Use as rodenticides of compounds that inhibit blood coagulation
View Patent ↗The invention relates to a use, a method and a poison in which a thrombin inhibitor, a thrombin receptor antagonist, a factor Xa inhibitor, a PAI (plasminogen activator inhibitor), a P2Y12 ADP receptor antagonist or a GPIIb/IIIa receptor antagonist are used as rodenticide.
1. A method of combatting a rodent, the method comprising administering to the rodent a rodenticide comprising at least a factor Xa inhibitor and an antagonist of the ADP receptor P2Y12,
wherein the inhibitor of factor Xa is a compound of the following formula or a salt or hydrate thereof tolerable for a rodent:
wherein Q 3 is:
R 59 is H, F, CI or Br, R 60 , R 61 , R 62 and R 63 are each independently H, F, Cl, Br, Me, NO 2 , OH, OMe, NH 2 , NHAc, NHSO 2 Me, CH 2 OH and CH 2 NH 2 and R 64 is F, Cl, Br, Me, OH or OMe; and
wherein the antagonist of the ADP receptor P2Y12 is:
i) a compound of the following formula or a salt or a hydrate thereof tolerable for a rodent:
wherein R 94 is H, a halogen, hydroxy or C 1-6 alkyl, R 95 is H, a halogen, hydroxy, nitro, C 1-6 alkyl or C 1-6 alkoxy and R 96 is H or a halogen;
ii) a compound of the following formula or a salt or a hydrate thereof tolerable for a rodent:
wherein Y 1 is —OR 98 or —N(R 99 )R 100 , wherein R 99 and R 100 are each independently H, a halogen or a C 1-4 alkyl group and R 98 is H or C 1-4 alkyl and R 97 is H, a halogen or C 1-4 alkyl group; or
iii) a compound of the following formula or a salt or a hydrate thereof tolerable for a rodent:
wherein R 101 is H, OH, amino, C 1 to C 4 alkoxy, Aryl-C 1-4 -alkyloxy, C 1-18 alkanoyloxy, C 3-6 alkenoyloxy or arylcarbonyloxy, R 102 is C 1-10 alkanoyl, C 3-6 alkenoyl, C 4-8 cycloalkylcarbonyl including 3 to 7 ring atoms, substituted benzoyl or 5,6-dihydro-1,4,2-dioxazine-3-yl, Y 2 is NH, O or S, R 103 is H, a halogen, OH, amino, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio or a carboxy group.
2. The method according to claim 1 , wherein the inhibitor of factor Xa comprises betrixaban and the antagonist of the ADP receptor P2Y12 comprises prasugrel.
3. The method according to claim 2 , wherein the rodenticide is administered as a series of doses.
4. The method according to claim 3 , wherein each dose does not result in acute toxicity to the rodent.
5. The method according to claim 3 , wherein each dose is nonlethal to humans.
6. The method according to claim 2 , wherein each dose of the rodenticide is provided in a food bait.
7. A harmful rodent bait comprising at least a rodenticidally effective amount of a factor Xa inhibitor and a rodenticidally effective amount of an antagonist of the ADP receptor P2Y12, wherein the inhibitor of factor Xa is a compound of the following formula or a salt or hydrate thereof tolerable for a rodent:
wherein Q 3 is:
R 59 is H, F, CI or Br, R 60 , R 61 , R 62 and R 63 are each independently H, F, Cl, Br, Me, NO 2 , OH, OMe, NH 2 , NHAc, NHSO 2 Me, CH 2 OH and CH 2 NH 2 and R 64 is F, Cl, Br, Me, OH or OMe; and
wherein the antagonist of the ADP receptor P2Y12 is:
i) a compound of the following formula or a salt or a hydrate thereof tolerable for a rodent:
wherein R 94 is H, a halogen, hydroxy or C 1-6 alkyl, R 95 is H, a halogen, hydroxy, nitro, C 1-6 alkyl or C 1-6 alkoxy and R 96 is H or a halogen;
ii) a compound of the following formula or a salt or a hydrate thereof tolerable for a rodent:
wherein Y 1 is —OR 98 or —N(R 99 )R 100 , wherein R 99 and R 100 are each independently H, a halogen or a C 1-4 alkyl group and R 98 is H or C 1-4 alkyl and R 97 is H, a halogen or C 1-4 alkyl group; or
iii) a compound of the following formula or a salt or a hydrate thereof tolerable for a rodent:
wherein R 101 is H, OH, amino, C 1 to C 4 alkoxy, Aryl-C 1-4 -alkyloxy, C 1-18 alkanoyloxy, C 3-6 alkenoyloxy or arylcarbonyloxy, R 102 is C 1-10 alkanoyl, C 3-6 alkenoyl, C 4-8 cycloalkylcarbonyl including 3 to 7 ring atoms, substituted benzoyl or 5,6-dihydro-1,4,2-dioxazine-3-yl, Y 2 is NH, O or S, R 103 is H, a halogen, OH, amino, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio or a carboxy group.
8. The harmful rodent bait according to claim 7 , wherein the inhibitor of factor Xa comprises betrixaban and the antagonist of the ADP receptor P2Y12 comprises prasugrel.
9. The harmful rodent bait according to claim 8 , further comprising a rodent food, the rodent food comprising the betrixaban and the prasugrel.
10. The harmful rodent bait according to claim 8 , wherein the rodent bait comprises a combined concentration of the betrixaban and the prasugrel that is nonlethal to humans when ingested.