Thrombin receptor antagonists
US5446131A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Oct 24, 1994 |
| Grant date | Aug 29, 1995 |
| Priority date | — |
| Expiry date | Oct 24, 2014 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K2319/74
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention relates to novel, biologically active molecules which bind to and inhibit the thrombin receptor. These thrombin receptor antagonists are further characterized by their ability to inhibit thrombin-induced platelet aggregation and their inability to inhibit platelet aggregation induced by an internal peptide fragment of the platelet thrombin receptor. More specifically, the thrombin receptor antagonist of this invention comprises the formula: A.sub.1 -X-X-X-A.sub.2 -X-A.sub.3 -X-A.sub.4 -B-X-A.sub.5 -C-X-A.sub.6 ; wherein each of A.sub.1 and A.sub.6, either the same or different, are selected from the group consisting of a positively charged amino acid and an acyl or alkyl chain comprising from 1 to 10 backbone atoms and a positively charged side group; each of A.sub.2, A.sub.3, A.sub.4 and A.sub.5, is a positively charged amino acid, either the same or different; each X is any amino acid, either the same or different; B is an amino acid containing an aryl side chain; and C is a polar amino acid. This invention also relates to compositions and methods which employ these molecules for therapeutic and prophylactic purposes.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.