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177 条记录 (耗时 0.054 秒)

    [4-(1,2-epoxycyclohexanyl)but-3-en-1-ynyl]aromatic and heteroaromatic acids and derivatives having retinoid-like biological activity
    92.
    发明授权
    [4-(1,2-epoxycyclohexanyl)but-3-en-1-ynyl]aromatic and heteroaromatic acids and derivatives having retinoid-like biological activity 失效
    [4-（1,2-环氧环己烷基）丁-3-烯-1-炔基]芳族和杂芳族酸和具有类视黄醇样生物活性的衍生物

    公开(公告)号：US5426118A

    公开(公告)日：1995-06-20

    申请号：US177620

    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 ,  C07D303/40 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  A61K31/44

    CPC分类号： C07D303/38 ,  C07D303/40 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06

    摘要： Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.7 are hydrogen, lower alkyl of 1-6 carbons, or halogen;Y is phenyl, pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl;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.14, CR.sub.14 (OR.sub.12).sub.2, or CR.sub.14 OR.sub.13 O, where 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, R.sub.13 is divalent alkyl radical of 2-5 carbons and R.sub.14 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, have retinoid-like biological activity.

    摘要翻译： 式1化合物其中R 1 -R 7是氢，1-6个碳的低级烷基或卤素; Y是苯基，吡啶基，呋喃基，噻吩基，哒嗪基，嘧啶基，吡嗪基，噻唑基或恶唑基; 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，-COR14，CR14（OR12）2或CR14OR13O，其中R8是烷基 1〜10个碳原子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分别独立地为氢，碳原子数1〜10的烷基或5-10个碳原子的环烷基 或苯基或低级烷基苯基，R 11为低级烷基，苯基或低级烷基苯基，R 12为低级烷基，R 13为2-5个碳原子的二价烷基，R 14为含有1至5个碳原子的烷基，环烷基或烯基，具有类视黄醇 类生物活性。

    Methods of treatment with compounds having RAR&agr; receptor specific or selective activity
    98.
    发明授权
    Methods of treatment with compounds having RAR&agr; receptor specific or selective activity 失效
    用具有RARα受体特异性或选择性活性的化合物治疗的方法

    公开(公告)号：US06610744B2

    公开(公告)日：2003-08-26

    申请号：US09998358

    申请日：2001-11-29

    申请人： Min Teng ,  Tien T. Duong ,  Roshantha A. Chandraratna

    发明人： Min Teng ,  Tien T. Duong ,  Roshantha A. Chandraratna

    IPC分类号： A61K31195

    CPC分类号： A61K31/353 ,  A61K31/203 ,  A61K31/44 ,  G01N25/4866

    摘要： Retinoid compounds which act specifically or selectively on RAR&agr; receptor subtypes in preference over RAR&bgr; and RAR&Ggr; receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.

    摘要翻译： 与RARbeta和RARGAMMA受体亚型相比，RARα受体亚型特异性或选择性地起作用的类视色素化合物具有与类维生素A相关的理想药学性质，特别适用于治疗肿瘤，如急性单核细胞白血病，子宫颈癌，骨髓瘤，卵巢癌 和头颈部癌，而不具有类维生素A的一种或多种不期望的副作用，例如诱导体重减轻，皮肤粘膜毒性，皮肤刺激和致畸性。