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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。
    • 8. 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。
    • 10. 发明授权
    • Synthesis of chroman derivatives
    • 色氨酸衍生物的合成
    • US5112972A
    • 1992-05-12
    • US531490
    • 1990-05-31
    • Rolf GerickeManfred BaumgarthIngeborg LuesRolf BergmannDe Peyer
    • Rolf GerickeManfred BaumgarthIngeborg LuesRolf BergmannDe Peyer
    • A61K31/44A61K31/50A61P9/00A61P9/08A61P9/10A61P9/12A61P25/02C07D405/12
    • C07D405/12
    • The invention relates to new chroman derivatives of the formula I ##STR1## in which R.sup.1 is A,R.sup.2 and R.sup.8 are each H or A,R.sup.1 and R.sup.2 together are also alkylene with 3-6 C atoms,R.sup.3 is OH, OA or OAc,R.sup.4 is H,R.sup.3 and R.sup.4 together are also a bond,R.sup.5 is Ar or C.sub.n H.sub.2n -R.sup.9,R.sup.9 is alkenyl or alkynyl with 2-4 C atoms in each case, OH, OA, CHO, CO-A, CS-A, COOH, COOA, COO-alkyl-Ar, CS-OA, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, SA, SO-A, SO.sub.2 -A or Ar,Ar is a phenyl group which is unsubstituted or substituted once or twice by R.sup.10, R.sup.6, R.sup.7 and R.sup.10 are each H, A, HO, AO, CHO, ACO, CF.sub.3 CO, ACS, HOOC, AOOC, AO-CS, ACOO, A-CS-O, hydroxy-alkyl, mercapto-alkyl, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, AS, 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, cyano-alkyl, A-C(.dbd.NOH), A-C(.dbd.NNH.sub.2), H.sub.2 PO.sub.3 or A.sub.2 PO.sub.3,n is 1, 2 or 3,A is alkyl with 1-6 C atoms,-alkyl is alkylene with 1-6 C atoms andAC is alkanoyl with 1-8 C atoms or aroyl with 7-11 C atoms,and the salts thereof which display effects on the cardiovascular system and can be used for the treatment or prophylaxis of heart failure, angina pectoris, high blood pressure, incontinence and alopecia.
    • 本发明涉及式Ⅰ的新的苯并二氢吡喃衍生物,其中R 1是A,R 2和R 8各自是H或A,R 1和R 2一起也是具有3-6个C原子的亚烷基,R 3是OH,OA或OAc R 4是H,R 3和R 4一起也是键,R 5是Ar或C n H 2n-R 9,R 9是每种情况下具有2-4个C原子的链烯基或炔基,OH,OA,CHO,CO-A,CS-A ,COOH,COOA,COO-烷基-Ar,CS-OA,NO2,NH2,NHA,NA2,CN,F,Cl,Br,I,CF3,SA,SO-A,SO2-A或Ar,Ar是 R 10,R 6,R 7和R 10未取代或取代一次或两次的苯基分别为H,A,HO,AO,CHO,ACO,CF 3 CO,ACS,HOOC,AOOC,AO-CS,ACOO,A-CS- O,羟基烷基,巯基烷基,NO2,NH2,NHA,NA2,CN,F,Cl,Br,I,CF3,AS,ASO,ASO2,AO-SO,AO-SO2,AcNH, NH,H2NSO,HANSO,A2NSO,H2NCO,HANCO2,A2NCO,H2NCS,HANCO,A2NCO,H2NCS,HANCS,A2NCS,ASONH,ASO2NH,AOSONH,AOSO2NH,ACO-烷基,硝基 - 烷基,氰基 - 烷基,AC(= NOH ),AC(= NNH 2),H 2 PO 3或A 2 PO 3,n为1,2或3,A为具有1-6个C原子的烷基, - 烷基为亚烷基 1-6个C原子,AC是具有1-8个C原子的烷酰基或7-11个C原子的芳酰基及其对心血管系统有影响的盐,可用于治疗或预防心力衰竭,心绞痛 ,高血压,失禁和脱发。