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Serving 500+ biopharmaceutical companies globally:

Express Scripts
Covington
Johnson and Johnson
US Army
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Farmers Insurance
Medtronic
UBS
Chubb
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Generated: September 26, 2017

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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 500+ biopharmaceutical companies globally:

Dow
Merck
Covington
Julphar
Queensland Health
Cipla
Fish and Richardson
Medtronic
Teva
Fuji

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

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