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    • 1. 发明授权
    • Pyrazolopyrimidinone antianginal agents
    • 吡唑嘧啶酮抗心绞痛药
    • US5346901A
    • 1994-09-13
    • US84827
    • 1993-06-29
    • Andrew S. BellDavid BrownNicholas K. Terrett
    • Andrew S. BellDavid BrownNicholas K. Terrett
    • C07D487/04A61K31/505
    • C07D487/04
    • Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalky)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 -C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.8 or C(NH)NR.sup.7 R.sup.8 ; R.sup.7 and R.sup.8 are each independently H, C.sub.1 -C.sub.4 alkyl, (C.sub.1 -C.sub.3 alkoxy)C.sub.2 -C.sub.4 alkyl or hydroxy C.sub.2 -C.sub.4 alkyl; and pharmaceutically acceptable salts thereof, are selective cGMP PDE inhibitors useful in the treatment of cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.
    • 下式的化合物:其中R 1是H,C 1 -C 3烷基,C 3 -C 5环烷基或C 1 -C 3全氟烷基; R2是H,任选被OH,C1-C3烷氧基或C3-C6环烷基取代的C1-C6烷基,或C1-C3全氟烷基; R3是C1-C6烷基,C3-C6炔基,C3-C6炔基,C3-C7环烷基,C1-C6全氟烷基或(C3-C6环烷基)C1-C6烷基; R4与其所连接的氮原子一起形成吡咯烷基,哌啶子基,吗啉代或4-N-(R6) - 哌嗪基; R5是H,C1-C4烷基,C1-C3烷氧基,NR7R8或CONR7R8; R6是H,C1-C6烷基,(C1-C3烷氧基)C2-C6烷基,羟基C2-C6烷基,(R7R8N)C2-C6烷基,(R7R8NCO)C1-C6烷基,CONR7R8,CSNR7R8或C(NH) NR7R8; R 7和R 8各自独立地为H,C 1 -C 4烷基,(C 1 -C 3烷氧基)C 2 -C 4烷基或羟基C 2 -C 4烷基; 及其药学上可接受的盐是用于治疗心血管疾病如心绞痛,高血压,心力衰竭和动脉粥样硬化的选择性cGMP PDE抑制剂。
    • 2. 发明授权
    • Pyrazolopyrimidinone antianginal agents
    • 吡唑嘧啶酮抗心绞痛药
    • US5250534A
    • 1993-10-05
    • US882988
    • 1992-05-14
    • Andrew S. BellDavid BrownNicholas K. Terrett
    • Andrew S. BellDavid BrownNicholas K. Terrett
    • C07D487/04A61K31/505
    • C07D487/04
    • Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalkyl)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 - C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.8 or C(NH)NR.sup.7 R.sup.8 ; R.sup.7 and R.sup.8 are each independently H, C.sub.1 -C.sub.4 alkyl, (C.sub.1 -C.sub.3 alkoxy)C.sub.2 -C.sub.4 alkyl or hydroxy C.sub.2 -C.sub.4 alkyl; and pharmaceutically acceptable salts thereof, are selective cGMP PDE inhibitors useful in the treatment of cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.
    • 下式的化合物:其中R 1是H,C 1 -C 3烷基,C 3 -C 5环烷基或C 1 -C 3全氟烷基; R2是H,任选被OH,C1-C3烷氧基或C3-C6环烷基取代的C1-C6烷基,或C1-C3全氟烷基; R3是C1-C6烷基,C3-C6烯基,C3-C6炔基,C3-C7环烷基,C1-C6全氟烷基或(C3-C6环烷基)C1-C6烷基; R4与其所连接的氮原子一起形成吡咯烷基,哌啶子基,吗啉代或4-N-(R6) - 哌嗪基; R5是H,C1-C4烷基,C1-C3烷氧基,NR7R8或CONR7R8; R6是H,C1-C6烷基,(C1-C3烷氧基)C2-C6烷基,羟基C2-C6烷基,(R7R8N)C2-C6烷基,(R7R8NCO)C1-C6烷基,CONR7R8,CSNR7R8或C(NH) NR7R8; R 7和R 8各自独立地为H,C 1 -C 4烷基,(C 1 -C 3烷氧基)C 2 -C 4烷基或羟基C 2 -C 4烷基; 及其药学上可接受的盐是用于治疗心血管疾病如心绞痛,高血压,心力衰竭和动脉粥样硬化的选择性cGMP PDE抑制剂。
    • 9. 发明授权
    • Pyridopyrimidinone antianginal agents
    • 吡啶并嘧啶酮抗心绞痛药
    • US5591742A
    • 1997-01-07
    • US379531
    • 1995-01-31
    • Andrew S. BellNicholas K. Terrett
    • Andrew S. BellNicholas K. Terrett
    • A61K31/505A61P9/00A61P9/10A61P9/12A61P43/00C07D471/04A61K31/535A61K31/435C07D413/14C07D487/02
    • C07D471/04
    • Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl CN or CONR.sup.4 R.sup.5 ; R.sup.2 is C.sub.2 -C.sub.4 alkyl; R.sup.3 is SO.sub.2 NR.sup.6 R.sup.7, NO.sub.2, NH.sub.2, NHCOR.sup.8 NHSO.sub.2 R.sup.8 or N(SO.sub.2 R.sup.8).sub.2 ; R.sup.4 and R.sup.5 are each independently selected from H and C.sub.1 -C.sub.4 alkyl; R.sup.6 and R.sup.7 are each independently selected from H and C.sub.1 -C.sub.4 alkyl optionally substituted with CO.sub.2 R.sup.9, OH, pyridyl 5-isoxazolin-3-onyl, morpholino or 1-imidazolidin-2-onyl; or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino, 1-pyrazolyl or 4-(NR.sup.10)-1-piperazinyl group wherein any of said groups may optionally be substituted with one or two substituents selected from C.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.9, NH.sub.2 and OH; R.sup.8 is C.sub.1 -C.sub.4 alkyl or pyridyl; R.sup.9 is H or C.sub.1 -C.sub.4 alkyl; and R.sup.10 is H, C.sub.1 -C.sub.4 alkyl or (hydroxy) C.sub.2 -C.sub.3 alkyl; are selected cGMP PDE inhibitors useful in the treatment of, inter alia, cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.
    • PCT No.PCT / EP93 / 02097 371日期1995年1月31日 102(e)日期1995年1月31日PCT提交1993年8月4日PCT公布。 公开号WO94 / 05661 日期:1994年3月17日化学式< IMAGE>及其药学上可接受的盐,其中R 1是H,C 1 -C 4烷基CN或CONR 4 R 5; R2是C2-C4烷基; R3是SO2NR6R7,NO2,NH2,NHCOR8 NHSO2R8或N(SO2R8)2; R 4和R 5各自独立地选自H和C 1 -C 4烷基; R 6和R 7各自独立地选自H和任选被CO 2 R 9,OH,吡啶基-5-异恶唑啉-3-基,吗啉代或1-咪唑烷-2-基基取代的C 1 -C 4烷基; 或与它们所连接的氮原子一起形成吡咯烷子基,哌啶子基,吗啉代,1-吡唑基或4-(NR10)-1-哌嗪基,其中任何所述基团可任选被一个或两个选自C 1 -C4烷基,CO 2 R 9,NH 2和OH; R8是C1-C4烷基或吡啶基; R 9为H或C 1 -C 4烷基; R 10为H,C 1 -C 4烷基或(羟基)C 2 -C 3烷基; 被选择用于治疗尤其是心血管疾病如心绞痛,高血压,心力衰竭和动脉粥样硬化的cGMP PDE抑制剂。