Sterol derivative, preparation method therefor and use thereof

    公开(公告)号:US10093695B2

    公开(公告)日:2018-10-09

    申请号:US14376481

    申请日:2013-02-04

    Abstract: The present disclosure discloses a sterol derivative, a preparation method therefor and a use thereof. The sterol derivative includes a sterol compound with Structural Formula (I) or a pharmaceutically acceptable salt thereof, or an extract containing the sterol compound, or a composition containing the sterol compound, wherein Structural Formula (I) is as follows: where R1 is —OH, ═O, H or C1-C3 alkyl; R2 is —OH, H or C1-C3 alkyl; R3 is —OH, ═O, H or C1-C3 alkyl; R4 is —OH, H or C1-C3 alkyl, and at least one of R1, R2, R3 and R4 is —OH. The compound with Structural Formula (I) can be used for preparing a drug having inhibitory effect on 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity and the prepared drug can effectively inhibit the HMG-CoA reductase activity or be used for preparing an anti-cancer drug.

    STEROLS DERIVATIVE, AND PREPARATION METHOD AND PURPOSE THEREOF
    5.
    发明申请
    STEROLS DERIVATIVE, AND PREPARATION METHOD AND PURPOSE THEREOF 审中-公开
    甾体衍生物及其制备方法及用途

    公开(公告)号:US20150031657A1

    公开(公告)日:2015-01-29

    申请号:US14368494

    申请日:2012-12-25

    CPC classification number: C07J71/0005 A61K36/06 A61K36/899 A61K2236/00

    Abstract: The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of —OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of —OH, ═O, H, and C1-C3 alkyl; R4 is selected from the group consisting of —OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

    Abstract translation: 本发明涉及药物化学领域,涉及固醇衍生物及其制备方法和用途。 具体地,本发明涉及式I化合物或其药学上可接受的盐,酯或醚,其中R 1选自-OH,= O(羰基),H和C 1 -C 3烷基 ; R 2选自-OH,H和C 1 -C 3烷基; R 3选自-OH,= O,H和C 1 -C 3烷基; R 4选自-OH,H和C 1 -C 3烷基; R 1,R 2,R 3和R 4中没有一个,两个,三个或四个是-OH。 本发明化合物可有效抑制HMG-CoA还原酶,肿瘤细胞和脂肪酶,是减少血脂,抗肿瘤或减肥的潜在药物。

    Sterol derivatives and preparation method and uses thereof

    公开(公告)号:US12227541B2

    公开(公告)日:2025-02-18

    申请号:US17071958

    申请日:2020-10-15

    Abstract: The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of —OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of —OH, ═O, H, and C1-C3 alkyl; R4 is selected from the group consisting of —OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

    STEROL DERIVATIVES AND PREPARATION METHOD AND USES THEREOF

    公开(公告)号:US20220387453A1

    公开(公告)日:2022-12-08

    申请号:US17818302

    申请日:2022-08-08

    Abstract: The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of —OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of —OH, ═O, H, and C1-C3 alkyl; R4 is selected from the group consisting of —OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

    STEROL DERIVATIVES AND PREPARATION METHOD AND USES THEREOF

    公开(公告)号:US20210024570A1

    公开(公告)日:2021-01-28

    申请号:US17071958

    申请日:2020-10-15

    Abstract: The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of —OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of —OH, ═O, H, and C1-C3 alkyl; R4 is selected from the group consisting of —OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

    Sterol derivatives and preparation method and uses thereof

    公开(公告)号:US11634454B2

    公开(公告)日:2023-04-25

    申请号:US17071963

    申请日:2020-10-15

    Abstract: The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of —OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of —OH, ═O, H, and C1-C3 alkyl; R4 is selected from the group consisting of —OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

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