发明名称 5-LIPOXYGENASE INHIBITORS
摘要 Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and havi ng formula (I) and the pharmaceutically acceptable salts thereof, wherein Ar1 i s a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl , 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, whi ch is bonded to X1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C1-4 alkyl and the like; X1 is a direct bond or C1-4 alkylene; Ar2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X2 is -A-X- or -X-A- wherein A is a direct bond or C1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar3 is phenylene, pyridylene, thienylene , furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C1-4 alkyl and the like; R1 and R2 are each C1-4 alkyl, or together they form a group of formul a - D1-Z-D2- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D1 and D2 are C1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D1 and D2 may be substituted by C1-3 alkyl; and Y is CONR3R4, CN, C(R3)=N-OR4, COOR3, COR3 orCSNR3R4, wherein R3 and R4 are each H or C1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
申请公布号 CA2202057(A1) 申请公布日期 1996.04.25
申请号 CA19952202057 申请日期 1995.05.29
申请人 PFIZER INC. 发明人 OKUMURA, YOSHIYUKI;NAKAO, KAZUNARI;STEVENS, RODNEY W.;MANO, TAKASHI
分类号 A61K31/35;A61K31/40;A61K31/415;A61K31/4164;A61K31/4192;A61K31/4196;A61P9/00;A61P29/00;A61P37/08;A61P43/00;C07D233/60;C07D309/04;C07D309/08;C07D405/12;C07D521/00;(IPC1-7):C07D405/12;C07D401/14;C07D405/14;C07D409/14;C07D413/14;C07D417/14;C07D207/323;A61K31/41;A61K31/44;C07D233/61 主分类号 A61K31/35
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