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    • 1. 发明授权
    • Avermectin derivatives
    • 阿维菌素衍生物
    • US06605595B1
    • 2003-08-12
    • US09890824
    • 2002-02-11
    • Satoshi OmuraToshiaki SunazukaAndreas TurbergGeorg von Samson-HimmelstjernaOlaf HansenAchim Harder
    • Satoshi OmuraToshiaki SunazukaAndreas TurbergGeorg von Samson-HimmelstjernaOlaf HansenAchim Harder
    • A01N4304
    • C07H17/08A61K31/7048
    • Avermectin derivatives represented by the general formula (I) or salts thereof: wherein —X----Y— represents —CH═CH—, —CH2—C(═O)—, —CH2—CH2—, or —CH2—CH(R13)—; for example, 1) when —X----Y— represents —CH═CH—, R1 represents (R11)(R12)C [wherein R11 represents a substituted or unsubstituted lower alkyl group; a formyl group; a lower alkoxylcarbonyl group etc.; and R12 represents a hydrogen atom or a lower alkyl group]; when the bond between R2 and a carbon atom at the 5-position is a single bond, R2 represents a hydroxyl group or a tri(lower alkyl)silyloxy group; or R2 forms a carbonyl group or a hydroxime group together with the carbon atom at the 5-position; 2) when —X----Y— represents —CH2—C(═O)—, R1 represents (R11a)(R12a)C [wherein R11a represents a lower alkoxycarbonyl group, or —COOCH2CH═CH2; and R12a represents a hydrogen atom]; and R2 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.
    • 由通式(I)表示的阿维菌素衍生物或其盐:其中-X-Y-表示-CH = CH-,-CH 2 -C(= O) - , - CH 2 -CH 2 - 或-CH 2 - CH(R 13) - ; 例如,1)当-X ----Y-表示-CH = CH-时,R1表示(R11)(R12)C [其中R11表示取代或未取代的低级烷基; 甲酰基; 低级烷氧基羰基等; R12表示氢原子或低级烷基]。 当R 2与5位的碳原子之间的键是单键时,R 2表示羟基或三(低级烷基)甲硅烷氧基; 或R 2与5-位上的碳原子一起形成羰基或羟基基团; 2)当-X ----Y-表示-CH2-C(= O) - 时,R1表示(R11a)(R12a)C [其中R11a表示低级烷氧基羰基或-COOCH2CH = CH2; R12a表示氢原子]; 并且R 2表示羟基或三(低级烷基)甲硅烷氧基。
    • 5. 发明授权
    • Lactacystin derivatives
    • 乳酸衍生物
    • US5869675A
    • 1999-02-09
    • US979637
    • 1997-11-28
    • Satoshi OmuraToshiaki SunazukaHaruo Tanaka
    • Satoshi OmuraToshiaki SunazukaHaruo Tanaka
    • C07D207/12C07D207/28C07D401/12
    • C07D401/12C07D207/28
    • Novel lactacystin derivatives other than lactacystin per se, with superior activity for the genesis of neurites and highly selective toxicity and low cytotoxicity as compared with known lactacystin have been prepared, of the formula ##STR1## wherein R is lower alkoxy, --S--(CH.sub.2).sub.n R.sup.1 or --S--(CH.sub.2) .sub.n --CH(R.sup.2)-(R.sup.3), in which R.sup.1 is branched or straight-chain lower alkyl, hydroxy, carboxyl, lower alkoxycarbonyl, optionally substituted phenyl, substituted or unsubstituted amino or pyridyl, R.sup.2 is substituted or unsubstituted amino, lower alkyl or amino acid residue, R.sup.3 is carboxyl, lower alkoxycarbonyl, lower alkenyloxycarbonyl or amino acid residue, and n is 0-4, or a pharmacologically acceptable salt thereof.
    • 与已知的乳胞蛋白相比,已经制备了除了乳糖蛋白本身以外的新型乳胞素衍生物,具有优异的神经突发生活性和高选择性毒性和低细胞毒性,其中R为低级烷氧基,-S - (CH2)nR1或-S-(CH2)n-CH(R2) - (R3),其中R1是支链或直链低级烷基,羟基,羧基,低级烷氧基羰基,任选取代的苯基,取代或未取代的氨基 或吡啶基,R2为取代或未取代的氨基,低级烷基或氨基酸残基,R3为羧基,低级烷氧基羰基,低级链烯氧基羰基或氨基酸残基,n为0-4,或其药理学上可接受的盐。