220269-80-7Relevant academic research and scientific papers
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA α5 inverse agonists for the treatment of cognitive dysfunction
Knust, Henner,Achermann, Guido,Ballard, Theresa,Buettelmann, Bernd,Gasser, Rodolfo,Fischer, Holger,Hernandez, Maria-Clemencia,Knoflach, Frederic,Koblet, Andreas,Stadler, Heinz,Thomas, Andrew W.,Trube, Gerhard,Waldmeier, Pius
, p. 5940 - 5944 (2009)
Lead optimisation of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine class led to the identification of two clinical leads [RO4882224 (11) and RO4938581 (44)] functioning as novel potent and selective GABAA α5 inverse agonists. The unique pharmacological profiles and optimal pharmacokinetic profiles resulted in in vivo activity in selected cognition models.
[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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Page/Page column 147, (2021/02/19)
The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
Substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
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Page/Page column 9, (2008/06/13)
The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower
Halogen substituted imidazol[1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives
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Page/Page column 12, (2008/06/13)
The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to pharmaceutica
Substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives
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Page/Page column 18, (2010/10/20)
The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted
Indole compounds as COX-2 inhibitors
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, (2008/06/13)
This invention provides a compound of the following formula: and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4alkylidene; Q is C1-6alkyl, C3-7cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1is hydrogen, C1-6alkyl or the like; R2is hydrogen, C1-4alkyl, C(O)R5wherein R5is C1-22alkyl or C2-22alkenyl, halosubstituted C1-8alkyl, halosubstituted C2-8alkenyl, —Y—C3-7cycloalkyl, —Y—C3-7cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4alkyl, hydroxy, C1-4alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula —Y—Q is not methyl or ethyl when X is hydrogen; L is oxygen; R1is hydrogen; and R2is acetyl. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.
