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    PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND THEIR STEREOISOMERS, THE PREPARATION PROCESSES AND USES THEREOF
    1.
    发明申请
    PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND THEIR STEREOISOMERS, THE PREPARATION PROCESSES AND USES THEREOF 有权
    苯甲酰胺衍生物及其立体异构体，其制备方法及其用途

    公开(公告)号：US20110224305A1

    公开(公告)日：2011-09-15

    申请号：US12810565

    申请日：2009-03-24

    申请人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    发明人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    IPC分类号： A61K31/165 ,  C07C237/20 ,  C07C231/02 ,  A61P3/04

    CPC分类号： C07C237/06 ,  C07B2200/07 ,  C07C237/22 ,  C07C2601/04

    摘要： Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t-butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro-demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.

    摘要翻译： 苯基环丁基酰胺衍生物及其光学异构体，其制备方法及其用途，其包括式（I）化合物，其纯立体异构体及其药学上可接受的盐。 式（I）中，R为H，甲酰基，乙酰基，卤代乙酰基，苯甲酰基，苄氧基羰基（Cbz），叔丁氧羰基（Boc）或9-芴基甲氧基羰基（Fmoc）。 本发明新型化合物具有药物活性，并通过外消旋，左旋或右旋甲基西布曲明和外消旋或D / L异亮氨酸在温和条件下的缩合反应制备。 证明本发明化合物对不同程度的肥胖模式大鼠具有减肥效果，并且通过动物实验效果优于西布曲明。 因此，由本发明化合物制备的药物或通过本发明化合物的组合物和其它药物活性化合物制备的药物可用于治疗肥胖症。

    Phenylcyclobutylamide derivatives and their stereoisomers, the preparation processes and uses thereof
    2.
    发明授权
    Phenylcyclobutylamide derivatives and their stereoisomers, the preparation processes and uses thereof 有权
    苯基环丁基酰胺衍生物及其立体异构体，其制备方法和用途

    公开(公告)号：US08497305B2

    公开(公告)日：2013-07-30

    申请号：US12810565

    申请日：2009-03-24

    申请人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    发明人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    IPC分类号： A61K31/165 ,  C07C237/06 ,  C07C237/22 ,  C07C237/20 ,  C07C231/02

    CPC分类号： C07C237/06 ,  C07B2200/07 ,  C07C237/22 ,  C07C2601/04

    摘要： Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t-butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro-demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.

    摘要翻译： 苯基环丁基酰胺衍生物及其光学异构体，其制备方法及其用途，其包括式（I）化合物，其纯立体异构体及其药学上可接受的盐。 式（I）中，R为H，甲酰基，乙酰基，卤代乙酰基，苯甲酰基，苄氧基羰基（Cbz），叔丁氧羰基（Boc）或9-芴基甲氧基羰基（Fmoc）。 本发明新型化合物具有药物活性，并通过外消旋，左旋或右旋甲基西布曲明和外消旋或D / L异亮氨酸在温和条件下进行缩合反应制备。 证明本发明化合物对不同程度的肥胖模式大鼠具有减肥效果，并且通过动物实验效果优于西布曲明。 因此，本发明化合物制备的药物或通过本发明化合物的组合物和其它药物活性化合物制备的药物可用于治疗肥胖症。

    Phenylcyclobutylamide derivatives and their stereoisomers, the preparation processes and uses thereof
    3.
    发明授权
    Phenylcyclobutylamide derivatives and their stereoisomers, the preparation processes and uses thereof 有权
    苯基环丁基酰胺衍生物及其立体异构体，其制备方法和用途

    公开(公告)号：US08673981B2

    公开(公告)日：2014-03-18

    申请号：US13926653

    申请日：2013-06-25

    申请人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    发明人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    IPC分类号： A61K31/165 ,  A61P3/04

    CPC分类号： C07C237/06 ,  C07B2200/07 ,  C07C237/22 ,  C07C2601/04

    摘要： Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t-butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro-demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.

    摘要翻译： 苯基环丁基酰胺衍生物及其光学异构体，其制备方法及其用途，其包括式（I）化合物，其纯立体异构体及其药学上可接受的盐。 式（I）中，R为H，甲酰基，乙酰基，卤代乙酰基，苯甲酰基，苄氧基羰基（Cbz），叔丁氧羰基（Boc）或9-芴基甲氧基羰基（Fmoc）。 本发明新型化合物具有药物活性，并通过外消旋，左旋或右旋甲基西布曲明和外消旋或D / L异亮氨酸在温和条件下的缩合反应制备。 证明本发明化合物对不同程度的肥胖模式大鼠具有减肥效果，并且通过动物实验效果优于西布曲明。 因此，本发明化合物制备的药物或通过本发明化合物的组合物和其它药物活性化合物制备的药物可用于治疗肥胖症。

    PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND THEIR STEREOISOMERS, THE PREPARATION PROCESSES AND USES THEREOF
    4.
    发明申请
    PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND THEIR STEREOISOMERS, THE PREPARATION PROCESSES AND USES THEREOF 有权
    苯甲酰胺衍生物及其立体异构体，其制备方法及其用途

    公开(公告)号：US20130289124A1

    公开(公告)日：2013-10-31

    申请号：US13926653

    申请日：2013-06-25

    申请人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    发明人： Shuqiang Zhao ,  Shouming Wen ,  Hao Ding ,  Yashi Yan ,  Xiaoping Chen

    IPC分类号： C07C237/06

    CPC分类号： C07C237/06 ,  C07B2200/07 ,  C07C237/22 ,  C07C2601/04

    摘要： Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t-butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro-demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.

    摘要翻译： 苯基环丁基酰胺衍生物及其光学异构体，其制备方法及其用途，其包括式（I）化合物，其纯立体异构体及其药学上可接受的盐。 式（I）中，R为H，甲酰基，乙酰基，卤代乙酰基，苯甲酰基，苄氧基羰基（Cbz），叔丁氧羰基（Boc）或9-芴基甲氧基羰基（Fmoc）。 本发明新型化合物具有药物活性，并通过外消旋，左旋或右旋甲基西布曲明和外消旋或D / L异亮氨酸在温和条件下的缩合反应制备。 证明本发明化合物对不同程度的肥胖模式大鼠具有减肥效果，并且通过动物实验效果优于西布曲明。 因此，本发明化合物制备的药物或通过本发明化合物的组合物和其它药物活性化合物制备的药物可用于治疗肥胖症。