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    • 5. 发明授权
    • Highly water-soluble metalloproteinase inhibitors
    • 高度水溶性金属蛋白酶抑制剂
    • US6147114A
    • 2000-11-14
    • US945356
    • 1997-10-24
    • Tetsunori FujisawaShinjiro OdakeYasuo MoritaTomoko HongoHajime ItoJunko YasudaEiko SudaKatsuhiro IgetaTadanori Morikawa
    • Tetsunori FujisawaShinjiro OdakeYasuo MoritaTomoko HongoHajime ItoJunko YasudaEiko SudaKatsuhiro IgetaTadanori Morikawa
    • A61K31/165C07C239/06C07C259/06C07C279/14C07C279/16C07C305/24C07C309/61C07C323/60C07F9/12A01N37/28C07C239/14
    • C07C323/60A61K31/165C07C239/06C07C259/06C07C279/14C07C279/16C07C305/24C07C309/61C07F9/12
    • New compounds of the general formula (I) ##STR1## (wherein R.sup.1 is a hydrogen atom, or a hydroxyl, aryl (C.sub.1 -C.sub.6)alkylene or --A--SOn--B group (A is a (C.sub.1 -C.sub.6) alkylene group; B is a (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) acyl, aryl or heterocyclyl group; n is 0, 1 or 2), R.sup.2 is a hydrogen atom, or a (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkyloxy 10 or (C.sub.1 -C.sub.6) alkylthio group, R.sup.3 and R.sup.4 are identical or different, representing a hydrogen atom, or a (C.sub.1 -C.sub.6) alkyl, aryl or aryl(C.sub.1 -C.sub.6)alkylene group, R.sup.5 is a --Y--C or C group (Y is a (C.sub.1 -C.sub.6) alkylene group, an oxygen atom, an imino group or a (C.sub.1 -C.sub.6) alkyleneimino group, C is a sulfonic acid, phosphonic acid, amidino, (C.sub.1 -C.sub.6) acyl, acylimidoyl, diphosphonomethine or dicarboxymethine group), and R.sup.6 is a hydrogen atom, or a nonsubstituted or substituted benzyl, trialkylsilyl, tert-butyldiphenylsilyl, tetrahydropyranyl or tert-butyl group) or stereoisomers thereof, and pharmaceutically acceptable salts thereof and solvates thereof, and the process for the preparation thereof, and metalloproteinase inhibitors which comprise one or more compounds selected from those compounds as effective ingredients and inhibit matrix metalloproteinases (MMPs) and/or TNF-.alpha. converting enzyme. Furthermore, the preparation intermediates to obtain the compounds of the formula (I) and the process for the preparation.
    • PCT No.PCT / JP96 / 01135 Sec。 371 1997年10月24日第 102(e)1997年10月24日PCT PCT 1996年4月25日PCT公布。 WO96 / 33968 PCT公开号 日期:1996年10月31日新化合物通式(Ⅰ)(其中R1是氢原子,或羟基,芳基(C1-C6)亚烷基或-A-SOn-B基团(A是(C1-C6) 亚烷基; B是(C1-C6)烷基,(C1-C6)酰基,芳基或杂环基; n是0,1或2),R2是氢原子或(C1-C6)烷基, C1-C6)烷氧基10或(C1-C6)烷硫基,R3和R4相同或不同,代表氢原子或(C1-C6)烷基,芳基或芳基(C1-C6)亚烷基,R5是 -YC或C基(Y是(C1-C6)亚烷基,氧原子,亚氨基或(C1-C6)亚烷基亚氨基),C是磺酸,膦酸,脒基,(C1-C6 )酰基,酰亚氨基,二亚膦酰基或二羧基甲基),R6为氢原子,或未取代或取代的苄基,三烷基甲硅烷基,叔丁基二苯基甲硅烷基,四氢吡喃基或叔丁基)或其立体异构体及其药学上可接受的盐及其溶剂合物 ,以及其准备过程 f和金属蛋白酶抑制剂,其包含一种或多种选自那些化合物的化合物作为有效成分并抑制基质金属蛋白酶(MMP)和/或TNF-α转化酶。 此外,制备中间体以获得式(I)化合物及其制备方法。