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177 条记录 (耗时 0.026 秒)

    1,2-epoxycyclohexanyl and bicyclic aromatic substituted ethyne compounds having retinoid-like biological activity
    83.
    发明授权
    1,2-epoxycyclohexanyl and bicyclic aromatic substituted ethyne compounds having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的1,2-环氧环己基和双环芳族取代的乙炔化合物

    公开(公告)号：US5451605A

    公开(公告)日：1995-09-19

    申请号：US177621

    申请日：1993-12-30

    申请人： Roshantha A. Chandraratna ,  Richard L. Beard

    发明人： Roshantha A. Chandraratna ,  Richard L. Beard

    IPC分类号： C07D303/38 ,  A61K31/335 ,  A61K31/336 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P17/00 ,  A61P35/00 ,  C07D303/40 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D303/12 ,  A61K31/235 ,  C07D303/17

    CPC分类号： C07D405/06 ,  C07D303/40 ,  C07D407/06 ,  C07D409/06

    摘要： Compounds of the formula ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, and Z is ##STR2## wherein R.sub.6 is hydrogen, lower alkyl of 1-6 carbons, or halogen, R.sub.6 can be attached to any available position on the Z group, and m is an integer between 0 to 4, have retinoid-like biological activity.

    摘要翻译： 其中R 1 -R 5是氢，1-6个碳的低级烷基或卤素的式“IMAGE”的化合物; A是（CH 2）n，其中n是0-5，具有3-6个碳的低级支链烷基，具有3-6个碳的环烷基，具有2-6个碳的烯基和1或2个双键，具有2-6个碳原子的炔基和 1或2个三键; B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12）2或CR7OR13O，其中R7是烷基 ，碳原子数为1〜5的环烷基或烯基，R8为碳原子数为1〜10的烷基或碳原子数为5〜10的环烷基，或R8为苯基或低级烷基苯基，R9和R10分别为氢，烷基 苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，和 Z为，其中R6为氢，1-6个碳的低级烷基或卤素，R6可以连接到Z基团上的任何可用位置，m为0至4之间的整数，具有类视黄醇样生物活性 。

    Compositions and methods for reducing serum glucose and triglyceride levels in diabetic mammals
    84.
    发明授权
    Compositions and methods for reducing serum glucose and triglyceride levels in diabetic mammals 失效
    用于降低糖尿病哺乳动物血清葡萄糖和甘油三酯水平的组合物和方法

    公开(公告)号：US07019034B2

    公开(公告)日：2006-03-28

    申请号：US10738808

    申请日：2003-12-17

    申请人： Yang-Dar Yuan ,  Richard L. Beard ,  Roshantha A. Chandraratna

    发明人： Yang-Dar Yuan ,  Richard L. Beard ,  Roshantha A. Chandraratna

    IPC分类号： C07C69/76 ,  A61K31/19

    CPC分类号： C07C69/734 ,  C07C59/72 ,  C07C2602/10

    摘要： Diabetic mammals are treated with compounds that are significantly more efficacious as agonists of RXRβ retinoid receptors than as agonists of RXRα or RXRγ retinoid receptors. The treatment reduces serum glucose and triglyceride levels of the mammals without the undesirable side effects of reducing serum thyroxine levels and a transient increase in serum triglyceride levels Compounds suitable for use in the methods of treatments of the present invention are selected by testing and identifying compounds of selective or specific efficacy as agonists of RXRβ retinoid receptors in preference over RXRα and/or RXRγ retinoid receptors. Novel compounds used in the methods of the invention have Formula 1 where the variables are defined as disclosed in the specification.

    摘要翻译： 糖尿病哺乳动物用作为RXRα2类视黄醇受体的激动剂比作为RXRα或RXRαγ类视黄醇受体的激动剂显着更有效的化合物治疗 。 该治疗降低了哺乳动物的血清葡萄糖和甘油三酯水平，而没有不利的降低血清甲状腺素水平的副作用和血清甘油三酯水平的瞬时增加。适用于本发明治疗方法的化合物通过测试和鉴定化合物 选择性或特异性的功效优于RXRα和/或RXRαγ类视黄醇受体的RXRβ类视黄醇受体的激动剂。 用于本发明方法的新化合物具有式1，其中变量如说明书中所公开的那样定义。