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filingDate 1999-07-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d361383c0cfb3f7d0753d17dc2626765
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publicationDate 2001-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber BR-9911175-A
titleOfInvention Phthalazine derivatives, pharmaceutical compositions containing them and use as phosphodiesterase 4 inhibitors
abstract <B> PHTHALAZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND USE AS PHOSPHODIESTERASE 4 INHIBITORS Compounds of formula (I), where - - - - is a single or double bond; Z is NH, methylene, an alkylene chain (C ~ 2 ~ -C ~ 6 ~) optionally branched and / or unsaturated and / or interrupted by a cycloalkyl residue (C ~ 5 ~ -C ~ 7 ~); A is phenyl or heterocycle optionally substituted by one or more substitutes selected from oxo, nitro, carboxy groups and halogen atoms or a COR ~ 4 ~ group where R ~ 4 ~ is hydroxy, alkoxy (C ~ 1 ~ -C ~ 6 ~ ), amino optionally substituted by one or two alkyl groups (C ~ 1 ~ -C ~ 6 ~) or by hydroxy; R is alkyl (C ~ 1 ~ -C ~ 6 ~) or polyfluoro alkyl group (C ~ 1 ~ -C ~ 6 ~); R ~ 1 ~ is absent when - - - - is a double bond or, when - - - - is a single bond, it is a) hydrogen; b) alkyl (C ~ 1 ~ -C ~ 6 ~) optionally substituted by aryl, heterocycle or a COR ~ 5 ~ group, where R ~ 5 ~ is hydroxy, alkoxy (C ~ 1 ~ -C ~ 4 ~) or hydroxyamino; c) -COR ~ 6 ~ where R ~ 6 ~ is hydrogen, aryl, aryl-alkyl (C ~ 1 ~ -C ~ 6 ~), optionally alkylated or monohydroxy amino, hydroxy, alkoxy (C ~ 1 ~ -C ~ 4 ~), carboxy, alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~), formula (1) or or alkyl (C ~ 1 ~ -C ~ 4 ~) optionally substituted by heterocycle; d) alkylsulfonyl (C ~ 1 ~ C ~ 4 ~); R ~ 2 ~ represents two hydrogen atoms or a group = O when - - - - is a single bond, or, when - - - - is a double bond, R ~ 2 ~ is hydrogen, cyano, alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~), starch, optionally substituted aryl or heterocycle, alkyl (C ~ 1 ~ -C ~ 8 ~), alkenyl (C ~ 2 ~ -C ~ 8 ~) or alkynyl (C ~ 2 ~ -C ~ 8 ~) optionally branched and / or substituted by aryl or heterocycle; aryloxy, heterocyclyloxy, aryl-alkoxy (C ~ 1 ~ -C ~ 4 ~), heterocyclyl-alkoxy (C ~ 1 ~ -C ~ 4 ~), amino substituted by one or two alkyl groups (C ~ 1 ~ -C ~ 4 ~), arylamino, heterocyclylamino, aryl-alkylamino (C ~ 1 ~ -C ~ 4 ~), heterocyclyl-alkylamino (C ~ 1 ~ -C ~ 4 ~); R ~ 3 ~ is hydrogen or an alkyl (C ~ 1 ~ -C ~ 8 ~), alkenyl (C ~ 2 ~ -C ~ 8 ~) or alkynyl group (C ~ 2 ~ -C ~ 8 ~) optionally substituted by hydroxy, oxo, aryl or heterocycle and, optionally interrupted by one or more heteroatoms or heterogroups; the N <sym> O derivatives of the compounds of formula (1) and the pharmaceutically acceptable salts thereof are PDE4 inhibitors.
priorityDate 1998-07-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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