Benzopyrans and pharmaceutical compositions containing them

Details Benzopyrans and pharmaceutical compositions containing them Benzopyrans and pharmaceutical compositions containing them

C - Chemistry, Metallurgy

07

D

C07D 405/04 (2006.01) A61K 31/435 (2006.01) A61K 31/55 (2006.01) C07D 311/70 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 493/04 (2006.01)

Patent

CA 2217821

The invention provides a compound of formula I Image wherein R1 is a mono- or bicyclic aromatic group optionally containing one or more nitrogen atoms and optionally substituted with up to three substituents selected from halogen, C1- 5alkyl, (halo)1-3-C1-5alkyl or C1-5alkoxy, R2 is H or C1-5alkyl, or is C2.5alkylene linked to R1, R3 is a group of formula -N(R9)-COR10 wherein R9 is hydrogen and R10 is phenyl or pyridyl, or R9 and R10 together are 1,3-butadienylene or represent a group of formula - (CH2)n- or Image in which n is an integer of from 3 to 5 inclusive and m is 1 or 2, R4 is hydrogen and R5 is hydroxy in the trans position with respect to R3, R6 and R7 are, independently, C1-5alkyl, and R8 is hydrogen or C1-5alkyl; or N-oxide thereof; or physiologically-hydrolysable and -acceptable ester of such a compound or N- oxide, or acid addition or quaternary ammonium salt of such a compound, N-oxide or ester. The invention also provides processes for their production; and their uses as pharmaceuticals, e.g. as K+ -channel openers, bronchodilators and agents for the suppression of airways hyperreactivity, e.g., for use in the treatment of asthma.

Nouveaux 2,2-di(alkyle C1-5)- ou trans-2,2-di(alkyle C1-5)-3,4-dihydro-3-hydroxy-4-carboxamido-6-(N-arylsulfonamido)-2H-1-benzopyrannes et N-oxydes, esters et sels desdits benzopyrannes. La présente invention concerne en outre leur production, et leur utilisation en tant que produits pharmaceutiques, par ex. en tant qu'ouvreurs des vannes K<+>, bronchodilatateurs et agents de lutte contre l'hyperactivité des voies respiratoires, pour le traitement de l'asthme, par exemple.

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