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公开(公告)号:US5591742A
公开(公告)日:1997-01-07
申请号:US379531
申请日:1995-01-31
IPC分类号: A61K31/505 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D471/04 , A61K31/535 , A61K31/435 , C07D413/14 , C07D487/02
CPC分类号: C07D471/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US5346901A
公开(公告)日:1994-09-13
申请号:US84827
申请日:1993-06-29
申请人: Andrew S. Bell , David Brown , Nicholas K. Terrett
发明人: Andrew S. Bell , David Brown , Nicholas K. Terrett
IPC分类号: C07D487/04 , A61K31/505
CPC分类号: C07D487/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US5250534A
公开(公告)日:1993-10-05
申请号:US882988
申请日:1992-05-14
申请人: Andrew S. Bell , David Brown , Nicholas K. Terrett
发明人: Andrew S. Bell , David Brown , Nicholas K. Terrett
IPC分类号: C07D487/04 , A61K31/505
CPC分类号: C07D487/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US5426107A
公开(公告)日:1995-06-20
申请号:US96743
申请日:1993-07-23
IPC分类号: A61K31/505 , A61K31/519 , A61K31/535 , A61K31/635 , A61P1/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P27/02 , A61P27/06 , A61P27/14 , A61P27/16 , A61P37/08 , C07D231/00 , C07D239/00 , C07D487/04
CPC分类号: C07D487/04
摘要: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.
摘要翻译: 式(I)的化合物及其药学上可接受的盐是选择性cGMP PDE抑制剂,其可用于治疗诸如心绞痛,高血压,充血性心力衰竭,血管通畅性降低,外周血管疾病, 中风,支气管炎,慢性哮喘,过敏性哮喘,过敏性鼻炎,青光眼,肠蠕动障碍等疾病。
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公开(公告)号:US5272147A
公开(公告)日:1993-12-21
申请号:US897735
申请日:1992-06-12
IPC分类号: A61K31/505 , A61K31/519 , A61K31/535 , A61K31/635 , A61P1/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P27/02 , A61P27/06 , A61P27/14 , A61P27/16 , A61P37/08 , C07D231/00 , C07D239/00 , C07D487/04
CPC分类号: C07D487/04
摘要: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof are selective cGMP PDE inhibitors which are useful in the treatment of such diseases and adverse conditions as angina, hypertension, congestive heart failure, reduced blood vessel patency, peripheral vascular disease, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, and diseases characterized by disorders of gut motility.
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公开(公告)号:US08336263B2
公开(公告)日:2012-12-25
申请号:US12912097
申请日:2010-10-26
申请人: Gary R. Schultz , Andrew S. Bell
发明人: Gary R. Schultz , Andrew S. Bell
IPC分类号: E02D27/00
CPC分类号: E04H4/0093 , E04H4/0087 , E04H4/1227 , E04H2004/146
摘要: A concrete container including a concrete footing including a shear key; a concrete wall inserted in the shear key; a plurality of footing reinforcing members inserted in the concrete footing on a support side of the shear key and extending above the concrete footing; a plurality of wall reinforcing members inserted in the concrete wall on a support side of the concrete wall and extending diagonally towards the concrete footing; a poured concrete moment connection substantially covering the plurality of footing reinforcing members extending from the pre-cast concrete footing and the plurality of wall reinforcing members extending from the wall.
摘要翻译: 包括具有剪切键的混凝土基础的混凝土容器; 将混凝土墙插入剪切钥匙; 多个基础加强构件,其在所述混凝土基座中插入所述剪切键的支撑侧并在所述混凝土基础之上延伸; 多个壁加强构件,其插入在混凝土壁的支撑侧上的混凝土壁中并对角地朝向混凝土基部延伸; 倾倒的混凝土力矩连接件基本上覆盖从预铸混凝土基脚延伸的多个基础加强构件和从壁延伸的多个壁加强构件。
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公开(公告)号:US20120096634A1
公开(公告)日:2012-04-26
申请号:US12912097
申请日:2010-10-26
申请人: Gary R. Schultz , Andrew S. Bell
发明人: Gary R. Schultz , Andrew S. Bell
CPC分类号: E04H4/0093 , E04H4/0087 , E04H4/1227 , E04H2004/146
摘要: A concrete container including a concrete footing including a shear key; a concrete wall inserted in the shear key; a plurality of footing reinforcing members inserted in the concrete footing on a support side of the shear key and extending above the concrete footing; a plurality of wall reinforcing members inserted in the concrete wall on a support side of the concrete wall and extending diagonally towards the concrete footing; a poured concrete moment connection substantially covering the plurality of footing reinforcing members extending from the pre-cast concrete footing and the plurality of wall reinforcing members extending from the wall.
摘要翻译: 包括具有剪切键的混凝土基础的混凝土容器; 将混凝土墙插入剪切钥匙; 多个基础加强构件,其在所述混凝土基座中插入所述剪切键的支撑侧并在所述混凝土基础之上延伸; 多个壁加强构件,其插入在混凝土壁的支撑侧上的混凝土壁中并对角地朝向混凝土基部延伸; 倾倒的混凝土力矩连接件基本上覆盖从预铸混凝土基脚延伸的多个基础加强构件和从壁延伸的多个壁加强构件。
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公开(公告)号:US5965553A
公开(公告)日:1999-10-12
申请号:US874089
申请日:1997-06-12
IPC分类号: A61K9/06 , A61K31/35 , A61K31/41 , A61K31/55 , A61K31/554 , A61P3/06 , A61P9/10 , A61P17/00 , A61P25/28 , A61P31/04 , A61P43/00 , C07D267/14 , C07D281/10 , C07D413/06 , C07D417/06 , C07D267/08 , C07D281/08
CPC分类号: C07D417/06 , C07D267/14 , C07D281/10
摘要: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, Alzheimer's agents or anti-acne agents.
摘要翻译: 本发明涉及可用作低胆固醇血症药,降血糖甘油三酯药,抗动脉粥样硬化药,抗真菌剂,阿尔茨海默病剂或抗痤疮剂的某些苯并氧氮杂酮和苯并噻唑酮。
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公开(公告)号:US5541203A
公开(公告)日:1996-07-30
申请号:US211609
申请日:1994-04-08
IPC分类号: C07D213/28 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P31/04 , C07D213/70 , C07D401/06 , C07D403/06 , C07D405/06 , C07D521/00 , C07D401/02
CPC分类号: C07D213/70 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06
摘要: The invention provides antifungal compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by up to 3 substituents each independently selected from halo and trifluoromethyl;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is ##STR2## R.sup.3 is --S(O).sub.m R.sup.4 ; R.sup.4 is C.sub.1 -C.sub.4 alkyl; andm is 0, 1 or 2, together with pharmaceutical compositions containing, and processes and intermediates for preparing, said compounds.
摘要翻译: PCT No.PCT / EP92 / 02278第 371日期1994年4月8日 102(e)日期1994年4月8日PCT提交1992年10月1日PCT公布。 公开号WO93 / 07139 日本时间1993年04月15日本发明提供下式的抗真菌化合物:其中R是被至多3个取代基取代的苯基,每个取代基各自独立地选自卤素和三氟甲基; R1是C1-C4烷基; R 2是-S(O)m R 4; R4是C1-C4烷基; 以及m为0,1或2,以及含有制备所述化合物的方法和中间体的药物组合物。
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