Benzocycloheptathiophene compounds

Details Benzocycloheptathiophene compounds Benzocycloheptathiophene compounds

C - Chemistry, Metallurgy

07

D

C07D 409/08 (2006.01) A61K 31/445 (2006.01) C07D 211/14 (2006.01) C07D 409/04 (2006.01)

Patent

CA 2283663

Disclosed are N-substituted hydroxyalkyl or carboxyalkyloxyalkyl analogs of 9- and/or 10-oxo-4Hbenzo[4,5]cyclohepta[1,2-b]thiophene compounds, or 9-OH and/or 10-OH-substituted analogs thereof having the formula: (see formula I) wherein: R is a member selected from the group consisting of hydroxyC2-6alkyl and carboxyC1-6 alkyloxyC1-6alkyl, and -A-B- is a moiety having the formula: (a) -CO-CH2-- (b) -CH2-CO- (c) -CH2--CH2- (d) -CHOH-CH2- (e) -CHOH-CHOH- (f) -CH2-CHOH- or (g) -CO-CO- which possess antihistaminic and antiasthmatic properties with reduced sedative side effects. The optically active isomers and the pharmaceutically acceptable salts thereof are also described. The compounds were also found to prevent smooth muscle hyperreactivity.

L'invention concerne des analogues hydroxyalkyle ou carboxyalkyloxyalkyle N-substitués de composés 9- et/ou 10- oxo-4Hbenzo[4,5]cyclohepta[1,2-b]thiophène, ou leurs analogues à substitution 9-OH et/ou 10-OH, lesquels possèdent des propriétés antihistaminiques et antiasthmatiques avec peu d'effets secondaires sédatifs. L'invention concerne également leurs isomères actifs optiquement et leurs sels acceptables du point de vue pharmaceutique. On a également découvert que les composés préviennent l'hyperréactivité des muscles lisses.

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