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    • 3. 发明申请
    • NOVEL USE OF ORGANIC COMPOUNDS
    • 有机化合物的新用途
    • US20090176873A1
    • 2009-07-09
    • US11920346
    • 2006-05-24
    • Ann FowlerDaniel RaederstorffGoede SchulerJoseph Schwager
    • Ann FowlerDaniel RaederstorffGoede SchulerJoseph Schwager
    • A61K31/365C07D307/87A61P19/02
    • A61K31/343
    • The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(α,β-dimethylacrylyloxy)-pentylidenyl; X is a residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation. The compounds of formula (I) as defined above may also be useful (for the manufacture of a composition) for the management of pain, fever and injuries, especially sport injuries. Moreover, the compounds of formula (I) as defined above may also be useful (for the manufacture of a composition) for the maintenance and regeneration of articular cartilage.
    • 本发明涉及式(I)化合物的用途,其中凝血线是任选的键; 如果R2是羟基,R1是丁基或丁酰基,如果R2是氢,则是丁基; 或者R 1和R 2一起是被羟基,甲基或3-(α,β-二甲基丙烯酰氧基) - 戊酰基任选取代的1-亚丁基; X是选自X1,X2,X3,X4和X5的残基; 其中如果式(I)中的虚线不存在,X是X 2,X 3或X 5; 如果虚线表示上述式(I)中的键,X为X 1,X 4或X 5; R3是羟基或丁酰基; 和n为1或2,作为预防,控制和治疗需要调节哺乳动物炎症的病症的药剂。 另一方面,本发明涉及式(I)化合物作为活性成分在制备用于预防,控制和治疗需要调节炎症的病症的药物/组合物中的用途。 如上定义的式(I)化合物也可用于治疗疼痛,发烧和损伤,特别是运动损伤(用于制造组合物)。 此外,如上定义的式(I)化合物也可用于维持和再生关节软骨(用于制备组合物)。