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    • 7. 发明授权
    • Cytokine production inhibitors
    • 细胞因子生成抑制剂
    • US06197811B1
    • 2001-03-06
    • US09292961
    • 1999-04-16
    • Martin A. HayesDavid J. HardickJenny S. TangHamish RyderAdrian J. FolkesToshio TatsuokaMasashi Matsui
    • Martin A. HayesDavid J. HardickJenny S. TangHamish RyderAdrian J. FolkesToshio TatsuokaMasashi Matsui
    • A61K3135
    • C07D309/32
    • A compound selected from the group consisting of a 5,6-dihydro-&agr;-pyrone of formula (I): wherein bond a is oriented either or ; X is O or NH; R1 is selected from the group consisting of: a group R3(O)C— wherein R3 is selected from the group consisting of: (i) a group of formula R4—CH═CH— wherein R4 is C1-C20 alkyl, C2-C20 alkenyl, an aryl group, or a 5- or 6-membered unsaturated heterocyclic ring containing one or two O, N or S atoms, (ii) C2-C20 alkyl; and (iii) an aryl group or a substituent which is a fused ring system of formula (1) or (2):  wherein each of R′ and R″, which are the same or different and may occupy any position on ring a or ring b of said fused ring system, is H or C1-C6 alkyl; a group ArCH2— wherein Ar is an aryl group; and a group R5O—CH2— wherein R5 is C1-C6 alkyl optionally interrupted by one or two O atoms; and R2 is CH3 or, when R1 is a group of formula (A) as defined below, R2 is R6OOC— or R6NOC— wherein R6 is C1-C6 alkyl; and the pharmaceutically and veterinarily acceptable salts and esters thereof; with the exception of compounds wherein bond a is oriented , X is O and R1 is a group of formula (A):  wherein R11 and R21 are H when R2 in formula (I) is CO2H or CH3, or one of R11 and R21 is H and the other is OH when R2 in formula (I) is CO2H.
    • 选自式(I)的5,6-二氢-α-吡喃酮的化合物:其中键合a定向为; X是O或NH; R1选自:组R3 (O)C-,其中R 3选自:(i)式R 4 -CH = CH-的基团,其中R 4是C 1 -C 20烷基,C 2 -C 20烯基,芳基或5-或 含有一个或两个O,N或S原子的6元不饱和杂环,(ii)C 2 -C 20烷基;和(iii)作为式(1)或(2)的稠环体系的芳基或取代基, :其中R'和R“各自相同或不同并且可以占据所述稠环系统的环a或环b上的任何位置是H或C 1 -C 6烷基;基团ArCH 2 - 其中Ar是 芳基; 和R5O-CH2-基团,其中R5是任选被一个或两个O原子中断的C 1 -C 6烷基; 并且R 2是CH 3,或者当R 1是如下定义的式(A)的基团时,R 2是R 60 OC-或R 6 NOC - ,其中R 6是C 1 -C 6烷基;和其药学和兽医学上可接受的盐和酯; 除了其中键a取向的化合物的化合物除外,X是O,R1是式(A)的基团: 当式(I)中的R 2为CO 2 H或CH 3时,R 11和R 21为H,或者R 11和R 21中的一个为H,另一个为OH,式(I)中的R 2为CO 2 H.