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发明授权
US5677451A Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity 失效
具有异双环基团的二取代乙炔和具有类视黄醇样活性的杂芳族或苯基

Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
摘要：
Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N-R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub. 2OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR11OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.9 is lower alkyl, R.sub.10 is divalent alkyl radical of 2-5 carbons and R.sub.11 is alkyl, cycloalkyl or alkenyl containing 1 to 5 carbons, have retinoic acid like activity.
摘要（中）：

其中R 1和R 2独立地为具有2至8个碳原子的烷基; R3是氢或低级烷基; X是S，O或N-R4，其中R4是氢或低级烷基; Y是苯基或吡啶基，噻吩基，呋喃基，哒嗪基，嘧啶基和吡嗪基; A是（CH 2）n，其中n是0-5，或低级支链烷基，具有2-6个碳的烯基和1或2个双键，具有2至6个碳的炔基和1或2个三键; B是氢，COOH或其盐，COOR5，CONR6R7，-CH2OH，CH2OR8，CH2OCOR8，CHO，CH（OR9）2，CHOR10O，-COR11，CR11（OR9）2或CR11OR10O，其中R5是1〜 10个碳原子或5至10个碳原子的环烷基，或R5为苯基或低级烷基苯基，R6和R7独立地为氢，1至10个碳原子的烷基或5至10个碳原子的环烷基，或苯基或低级烷基苯基，R8为烷基 1〜10个碳原子，苯基或低级烷基苯基，R9为低级烷基，R10为2-5个碳原子的二价烷基，R11为含1〜5个碳原子的烷基，环烷基或烯基，具有视黄酸类活性。

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