VAN GOOL MICHIEL LUC MARIA,VANHOOF GRETA CONSTANTIA PETER,CONDE-CEIDE SUSANA,MACDONALD GREGOR JAMES,BARTOLOME-NEBREDA JOSE MANUEL,PASTOR-FERNANDEZ JOAQUIN,MARTIN-MARTIN MARIA LUZ
申请号:
NZ60193111
公开号:
NZ601931A
申请日:
2011.03.08
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
601931 Disclosed is are imidazo[1,2-a]pyrazine compounds of formula (I), wherein: R1 is a saturated nitrogen containing heterocycle as defined herein which is attached to the imidazo[1,2-a]pyrazine through a nitrogen atom, or else R1 is selected from the group consisting of unsubstituted pyridinyl pyridinyl substituted with 1 or 2 substituents selected from the group consisting of halogen, alkyl, trifluoromethyl and alkyloxy and unsubstituted tetrahydropyranyl R2 is selected from the group consisting of hydrogen alkyl trifluoromethyl cycloalkyl alkyloxy and cyano R3 is selected from the group consisting of hydrogen alkyl cycloalkyl and alkyl substituted with 1,2 or 3 fluoro atoms Het is a 5- or 6- membered heterocyclic ring, selected from the group consisting of pyridinyl pyrimidinyl pyridazinyl pyrazinyl pyrrolyl oxazolyl thiazolyl imidazolyl pyrazolyl isothiazolyl isoxazolyl oxadiazolyl and triazolyl and wherein the remaining substituents are as defined within the specification. Representative compounds include 2-methyl-8-(4-morpholinyl)-3-[6-(tetrahydro-2H-pyran-4-yl)-3-pyridinyl]-imidazo[1,2-a]pyrazine, 3-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]-2-methyl-8-(4-morpholinyl)imidazo[1,2-a]pyrazine, 3-[6-(2-methoxyethoxy)-3-pyridinyl]-2-methyl-8-(4-morpholinyl)-imidazo[1,2-a]pyrazine, 3-(6-cyclopropyl-3-pyridinyl)-2-methyl-8-(4-morpholinyl)-imidazo[1,2-a]pyrazine, 3-[6-(ethoxymethyl)-3-pyridinyl]-2-methyl-8-(4-morpholinyl)imidazo[1,2-a ]pyrazine and 3-[2-(2-methoxyethyl)-5-pyrimidinyl]-2-methyl-8-(4-morpholinyl)imidazo[1,2-a]pyrazine. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above and a pharmaceutically acceptable carrier or excipient, for the treatment or the prevention of neurological, psychiatric or metabolic disorders and diseases, including schizophrenia, drug induced psychosis, obsessive-compulsive disorder, generalized anxiety disorder, Huntington&rsquos disease, dyskinesia, Parkinson&