AR059353A1 - DERIVATIVES OF OXAZOL AND TIAZOL. PHARMACEUTICAL COMPOSITIONS AND USES. - Google Patents

Abstract

Compounds in the treatment of diseases where an activation of M3 receptors is involved, such as respiratory tract diseases. Claim 1: A compound of formula (1); in which (i) R 1 is C 1-6 alkyl or hydrogen; and R2 is hydrogen or a group R7, -Z-Y-R7, -Z-NR9R10; -Z-CO-NR9R10, -Z-NR9-C (O) O-R7, or -Z-C (O) -R7; and R3 is a solitary pair or C1-6 alkyl, or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a solitary pair or a group -R7, -ZY-R7, -Z-NR9R10, -Z-CO-NR9R10, -Z-NR9-C (O) O-R7 or -ZC (O) -R7; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and said ring is 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 solitary pair or C1-6 alkyl; and R4 and R5 are independently selected from the group comprising aryl, fused heterocycloalkyl or aryl, heteroaryl, C1-6 alkyl, cycloalkyl; R6 is -OH, halogen, C1-6 alkyl, C1-6 alkoxy, hydroxy-C1-6 alkyl, nitrile, a CONR82 group or an H; A is O or S; X is alkynylene, alkenylene or alkynylene; R7 is a C1-6 alkyl, aryl, aryl fused cycloalkyl, aryl fused heterocycloalkyl, heteroaryl, aryl (C1-8 alkyl) -, heteroaryl (C1-8 alkyl) -, cycloalkyl or heterocycloalkyl group; R8 is C1-6 alkyl or a hydrogen atom; Z is a C1-16 alkylene, C2-16 alkenylene or C2-16 alkynylene group; And it is a hydrogen bond or atom; R9 and R10 are independently an atom of H, C1-6 alkyl, aryl, aryl fused heterocycloalkyl, aryl fused cycloalkyl, heteroaryl, aryl (C1-6 alkyl) or heteroaryl (C1-6 alkyl) -; or R9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 4-8 atoms, which optionally contains another nitrogen or oxygen atom; or its pharmaceutically acceptable salt, solvate, N-oxide or prodrug.