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1.发明授权
公开(公告)号：US5618804A
公开(公告)日：1997-04-08
申请号：US178320
申请日：1994-01-14
CPC分类号： C07F9/3865 , C07F9/386 , C07F9/4025
摘要： 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.
摘要翻译： PCT No.PCT / JP93 / 00014 Sec。 371日期1994年1月14日 102（e）日期1994年1月14日PCT提交1993年1月8日PCT公布。 第WO94 / 01442号公报 日本1994年1月20日由通式（I）表示的甲烷二膦酸衍生物：其中X和Y在说明书中定义; m表示0〜3的整数， n表示0〜4的整数， （X）m的每个X和（Y）n的每个Y可以相同或不同; + E，uns。 。 + EE表示双键或单键; A是 - （CH 2）a - （D）b - （CH 2）c - （其中D是硫，氧，NH，烷基取代的N或CH 2，a和c是0至10的整数，b是0或 1）或 - （CH = CH）d = CH =（其中d为0〜2的整数，当A表示-CH = CH时，B不存在）d-CH =），B表示氢原子 烷基，氨基，一烷基氨基，二烷基氨基，酰氨基，羟基，烷氧基，三烷基甲硅烷氧基或酰氧基，R 1，R 2，R 3和R 4各自为氢原子，具有1〜 7个碳原子或药理学上允许的阳离子，并且它们可以相同或不同，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，抗风湿药物或自身免疫疾病药物。
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2.发明授权Methanediphosphonate derivative, its manufacturing process and its pharmaceutical applications 失效甲烷二膦酸衍生物，其制造工艺及其制药应用
公开(公告)号：US5527940A
公开(公告)日：1996-06-18
申请号：US340819
申请日：1994-11-17
CPC分类号： C07F9/386 , C07F9/3865 , C07F9/4025 , C07F9/404 , C07F9/405
摘要： The present invention relates to a methanediphosphonate derivative, its manufacturing process and pharmaceutical applications, that is represented with the following formula: ##STR1## (wherein, B is either hydrogen, an alkyl group, hydroxyl group, alkoxy group or amino group, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2 or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to 7 carbon atoms or pharmaceutically allowable cations). The compound of the present invention has excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and is useful as an antiinflammatory agent, antirheumatic, bone metabolic disease drug, autoimmune disease drug, osteoporosis drug and so forth.
摘要翻译： 本发明涉及由下式表示的甲基二膦酸酯衍生物，其制备方法和药物应用：其中，B为氢，烷基，羟基，烷氧基或氨基 ，D是硫，氧，NH，烷基取代的N，CH 2或SCH 2，X表示烷基，具有杂原子作为取代基的烷基，芳基或酰基，m表示1的整数 至5，R 1，R 2，R 3和R 4独立地表示氢，具有1至7个碳原子的烷基或药学上允许的阳离子）。 本发明化合物具有优异的IL-1抑制作用，抗氧化作用和骨吸收抑制作用，可用作抗炎剂，抗风湿剂，骨代谢疾病药物，自身免疫疾病药物，骨质疏松症药物等。
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公开(公告)号：US5683992A
公开(公告)日：1997-11-04
申请号：US617937
申请日：1996-03-15
CPC分类号： C07F9/386 , C07F9/3865 , C07F9/4025 , C07F9/404 , C07F9/405
摘要： The present invention relates to a methanediphosphonate derivative, its manufacturing process, and pharmaceutical applications, that is represented with the following formula: ##STR1## wherein, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2, or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to carbon atoms or pharmaceutically allowable cations. .function.The compounds of the present invention have excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and are useful as antiinflammatory agents, antirheumatic agents, bone metabolic disease drugs, autoimmune disease drugs, or osteoporosis drugs.
摘要翻译： 本发明涉及由下式表示的甲基二膦酸酯衍生物，其制备方法和药物应用：
或 取代的N，CH 2或SCH 2，X表示烷基，具有 杂原子作为取代基，芳基或酰基，m表示1〜5的整数，R 1，R 2，R 3和R 4分别表示氢，具有1〜碳原子的烷基或药学上可允许的阳离子。 f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，可用作抗炎剂，抗风湿剂，骨代谢疾病药物，自身免疫性疾病药物或骨质疏松症药物。 -
4.发明授权Methane diphosphonic acid derivative, its production process and its pharmaceutical applications 失效甲烷二膦酸衍生物，其生产工艺及其制药应用
公开(公告)号：US5565440A
公开(公告)日：1996-10-15
申请号：US256186
申请日：1994-06-28
申请人： Keijiro Takanishi , Norio Kawabe , Teruo Nakadate
发明人： Keijiro Takanishi , Norio Kawabe , Teruo Nakadate
IPC分类号： A61K31/67 , A61P3/00 , A61P29/00 , C07D335/06 , C07F9/6553 , A61K31/38 , C07D333/64 , C07D337/08
CPC分类号： C07F9/65539 , C07F9/655354 , C07F9/655372
摘要： The present invention discloses a methane diphosphonate derivative, a process for producing said derivative and its pharmaceutical applications, said methane diphosphonate derivative indicated with general formula (1): ##STR1## (wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a pharmacologically acceptable cation, a hydrogen atom or a straight chain or branched alkyl group having 1-4 carbon atoms, R.sub.5 is a hydrogen atom or a trialkylsilyl group, m is an integer of 0 to 3, n is an integer of 1 to 3, R.sub.6 and R.sub.7 are independently a hydrogen atom or an alkyl group, and X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group).The compounds of the present invention are useful as an anti-inflammatory, antipyretic, analgesic, antirheumatic drug, antiarthritic or anti-osteoporosis drug as a result of having anti-inflammatory action, antipyretic and an algesic action, or action which improves bone metabolic disorders caused by rheumatism, arthritis, osteoporosis and so forth.
摘要翻译： PCT No.PCT / JP93 / 01579 Sec。 371日期：1994年6月28日 102（e）日期1994年6月28日PCT提交1993年10月29日PCT公布。 WO94 / 10181 PCT出版物 日期：1994年5月11日本发明公开了一种甲烷二膦酸酯衍生物，所述衍生物及其药物应用的制备方法，所述甲基二膦酸酯衍生物用通式（1）表示：其中R1，R2，R3 R4独立地为药理学上可接受的阳离子，氢原子或具有1-4个碳原子的直链或支链烷基，R5为氢原子或三烷基甲硅烷基，m为0-3的整数，n为整数 为1〜3，R6和R7独立地为氢原子或烷基，X为氢原子，卤素原子，烷基，烷氧基或烷硫基。 本发明的化合物可用作抗炎，解热，止痛，抗风湿药物，抗关节炎或抗骨质疏松症药物，具有抗炎作用，解热和止痛作用或改善骨代谢紊乱的作用 由风湿病，关节炎，骨质疏松症等引起。
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