发明名称 5-lipoxygenase inhibitors
摘要 Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: <IMAGE> I and the pharmaceutically acceptable salts thereof, wherein Ar1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which 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, and C1-4 alkyl; X1 is a direct bond or C1-4 alkylene; Ar2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino 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 and C1-4 alkyl; R1 and R2 are each C1-4 alkyl, or together they form a group of formula -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 or CSNR3R4, 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 US5883106(A) 申请公布日期 1999.03.16
申请号 US19980020014 申请日期 1998.02.06
申请人 PFIZER INC. 发明人 STEVENS, RODNEY W.;MANO, TAKASHI;NAKAO, KAZUNARI;OKUMURA, YOSHIYUKI
分类号 C07D231/12;C07D309/08;C07D521/00;(IPC1-7):A61K31/085;A61K31/11;A61K31/15;A61K31/19;A61K31/34;A61K31/40;A61K31/44;C07C69/76;C07C323/23;C07C235/40;C07C233/28;C07C233/64;C07D207/30;C07D249/04;C07D309/32 主分类号 C07D231/12
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