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US 5,849,693 AGranted
Cyclic compounds linked by a heterocyclic ring useful as inhibitors of platelet glycoprotein IIb/IIIa
AssigneeThe DuPont Merck Pharmaceutical Company
InventorsGregory James Wells, John Wityak, Anju Parthasarathy, William Frank DeGrado, Sharon Anne Jackson, Shaker Ahmed Mousa
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Abstract
This invention relates to novel cyclic compounds linked by a heterocyclic ring system, which are useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, and to methods of using these compounds for the inhibition of platelet aggregation.
Claims18
A compound or a pharmaceutically acceptable salt form thereof with the formula (Ia):
- ##STR78## wherein:
- R.sup.1 is H or C.sub.1 -C.sub.4 alkyl;
- R.sup.2 is H or methyl;
- R.sup.10 is H, halogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkoxy;
- n' is 0-1;
- n" is 0-1;
- R.sup.31 is a 5 or 6 membered aromatic heterocycle, said heterocycle being substituted with 0-2 R.sup.10, said heterocycle being selected from the group consisting of:
- furan, thiophene, pyrrole, imidazole, pyrazole, oxazole, isoxazole, thiazole, isothiazole, oxadiazole, thiadiazole, pyridine, pyridazine, pyrimidine, and pyrazine;
- J is D-Ala, D-Val, D-Ile, D-Leu, D-Nle, D-phenylGly, D-Phe, D-Lys, D-Orn, D-Met, D-Pro, D-Tyr, D-Ser, D-cyclohexylGly, D-cyclohexylmethylGly, D-norvaline, D-2-aminobutyric acid, or D-2-aminopentanoic acid;
- K is N.sup..alpha. -MeArg, N.sup..alpha. -MeLys, N.sup..epsilon.,N.sup..alpha. -diMeLys, N.sup..alpha. -p-aminomethylPhe, or N.sup..alpha. -p-guanidinylPhe;
- L is Gly;
- and
- M is Asp, .beta.-MeAsp, or NMeAsp.
10 more elements
Dependencies are inferred from the claim text.