having the formula H 2 N-(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
14 words
A peptide according to claim 4 having the formula H 2 N-(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
34 words
A peptide according to claim 4 having the formula H 2 N-(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
12 words
A peptide according to claim 9 having the formula H 2 N-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
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Asp-Val-H.
Claim 16
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-Lys-Lys-Lys-Lys-Lys-Lys-Arg-Gly-Asp-Val-H.
Claim 17
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-D-Ala-Arg-Lys-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 18
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-D-Ala-Gly-Gly-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 19
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-Lys-Arg-Lys-Arg-Lys-Arg-Arg-Gly-Asp-Ser-H.
Claim 20
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-Lys-Arg-Lys-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 21
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-Lys-Lys-Lys-Lys-Lys-Lys-Lys-Lys-Arg-Gly-Asp-Val-H.
Claim 22
Dependent Claim
13 words
A peptide according to claim 3 which has the formula H 2 N-His-His-Leu-Arg-Lys-Arg-Lys-Gln-Arg-Gly-Asp-Val-H.
Claim 23
Dependent Claim
96 words
A peptide having the formula ##STR6## wherein (Cx) is a chain of 1 to 20 amino acid residues with the proviso that (Cx) does not include the amino acid residues, Cys, Thr, or Ser when p is 1, (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
96 words
A peptide having the formula ##STR6## wherein (Cx) is a chain of 1 to 20 amino acid residues with the proviso that (Cx) does not include the amino acid residues, Cys, Thr, or Ser when p is 1, (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)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-07-27 | 1991-01-26 | 1991-07-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-07-27 | 1995-01-26 | 1995-07-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-07-27 | 1999-01-26 | 1999-07-28 | $7700.00 | Window Closed / Lapsed |