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grantDate 2009-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_350caa1bbcab5be3a536c30cc775e23d
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publicationDate 2009-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2315546-T3
titleOfInvention PHOSPHODESTERASE INHIBITORS OF CYCLIC NUCLEOTIDES, WHICH PRESENT A BENZODIAZEPIN STRUCTURE, AND ITS USE IN THERAPY.
abstract Compound of general formula (I): (See formula) in which: * Z represents an oxygen, sulfur atom or an NR2 radical, * R1 is a hydrogen atom or an unsubstituted (C1-C6) alkyl group, * R2 is a hydrogen atom, a (C1-C6) alkyl group, an aryl (C6-C18) group or a (C1-C6) -aryl (C6-C18) or aryl (C6-C18) -alkyl group (C1-C4), where R1 and R2 may eventually form together a linear or branched hydrocarbon chain having from 2 to 6 carbon atoms, possibly comprising another or other double bonds and / or eventually interrupted by an oxygen atom, sulfur or nitrogen, * R3 and R3 0, identical or different, represent the hydrogen atom, a (C1-C12) alkyl, cycloalkyl (C3-C6), aryl (C6-C18), aryl (C6-C18) - group (C1-C4) alkyl, (C1-C12) alkyl-(C6-C18) aryl or a (C5-C18) heterocycle, aromatic or not, comprising 1 to 3 heteroatoms, a NO2, CF3, CN group, NR''R ", SR '', OR '', COOR '', CONR''R" or NHCOR''R ", where R '' and R ", independently of each other, selected from the hydrogen atom, a (C1-C6) alkyl, cycloalkyl (C3-C6), aryl (C6-C12), and a heterocycle at (C5-C12) group ), aromatic or not, comprising 1 to 3 heteroatoms; * R5 represents a phenyl group at least substituted in position 3, a naphthyl group, a (C5-C18) heterocycle, aromatic or not, comprising 1 to 3 heteroatoms, selected from the radical pyridyl, isoquinolyl, quinolyl and piperazinyl, with the proviso that when R5 is a naphthyl group substituted in position 6, the latter is then not linked to the rest of the molecule in position 2, or when R5 is a pyridyl group, then it is not linked to the rest of the molecule in position 4, or when R5 is a 1,2,3,4-isoquinolyl tetrahydro group, then it is not linked to the rest of the molecule in position 2, when R5 represents a phenyl group at least substituted in position 3, said being substituent selected from: an alkyl, halogenoalkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl, heterocycle, heterocycloalkyl radical, an OH group, = O, NO2, NH2, CN, CF3, COR '', COOR '', alkoxy ( C1-C6), (di) (C1-C6) alkyl-amino, NHCOR '', CO NR''R ", in which R '' and R" are as defined above, CHO, CONH2, phenyl optionally substituted, in particular by an acetyl radical, by a halogen atom (Cl), by a group CONH2 or by a CN group, prop-1-inyl optionally substituted, in particular by a benzyloxy or tert-butyl carbamate, hex-1-inyl optionally substituted, in particular by a CN or NH2 group, optionally substituted pentyl, in particular by a CONH2, hexyl, piperidinyl group optionally substituted, in particular by a prop-1-inyl, benzylaminomethyl, acetamide (CH3CONH), aminomethyl, NH2CS-, 4-phenyl-1,3-thiazol-2-yl, -CONHBenzyl radical , -COOEthyl, -CONHiPropyl, -CONH- (CH2) n-CONH2 (representing n an integer from 1 to 6), -CONR''R ", being R '' and R", identical or different, representing a radical C1-C6 alkyl or a hydrogen atom, - (4-benzylpiperazin-1-yl) carbonyl, -CONH- (CH2) n-phenyl (representing n an integer from 1 to 6), imidazolyl, piperazi Nyl optionally substituted, in particular by a phenyl radical, * R7 and R8, independently of one another, represent an OR10 group, in which R10 is a (C1-C6) alkyl group, preferably an ethyl or methyl group, advantageously methyl, or R7 and R8 both represent an ethoxy or methoxy group, advantageously methoxy, or one represents a hydrogen atom and the other an ethoxy or methoxy group, advantageously methoxy, * R6 is selected from the hydrogen atom, a halogen atom, an alkyl, cycloalkyl, alkenyl, alkynyl, an aryl, aralkyl, heterocycle, heterocycloalkyl and an OR10 group radical, R10 being as defined above, the alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl, phenyl group being, naphthyl, heterocycle, heterocycloalkyl or the above-defined hydrocarbon chain eventually substituted by one or more substituents, identical or different, preferably selected from a hal atom Oxygen, an alkyl, halogenoalkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl, heterocycle, heterocycloalkyl radical, an OH group, = O, NO2, NH2, CN, CF3, COR '', COOR '', (C1-C6) alkoxy ), (di) (C1-C6) alkyl-amino, NHCOR "and CONR" R ", in which R" and R "are as defined above, and the substituents may also be substituted, * R9 it is a hydrogen atom, and the salts of the compounds of formula (I), with the exception of the compounds of formula (I), in which ...
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Total number of triples: 872.