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41. 发明申请

US20100216768A1 N-SUBSTITUTED AZAINDOLES AND METHODS OF USE 有权
标题翻译： N-取代的胺和其使用方法
公开(公告)号：US20100216768A1
公开(公告)日：2010-08-26
申请号：US12664303
申请日：2008-06-11
申请人： Hazel Joan Dyke , Stephen Price , Karen Williams
发明人： Hazel Joan Dyke , Stephen Price , Karen Williams
IPC分类号： A61K31/50 , C07D471/04 , A61K31/437 , C07D487/04 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention relates to N-substituted azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to N-substituted 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/或抗炎活性的更优选的具有抗癌和/或抗炎活性的式I的N-取代的氮杂吲哚基化合物，更具体地涉及抑制MEK激酶活性的N-取代的阿魏酰基化合物。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。

42. 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。

43. 发明授权

US07015234B2 Hydroxamic acid derivatives 失效
标题翻译：羟肟酸衍生物
公开(公告)号：US07015234B2
公开(公告)日：2006-03-21
申请号：US10485905
申请日：2002-08-07
申请人： Hazel Joan Dyke , Robert John Watson
发明人： Hazel Joan Dyke , Robert John Watson
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： C07D405/12
摘要： Compounds of the general formula (I) are described wherein R1 and R2, which may be the same or different, is each a hydrogen atom or a CF3, CF2H or CFH2 group, provided that when one of R1 and R2 is a hydrogen atom, then the other is a CF3, CF2H or CFH2 group, and the salts, solvates or hydrates thereof. Compounds of the invention are potent MMP inhibitors which advantageously do not cause tendonitis in a relevant animal model. Compounds of the invention may be expected to be of use in medicine, especially where the avoidance of side effects, such as joint pain, is desired.
摘要翻译：描述了通式（I）的化合物，其中R 1和R 2可以相同或不同，各自为氢原子或CF 3，CF 2 H或CFH 2基团，条件是当R 1和R 2中的一个 SUP>是氢原子，则另一个是CF 3，CF 2 H或CFH 2 H 2基团，其盐，溶剂化物或其水合物。本发明的化合物是有效的MMP抑制剂，其有利地不会导致相关动物模型中的腱炎。预期本发明的化合物可用于医学中，特别是在需要避免副作用（例如关节疼痛）的情况下。

44. 发明授权

US06469020B2 Hydroxamic and carboxylic acid derivatives 失效
标题翻译：羟肟酸和羧酸衍生物
公开(公告)号：US06469020B2
公开(公告)日：2002-10-22
申请号：US09855978
申请日：2001-05-15
申请人： Duncan Batty , Verity Margaret Sabin , Robert John Watson , Hazel Joan Dyke , Andrew Sharpe , Richard John Davenport , David Alan Owen , Andrew Douglas Baxter
发明人： Duncan Batty , Verity Margaret Sabin , Robert John Watson , Hazel Joan Dyke , Andrew Sharpe , Richard John Davenport , David Alan Owen , Andrew Douglas Baxter
IPC分类号： A61K314355
CPC分类号： C07D401/12 , C07D217/08 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula: are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of matrix metalloproteinase, ADAM, ADAM-TS enzymes, and or INF&agr;-mediated diseases including degenerative diseases and certain cancers.
摘要翻译：本发明涉及异羟肟酸和羧酸衍生物。公开了下式的化合物。这些化合物可用于治疗由基质金属蛋白酶，ADAM，ADAM-TS酶和/或INFalpha介导的疾病包括退行性疾病和某些癌症的抑制剂介导的疾病。

45. 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

46. 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).

47. 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。

48. 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。

49. 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。

50. 发明申请

US20110183938A1 1,7-DIAZACARBAZOLES AND METHODS OF USE 审中-公开
标题翻译： 1,7-DIAZACARBAZOLES和使用方法
公开(公告)号：US20110183938A1
公开(公告)日：2011-07-28
申请号：US12967864
申请日：2010-12-14
申请人： Hazel Joan Dyke , Lewis Gazzard , Karen Williams
发明人： Hazel Joan Dyke , Lewis Gazzard , Karen Williams
IPC分类号： A61K31/695 , C07D413/14 , A61K31/5377 , C07D471/14 , A61K31/397 , A61K31/4375 , A61K31/496 , C07F7/10 , A61K31/55 , A61P35/00
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D453/02 , C07D519/00
摘要： The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as 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：本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况。

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