Tricyclic fused heterocycle compounds, process for preparing...

C - Chemistry – Metallurgy – 07 – D

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C07D 313/14 (2006.01) A61K 31/31 (2006.01) A61K 31/335 (2006.01) A61K 31/343 (2006.01) A61K 31/38 (2006.01) A61K 31/381 (2006.01) A61K 31/4353 (2006.01) A61K 31/4427 (2006.01) A61P 11/06 (2006.01) A61P 11/08 (2006.01) A61P 29/00 (2006.01) C07D 337/14 (2006.01) C07D 405/04 (2006.01) C07D 407/04 (2006.01) C07D 409/04 (2006.01) C07D 491/04 (2006.01) C07D 491/06 (2006.01)

Patent

CA 2370013

Compounds represented by general formula (1) or pharmaceutically acceptable salts thereof. In said formula, X is CH, CH2, CHR (wherein R is lower alkyl or substituted lower alkyl), or CRR' (wherein R and R' are each as defined above as to R); Y is CH, CH2, or C=O; Z is O, S, S=O, or SO2; U is C or N; R1 to R4 are each independently hydrogen, OR, SR (wherein R is as defined above), an aromatic ring, a heterocycle, or the like; and at least one of R5 to R8 is OH. The compounds exhibit excellent pharmacological activities such as relaxation of tracheal smooth muscle, suppression of respiratory tract hypersensitiveness, and inhibition of phlogocytic infiltration into the respiratory tract.

L'invention se rapporte à des composés représentés par la formule générale (1) et à des sels pharmaceutiquement acceptables de ces composés. Dans la formule (1), X est CH, CH¿2?, CHR (où R est un alkyle inférieur ou un alkyle inférieur substitué), ou CRR' (R et R' sont chacun définis comme R l'est ci-dessus); Y est CH, CH¿2? ou C=O; Z est O, S, S=O ou SO¿2?; U est C ou N; R¿1? à R¿4? sont indépendamment hydrogène, OR, SR (où R est tel que défini ci-dessus), un noyau aromatique, un hétérocycle ou analogue; et l'un au moins des radicaux que sont R¿5? à R¿8? est OH. Les composés de cette invention sont dotés d'excellentes fonctions pharmacologiques telles que la fonction de relaxation des muscles lisses trachéaux, celle de suppression de l'hypersensibilité du tractus respiratoire et celle d'inhibition des infiltrations inflammatoires dans le tractus respiratoire.

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