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    Avermectin derivatives
    3.
    发明申请
    Avermectin derivatives 有权
    阿维菌素衍生物

    公开(公告)号：US20050148520A1

    公开(公告)日：2005-07-07

    申请号：US10997869

    申请日：2004-11-29

    Applicant: Satosh Omura ,  Kenichiro Nagai ,  Toshiaki Sunazuka

    Inventor： Satosh Omura ,  Kenichiro Nagai ,  Toshiaki Sunazuka

    IPC: A61K31/365 ,  A61P33/10 ,  C07H17/08 ,  A01N43/04

    CPC classification number: A61K31/7048 ,  A61K31/365 ,  C07H17/08

    Abstract: A compound represented by the general formula (I) or a salt thereof: wherein represents —CH═CH—, —CH2—CH2— or the like, between R1 and the carbon atom at 4′-position represents a single bond or a double bond, between R2 and the carbon atom at 5-position represents a single bond or a double bond, and for example, 1) when represents —CH═CH— or —CH2—CH2—, and between R1 and the carbon atom at 4′-position represents a double bond, R1 represents ═C(R11)(R12) (wherein R13 represents a lower alkyl group or the like and R12 represents a hydrogen atom or the like) or the like, and R2 represents a hydroxyl group or the like, or R2 may be combined together with the carbon atom at 5-position to form a carbonyl group, and 2) when represents —CH═CH— or —CH2—CH2—, and between R1 and the carbon atom at 4′-position represents a single bond, R1 represents —OCH(R1a)(R1b) (wherein R1a represents a lower alkyl or the like and R1b represents a hydrogen atom or the like) or the like, and R2 represents a hydroxyl group or the like.

    Abstract translation: 由通式（I）表示的化合物或其盐：其中表示-CH-CH-，-CH 2 -CH 2 - 等，R 1位和4位的碳原子代表单键或双键，在R 2和5位之间的碳原子表示单键或 双键，例如1）当代表-CH-CH-或-CH 2 -CH 2 - ，且R 1〜 并且4'-位上的碳原子表示双键，R 1表示-C（R 11）（R 12）（其中R' R 13表示低级烷基等，R 12表示氢原子等）等，R 2表示 羟基等或R 2可以与5-位上的碳原子一起形成羰基，和2）当-CH-CH-或-CH 2 CH 2 - ，和R 1和4'之间的碳原子表示 发生单键，R 1表示-OCH（R 1a）（R 1b）（R 1b）（其中R 1a， 表示低级烷基等，R 1b表示氢原子等）等，R 2表示羟基等。

    Lactacystin derivatives
    5.
    发明授权
    Lactacystin derivatives 失效
    乳酸衍生物

    公开(公告)号：US5869675A

    公开(公告)日：1999-02-09

    申请号：US979637

    申请日：1997-11-28

    Applicant: Satoshi Omura ,  Toshiaki Sunazuka ,  Haruo Tanaka

    Inventor： Satoshi Omura ,  Toshiaki Sunazuka ,  Haruo Tanaka

    IPC: C07D207/12 ,  C07D207/28 ,  C07D401/12

    CPC classification number: C07D401/12 ,  C07D207/28

    Abstract: 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.

    Abstract translation: 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。

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