申请人:Bjork Anders
公开号:US20060004038A1
公开(公告)日:2006-01-05
A compound of formula (I)
wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl;
R′ is hydrogen, C
1
-C
4
alkyl, C
1
-C
3
alkoxy; halogen, trifluoromethyl or OCH
x
F
y
, R″ is hydrogen, fluoro or chloro, that R″ being fluoro or chloro only when R′ is fluoro or chloro;
R
3
is hydrogen or C
1
-C
5
alkyl
R
4
is hydrogen, CH
2
OCOC(CH
3
)
3
, pharmaceutically acceptable inorganic or organic cations, or COR
4
′ wherein R
4
′ is C
1
-C
5
alkyl, phenyl, benzyl or phenethyl;
R
7
is methyl or ethyl;
one of A and B is sulphur and the other is C—R
2
;
when A is S, R
2
is selected from hydrogen and methyl, with the proviso that R
2
is methyl only when R
3
is not hydrogen; and
when B is S, R
2
is hydrogen; and any tautomer thereof. A pharmaceutical composition comprising a compound of formula (I), a method of treating malignant tumours or diseases resulting from autoimmunity or pathologic inflammation.
化合物的化学式为(I),其中R为甲基、乙基、正丙基、异丙基、正丁基或烯丙基;R′为氢、C1-C4烷基、C1-C3烷氧基、卤素、三氟甲基或OCHxFy;R″为氢、氟或氯,当R′为氟或氯时,R″仅为氟或氯;R3为氢或C1-C5烷基;R4为氢、CH2OCOC(CH3)3、药学上可接受的无机或有机阳离子,或COR4′,其中R4′为C1-C5烷基、苯基、苄基或苯乙基;R7为甲基或乙基;A和B中的一个为硫,另一个为C-R2;当A为S时,R2从氢和甲基中选择,但R3不为氢时,R2仅为甲基;当B为S时,R2为氢;以及其任何互变异构体。一种包含化合物(I)的药物组合物,一种治疗恶性肿瘤或由自身免疫或病理性炎症引起的疾病的方法。