Nitrogenous fused-ring compounds, process for the...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/96 (2006.01) A61K 31/505 (2006.01) C07D 401/06 (2006.01) C07D 401/14 (2006.01) C07D 471/04 (2006.01) C07D 475/02 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2302453

Compounds represented by general formula (I) or salts thereof, which exhibit an antihistaminic activity and an eosinochemotaxis inhibitory activity and are therefore useful as preventive and therapeutic agents for asthma, allergic conjunctivitis, allergic rhinitis, urticaria, atopic dermatitis and so on. In said formula, A is a (substituted) homocycle or nitrogenous heterocycle; D and E are each O or S; and one of R1 and R2 is a group represented by general formula (II), [wherein Ar1 and Ar2 are each a (substituted) aromatic group or they together with the carbon atom adjacent to them may form a (substituted) fused-ring group; B is a (substituted) nitrogenous heterocycle; X and Y are each a bond, O, S(O)p (wherein p is an integer of 0 to 2), NR4 (wherein R4 is H or lower alkyl) or a divalent (substituted) linear lower hydrocarbon group optionally interrupted by a heteroatom; and R3 is H, (substituted) hydroxyl or (esterified) carboxyl], and the other of them is H, cyano or a (substituted) hydrocarbon group.

L'invention concerne des composés représentés par la formule générale (I), ou des sels de ces derniers. Ces composés démontrent une activité antihistaminique et une activité inhibitrice de l'éosinochimiotaxie et sont par conséquent utiles comme agents préventifs et thérapeutiques pour l'asthme, les conjonctivites allergiques, les rhinites allergiques, l'urticaire, les dermatites atopiques etc. Dans cette formule, A est un homocycle (substitué) ou un hétérocycle azoté; D et E sont chacun O ou S; et R?1¿ ou R?2¿ est un groupe représenté par la formule générale (II), [dans laquelle Ar?1¿ et Ar?2¿ sont chacun un groupe aromatique (substitué) ou Ar?1¿ et Ar?2¿ peuvent se joindre à l'atome de carbone adjacent pour former un groupe (substitué) à cycles concentrés; B est un hétérocycle azoté (substitué); X et Y sont chacun une liaison, O, S(O)¿p? (où p est un nombre entier de 0 à 2), NR?4¿ (où R?4¿ est H ou l'alkyle inférieur) ou un groupe hydrocarbure inférieur linéaire (substitué) divalent éventuellement interrompu par un hétéroatome; et R?3¿ est H, l'hydroxy (substitué) ou le carboxyle (estérifié)] l'autre étant H, cyano ou un groupe hydrocarbure (substitué).

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