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公开(公告)号:US5238937A
公开(公告)日:1993-08-24
申请号:US802093
申请日:1991-12-04
IPC分类号: A61K31/435 , A61K31/35 , A61K31/395 , A61K31/443 , A61K31/4433 , A61K31/495 , A61K31/50 , A61K31/501 , A61K31/505 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , C07D405/12
CPC分类号: C07D405/12
摘要: The invention relates to novel chroman derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 have the meanings given in [Patent claim 1], and which, like their salts, show effects on the cardiovascular system and can be used for the treatment or prophylaxis of cardiac insufficiency, angina pectoris, high blood pressure, incontinence and alopecia.
摘要翻译: 本发明涉及式I的新的苯并二氢吡喃衍生物,其中R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8和R 9具有[权利要求1]中给出的含义, 盐对心血管系统产生影响,可用于治疗或预防心功能不全,心绞痛,高血压,失禁和秃发。
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公开(公告)号:US5013853A
公开(公告)日:1991-05-07
申请号:US347710
申请日:1989-05-05
IPC分类号: A61K31/44 , A61K31/443 , A61K31/495 , A61K31/50 , A61K31/505 , A61P9/00 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P21/02 , C07D311/22 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D493/04
CPC分类号: C07D405/04 , C07D311/22 , C07D405/10 , C07D405/12 , C07D405/14 , C07D493/04
摘要: A compound of the formula: ##STR1## where in x-y is --CO--CH.sub.2 --, --COCR.sup.10-, --CHOHCHR.sup.8-, --CH.dbd.CR.sup.8 -- or ##STR2## and R.sup.9 is various, R.sup.1 and R.sup.8 are alkyl, R.sub.2 is H or alkyl and R.sup.1 and R.sup.2 are alkylene, are disclosed as useful as intermediates for cardiovascular agents.
摘要翻译: 下式的化合物:其中在xy是-CO-CH 2 - ,-COCR 10 - , - CHOHCHR 8 - , - CH = CR 8 - 或
和R 9是各种,R 1和R 8是烷基,R 2是H 或烷基,R 1和R 2为亚烷基,可用作心血管药物的中间体。 -
公开(公告)号:US5132307A
公开(公告)日:1992-07-21
申请号:US432836
申请日:1989-11-07
IPC分类号: C07D237/14 , A61K31/44 , A61K31/4402 , A61K31/4412 , A61K31/4418 , A61K31/4425 , A61K31/495 , A61K31/50 , A61K31/505 , A61P9/06 , A61P9/12 , A61P11/00 , A61P17/00 , C07D207/38 , C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D237/16 , C07D237/18 , C07D237/24 , C07D239/36 , C07D239/54 , C07D241/18
CPC分类号: C07D213/69 , C07D213/64 , C07D213/70 , C07D213/74 , C07D237/16 , C07D237/18
摘要: New tetralin derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 and Z have the meanings indicated herein and salts thereof, exhibit an effect on the cardiovascular system.
摘要翻译: 式Ⅰ的新的四氢化萘衍生物,其中R1至R8和Z具有本文所述的含义及其盐,对心血管系统表现出影响。
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公开(公告)号:US4931454A
公开(公告)日:1990-06-05
申请号:US248502
申请日:1988-09-23
IPC分类号: A61K31/44 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D491/04 , C07D491/052 , C07D491/107 , C07D491/153
CPC分类号: C07D491/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US5130322A
公开(公告)日:1992-07-14
申请号:US562542
申请日:1990-08-03
IPC分类号: C07D311/22 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/50 , A61P9/08 , A61P9/10 , A61P25/02 , C07D311/58 , C07D311/68 , C07D405/04 , C07D405/12 , C07D493/04
CPC分类号: C07D405/04
摘要: The invention relates to chroman derivatives of the formula I ##STR1## in which R.sup.1 is A,R.sup.2 is OA,R.sup.3 is OH,R.sup.4 is H, orR.sup.3 and R.sup.4 together are a bond,R.sup.5 is a 2-oxo-1,2-dihydro-1-pyridyl or 2-oxo-2,3-dihydro-4-pyrodyl radical which is optionally monosubstituted by A,R.sup.6 is CN,R.sup.7 and R.sup.8 are each H,Z is O, NH or a bond, andA is alkyl having 1-6 C atoms,or a physiologically acceptable salt thereof.
摘要翻译: 本发明涉及式Ⅰ的苯并二氢吡喃衍生物,其中R1是A,R2是OA,R3是OH,R4是H,或R3和R4同时是一个键,R5是2-氧代-1, 任选被A,R6单取代的2-二氢-1-吡啶基或2-氧代-2,3-二氢-4-烟酰基是CN,R 7和R 8各自为H,Z为O,NH或键,并且 A是具有1-6个C原子的烷基,或其生理上可接受的盐。
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公开(公告)号:US5112839A
公开(公告)日:1992-05-12
申请号:US549043
申请日:1990-07-06
IPC分类号: A61K31/35 , A61K31/44 , A61K31/443 , A61P9/12 , A61P25/02 , C07D405/04
CPC分类号: C07D405/04
摘要: Novel chroman derivatives of the formula I ##STR1## in which R.sup.1 to R.sup.10 have the meanings given in patent claim 1, and their salts show effects on the cardiovascular system and can be used for the treatment or prophylaxis of cardiac insufficiency, angina pectoris, high blood pressure, incontinence and alopecia.
摘要翻译: R1至R10具有权利要求1中给出的含义的式I
的新型苯并二氢吡喃衍生物及其盐显示对心血管系统的作用,可用于治疗或预防心功能不全,心绞痛,高 血压,失禁和脱发。 -
公开(公告)号:US5232944A
公开(公告)日:1993-08-03
申请号:US870749
申请日:1992-04-20
IPC分类号: C07D311/22 , C07D311/68 , C07D407/12 , C07D409/12
CPC分类号: C07D407/12 , C07D311/22 , C07D311/68 , C07D409/12
摘要: 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.
摘要翻译: 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。 -
公开(公告)号:US5143924A
公开(公告)日:1992-09-01
申请号:US555700
申请日:1990-07-23
IPC分类号: C07D311/58 , A61K31/35 , A61K31/352 , A61K31/435 , A61K31/44 , A61K31/443 , A61K31/495 , A61K31/50 , A61K31/505 , A61P9/08 , A61P9/10 , A61P25/02 , C07D311/22 , C07D311/68 , C07D405/04 , C07D405/12
CPC分类号: C07D405/04 , C07D311/22 , C07D405/12
摘要: Novel chroman derivatives of the formula I ##STR1## in which R.sup.1 to R.sup.6 and Z have the meanings given in Patent Claim 1, and their salts show effects on the cardiovascular system and can be used for the treatment or prophylaxis of cardiac insufficiency, angina pectoris, high blood pressure, incontinence and alopecia.
摘要翻译: R1至R6和Z具有权利要求1中给出的含义的式I(I)的新型色氨酸衍生物,其盐显示对心血管系统的作用,可用于治疗或预防心功能不全 ,心绞痛,高血压,失禁和脱发。
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公开(公告)号:US5112972A
公开(公告)日:1992-05-12
申请号:US531490
申请日:1990-05-31
申请人: Rolf Gericke , Manfred Baumgarth , Ingeborg Lues , Rolf Bergmann , De Peyer
发明人: Rolf Gericke , Manfred Baumgarth , Ingeborg Lues , Rolf Bergmann , De Peyer
CPC分类号: C07D405/12
摘要: 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.
摘要翻译: 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。
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10.
公开(公告)号:US5036068A
公开(公告)日:1991-07-30
申请号:US440622
申请日:1989-11-22
IPC分类号: A61K31/535 , A61P9/12 , A61P21/02 , C07D413/04 , C07D413/12
CPC分类号: C07D413/04 , C07D413/12
摘要: Novel benzoxazine derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.5 have the meanings defined herein, and salts thereof, exhibit effects on the cardiovascular system.
摘要翻译: 式I的新型苯并恶嗪衍生物其中R 1至R 5具有本文定义的含义及其盐对心血管系统具有影响。
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