Patent ID: 6800621
Filing Date: 2004-10-05
Classification: A61P,C07D

Abstract:
A compound of formula(I): wherein,X is N; R1 is amino or protected amino; R2 is hydrogen, lower alkyl optionally substituted with one or more groups selected from the group consisting of halogen, hydroxy, carboxy, cyano, amino, carbamoyloxy, sulfamoyl, lower alkoxycarbonyl and lower alkylthio or cycloalkyl optionally substituted with one or more groups selected from the group consisting of halogen, hydroxy, carboxy, cyano, amino, carbamoyloxy, sulfamoyl, lower alkoxycarbonyl and lower alkylthio; R3 is hydrogen; R4 is lower alkyl substituted with one or more groups selected from the group consisting of carbamoyl optionally substituted with methyl, ethyl, propyl or â€”(CH2)3CH(NH2)CONH2, halogen, amino optionally substituted with lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy carbonyl, hydroxyl(lower) alkyl, sulfonic acid-oxy(lower)alkyl or amino(lower) alkyl; lower alkenyl amino, â€”CO(CH2)nCH(NH2)CONH2 (n=1 to 3), lower alkoxy, lower alkoxycarbonyl and a N-containing heterocyclic group, lower alkenyl optionally substituted with one or more groups selected from the group consisting of hydroxy, optionally substituted carbamoyl, halogen, â€”CO(CH2)nCH(NH2)CONH2 (n1 to 3), amino optionally substituted with lower alkyl, lower alkenyl, cycloalkyl, lower alkoxycarbonyl, hydroxy(lower)alkyl, sulfonic acid-oxy(lower) alkyl or amino(lower) alkyl, lower alkoxy, lower alkoxycarbonyl and a N-containing heterocyclic group, lower alkoxy optionally substituted with one or more groups selected from the group consisting of hydroxy, optionally substituted carbamoyl, halogen, â€”CO(CH2)nCH(NH2)CONH2 (n=1 to 3), amino optionally substituted with lower alkyl, lower alkenyl, cycloalkyl, lower alkoxycarbonyl, hydroxy(lower)alkyl, sulfonic acid-oxy(lower) alkyl or amino(lower) alkyl, lower alkoxy, lower alkoxycarbonyl and a N-containing heterocyclic group, cycloalkyl optionally substituted with one or more groups selected from the group consisting of hydroxy, optionally substituted carbamoyl, halogen, â€”CO(CH2)nCH(NH2)CONH2 (n=l to 3), amino optionally substituted with lower alkyl, lower alkenyl, cycloalkyl, lower alkoxycarbonyl, hydroxy(lower)alkyl, sulfonic acid-oxy(lower) alkyl or amino(lower) alkyl, lower alkoxy, lower alkoxycarbonyl and a N-containing heterocyclic group, cycloalkyl(lower)alkyl optionally substituted with one or more groups selected from the group consisting of hydroxy, optionally substituted carbamoyl, halogen, â€”CO(CH2)nCH(NH2)CONH2 (n=1 to 3), amino optionally substituted with lower alkyl, lower alkenyl, cycloalkyl, lower alkoxycarbonyl, hydroxy(lower)alkyl, sulfonic acid-oxy(lower) alkyl or amino(lower) alkyl, lower alkoxy, lower alkoxycarbonyl and a N-containing heterocyclic group, or a N-containing heterocyclic group, wherein said N-containing heterocyclic group is selected from the group consisting of azetidinyl, pyrrolidinyl, piperidinyl, imidazolydinyl, pyrazolidinyl, piperizinyl, thiazolidinyl, oxazolidinyl, morpholinyl, thiomorholinyl, thiazolinyl, oxazolinyl, imidazolinyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isooxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, imidazolyl, triazolyl, and tetrazolyl, and is optionally substituted with a group selected from the group consisting of halogen, hydroxy, hydroxy(lower) alkyl, carbamoyl, lower alkyl, lower alkoxy, imino(lower) alkyl, halogenated lower alkyl, optionally esterified carboxy, cyano, nitro, lower alkylthio, lower alkoxyalkoxy, a lower alkoxycarbonyl and acylamino; R5 is hydrogen; or R4 and R5 taken together may form â€”(CH2)3â€”N(Me)-; and a wavy line means syn- or anti-isomerism or a mixture thereof, an ester, a pharmaceutically acceptable salt or a solvate thereof.