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    • 3. 发明授权
    • Azachroman derivatives with effects on the cardiovascular system
    • 偶氮染料衍生物对心血管系统有影响
    • US4931454A
    • 1990-06-05
    • US248502
    • 1988-09-23
    • Manfred BaumgarthRolf GerickeIngeborg LuesJacques De PeyerRolf Bergmann
    • Manfred BaumgarthRolf GerickeIngeborg LuesJacques De PeyerRolf Bergmann
    • A61K31/44A61P9/08A61P9/10A61P9/12A61P25/02C07D491/04C07D491/052C07D491/107C07D491/153
    • C07D491/04
    • An azachroman derivative of the formula ##STR1## wherein Z is(a) --N.dbd.CH--CH.dbd.CH--,(b) --CH.dbd.N--CH.dbd.CH--,(c) --CH.dbd.CH--N.dbd.CH-- or(d) --CH.dbd.CH--CH.dbd.N--;R.sup.1 is A,R.sup.2 is H or A, orR.sup.1 and R.sup.2 together are alkylene with 3-6 C atoms;R.sup.3 is OH or OAc,R.sup.4 is H, orR.sup.3 and R.sup.4 together are a bond;R.sup.5 is 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl, or 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl mono- or disubstituted by A, F, Cl, Br, I, OH, OA, OAc, NO.sub.2, NH.sub.2, AcNH, HOOC or AOOC;A is C.sub.1-6 -alkyl andAc is C.sub.1-18 -alkanoyl or C.sub.7-11 -aroyl;or a pharmaceutically acceptable salt thereof is claimed. This compound exhibits vasodilatory and anti-hypertensive effects and is suitable for the treatment of alopecia.
    • 其中Z是(a)-N = CH-CH = CH-,(b)-CH = N-CH = CH-,(c)-CH = CH-N = CH- 或(d)-CH = CH-CH = N-; R1是A,R2是H或A,或者R1和R2一起是3-6个碳原子的亚烷基; R3是OH或OAc,R4是H或R3和R4一起是键; R5是1H-2-吡啶酮-1-基,1H-6-哒嗪酮-1-基,1H-2-嘧啶酮-1-基,1H-6-嘧啶酮-1-基,1H-2-吡嗪酮-1-基, 或1H-2-吡啶酮-1-基或1H-2-吡啶酮-1-基,1H-6-哒嗪酮-1-基,1H-2-嘧啶酮-1-基,1H-6-嘧啶酮-1 由A,F,Cl,Br,I,OH,OA,OAc,NO 2,NH 2,AcNH,HOOC单取代或被二取代的1H-2-吡嗪酮-1-基或1H-2-硫代吡啶-1-基 或AOOC; A是C 1-6 - 烷基,Ac是C 1-18 - 烷酰基或C 7-11 - 芳酰基; 或其药学上可接受的盐。 该化合物具有血管扩张和抗高血压作用,适用于治疗脱发。
    • 6. 发明授权
    • Chroman derivatives
    • 色原衍生物
    • US5232944A
    • 1993-08-03
    • US870749
    • 1992-04-20
    • Rolf GerickeManfred BaumgarthIngeborg LuesJacques De PeyerRolf Bergmann
    • Rolf GerickeManfred BaumgarthIngeborg LuesJacques De PeyerRolf Bergmann
    • C07D311/22C07D311/68C07D407/12C07D409/12
    • C07D407/12C07D311/22C07D311/68C07D409/12
    • Novel chroman derivatives of the formula I ##STR1## in which X is O or NR.sup.11,Z is CH.sub.2, O, S or CHHal,R.sup.1 and R.sup.5 are each A,R.sup.2 is H or A,R.sup.1 and R.sup.2 together are also alkylene having 3-6 C atoms,R.sup.3 is OH or OAc,R.sup.4 is H,R.sup.3 and R.sup.4 together are also a bond,R.sup.6 and R.sup.7 are each H, A, HO, AO, CHO, ACO, ACS, HOOC, AOOC, AO--CS, ACOO, A--CS--O, hydroxyalkyl, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, ASO, ASO.sub.2, AO--SO, AO--SO.sub.2, AcNH, AO--CO--NH, H.sub.2 NSO, HANSO, A.sub.2 NSO, H.sub.2 NSO.sub.2, HANSO.sub.2, A.sub.2 NSO.sub.2, H.sub.2 NCO, HANCO, A.sub.2 NCO, H.sub.2 NCS, HANCS, A.sub.2 NCS, ASONH, ASO.sub.2 NH, AOSONH, AOSO.sub.2 NH, ACO-alkyl, nitro-alkyl, cyanoalkyl, A--C(.dbd.NOH) or A--C(.dbd.NNH.sub.2),R.sup.8 and R.sup.9 are each H or A or together are .dbd.O or .dbd.S,R.sup.10 is H, Hal, CHO or CH.sub.2 OH,R.sup.11 is H, A, Ac or CH.sub.2 OH,m is 1, 2 or 3,Hal is F, Cl, Br or I,A is alkyl having 1-6 C atoms,-alkyl is alkylene having 1-6 C atoms andAc is alkanoyl having 1-8 C atoms or aroyl having 7-11 C atoms,and their salts show effects on the cardiovascular system.
    • 式I 的新型色满衍生物,其中X为O或NR11,Z为CH2,O,S或CHHal,R1和R5各自为A,R2为H或A,R1和R2一起也为3 -6个C原子,R3是OH或OAc,R4是H,R3和R4同时也是键,R6和R7分别是H,A,HO,AO,CHO,ACO,ACS,HOOC,AOOC,AO-CS ,ACOO,A-CS-O,羟烷基,NO2,NH2,NHA,NA2,CN,F,Cl,Br,I,CF3,ASO,ASO2,AO-SO,AO-SO2,AcNH,AO-CO-NH ,H2NSO,HANSO2,A2NSO,H2NCO,HANCO,A2NCO,H2NCS,HANCO,A2NCS,H2NCS,HANCS,A2NCS,ASONH,ASO2NH,AOSONH,AOSO2NH,ACO-烷基,硝基 - 烷基,氰基烷基,AC(= NOH) (= NNH 2),R 8和R 9各自为H或A或一起为= O或= S,R 10为H,Hal,CHO或CH 2 OH,R 11为H,A,Ac或CH 2 OH,m为1,2或3, Hal是F,Cl,Br或I,A是具有1-6个C原子的烷基, - 烷基是具有1-6个C原子的亚烷基,Ac是具有1-8个C原子的烷酰基或具有7-11个C原子的芳酰基,以及 它们的盐显示对心血管系统的影响。