| 摘要 |
The present invention is concerned with novel triazole compounds of formula (I);
wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments. |
| 主权项 |
1. A compound of formula (I) wherein A is —CH2—O—; wherein X is N, Y is CR9 and Z is CR10, or X is CH, Y is N and Z is CR10; or X is N, Y is CR9 and Z is N; or X is N, Y is N and Z is CR10; R1 and R2 are each independently alkyl, aryl optionally substituted by one halo or heteroaryl optionally substituted by one halo, wherein one of R1 or R2 is alkyl; R3 is halo, haloalkyl, —C(O)R4, or —C(O)NR5R6; R4 is alkoxy; R5 is alkyl, haloalkyl, hydroxyalkyl, halohydroxyalkyl, —(CH2)n-cycloalkyl, —(CH2)n-heterocycloalkyl, or —(CH2)n—NR7R8, wherein said heterocycloalkyl is optionally substituted by one or two alkyl or oxo; R6 is H, alkyl, or is alkylene together with R9 or R10; or R5 and R6 together with the nitrogen to which they are bound form a heterocycloalkyl optionally substituted by one or more oxo; R7 and R8 are each independently alkyl; R9 and R10 are each independently H, or one of R9 or R10 is alkylene together with R6; and n is an integer from 0 to 1;or a pharmaceutically acceptable salt or ester thereof.
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