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    • 67. 发明授权
    • Substituted benzylthiazolidine-2, 4-dione derivatives
    • 取代的苄基噻唑烷-2,4-二酮衍生物
    • US06730687B1
    • 2004-05-04
    • US10049645
    • 2002-02-25
    • Hiroyuki MiyachiMasahiro NomuraTakahiro TanaseKoji MurakamiMasaki Tsunoda
    • Hiroyuki MiyachiMasahiro NomuraTakahiro TanaseKoji MurakamiMasaki Tsunoda
    • A61K31426
    • C07D277/34
    • The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives that bind to receptor to activate as ligands of human peroxisome proliferator-activated receptor (PPAR) and exhibit blood glucose-decreasing action and lipid-decreasing action, and processes for preparing them. It relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein the bond mode of A denotes —CH2CONH—, —NHCONH—, —CH2CH2CO— or —NHCOCH2—, and B denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, halogen atom, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and processes for preparing them.
    • 本发明提供了新的取代的苄基噻唑烷-2,4-二酮衍生物,其结合受体以作为人类过氧化物酶体增殖物激活受体(PPAR)的配体活化并显示出血糖降低作用和降脂作用,以及制备它们的方法。 它涉及由通式(1)表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A的键合模式表示-CH 2 CONH-,-NHCONH-,-CH 2 CH 2 CO-或-NHCOCH 2 - ,B表示低级烷基 具有1至4个碳原子的烷基,具有1至3个碳原子的低级烷氧基,卤素原子,三氟甲基,三氟甲氧基,未取代或可具有取代基的苯基,未被取代或可具有取代基的苯氧基或可具有取代基的苯氧基 未取代或可具有取代基的基团],它们的药学上可接受的盐,它们的水合物及其制备方法。
    • 69. 发明授权
    • Cancer metastasis inhibitor
    • 癌转移抑制剂
    • US5750515A
    • 1998-05-12
    • US737799
    • 1996-11-26
    • Jiro ShibataKonstanty WierzbaKoji MurakamiYuji YamadaKoichi Shudo
    • Jiro ShibataKonstanty WierzbaKoji MurakamiYuji YamadaKoichi Shudo
    • A61K31/192A61K31/196A61K31/695A61P35/04A61K31/19A61K31/20
    • A61K31/695A61K31/192A61K31/196
    • The present invention relates to a cancer metastasis inhibitor comprising a benzoic acid derivative as an active ingredient represented by the formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each represents hydrogen atom, hydroxyl group or trimethylsilyl group, or R.sub.3 and R.sub.4 are bonded to each other to form a tetramethylene group substituted with lower alkyl group, and X represents group --COCH.dbd.C(OH)--, group --NHCO-- or group --CONH--, provided that when R.sub.3 and R.sub.4 are bonded to each other to form a tetramethylene group substituted with lower alkyl group, X is group --COCH.dbd.C(OH)-- or group --CONH--, use of the benzoic acid derivative for preparing the cancer metastasis inhibitor and method of inhibiting cancer metastasis, characterized in that an effective amount of the benzoic acid derivative is administered to a mammalian animal for inhibiting metastasis of cancer. The benzoic acid derivative represented by the above formula (I) has extremely good metastasis inhibiting properties.
    • PCT No.PCT / JP96 / 00980 Sec。 371日期1996年11月26日 102(e)1996年11月26日PCT PCT 1996年4月10日PCT公布。 第WO96 / 32101号公报 日期:1996年10月17日本发明涉及包含苯甲酸衍生物作为由式(I)表示的活性成分的癌症转移抑制剂,其中R1,R2,R3和R4相同或不同, 各自表示氢原子,羟基或三甲基甲硅烷基,或者R 3和R 4相互键合形成被低级烷基取代的四亚甲基,X表示-COCH = C(OH) - 基团,-NHCO-或基团 -CONH-,条件是当R 3和R 4彼此键合以形成被低级烷基取代的四亚甲基时,X是基团-COCH = C(OH) - 或基团-CONH-,使用苯甲酸衍生物 制备癌转移抑制剂和抑制癌转移的方法,其特征在于向哺乳动物施用有效量的苯甲酸衍生物以抑制癌转移。 上述式(I)表示的苯甲酸衍生物具有极好的转移抑制性质。