Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2005-12-08
2008-10-07
Coleman, Brenda L (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C540S555000
Reexamination Certificate
active
07432256
ABSTRACT:
The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula IwhereinR1is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′;R2is hydrogen or methyl;R3is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy;R′ is hydrogen or lower alkyl;R″ is hydrogen, hydroxy or lower alkyl;n is 0, 1 or 2;m is 1, 2 or 3; ando is 1 or 2;and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.
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Buettelmann Bernd
Knust Henner
Thomas Andrew William
Coleman Brenda L
Hoffman-La Roche Inc.
Johnston George W.
Prior Kimberly J.
Rocha-Tramaloni Patricia S.
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