Patent ID: 6509328
Filing Date: 2003-01-21
Classification: A61P,C07D

Abstract:
A compound of the formula: whereinX is an ethynediyl group; R1 is hydrogen,unsubstituted lower alkyl or lower alkyl substituted with a substitutent selected from the group consisting of hydroxy and halo-lower alkyl, unsubstituted lower cycloalkyl lower cycloalkyl substituted with a substitutent selected from the group consisting of hydroxy, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, and halogen; unsubstituted lower cycloalkenyl, lower cycloalkenyl substituted with a substitutent selected from the group consisting of lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, halogen, and oxo; lower alkenyl; unsubstituted phenyl, phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy, and halo; an unsusbstituted 5 or 6 membered heterocyclic ring, a 5 or 6 membered heterocyclic ringsubstituted with a substitutent selected from the group consisting of lower alkyl, halogen, oxo, benzyloxy, benzoyl, methanesulfonyl, benzenesulfonyl, acetyl, pivaloyl, tert, butoxycarbonyl,; tert, butylcarbonyl, and benzofuranyl; and R3 is selected from the group consisting of unsubstituted phenyl, unsubstituted pyridine, unsubstituted thiophenyl, unsubstituted thiazolyl, substituted phenyl, substituted pyridine, substituted thiophenyl and substituted thiazolyl, said substituted phenyl, said substituted pyridine, said substituted thiophenyl and said unsubstituted thiazoyl substituted by a substitutent selected from the group consisting of halogen, cyano, nitro, azido, hydroxy, carboxy, morpholine-4-carbonyl, carbamoyl, thiocarbamoyl, N-hydroxycarbamoyl, trimethylsilyl-ethynyl, unsubstituted lower alkyl, lower alkynyl, lower alkoxy, halo-lower alkyl, 4-lower alkyl-piperazine-1-carbonyl, lower alkylaminocarbonyl, substituted lower alkyl, lower alkynyl, lower alkoxy, halo-lower alkyl, 4-lower alkyl-piperazine-1-carbonyl, lower alkylaminocarbonyl, substituted a substitutent selected from the group consisting of amino, lower alkylamino, acylamino, oxo, hydroxy; lower alkoxy, lower alkylthio, unsubstituted carboxy, esterified or amidated carboxy, an unsubstituted 5-membered aromatic heterocycle, a 5-membered aromatic heterocycle substituted by a substituent selected from the group consisting of amino, lower alkylamino, acylamino, oxo, hydroxy, lower alkoxy, lower alkylthio, carboxy, carboxy esterified with lower alkyl, carboxy amidated with lower alkylamino which is eventually substituted by hydroxy, lower alkyl, lower alkylsubstituted by a substituent selected from the group consisting of halogen, hydroxy, amino, lower alkylamino, acylamino, amidino, amidino substituted by a substituent selected from the group consisting of lower alkyl, â€”C(NRRâ€²)&boxH;NRâ€³ (where R, Râ€² and Râ€³ are hydrogen or lower alkyl), hydroxy, lower alkoxy, lower alkylthio, acyloxy, lower alkylsulfinyl, lower alkylsulfonyl, lower alkoxy-lower alkylsulfanyl, lower alkylsulfanyl, cycloalkylsulfinyl, cycloalkylsulfonyl, hydroxyimino, lower alkoxyimino, lower alkoximino which is esterified or amidated, lower alkenyl, oxo, cyano, carbamoyloxy, sulfamoyl and sulfamoyl substituted by lower alkyl, or a pharmaceutically acceptable acid addition salt thereof.