Substituted benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepines as GABA A GAMMA1 positive allosteric modulators
Compounds having the general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and X are as described herein, compositions including the compounds and methods of using the compounds.
1 . A method for treating a gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition in a subject, wherein the method comprises administering to the subject in need thereof an effective amount of a compound selected from the group consisting of:
or a pharmaceutically acceptable salt thereof;
wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is selected from the group consisting of anxiety, autism spectrum disorder, fragile-X disorder, generalized anxiety disorder, post-traumatic stress disorder, Rett syndrome, and social anxiety disorder.
2 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is anxiety.
3 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is selected from the group consisting of autism spectrum disorder, fragile-X disorder, post-traumatic stress disorder, and Rett syndrome.
4 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is autism spectrum disorder.
5 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is fragile-X disorder.
6 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is generalized anxiety disorder.
7 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is post-traumatic stress disorder.
8 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is Rett syndrome.
9 . The method of claim 1 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is social anxiety disorder.
10 . The method of claim 1 , wherein the compound is:
or a pharmaceutically acceptable salt thereof.
11 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is anxiety.
12 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is selected from the group consisting of autism spectrum disorder, fragile-X disorder, post-traumatic stress disorder, and Rett syndrome.
13 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is autism spectrum disorder.
14 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is fragile-X disorder.
15 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is generalized anxiety disorder.
16 . The method of claim 2 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is post-traumatic stress disorder.
17 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is Rett syndrome.
18 . The method of claim 10 , wherein the gamma-aminobutyric acid A gamma1 (GABA A γ1) receptor related disease or condition is social anxiety disorder.