http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2009508905-A

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filingDate 2006-09-07^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2009-03-05^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2009508905-A
titleOfInvention Isoxazolo derivatives as GABAAα5 inverse agonists
abstract The present invention provides an aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivative of formula (I) wherein R 1 is hydrogen, halogen, lower alkoxy, phenoxy, or benzyloxy; R 2 is a lower alkyl, (CH2) n-O- lower alkyl or phenyl,; R 3 is hydrogen or lower alkyl; R 4 / R 5 is, independently of each other, hydrogen, lower alkyl, halogen Substituted lower alkyl, lower alkynyl, or — (CHR) n -aryl (unsubstituted or substituted with halogen, lower alkyl, or lower alkoxy), — (CH 2 ) n -non-aromatic heterocycle ( Unsubstituted or substituted with one or two lower alkyl groups), — (CH 2 ) n -aromatic heterocycle, — (CR 2 ) n -cycloa Rualkyl (unsubstituted or substituted with 1 to 3 substituents selected from the group consisting of hydroxy or lower alkyl), — (CHR) n —O-lower alkyl, — (CR 2 ) n —OH, -(CHR) n -NR'R "or R 4 / R 5 together with the N atom to which they are attached, the ring: -8-azabicyclo [3.2.1] octane (Substituted with hydroxy), or 3,4-dihydro-1H-isoquinoline, or -nonaromatic heterocycle (unsubstituted or substituted with C (O) O-lower alkyl, lower alkyl, halogen) 1 or 2 substituents selected from the group consisting of lower alkyl, cycloalkyl, hydroxy, halogen, N (R) C (O) -lower alkyl, — (CH 2 ) n —O-lower alkyl, Or good R is hydrogen, hydroxy, or lower alkyl, where R is R 2 is the same or different; R ′ / R ″ are Independently hydrogen or lower alkyl; n is 0, 1, 2, 3, or 4; m is 1, 2, or 3] and pharmaceutically acceptable acid addition salts thereof . This class of compounds has shown high affinity and selectivity for the GABA Aα5 receptor binding site and has been found useful as a cognitive enhancer or in the treatment of cognitive disorders such as Alzheimer's disease.
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priorityDate 2005-09-19^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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