Pyrazolopyridylpyridazinone derivatives and process for the...

Details Pyrazolopyridylpyridazinone derivatives and process for the... Pyrazolopyridylpyridazinone derivatives and process for the...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/50 (2006.01) A61P 11/08 (2006.01)

Patent

CA 2267103

Novet pyrazolopyridylpyridazinone derivatives characterized by being represented by general formula (1) and pharmacologically acceptable salts thereof, which exhibit a phosphodiesterase inhibiting activity and have a selective potent bronchodilating effect on the respiratory tract; a process for the preparation of them; and bronchodilators containing the same as the active ingredient; wherein R1 is C1 -C4 lower alkyl or C3 -C6 cycloalkyl; and R2, R3 , R4 and R5 are each independently hydrogen, C1 -C4 lower alkyl or phenyl, or alternatively R3 and R5 may be united to form a double bond.

Cette invention concerne de nouveaux dérivés de pyrazolopyridylpyridazinone, lesquels correspondent à la formule générale (1) où R<1> représente alkyle inférieur C1-C4 ou cycloalkyle C3-C6. R<2>, R<3>, R<4> et R<5> représentent chacun indépendamment hydrogène, phényle ou alkyle inférieur C1-C4, R<3> et R<5> pouvant encore former tous deux une liaison double. Cette invention concerne également les sels de ces dérivés acceptables sur le plan pharmaceutiques. Ces dérivés possèdent une activité inhibant la phosphodiestérase, et ont un effet de broncho-dilatation sélectif et puissant sur les voies respiratoires. Cette invention concerne en outre un procédé de fabrication de ces dérivés, ainsi que des agents de broncho-dilatation qui contiennent ces dérivés en qualité d'ingrédient actif.

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