| abstract |
A compound of the formula IR-X-W-Y-R1 and its enantiomers, diastereomers, pharmaceutically acceptable salts and N-oxides, wherein R is where Z is selected from N or CR7; Z1 is selected from N or CR7; W is selected from the group consisting of substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl, substituted or unsubstituted pyrimidinyl, substituted or unsubstituted pyridazinyl and substituted or unsubstituted pyrazinyl; X is O; Y is selected from -NRaC(=O)-(CR3R4)p- and -NRaC(=S)-(CR3R4) p-; Ra is selected from the group consisting of H, alkyl, heterocyclyl, aryl, alkenyl and alkynyl; R1 is selected from: where Rb is independently selected in each case from the group consisting of H, arylalkyl, 5-6-membered heterocyclyl- C1-3 alkyl. C1-6-alkyl, C6-10 aryl, C6-10 heteroaryl, C3-6 cycloalkyl, benzyl, C1-3 alkylaryl, C1-3alkylheteroaryl, methyl, ethyl, isopropyl, butyl, sec-butyl, isobutyl, methoxymethyl, -( C1-6)alkyl, 2-hydroxy 2-methylbutyl, 2-hydroxy-2-methylpropyl, 2-hydroxypropyl, 1-(1-hydroxycyclopropyl) methyl, ethylaminomethyl, piperidin-1-ylmethyl, pyrrolidin-1-ylmethyl, pyridyl, thienyl, phenyl, 1-naphthyl, nitrile, -C(=O)OR5a, -C(=O)NR5aRa and -C(=O)R5a; where Rc is one or more substituents selected from H, methyl, isopropyl, tert -butyl, bromo, fluoro and hydroxyl; each R 3 and R 4 are independently selected from the group consisting of H, alkyl, aryl, heterocyclyl, arylalkyl, cycloalkyl and cycloalkylalkyl; alternatively R3 and R4, together with the atom to which they are attached, form a 3-6-membered ring; R5 is independently selected in each case from the group consisting of H, alkyl, haloalkyl, heterocyclylalkyl, cycloalkylalkyl, aryl and heterocyclyl; R5a is independently selected in each case of H, alkyl, haloalkyl, arylalkyl aminoalkyl, heterocyclylalkyl, cycloalkylalkyl, aryl, heterocyclyl, alkenyl, alkynyl and cycloalkyl; R7 is selected from the group consisting of H, halo, cyano and alkyl; R8* is one or more substituents independently selected in each case from OC(=O)NRaR 5 , -NRaC(=O)OR 5 and -NRaC(=O)-R 5 ; p is 0, 1, 2 or 3; wherein each alkyl, aryl, heteroaryl, cycloalkyl, alkenyl, alkynyl, heterocyclyl and alkoxy group of any R, R1, R3, R4, R5, R7, R8* and Ra is optionally independently substituted with one or more groups independently selected in each case of halo, oxo, -NRaR5, -OR5a, -CO2R5, -C(=O)R5, (C1-C6)alkylamino, -NH-N=NH, (C1-C6)alkyl, (C1-C6)alkynyl , (C3-C6)cycloalkyl, (C1-C6)haloalkyl, di(C1-C6)alkylamino, (C1-C6)alkylamino-(C1-C6)alkyl, (C1-C6)hydroxyalkylamino, (C1-C6)alkylamino -(C1-C6)alkylamino, phenyl, heterocyclic, heteroaryl, -(CR3R4)palkyl-S(=O)-alkyl and -(CR3R4)palkyl-S(O)2-alkyl, wherein each alkenyl is specified herein in to the previous text - a linear or branched radical of two to twelve carbon atoms that has at least one carbon-carbon double bond and each alkynyl listed here in the previous text is a linear or branched radical of two to twelve carbon atoms that has at least one carbon-carbon triple bond. The application contains 17 more patent claims. |