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Serving leading biopharmaceutical companies globally:

US Army
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Generated: November 22, 2017

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Claims for Patent: 4,001,411

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Claims for Patent: 4,001,411

Title: 2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the preparation thereof
Abstract:2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.
Inventor(s): Seubert; Jurgen (Darmstadt, DT), Thomas; Herbert (Wuppertal, DT), Andrews; Peter (Wuppertal, DT)
Assignee: Merck Patent Gesellschaft mit beschrankter Haftung (Darmstadt, DT)
Application Number:05/533,467
Patent Claims: 1. A compound of the formula ##STR5## wherein R is (a) cycloalkyl of 3-7 carbon atoms, or a corresponding group mono-substituted by fluorine, chlorine, nitro, hydroxy, amino, formylamino, acetylamino, pentanoylamino, hexanoylamino, octanoylamino, oleoylamino, methoxyacetylamino, methylamino, dimethylamino or allylamino;

b. alkyl of up to 7 carbon atoms or a corresponding group substituted by methoxy or ethoxy; (c) oxocyclobutyl, oxocyclopentyl or oxocyclohexyl; or (d) cyclohexenyl; and the physiologically acceptable acid addition salts thereof.

2. A compound of claim 1 wherein R is alkyl of 1-6 carbon atoms.

3. A compound of claim 1 wherein R is cycloalkyl of 3-7 carbon atoms.

4. a compound of claim 1, 2-cyclohexylcarbonyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoqu inoline.

5. A compound of claim 1, 2-propionyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.

6. A compound of claim 1, 2-isobutyryl-4-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.

7. A compound of claim 1, 2-cyclopropylcarbonyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoq uinoline.

8. A compound of claim 1, 2-cyclobutylcarbonyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoqu inoline.

9. A compound of claim 1, 2-cyclopentylcarbonyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoq uinoline.

10. A compound of claim 1, 2-(3-cyclohexenylcarbonyl)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a ]isoquinoline.

11. A compound of claim 1, 2-(4-oxocyclohexylcarbonyl)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1- a]isoquinoline.

12. A compound of claim 1, 2-(4-hydroxycyclohexylcarbonyl)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazinl[ 2,1-a]isoquinoline.

13. A compound of claim 1, 2-cycloheptylcarbonyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoq uinoline.

14. A compound of claim 1, 2-acetyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.

15. A pharmaceutical composition consisting essentially of an anthelmintically effective amount per unit dosage of a compound of claim 1 in admixture with a pharmaceutically acceptable carrier.

16. A method of treating cestode and trematode infestations which comprises administering to an animal infested with cestodes or trematodes an anthelmintically effective amount of a compound of claim 1.
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Serving leading biopharmaceutical companies globally:

Fish and Richardson
Argus Health
Express Scripts
Cantor Fitzgerald
Boehringer Ingelheim
Farmers Insurance
Daiichi Sankyo

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