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公开(公告)号:US06403791B1
公开(公告)日:2002-06-11
申请号:US09779963
申请日:2001-02-09
申请人: Hazel Joan Dyke , Alan Findlay Haughan , Christopher Lowe , George Martin Buckley , Richard John Davenport , Andrew Sharpe , Hannah Jayne Kendall , Verity Margaret Sabin , John Gary Montana , Catherine Louise Picken
发明人: Hazel Joan Dyke , Alan Findlay Haughan , Christopher Lowe , George Martin Buckley , Richard John Davenport , Andrew Sharpe , Hannah Jayne Kendall , Verity Margaret Sabin , John Gary Montana , Catherine Louise Picken
IPC分类号: C07D41304
CPC分类号: C07D413/12
摘要: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is C1-6 alkyl, cycloalkyl or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.
摘要翻译: 式(Ⅳ)的化合物是任选被一个或多个氟取代的C 1-3烷基; R 2是C 1-6烷基,环烷基或NR 4 R 5; R 3是部分式(A),(B)或(B)的吡唑,咪唑或异恶唑基, C)NR4R5是含氮杂环; R6是C1-3烷基; 和R 7和R 8相同或不同,各自表示C 1-3烷基,卤素,CF 3或CN;或其药学上可接受的盐。
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公开(公告)号:US06455561B1
公开(公告)日:2002-09-24
申请号:US09976811
申请日:2001-10-12
IPC分类号: A61K3142
CPC分类号: C07D405/12 , C07D413/12
摘要: The present invention pertains to compositions and methods for treating disease states which are capable of being modulated by inhibition of phosphodiesterase IV or Tumour Necrosis Factor, or that is a pathological condition associated with a function of phosphodiesterase IV, eosinophil accumulation or a function of the eosinophil, said method comprising administering to a person or animal in need of such treatment an effective amount of the compound of a formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C 1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof
摘要翻译: 本发明涉及用于治疗能够通过抑制磷酸二酯酶IV或肿瘤坏死因子调节的疾病状态的组合物和方法,或者是与磷酸二酯酶IV,嗜酸性粒细胞积累或嗜酸性粒细胞的功能相关的病理状况 所述方法包括向需要这种治疗的人或动物施用有效量的化学式R 1是任选被一个或多个氟取代的C 1-3烷基; R 2是CH 2 OCH 3或2或3-四氢呋喃基; R 3是 部分式(A),(B)或(C)R 4的吡唑,咪唑或异恶唑基是C 1-3烷基; 和R 5和R 6可以相同或不同,各自表示C 1-3烷基,卤素,CF 3或CN;或其药学上可接受的盐
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公开(公告)号:US5728712A
公开(公告)日:1998-03-17
申请号:US650672
申请日:1996-05-20
IPC分类号: C07D209/08 , C07D215/58 , C07D217/08 , C07D237/32 , A61K31/435 , C07D217/24
CPC分类号: C07D215/58 , C07D209/08 , C07D217/08 , C07D237/32
摘要: 3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.
摘要翻译: 3,4-二取代苯基磺酰胺通过TNF或磷酸二酯酶抑制具有治疗效用。
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公开(公告)号:US5925636A
公开(公告)日:1999-07-20
申请号:US859509
申请日:1997-05-20
IPC分类号: C07D307/79 , A61K31/00 , A61K31/34 , A61K31/343 , A61K31/345 , A61K31/415 , A61K31/4155 , A61K31/425 , A61K31/435 , A61K31/4353 , A61K31/4375 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/14 , A61P11/16 , A61P17/06 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/10 , A61P35/02 , A61P37/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/84 , C07D307/86 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D307/83 , C07D401/12
CPC分类号: C07D405/12 , C07D307/86 , C07D405/14 , C07D417/14
摘要: Compounds having the formula (i), ##STR1## wherein the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined herein. The compounds of the present invention can be utilized to treat disease states capable of being modulated by inhibition of proteins which mediate cellular activity, such as tumor necrosis factor (TNF) and/or phosphodiesterase IV (PDE IV).
摘要翻译: 具有式(i)的化合物,其中基团R 1,R 2,R 3,R 4和R 5在本文中定义。 本发明的化合物可用于治疗能够通过抑制介导细胞活性的蛋白质(例如肿瘤坏死因子(TNF))和/或磷酸二酯酶IV(PDE IV)来调节的疾病状态。
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公开(公告)号:US06331556B2
公开(公告)日:2001-12-18
申请号:US09780657
申请日:2001-02-09
IPC分类号: A61K31422
CPC分类号: C07D405/12 , C07D413/12
摘要: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.
摘要翻译: 式R 1的化合物是任选被一个或多个氟取代的C 1-3烷基; R 2是CH 2 OCH 3或2或3-四氢呋喃基; R 3是部分式(A),(B)或(B)的吡唑,咪唑或异恶唑基, C)R 4是C 1-3烷基; 和R 5和R 6可以相同或不同,各自表示C 1-3烷基,卤素,CF 3或CN;或其药学上可接受的盐。
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公开(公告)号:US6066657A
公开(公告)日:2000-05-23
申请号:US246335
申请日:1999-02-09
申请人: Hazel Joan Dyke , John Gary Montana , Christopher Lowe , Karen Ann Runcie , Alan Findlay Haughan , Verity Margaret Sabin , Duncan Hannah , Louise Picken , Andrew Sharpe
发明人: Hazel Joan Dyke , John Gary Montana , Christopher Lowe , Karen Ann Runcie , Alan Findlay Haughan , Verity Margaret Sabin , Duncan Hannah , Louise Picken , Andrew Sharpe
IPC分类号: C07D307/80 , A61K31/343 , A61K31/443 , A61K31/4545 , A61K31/506 , A61P1/04 , A61P3/14 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/16 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D307/82 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/44 , A61K31/36
CPC分类号: C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要: A compound of formula (i) ##STR1## has therapeutic utility via inhibition of phosphodiesterase and THF release.
摘要翻译: 式(i)化合物通过抑制磷酸二酯酶和THF释放具有治疗效用。
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公开(公告)号:US5804588A
公开(公告)日:1998-09-08
申请号:US859508
申请日:1997-05-20
申请人: Hazel Joan Dyke , John Gary Montana , Christopher Lowe , Hannah Jayne Kendall , Verity Margaret Sabin
发明人: Hazel Joan Dyke , John Gary Montana , Christopher Lowe , Hannah Jayne Kendall , Verity Margaret Sabin
IPC分类号: C07D215/26 , A61K31/00 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K45/06 , A61P43/00 , C07D215/48 , C07D401/12 , C07D401/14 , C07D417/12 , C07D215/00
CPC分类号: C07D401/12 , A61K45/06 , C07D215/48 , C07D401/14 , C07D417/12
摘要: The subject invention concerns novel compounds of the general formula (i) ##STR1## that are useful in treating disease states, such as those states associated with proteins that mediate cellular activity. The compounds of the subject invention can be used, for example, to inhibit tumor necrosis factor and/or phosphodiesterase IV, The subject invention also concerns methods for treating disease states using the compounds of the invention.
摘要翻译: 本发明涉及可用于治疗疾病状态的通式(i)“IMAGE”的新化合物,例如与介导细胞活性的蛋白质相关的那些状态。 本发明的化合物可用于例如抑制肿瘤坏死因子和/或磷酸二酯酶IV。本发明还涉及使用本发明化合物治疗疾病状态的方法。
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公开(公告)号:US5773467A
公开(公告)日:1998-06-30
申请号:US761102
申请日:1996-12-05
IPC分类号: A61K31/00 , A61K31/34 , A61K31/343 , A61K31/44 , A61K31/4427 , A61K31/443 , A61P11/00 , A61P11/06 , A61P29/00 , A61P43/00 , C07D307/79 , C07D307/80 , C07D307/86 , C07D405/12 , C07D405/14 , C07D307/78
CPC分类号: C07D307/79 , C07D307/80 , C07D307/86 , C07D405/12 , C07D405/14
摘要: Benzofuran carboxides and sulphonamides have therapeutic utility, e.g. in the treatment of inflammation and asthma, by virtue of their ability to inhibit phosphodiesterases and tumor necrosis factor.
摘要翻译: 苯并呋喃羧酰胺和磺酰胺具有治疗效用,例如 在治疗炎症和哮喘方面,凭借其抑制磷酸二酯酶和肿瘤坏死因子的能力。
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公开(公告)号:US06642254B2
公开(公告)日:2003-11-04
申请号:US10150281
申请日:2002-05-16
申请人: Hazel Joan Dyke , John Gary Montana
发明人: Hazel Joan Dyke , John Gary Montana
IPC分类号: A61K3147
CPC分类号: C07D401/12 , Y10S514/912
摘要: N-oxides of formula (i) wherein R1 is CH3, CH2F, CHF2 or CF3; R2 is CH3 or CF3; R3 is F, Cl, Br, CN or CH3; and R4 is H, F, Cl, Br, CN or CH3; and pharmaceutically-acceptable salts thereof, are useful as therapeutic agents, e.g., for the treatment of inflammatory diseases.
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公开(公告)号:US06262070B1
公开(公告)日:2001-07-17
申请号:US09433274
申请日:1999-11-03
申请人: Hazel Joan Dyke , John Gary Montana
发明人: Hazel Joan Dyke , John Gary Montana
IPC分类号: C07D40112
CPC分类号: C07D401/12 , Y10S514/912
摘要: N-oxides of formula (i) wherein R1 is CH3, CH2F, CHF2 or CF3; R2 is CH3 or CF3; R3 is F, Cl, Br, CN or CH3; and R4 is H, F, Cl, Br, CN or CH3; and pharmaceutically-acceptable salts thereof, are useful as therapeutic agents, e.g. for the treatment of inflammatory diseases.
摘要翻译: 式(ⅰ)的N-氧化物,其中R 1是CH 3,CH 2 F,CHF 2或CF 3; R 2是CH 3或CF 3; R 3是F,Cl,Br,CN或CH 3; 和R 4是H,F,Cl,Br,CN或CH 3;及其药学上可接受的盐,可用作治疗剂。 用于治疗炎性疾病。
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