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filingDate 2008-07-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3f997013e9ef62c37a1abd4fa8bf7ea4
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publicationDate 2010-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2009044018-A9
titleOfInvention Derivatives of 1-oxo-1,2-dihydroisoquinoline-5-carboxamides and of 4-oxo-3,4-dihydroquinazoline-8-carboxamides, preparation thereof and application thereof in therapeutics
abstract The invention relates to the derivatives of 1-oxo-1,2-dihydro­isoquinoline-5-carboxamides and of 4-oxo-3,4-dihydroquinazoline-8-carboxamides, of general formula (I) in which: R1 represents a hydrogen atom, a (C 1 -C 10 )alkyl, (C 3 -C 7 )cycloalkyl, (CH 2 ) n -(C 1 -C 6 )alkenyl, (CH 2 ) n -(C 1 -C 6 )alkynyl or (C 1 -C 6 )alkyl-Z-(C 1 -C 6 )alkyl group in which Z represents a heteroatom chosen from O, N and S(O) m , or else R1 represents a COOR or S(O) m R group, an aryl or an aralkyl, the (C 1 -C 10 )alkyl, (C 3 -C 7 )cycloalkyl, (CH 2 ) n -(C 1 -C 6 )alkenyl, (CH 2 ) n -(C 1 -C 6 )alkynyl, (C 1 -C 6 )alkyl-Z-(C 1 -C 6 )alkyl, aryl or aralkyl groups; R2 represents one or more groups chosen from a hydrogen atom, a halogen atom, a (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, (C 1 -C 6 )alkenyl, (C 1 -C 6 )alkynyl or (C 1 -C 6 )alkyl-Z-(C 1 -C 6 )alkyl group, in which Z represents a heteroatom chosen from O, N and S(O) m , or else R2 represents a halo(C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkoxy, hydroxy, (C 1 -C 6 )alkoxy, nitro, cyano or amino group, an NR7R8, COOR, CONR7R8, OCO(C 1 -C 6 )alkyl or S(O) m -NR7R8 group, or an aryl group; R4 and R5 represent, independently of one another, a hydrogen atom, or else R4 and R5 form, with the carbon atom which bears them, a saturated ring containing from 3 to 6 carbon atoms and optionally containing from 0 to 1 heteroatoms chosen from O, N or S; R6 represents a group chosen from a hydrogen atom, a halogen atom, a (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl or (C 3 -C 7 )cycloalkyl(C 1 -C 6 )alkyl group, a halo(C 1 -C 6 )alkyl, nitro or amino group, an NR7R8 or COOR group, an NR7(SO 2 )R8 or CONR7R8 group, or an aryl group; X represents a carbon atom or a nitrogen atom; m represents an integer between 0 and 2 and n represents an integer between 1 and 6. The invention also relates to the method of producing said derivatives and the application thereof in therapeutics as β-secretase for treating neurodegenerative disorders such as Alzheimer's disease.
priorityDate 2007-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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