Patent EA-004867-B1 (EA)
Title: Substituted pyrymidinone compounds, composition and method for the treatment, inhibiting and prevention of thrombotic conditions in mammals
Inventor: SOUTH MICHAEL S
IPC: A61K31/53
Filed: 2000-05-17
Abstract: 1. A compound having the formula: or a pharmaceutically acceptable salt thereof, wherein; B is selected from the group consisting of phenyl, C3-C6 cycloalkyl, C1-C6 alkyl; A is selected from the group consisting of -CH2-SO2-, -CH2-, -CH2-CH2- or a covalent single bond; ( is NH; M is CH; R<2> is selected from the group consisting of phenyl, -S-phenyl, aminophenyl, optionally substituted with amino, carboxy, alkoxycarbonyl or alkylaminocarbonyl, pyridyl; -K-E<0>- is -CH2-C (O) NH-; Y<0> is benzyl, substituted amidino. 2. The compound of claim 1 having the formula: or a pharmaceutically acceptable salt thereof, wherein; B is phenyl; A is selected from the group consisting of -CH2-SO2-, -CH2-CH2-; R<2> is phenyl. 3. The compound of claim 2 or a pharmaceutically acceptable salt thereof, wherein A is -CH2-SO2-. 4. The compound of claim 2 or a pharmaceutically acceptable salt thereof, wherein A is -CH2-CH2-. 5. The compound of claim 1 having the formula: or a pharmaceutically acceptable salt thereof, wherein; B is selected from the group consisting of phenyl, C1-C6 alkyl; A is selected from the group consisting of -CH2-CH2-, -CH2- or a covalent single bond; R<2> is pyridyl. 6. The compound of claim 1 having the formula: or a pharmaceutically acceptable salt thereof, wherein; B is selected from the group consisting of C3-C6 cycloalkyl, C1-C6 alkyl; A is a covalent single bond; R<2> is aminophenyl, optionally substituted with amino, carboxy, alkoxycarbonyl or alkylaminocarbonyl, pyridyl. 7. A composition for inhibiting thrombotic conditions in blood comprising a compound of any one of claims 1 through 6 and a pharmaceutically acceptable carrier. 8. A composition for inhibiting thrombotic conditions in blood comprising adding to blood a therapeutically effective amount of a composition of any one of claims 1 through 6. 9. A method for inhibiting formation of blood platelet aggregates in blood comprising adding to blood a therapeutically effective amount of a composition of any one of claims 1 through 6. 10. A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a composition of any one of claims 1 through 6. 11. A method for treating or preventing venuous thromboembolism and pulmonary embolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of any one of claims 1 through 6. 12. A method for treating or preventing deep vein thrombosis in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of any one of claims 1 through 6. 13. A method for treating or preventing cardiogenic thromboembolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of any one of claims 1 through 6. 14. A method for treating or preventing thromboembolic stroke in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of any one of claims 1 through 6 15. A method for treating or preventing thrombosis associated with cancer and cancer chemotherapy in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of any one of claims 1 through 6 16. A method for treating or preventing unstable angina in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of any one of claims 1 through 6. 17. A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a compound of any one of claims 1 through 6 in combination with a therapeutically effective amount of fibrinogen receptor antagonist. 18. The use of a compound of any one of claims 1 through 6, or a pharmaceutically acceptable salt thereof, in the manufacture of medicament for inhibiting thrombus formation, treating thrombus formation, or preventing thrombus formation in a mammal.