申请人:Toray Industries, Inc.
公开号:US05618804A1
公开(公告)日:1997-04-08
A methane diphosphonic acid derivative represented by the general formula (I): ##STR1## wherein, X and Y are defined in the specification; m represents an integer of 0 to 3; n represents an integer of 0 to 4; and each X of the (X).sub.m and each Y of the (Y).sub.n may be either identical or different; . . . represents a double bond or single bond; A is --(CH.sub.2)a--(D)b--(CH.sub.2)c-- (wherein D is sulfur, oxygen, NH, alkyl-substituted N, or CH.sub.2, a and c are integers of 0 to 10 and b is 0 or 1), or --(CH.dbd.CH)d.dbd.CH= (wherein d is an integer of 0 to 2, and B does not exist when A represents --CH.dbd.CH)d--CH.dbd.), B refers to a hydrogen atom, alkyl group, amino group, monoalkylamino group, dialkylamino group, acylamino group, hydroxyl group, alkoxy group, trialkylsiloxy group or acyloxy group, and each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is hydrogen atom, straight or branched alkyl group having 1 to 7 carbon atoms, or pharmacologically allowed cation, and these may be identical or different, as described. The compounds of the present invention have excellent IL-1 inhibitory action, antioxidative action and bone resorption inhibitory action, and are useful as an antiinflammatory drug, antirheumatic drug, or autoimmune disease drug.
通式(I)所表示的甲烷二膦酸衍生物:##STR1## 其中,X和Y在规范中定义;m代表0至3的整数;n代表0至4的整数;(X).sub.m和(Y).sub.n中的每个X和每个Y可以相同也可以不同;......表示双键或单键;A是--(CH.sub.2)a--(D)b--(CH.sub.2)c--(其中D是硫,氧,NH,烷基取代的N或CH.sub.2,a和c是0至10的整数,b为0或1),或--(CH.dbd.CH)d.dbd.CH=(其中d是0至2的整数,当A代表--CH.dbd.CH时,B不存在),B指的是氢原子,烷基,氨基,单烷基氨基,二烷基氨基,酰基氨基,羟基,烷氧基,三烷基硅氧基或酰氧基,每个R.sup.1,R.sup.2,R.sup.3和R.sup.4是氢原子,1至7个碳原子的直链或支链烷基,或药理学上允许的阳离子,它们可以相同也可以不同,如所述。本发明的化合物具有优异的IL-1抑制作用,抗氧化作用和骨吸收抑制作用,可用作抗炎药,抗风湿药或自身免疫疾病药。