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公开(公告)号:EP0294973A1
公开(公告)日:1988-12-14
申请号:EP88304852.2
申请日:1988-05-27
IPC分类号: C07D233/84 , A61K31/415
CPC分类号: C07D233/84
摘要: Compounds of the formula (I):
wherein X is H, F, Cl, Br, I, C₁₋₄alkyl, CN, NO₂, SO₂NH₂, COOH, OH, CHO, C₁₋₄alkoxy, CH₂OH, CH₂OC₁₋₄alkyl, CF₃, C₂F₅, C₃F₇, SO₂CH₃, SO₂CF₃, or CO₂C a H 2a+1 wherein a is 1-5, or any accessible combination thereof of up to 5 substituents; R and R′ independently are H or C₁₋₄alkyl; and n is 1-5; or any pharmaceutically acceptable salt or hydrate thereof, processes for their preparation; intermediates used in their preparation; compositions containing them and their use in therapy as dopamine-β-hydroxylase inhibitors.摘要翻译: 式(I)化合物:其中X是H,F,Cl,Br,I,C 1-4烷基,CN,NO 2,SO 2 NH 2,COOH,OH,CHO,C 1-4烷氧基,CH 2 OH,CH 2 OC 1-4烷基, CF3,C2F5,C3F7,SO2CH3,SO2CF3或CO2CaH2a + 1,其中a为1-5,或其任何可接受的至多5个取代基的组合; R和R min独立地是H或C 1-4烷基; n为1-5; 或其任何药学上可接受的盐或水合物,其制备方法; 用于制备的中间体; 含有它们的组合物及其在治疗中作为多巴胺-β-羟化酶抑制剂的用途。
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公开(公告)号:EP0225718A3
公开(公告)日:1988-03-30
申请号:EP86308481
申请日:1986-10-30
IPC分类号: C07D249/12 , A61K31/41 , C07C159/00
CPC分类号: C07D249/12
摘要: Compounds of formula
in which:
n is 0-5; R is hydrogen or C 1-4 alkyl; and X is hydrogen, halo, C 1-4 alkyl, CN, N0 2 S0 2 NH 2 , COOH, CHO, OH, CH 2 0H, C 1-4 alkoxy, CF 3 , S0 2 CH 3 , S0 2 CF 3 , or CO 2 C a H 2a+1 where a is 1-5, or any accessible combination thereof of up to 5 substituents; processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine-β-hydroxylase inhibitors.摘要翻译: 下式的化合物其中:n是0-5; R是氢或C 1-4烷基; 和X是氢,卤素,C 1-4烷基,CN,NO 2,SO 2 NH 2,COOH,CHO,OH,CH 2 OH,C 1-4烷氧基,CF 3,SO 2 CH 3,SO 2 CF 3或CO 2 CaH 2 a + 至多5个取代基的组合; 它们的制备方法,用于其制备的中间体,含有它们的药物组合物以及它们作为多巴胺-β-羟化酶抑制剂在治疗中的用途。
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公开(公告)号:EP0323737A1
公开(公告)日:1989-07-12
申请号:EP88312197.2
申请日:1988-12-22
IPC分类号: C07D249/12 , C07C159/00 , A61K31/41
CPC分类号: C07D249/12 , C07C335/40
摘要: Compounds of formula (I)
and pharmaceutically acceptable salts thereof are described in which, n is 0 to 5; X¹ to X⁵ are any accessible combination of hydrogen, halogen, C₁₋₆alkyl, C₁₋₆alkoxy, cyano, nitro, SONH₂, SO₂NH₂, SO₂CH₃, SO₂CH₂F, SO₂CHF₂, SO₂CF₃, CF₃, CHO, OH, CH₂OH, CO₂H, or CO₂C p H 2p+1 wherein p is 1 to 4; R¹ is phenyl substituted by X¹ to X⁵, C₁₋₄alkyl, C₃₋₆cycloalkyl, or an arylC₁₋₄alkyl group substituted by X¹ to X⁵; R² is hydrogen, C₁₋₄alkyl or (CH₂) m -CO₂R³; m is 0 to 5; and R³ is H or C₁₋₄alkyl.
These compounds are dopamine-β-hydroxylase inhibitors. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of these compounds are described.摘要翻译: 描述式(I)化合物
及其药学上可接受的盐,其中n为0至5; X 1〜X 5是氢,卤素,C 1-6烷基,C 1-6烷氧基,氰基,硝基,SONH 2,SO 2 NH 2,SO 2 CH 3,SO 2 CH 2 F,SO 2 CHF 2,SO 2 CF 3,CF 3,CHO,OH,CH 2 OH, CO2H或CO2CpH2p + 1,其中p为1至4; R 1是被X 1取代的苯基,X 5,C 1-4烷基,C 3-6环烷基或被X 1至X 5取代的芳基C 1-4烷基; R 2是氢,C 1-4烷基或(CH 2)m -CO 2 R 3; m为0〜5; 且R 3为H或C 1-4烷基。 这些化合物是多巴胺-β-羟化酶抑制剂。 药物组合物被描述为使用的方法。 描述了这些化合物的制备方法。 -
公开(公告)号:EP0246888A3
公开(公告)日:1988-09-28
申请号:EP87304504
申请日:1987-05-20
IPC分类号: C07D249/12 , A61K31/41 , C07C133/02 , C07C159/00
CPC分类号: C07D249/12
摘要: Compounds of Formula :
in which n is 0 to 5, R is hydrogen or C 1-4 alkyl and X is hydrogen, halo, C 1-4 alkyl, CN, NO₂, SO₂NH₂, COOH, CHO, OH, CH₂OH, C 1-4 alkoxy, CF₃, SO₂CH₃, SO₂CF₃ or CO₂C a H 2a+1 wherein a is 1 to 5 or any synthetically accessible combination thereof of up to 5 substituents or any pharmaceutically acceptable salt or hydrate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine β-hydroxylase inhibitors.摘要翻译: 式中n为0-5,R为氢或C1-4烷基,X为氢,卤素,C1-4烷基,CN,NO2,SO2NH2,COOH,CHO,OH,CH2OH,C1-4烷氧基,CF3, SO 2 CH 3,SO 2 CF 3或CO 2 CaH 2 a + 1,其中a为1至5或至多5个取代基的任何可合成获得的组合,或其任何药学上可接受的盐或水合物,其制备方法,含有它们的药物组合物以及它们作为多巴胺β - 羟化酶抑制剂。
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公开(公告)号:EP0246888A2
公开(公告)日:1987-11-25
申请号:EP87304504.1
申请日:1987-05-20
IPC分类号: C07D249/12 , A61K31/41 , C07C133/02 , C07C159/00
CPC分类号: C07D249/12
摘要: Compounds of Formula :
in which n is 0 to 5, R is hydrogen or C 1-4 alkyl and X is hydrogen, halo, C 1-4 alkyl, CN, NO₂, SO₂NH₂, COOH, CHO, OH, CH₂OH, C 1-4 alkoxy, CF₃, SO₂CH₃, SO₂CF₃ or CO₂C a H 2a+1 wherein a is 1 to 5 or any synthetically accessible combination thereof of up to 5 substituents or any pharmaceutically acceptable salt or hydrate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine β-hydroxylase inhibitors.摘要翻译: 化合物:其中n为0至5,R为氢或C 1-4烷基,X为氢,卤素,C 1-4烷基,CN,NO 2,SO 2 NH 2,COOH,CHO,OH,CH 2 OH,C 1-4烷氧基 ,CF3,SO2CH3,SO2CF3或CO2CaH2a + 1,其中a为1-5或其最多5个取代基的任何合成可及的组合或其任何药学上可接受的盐或水合物,其制备方法,含有它们的药物组合物及其在治疗中的用途 作为多巴胺β-羟化酶抑制剂。
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公开(公告)号:EP0284375A1
公开(公告)日:1988-09-28
申请号:EP88302573.6
申请日:1988-03-23
IPC分类号: C07D233/84 , C07C233/02 , A61K31/415
CPC分类号: C07D233/90
摘要: Compounds of formula (I) :
in which X is H, F, Cl, Br, I, C₁₋₄alkyl, CN, NO₂, SO₂NH₂, COOH, CHO, C₁₋₄alkoxy, CH₂OH, CF₃, SO₂CH₃, SO₂CF₃ or CO₂C a H 2a+1 wherein a is 1-5; n is 0-5; R is hydrogen or C₁₋₄alkyl, and R¹ is OH or NHC₁₋₄alkylNH₂; and pharmaceutically acceptable salts or hydrates thereof, processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine-β-hydroxylase inhibitors.摘要翻译: 式(I)化合物:其中X是H,F,Cl,Br,I,C 1-4烷基,CN,NO 2,SO 2 NH 2,COOH,CHO,C 1-4烷氧基,CH 2 OH,CF 3,SO 2 CH 3,SO 2 CF 3或 C 2 H 2a = 1,其中a为1-5; n为0-5; R是氢或C 1-4烷基,R 1是OH或NHC 1-4烷基NH 2; 及其药学上可接受的盐或水合物,其制备方法,可用于其制备的中间体,含有它们的药物组合物及其在治疗中作为多巴胺-β-羟化酶抑制剂的用途。
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公开(公告)号:EP0261804A1
公开(公告)日:1988-03-30
申请号:EP87307511.3
申请日:1987-08-25
IPC分类号: C07D249/12 , C07D295/14 , A61K31/41
CPC分类号: C07D295/15 , C07D249/12
摘要: Compounds of Formula (I):
in which X is H, F, Cl, Br, I, C 1-4 alkyl, CN NO₂, SO₂NH₂, COOH, OH, CHO, C 1-4 alkoxy, CH₂OH, CF₃, SO₂CH₃, SO₂CF₃, or CO₂C a H 2a+1 wherein a is 1-5, or any synthetically accessible combination thereof of up to 5 substituents, n is 0-5, R and Rʹ independently are H or C 1-4 alkyl, or any pharmaceutically acceptable salt or hydrate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine-β-hydroxylase inhibitors.摘要翻译: 式(I)化合物:其中X为H,F,Cl,Br,I,C 1-4烷基,CN NO 2,SO 2 NH 2,COOH,OH,CHO,C 1-4烷氧基,CH 2 OH,CF 3,SO 2 CH 3 ,SO 2 CF 3或CO 2 C a H 2a + 1,其中a为1-5,或其任何合成可及的至多5个取代基的组合,n为0-5,R和R'独立地为H或C 1-4烷基,或任何药学上 可接受的盐或其水合物,其制备方法,含有它们的药物组合物及其在治疗中作为多巴胺-β-羟化酶抑制剂的用途。
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公开(公告)号:EP0225718A2
公开(公告)日:1987-06-16
申请号:EP86308481.0
申请日:1986-10-30
IPC分类号: C07D249/12 , A61K31/41 , C07C159/00
CPC分类号: C07D249/12
摘要: Compounds of formula
in which:
n is 0-5;
R is hydrogen or C 1-4 alkyl; and
X is hydrogen, halo, C 1-4 alkyl, CN, N0 2 S0 2 NH 2 , COOH, CHO, OH, CH 2 0H, C 1-4 alkoxy, CF 3 , S0 2 CH 3 , S0 2 CF 3 , or CO 2 C a H 2a+1 where a is 1-5, or any accessible combination thereof of up to 5 substituents; processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine-β-hydroxylase inhibitors.摘要翻译: 式中的化合物
...其中:... n为0-5; ... R为氢或C1-4烷基; 和... X是氢,卤素,C 1-4烷基,CN,NO 2 SO 2 NH 2,COOH,CHO,OH,CH 2 OH,C 1-4烷氧基,CF 3,SO 2 CH 3,SO 2 CF 3或CO 2 C a H 2a + 1,其中a是1-5, 最多5个取代基的可及组合; 其制备方法,可用于其制备的中间体,含有它们的药物组合物及其在治疗中作为多巴胺-β-羟化酶抑制剂的用途。
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