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filingDate 1999-07-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2356f665b35529a61a799f8088c3b5bc
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publicationDate 2002-11-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber NZ-507930-A
titleOfInvention Phthalazine derivatives as PDE 4 inhibitors for the treatment of respiratory diseases and allergic and inflammatory conditions
abstract A class of phthalazine derivatives able to inhibit PDE 4 and TNF-alpha is described. In particular compounds of the formula (I) wherein ------ is a single or double bond; B is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalkyl residue; A is phenyl or heterocycle optionally substituted by one or more substituent(s) or a COR4 group wherein R4 is hydroxy, C1-4 alkyl, amino optionally mono- or di-substituted by a C1-6-alkyl group or monohydroxylated; R represents two hydrogen atoms or a C=O group when ------ is a single bond or, when ------ is a double bond, is hydrogen, optionally substituted aryl or heterocycle, (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl optionally substituted by aryl or heterocycle; aryloxy, heterocyclyloxy, aryl-C1-4-alkoxy, heterocyclyl-C1-4-alkoxy, amino substituted by one or two C1-4-alkyl group(s), aryl-amino, heterocyclyl-amino, aryl-C1-4-alkyl-amino, heterocyclyl-C1-4-alkylamino; R1 is a C1-6-alkyl, aryl, aryl-C1-10-alkyl, C4-7-cycloalkyl group optionally containing an oxygen atom and/or substituted by a polar substituent; R2 is a C1-6 -alkyl, polyfluoroC1-6-alkyl group; R3 is absent when ------ is a double bond, or, when ------ is a single bond, is a) hydrogen; b) C1-6-alkyl optionally substituted by aryl, by heterocycle or by a COR5 group wherein R5 is hydroxy, C1-4-alkoxy or hydroxyamino; c) -COR6 wherein R6 is hydrogen, aryl, aryl-C1-6-alkyl, amino optionally alkylated or monohydroxylated, hydroxy, C1-4-alkoxy, carboxy, C1-4-alkoxycarbonyl, or C1-4-alkyl optionally substituted by heterocycle; d) C1-4-alkyl-sulfonyl; the N--O derivatives of the compounds of formula (I) and the pharmaceutically acceptable salts thereof are PDE 4 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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