US4857508A
Expired / Lapsed
US
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Novel platelet-aggregation inhibitor peptide derivatives
Assignee: GD Searle LLC
•
Filing: 1987-12-03
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Granted: 1989-08-15
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Expires: 2007-12-03
Abstract
Abstract Novel tetrapeptide derivatives are provided which have useful activity as inhibitors of platelet aggregation. These compounds have the sequence X-Gly-Asp-Y wherein X is illustrated by arginine and Y is illustrated by O-methyltyrosine amide.
Inventors
- 👤 Steven P. Adams
- 👤 Larry P. Feigen
- 👤 Masateru Miyano
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 23:57
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/10; C07K5/1019; A; A61; A61P; A61P7/00; A61P7/02; C07K5/08; C07K5/0802; C07K5/0804; C07K5/0806; C07K5/0815; C07K5/0817; A61K; A61K38/00
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
130 words
A tetrapeptide derivative having inhibitory activity toward platelet aggregation selected from the group consisting of X-Gly-Asp-Y ##STR4## Z=H, NH 2 or NH-Acyl, n=1 to 4, ##STR5## R 1 =H, alkyl, phenyl or phenylalkyl, R 2 =H, COOH, CONH 2 , COCH 3 , CH 2 OH, CH 2 NH 2 , C(NH)CH 3 or C(NH)NH 2 , R 3 =phenyl, unsubstituted biphenyl or naphthyl, each substituted with 1 to 3 alkyl or alkoxy groups, or an unsubstituted naphthyl, biphenyl or unsubstituted pyridyl group, m=0 to 2, wherein alkyl and alkoxy each have 1 to 4 carbons, provided that when Y is Tyr-NH 2 or Phe-NH 2 , X is Acetyl-Arg, and provided further that when Z is NH 2 or NH-Acyl, X is in the D- or L-amino acid stereo-configuration.
Claim 2
Dependent Claim
130 words
A tetrapeptide derivative having inhibitory activity toward platelet aggregation selected from the group consisting of X-Gly-Asp-Y ##STR4## Z=H, NH 2 or NH-Acyl, n=1 to 4, ##STR5## R 1 =H, alkyl, phenyl or phenylalkyl, R 2 =H, COOH, CONH 2 , COCH 3 , CH 2 OH, CH 2 NH 2 , C(NH)CH 3 or C(NH)NH 2 , R 3 =phenyl, unsubstituted biphenyl or naphthyl, each substituted with 1 to 3 alkyl or alkoxy groups, or an unsubstituted naphthyl, biphenyl or unsubstituted pyridyl group, m=0 to 2, wherein alkyl and alkoxy each have 1 to 4 carbons, provided that when Y is Tyr-NH 2 or Phe-NH 2 , X is Acetyl-Arg, and provided further that when Z is NH 2 or NH-Acyl, X is in the D- or L-amino acid stereo-configuration.
Claim 3
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence Arg-Gly-Asp-(O-methyltyrosine)-amide.
Claim 4
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence Arg-Gly-Asp-(O-ethyltyrosine)-amide.
Claim 5
Dependent Claim
11 words
The tetrapeptide derivative of claim 1 having the sequence acetyl-Arg-Gly-Asp-(O-methyl tyrosine)-amide.
Claim 6
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence acetyl-(D-Arg)-Gly-Asp-O-methyltyrosine)-amide.
Claim 7
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence Arg-Gly-Asp-(4-methoxy-1-naphthylalanine)-amide.
Claim 8
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence Arg-Gly-Asp-(2,6-dimethyl-O-methyltyrosine)-amide.
Claim 9
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence desamino-Arg-Gly-Asp-(O-methyltyrosine)-amide.
Claim 10
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence desamino-(homoarginine)-Gly-Asp-(O-methyl-tyrosine)-amide.
Claim 11
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence Arg-Gly-Asp-(p-phenyl-phenylalanine)-amide.
Claim 12
Dependent Claim
10 words
The tetrapeptide derivative of claim 1 having the sequence acetyl-Arg-Gly-Asp-Tyr-amide.
Claim 13
Dependent Claim
31 words
The method of inhibiting platelet aggregation in a warm blooded mammal comprising administering to said mammal an effective amount of the tetrapeptide derivative of claim 1 in a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
14 words
The method of claim 12 in which the tetrapeptide derivative has the sequence Arg-Gly-Asp-(O-methyltyrosine)-amide.
Claim 15
Dependent Claim
33 words
The method of inhibiting formation of a thrombus in a warm blooded mammal comprising administering to said mammal an effective amount of the tetrapeptide derivative of claim 1 in a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
14 words
The method of claim 14 in which the tetrapeptide derivative has the sequence Arg-Gly-Asp-(O-methyltyrosine)-amide.
Claim 17
Dependent Claim
15 words
A pharmaceutical composition comprising the tetrapeptide derivative of claim 1 in a pharmaceutically acceptable carrier.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-14 | 1993-02-13 | 1993-08-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-14 | 1997-02-13 | 1997-08-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-14 | 2001-02-13 | 2001-08-15 | $7700.00 | Window Closed / Lapsed |