Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsHenner Knust, Heinz Stadler, Andrew William Thomas
Life of this patent
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Abstract
The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.
Claims16
A method of treating Alzheimer's disease comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I
- wherein
- R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R;
- R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy;
- and
- R3 is hydrogen, lower alkyl, lower alkoxy, or —NH2R;
- or a pharmaceutically acceptable acid addition salt thereof.
The method of claim 12, wherein the compound is selected from the group consisting of
- 3-bromo-9H-imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine-10-carbaldehyde and
- 3-chloro-9H-imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine-10-carbaldehyde.
A compound of formula I-A
- wherein
- R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R;
- or —NHSO2R;
- R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy;
- and
- R3 is lower alkyl;
- or a pharmaceutically acceptable acid addition salt thereof.
A composition comprising a therapeutically effective amount of compound of formula I-A
- wherein
- R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R;
- R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy;
- and
- R3 is lower alkyl;
- or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.