Patent TW-201018679-A (TW)
Title: New 2-amidothiadiazole derivatives
Inventor: GRIMA POVEDA PEDRO MANUEL
IPC: A61P37/00
Filed: 2009-10-12
Abstract: New 2-amidothiadiazole derivatives having the chemical structure of formula (I) or pharmaceutically acceptable salts or N-oxides thereof wherein R1 represents: an 8 to 10 membered bicyclic N-containing heteroaryl group optionally substituted by one or more substitutents selected from halogen atoms, hydroxycarbonyl groups, C1-4 alkyl groups, C1-4 haloaklyl groups, C1-4 alkoxy groups and C3-4 cycloalkyl groups; a pyridyl group substituted with one or more substituents selected from halogen atoms, hydroxy groups, hydroxycarbonyl groups, C1-4 alkyl groups, C1-4 haloaklyl groups, C1-4 alkoxy groups, C3-4 cycloalkyl groups and, -NR'R'' groups, wherein R' represents a hydrogen atom or a C1-4 alkyl group and R'' represents a hydrogen atom or a C1-4 alkyl group optionally substituted by a hydroxy group; a pyridone group substituted with one or more substituents selected from halogen atoms, C1-4 alkyl groups and C1-4 haloaklyl groups; or a group of formula: wherein: Ra represents a hydrogen atom or a C1-4 alkyl group, Rb represents a hydrogen atom, halogen atom or C1-4 alkyl group, Rd represents a hydrogen atom, a C1-4 alkyl group or a C3-4 cycloalkyl group, Rc represents a hydroxy group; a C1-4 alkoxy group which is optionally substituted with one or more substituents selected from hydroxy groups, C1-3 alkoxy groups, hydroxycarbonyl groups, C1-4 alkoxycarbonyl groups and NHR4 groups, wherein R4 represents a hydrogen atom; or Rc is a C2-4 acyl group or a C1-4 alkyl group optionally substituted by a hydroxycarbonyl group, or Rc represents -(CH2)(0-4)-L-R5 wherein L represents -C(O)O-, -C(O)NH-, -S(O)2NH-, -NH-, -CONHS(O)2- or a group of formula: wherein n and m independently are integer from 1 to 2, and R5 represents a hydrogen atom or a C1-4 alkyl group optionally substituted by a hydroxycarbonyl group; R2 represents: a monocyclic or bicyclic C5-10 aryl group optionally substituted with one or more substituents selected from halogen atoms, C1-4 alkyl groups, C1-4 alkoxy groups and phenyl groups, wherein the alkyl group is optionally substituted by one or more halogen atoms, a monocyclic or bicyclic 5-10 membered heteroaryl group comprising one or more heteroatoms selected from N, S and O optionally substituted with one or more substituents selected from halogen atoms, C1-4 alkyl and C1-4 alkoxy groups, wherein the C1-4 alkyl group is optionally substituted by one or more halogen atoms, a dihydrobenzodioxine group or a benzyl group which is optionally substituted with one or more substituents selected from halogen atoms, and R3 represents: a linear or branched C1-6 alkyl, C3-6 cycloalkyl-C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, di-alkylamino-C1-4alkyl group, or phenyl-C1-4alkyl group; With the proviso that when Rc represents a methoxy or ethoxy group, then one of Rb or Rd can not be a hydrogen atom; With the additional proviso that the compound of formula (I) is not N-methyl-N-(5-(6-methylpyridin-3-yl)-1, 3,4-thiadiazol-2-yl) nicotinamide, nor N-methyl-N-(5-(6-methylpyridin-3-yl)-1, 3,4-thiadiazol-2-yl)isonicotinamide.