Patent ID: 7148224
Filing Date: 2006-12-12
Classification: A61P,C07D

Abstract:
1. A pyrazinone derivative of the general formula (I): wherein Ar 1 is an aryl group or a 5- or 6-membered aromatic heterocycle selected from the group consisting of pyridyl, pyrimidinyl, pyrrolyl, pyrazolyl, thienyl and pyrazinyl, said aryl or heterocycle being fused to the adjacent pyrazinone ring at the 5th and 6th positions of the pyrazinone ring; X is CO; Y is N; Z is N; V is CH or N; R lower alkyl, lower alkenyl or lower alkynyl wherein said lower alkyl, lower alkenyl or lower alkynyl may have one or more substituents, which are the same or different, selected from <substituent group α>; or an aliphatic or aromatic ring substituent selected from the group consisting of C a 5- or 6-membered aromatic or aliphatic heterocycle containing at least one of N, S or O, selected from <substituent group β> wherein said aromatic or aliphatic heterocycle may have one or more substituents selected from the group consisting of a substituent selected from <substituent group α> and/or a lower alkyl group which may be substituted by one or more substituents, which are the same or different, selected from an aryl group and a substituent of <substituent group β>; or a lower alkyl substituted by said aromatic or aliphatic heterocycle; R R wherein R 1 and R 2 are each CH 2 , and m is an integer of 1 to 3 and wherein said saturated aliphatic heterocycle may have one or more substituents selected from the group consisting of a substituent selected from <substituent group α> and/or a substituent selected from lower alkyl, lower alkenyl, aryl and aralkyl, said substituents being optionally substituted by one or more substituents, which are the same or different, selected from <substituent group α>; R R a substituent selected from the group consisting of <substituent group α> and <substituent group γ>; or a group of the formula: Y W is a single bond, oxygen atom, sulfur atom, sulfinyl, sulfonyl, NR Y an aliphatic or aromatic ring substituent selected from the group consisting of C a 5- to 6-membered aromatic or aliphatic heterocycle containing at least one of N, S and O, selected from <substituent group β> wherein said aromatic or aliphatic heterocycle may be substituted with lower alkyl; lower alkyl which is substituted by C <substituent group α>, <substituent group β>><substituent group γ>, <substituent group δ>, and <substituent group ε> each have the meaning as shown below: <substituent group α>: hydroxy, cyano, halogen atom, nitro, carboxyl, carbamoyl, formyl, lower alkanoyl, lower alkoxy, lower alkoxycarbonyl, lower alkylcarbonyloxy, lower alkylcarbamoyl, di-lower alkylcarbamoyl, carbamoyloxy, lower alkylcarbamoyloxy, di-lower alkylcarbamoyloxy, amino, lower alkylamino, di-lower alkylamino, tri-lower alkylammonio, lower alkanoylamino, aroylamino, lower alkanoylamidino, lower alkyl-sulfonylamino, hydroxyimino, lower alkoxyimino, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl and sulfamoyl; <substituent group β>: pyrrolyl, pyrrolidyl, thienyl, furyl, thiazolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, piperidyl, piperazinyl and morpholinyl; <substituent group γ>: hydroxy-lower alkyl, cyano-lower alkyl, halo-lower alkyl, carboxy-lower alkyl, carbamoyl-lower alkyl, amino-lower alkyl, lower alkyl-amino-lower alkyl, di(lower alkyl)amino-lower alkyl, and tri(lower alkyl)ammonio-lower alkyl; <substituent group δ>: imidazolyl, isoxazolyl, isoquinolyl, isoindolyl, indazolyl, indolyl, indoilidinyl, isothiazolyl, ethylenedioxyphenyl, oxazolyl, pyridyl, pyrazyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyrazolyl, quinoxalinyl, quinolyl, dihydroisoindolyl, dihydroindolyl, thionaphthenyl, naphthyridinyl, phenazinyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzotriazolyl, benzofuranyl, thiazolyl, thiadiazolyl, thienyl, pyrrolyl, furyl, furazanyl, triazolyl and methylenedioxyphenyl; and <substituent group ε>: imidazolidinyl, tetrahydrofuranyl, piperazinyl, piperidyl, pyrrolidyl, pyrrolinyl, morpholino, tetrahydroquinolyl and tetrahydroisoquinolyl, or a pharmaceutically acceptable salt or ester thereof.