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    • 30. 发明授权
    • Tetrahydronaphthyl and cyclopropyl substituted 1,3-butadienes having
retinoid-like activity
    • 四氢萘基和具有类视黄醇样活性的环丙基取代的1,3-丁二烯
    • US5344959A
    • 1994-09-06
    • US63540
    • 1993-05-18
    • Roshantha A. Chandraratna
    • Roshantha A. Chandraratna
    • C07C13/44C07C13/45C07C13/47C07C17/16C07C22/04C07C25/24C07C33/30C07C33/38C07C45/29C07C45/46C07C47/238C07C47/453C07C49/225C07C49/563C07C49/792C07C61/39C07C69/743C07C69/753C07F9/54C07C69/76C07C63/36
    • C07F9/5428C07C17/16C07C33/30C07C45/292C07C45/46C07C49/792C07C61/39C07C69/743
    • Compounds of the formula ##STR1## wherein m is 1-4; R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; 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 aklylphenyl, 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, have retinoid-like activity.
    • 其中m为1-4的式的化合物: R1-R4独立地是氢,1至6个碳的低级烷基,C1,Br或I; R5是氢,1-6个碳的低级烷基,C1-6的低级烷氧基或低级烷氧基; R6是氢,低级烷基,Cl,Br,I,OR11,SR11,OCOR11,SCOR11,NH2,NHR11,N(R11)2,NHCOR11或NR11-COR11; R 20独立地是氢或低级烷基; 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,-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 1〜10个碳原子的环烷基或5-10个碳原子的环烷基,或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,具有 类视黄醇样活性。