abstract |
Claim 1: A compound of the formula (1) or a pharmaceutically acceptable salt or a pharmaceutically acceptable and dissociable ester, or an acid addition salt thereof: wherein: R 1 is selected from: halogen, cyano, hydroxyl, mercapto, (aryl, aryl-C 1-6 alkyl, C 2-6 arylalkyl, monocyclic heteroaryl, C 1-6 heteroaryl-aryl, C 2-6 hetero-aryl-alkenyl, aryl-amino, hetero-aryl-amino, aryloxy, hetero-aryloxy, C1-6 alkyl, C3-7 cycloalkyl, C1-6 alkoxy, C1-6-amino alkyl, C2-6 alkenyl, C2-6 alkynyl, hetero-cycloalkyl, hetero-cycloalkyl-C1-6 alkyl , optionally substituted heterocycloalkyl-alkenyl, hetero-cycloalkylamino, hetero-cycloalkyloxy, amino), wherein the optional substituents on R1 are selected from halogen, cyano, hydroxyl, mercapto, sulfonyl, amino, C1-6 alkyl -amino, di- C 1-6 alkyl-amino, aryl, monocyclic hetero-aryl, C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 heterocycloalkyl , carboxyl, carbonyl-C1-7 alkyl, each of which, where applicable, may be optionally substituted by C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl, C3-7 heterocycloalkyl, C1- alkoxy 6, C 1-6 alkenyl, C 1-6 alkynyl, halogen, hydroxyl, mercapto, cyano, amino, C 3-7 heterocycloalkylcarbonyl; each of which, where applicable, may optionally be substituted by C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl, C 3-7 heterocycloalkyl, C 1-6 alkoxy, C 1-6 alkenyl, C 1-6 alkynyl 6, halogen, hydroxy, mercapto, cyano, amino, C 3-7 heterocycloalkylcarbonyl; X is O, S or NOH; R2 represents the group -C (A) (Q) -Y, where Q is H or C1-6 alkyl; A is H or C1-6 alkyl; Y is amino, amino-oxyl, hydroxyl, C1-6 alkoxy, C1-6-alkyl or hydrazine, which in each case may be optionally substituted, the optional substituents on Y being selected from C1-6 alkyl, halogen, hydroxyl ; R3 is -OH, -OR4 or -NHR4, where R4 is H or C1-6 alkyl; or R2 and R3 join to collectively denote the group -R2-R3- to form a ring of 5, 6, or 7 members, the collective group -R2-R3- being selected from: - (CH2) nNR5-, - CH2ONH-, - (CH2) n-, -CH = N-NH-, - (CH2) n-NR6-NH- where R5 is selected from H or (C1-6 alkyl, aryl-C1-6 alkyl , hetero-aryl-C 1-6 alkyl, C 3-7 cycloalkyl-C 1-6 alkyl, optionally substituted C 3-7 heterocycloalkyl); the optional substituents on R5 being one or more groups independently selected from halogen, C1-6 alkyl, C1-6 alkoxy, amino, trifluoro-methyl, sulfonyl, hydroxyl; and R6 is selected from H or optionally substituted C1-6 alkyl, carbonyl, sulfonyl; the optional substituents on R 6 being one or more groups independently selected from C 1-6 alkyl, lower alkoxy, amino, alkyl amino, hydroxyl; where n is 1, 2 or 3; and R7 is selected from H and optionally substituted C1-6 alkyl, the optional substituents being selected from amino, hydroxyl, halogen, and carboxyl. |