US5100875A
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US
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Novel peptides having plateler aggregation inhibitory activity
Assignee: Institut National de la Santé et de la Recherche Médicale
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Filing: 1990-10-22
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Granted: 1992-03-31
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Expires: 2010-10-22
Abstract
Abstract The subject of the invention is peptide derivatives corresponding to formula X.sup.1 - X.sup.2 - Gly - Asp-X.sup.3 - X.sup.4 (I) in which: X 1 represents a hydrogen atom, a N-protecting group, an amino acid residue or a N-protected amino acid residue, X 2 represents a residue of L-Arg or D-Arg, L-Orn or D-Orn, N-aminocarbonyl -L-Orn or N-aminocarbonyl-D-Orn, or L-Lys, or D-Lys, X 3 represents a residue of L-Trp, D-Trp, L-Leu, D-Leu, L-Ile, D-Ile, L-Phe, D-Phe or a chain of 2 or 3 of these residues, and X 4 represents a -OH group, -NH 2 group, -OR 1 group in which R 1 represents an alkyl radical of C 1 to C 4 , a NHR 2 group in which R 2 represents an alkyl radical of C 1 to C 4 , or an amino acid residue. These derivatives are useful in therapy on account of their platelet aggregation inhibiting activity.
Inventors
- 👤 Gerard A. Marguerie de Rotrou
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:22
CPC Classifications
C; C12; C12Q; C12Q1/00; C12Q1/56; A; A61; A61P; A61P7/00; A61P7/02; C07; C07K; C07K14/00; C07K14/435; C07K14/745; C07K14/75; C07K5/00; C07K5/04; C07K5/10; C07K5/1019; A61K; A61K38/00; G; G01; G01N; G01N2333/00; G01N2333/435; G01N2333/745; G01N2333/75; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
99 words
A compound selected from the compounds of the general formula X.sup.1 -X.sup.2 -Gly-Asp-X.sup.3 -X.sup.4 (I) in which: X 1 is selected from the group consisting of hydrogen and a N-protecting group, X 2 is selected from a residue of L-Arg, D-Arg, L-Orn, D-Orn, N-aminocarbonyl -L-Orn, N-aminocarbonyl-D-Orn, L-Lys and D-Lys, X 3 is selected from a residue of L-Trp, D-Trp, L-Leu, D-Leu, L-Ile, and D-Ile, and X 4 is selected from the group consisting of --OH, --NH 2 , --OR 1 in which R 1 is C 1-4 alkyl, and NHR 2 in which R 2 is C 1-4 alkyl.
Claim 2
Dependent Claim
99 words
A compound selected from the compounds of the general formula X.sup.1 -X.sup.2 -Gly-Asp-X.sup.3 -X.sup.4 (I) in which: X 1 is selected from the group consisting of hydrogen and a N-protecting group, X 2 is selected from a residue of L-Arg, D-Arg, L-Orn, D-Orn, N-aminocarbonyl -L-Orn, N-aminocarbonyl-D-Orn, L-Lys and D-Lys, X 3 is selected from a residue of L-Trp, D-Trp, L-Leu, D-Leu, L-Ile, and D-Ile, and X 4 is selected from the group consisting of --OH, --NH 2 , --OR 1 in which R 1 is C 1-4 alkyl, and NHR 2 in which R 2 is C 1-4 alkyl.
Claim 3
Dependent Claim
5 words
Peptide of the formula H-Arg-Gly-Asp-Trp-OH.
Claim 4
Dependent Claim
5 words
Peptide of the formula H-Arg-Gly-Asp-Trp-OH.
Claim 5
Dependent Claim
30 words
A therapeutic composition for the treatment and the prevention of thromboses comprising an effective amount of a compound as claimed in claim 1 in admixture with a pharmaceutically acceptable excipient.
Claim 6
Dependent Claim
13 words
A composition as claimed in claim 3, in which the compound is H-Arg-Gly-Asp-Trp-OH.
Claim 7
Dependent Claim
122 words
A process for the treatment and the prevention of thromboses, which comprises administering to a human in need thereof an effective amount of a compound selected from the compounds of the general formula X.sup.1 -X.sup.2 -Gly-Asp-X.sup.3 -X.sup.4 (I) in which: X 1 is selected from the group consisting of hydrogen and a N-protecting group, X 2 is selected from a residue of L-Arg, D-Arg, L-Orn, D-Orn, N-aminocarbonyl -L-Orn, N-aminocarbonyl-D-Orn, L-Lys and D-Lys, X 3 is selected from a residue of L-Trp, D-Trp, L-Leu, D-Leu, L-Ile, and D-Ile, and X 4 is selected from the group consisting of --OH, --NH 2 , --OR 1 in which R 1 is C 1-4 alkyl, and NHR 2 in which R 2 is C 1-4 alkyl.
Claim 8
Dependent Claim
122 words
A process for the treatment and the prevention of thromboses, which comprises administering to a human in need thereof an effective amount of a compound selected from the compounds of the general formula X.sup.1 -X.sup.2 -Gly-Asp-X.sup.3 -X.sup.4 (I) in which: X 1 is selected from the group consisting of hydrogen and a N-protecting group, X 2 is selected from a residue of L-Arg, D-Arg, L-Orn, D-Orn, N-aminocarbonyl -L-Orn, N-aminocarbonyl-D-Orn, L-Lys and D-Lys, X 3 is selected from a residue of L-Trp, D-Trp, L-Leu, D-Leu, L-Ile, and D-Ile, and X 4 is selected from the group consisting of --OH, --NH 2 , --OR 1 in which R 1 is C 1-4 alkyl, and NHR 2 in which R 2 is C 1-4 alkyl.
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