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1. 发明授权

US07893085B2 Aza-benzothiophenyl compounds and methods of use 有权
标题翻译：氮杂 - 苯并噻吩基化合物及其使用方法
公开(公告)号：US07893085B2
公开(公告)日：2011-02-22
申请号：US11894345
申请日：2007-08-20
申请人： Pascal Pierre Savy , Stephen Price , Hazel Joan Dyke , John Gary Montana , Karen Williams , Mark S. Stanley , Liang Bao
发明人： Pascal Pierre Savy , Stephen Price , Hazel Joan Dyke , John Gary Montana , Karen Williams , Mark S. Stanley , Liang Bao
IPC分类号： C07D221/00 , A61K31/4365 , A61P35/00 , A61P29/00 , C07D241/00 , C07D487/04 , A61K31/519 , A61K31/5025
CPC分类号： C07D495/04
摘要： The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的式I的氮杂苯并噻吩基化合物，更具体地涉及抑制MEK激酶活性的氮杂苯并噻吩基化合物。本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

2. 发明申请

US20080242655A1 AZA-INDOLYL COMPOUNDS AND METHODS OF USE 有权
标题翻译： AZA-INDOLYL化合物及其使用方法
公开(公告)号：US20080242655A1
公开(公告)日：2008-10-02
申请号：US11947656
申请日：2007-11-29
申请人： Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
发明人： Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
IPC分类号： A61K31/397 , C07D471/02 , A61K31/4439 , C07D209/04 , A61P35/00 , A61P29/00 , A61K31/404 , C07D237/26 , A61K31/5025
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的具有式I的唑烷基化合物，更具体地涉及抑制MEK激酶活性的唑烷基化合物。本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

3. 发明授权

US07855216B2 Aza-indolyl compounds and methods of use 有权
标题翻译：氮杂 - 吲哚基化合物及其使用方法
公开(公告)号：US07855216B2
公开(公告)日：2010-12-21
申请号：US11947656
申请日：2007-11-29
申请人： Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
发明人： Simon Charles Goodacre , Karen Williams , Stephen Price , Hazel Joan Dyke , John Gary Montana , Mark S. Stanley , Liang Bao , Wendy Lee
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P35/00 , C07D487/04 , A61K31/519 , A61K31/5025
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及具有抗癌和/或抗炎活性的具有式I的唑烷基化合物，更具体地涉及抑制MEK激酶活性的唑烷基化合物。本发明提供了可用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

4. 发明授权

US06455561B1 Heterocyclic compounds and their therapeutic use 失效
标题翻译：杂环化合物及其治疗用途
公开(公告)号：US06455561B1
公开(公告)日：2002-09-24
申请号：US09976811
申请日：2001-10-12
申请人： Hazel Joan Dyke , Christopher Lowe , John Gary Montana
发明人： Hazel Joan Dyke , Christopher Lowe , John Gary Montana
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

5. 发明授权

US5972936A Benzofuran carboxamides and their therapeutic use 失效
公开(公告)号：US5972936A
公开(公告)日：1999-10-26
申请号：US859510
申请日：1997-05-20
申请人： Hazel Joan Dyke , John Gary Montana
发明人： Hazel Joan Dyke , John Gary Montana
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).

6. 发明授权

US5919789A Xanthines and their therapeutic use 失效
标题翻译：黄嘌呤及其治疗用途
公开(公告)号：US5919789A
公开(公告)日：1999-07-06
申请号：US971857
申请日：1997-11-17
申请人： Hazel Joan Dyke , John Gary Montana
发明人： Hazel Joan Dyke , John Gary Montana
IPC分类号： A61K31/522 , A61P1/00 , A61P3/10 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P19/08 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P33/00 , A61P35/02 , A61P37/02 , A61P43/00 , C07D473/04 , C07D473/06 , A61K31/52 , C07D247/02 , C07D473/10
CPC分类号： C07D473/04 , C07D473/06
摘要： Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase.
摘要翻译：式（ⅰ）的化合物通过抑制TNF或phophodiesterase具有治疗效用。

7. 发明授权

US5834485A Quinoline sulfonamides and their therapeutic use 失效
标题翻译：喹啉磺酰胺及其治疗用途
公开(公告)号：US5834485A
公开(公告)日：1998-11-10
申请号：US858969
申请日：1997-05-20
申请人： Hazel Joan Dyke , John Gary Montana
发明人： Hazel Joan Dyke , John Gary Montana
IPC分类号： A61K31/00 , A61K31/47 , A61K45/06 , A61P43/00 , C07D215/36 , C07D215/48 , C07D401/12 , C07D401/14 , C07D417/12
CPC分类号： C07D401/12 , A61K45/06 , C07D215/36 , C07D215/48 , C07D401/14 , C07D417/12
摘要： The subject invention pertains to quinolinesulfonamides. The subject compounds can be used to treat disease states, such as those that are associated with proteins that mediate cellular activity, for example, by inhibiting phosphodiesterase IV (PDE IV) or tumor necrosis factor (TNF). The invention also pertains to methods of treating disease states, including those states capable of being modulated by inhibition of PDE IV or TNF.
摘要翻译：本发明涉及喹啉磺酰胺。主题化合物可用于治疗疾病状态，例如与介导细胞活性的蛋白质相关的疾病状态，例如通过抑制磷酸二酯酶IV（PDE IV）或肿瘤坏死因子（TNF）。本发明还涉及治疗疾病状态的方法，包括能够通过抑制PDE IV或TNF调节的那些状态。

8. 发明授权

US5728712A 3,4-disubstituted-phenylsulphonamides and their therapeutic use 失效
标题翻译： 3,4-二取代苯基磺酰胺及其治疗用途
公开(公告)号：US5728712A
公开(公告)日：1998-03-17
申请号：US650672
申请日：1996-05-20
申请人： John Gary Montana , Hazel Joan Dyke , Robert James Maxey , Christopher Lowe
发明人： John Gary Montana , Hazel Joan Dyke , Robert James Maxey , Christopher Lowe
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。

9. 发明授权

US06642254B2 Heterocyclic compounds and their therapeutic use 失效
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.

10. 发明授权

US06403791B1 Heterocyclic compounds and their therapeutic use 失效
标题翻译：杂环化合物及其治疗用途
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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