MY148341A - Azole derivatives and their uses - Google Patents

Abstract

COMPOUNDS OF FORMULA (I) ARE USEFUL IN THE TREATMENT OF DISEASES WHERE ENHANCED M3 RECEPTOR ACTIVATION IS IMPLICATED, SUCH AS RESPIRITORYTRACT DISEASES: WHEREIN (I) R1 IS C1-C6-ALKYL OR HYDROGEN; AND R2 IS HYDROGEN OR A GROUP -R7, -Z-Y-R7 ,-Z-NR9R10; -Z-CO-NR9 R10 -Z-NR9-C(O)O-R7, OR -Z-C(O)-R7;AND R3 IS A LONE PAIR, OR C1-C6-ALKYL; OR (II) R1 AND R3 TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED FORM A HETEROCYCLOALKYL RING, AND R 2 IS A LONE PAIR OR A GROUP ?R7, -Z-Y-R7, -Z-NR9R10,-Z-CO-NR9R10, -Z-NR9-C(O)O-R7; OR; -Z-C(O)-R7; OR (III) R1 AND R2 TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED FORM A HETEROCYCLOALKYL RING, SAID RING BEING SUBSTITUTED BY A GROUP -Y-R7 , -Z-Y-R7 , -Z-NR9R10; -Z-CO-NR9R10; -Z-NR9-C(O)O-R7; OR ; -Z-C(O)-R7; AND R3 IS A LONE PAIR, OR C1-C6-ALKYL; R4 AND R5 ARE INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF ARYL, ARYL-FUSED-HETEROCYCLOALKYL, HETEROARYL, C 1- C6-ALKYL, CYCLOALKYL; R6 IS -OH, C1-C6-ALKYL, C,-C6-ALKOXY, HYDROXY-C1-C6-ALKYL, NITRILE, A GROUP CONR82 OR A HYDROGEN ATOM; A IS AN OXYGEN OR A SULFUR ATOM; X IS AN ALKYLENE, ALKENYLENE OR ALKYNYLENE GROUP; R7 IS AN C1-C6-ALKYL, ARYL, ARYL-FUSED-CYCLOALKYL, ARYL�FUSED-HETEROCYCLOALKYL, HETEROARYL, ARYL(C1-C8-ALKYL)-, HETEROARYL(C1-C8-ALKY)-, CYCLOALKYL OR HETEROCYCLOALKYL GROUP; R8 IS C1-C6-ALKYL OR A HYDROGEN ATOM; Z IS A C 1- C16ALKYLENE, C2-C16-ALKENYLENE OR C2-C16-ALKYNYLENE GROUP; Y IS A BOND OR OXYGEN ATOM; R9 AND R10 ARE INDEPENDENTLY A HYDROGEN ATOM, C1-C6-ALKYL, ARYL, ARYL-FUSED-HETEROCYCLOALKYL, ARYL-FUSED-CYCLOALKYL, HETEROARYL, ARYL(C1-C6-ALKYL)-, OR HETEROARYL(C1- C6-ALKYL)- GROUP; OR R 9 AND R10 TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED FORM A HETEROCYCLIC RING OF 4-8 ATOMS, OPTIONALLY CONTAINING A FURTHER NITROGEN OR OXYGEN ATOM.