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21. 发明申请

US20100144787A1 Quinolines and Their Therapeutic Use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US20100144787A1
公开(公告)日：2010-06-10
申请号：US12531935
申请日：2008-04-03
申请人： John Gary Montana , Harry Finch , George Hynd , Michael Colin Cramp , Rosa Arienzo , Neville McLean
发明人： John Gary Montana , Harry Finch , George Hynd , Michael Colin Cramp , Rosa Arienzo , Neville McLean
IPC分类号： A61K31/4709 , C07D215/233 , C07D215/227 , C07D215/12 , A61P11/06 , A61P11/08 , A61P11/16 , A61P11/02
CPC分类号： C07D401/10 , C07D215/227 , C07D215/233 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(═O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.
摘要翻译：式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R1是卤素或氰基; R2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6烷基或C 3 -C 6环烷基，后两个基团任选被一个或多个卤素原子取代; R5是氢或卤素; R6是C1C6烷基或C3-C6环烷基，其任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y1中的一个是氢，另一个是选自本说明书中提到的那些的OR 6，-C（= O）R 7，NR 8 SO 2 R 6或杂环基; R6，R7和R8如说明书中所定义。

22. 发明申请

US20100144786A1 QUINOLINE DERIVATIVES AS CRTH2 RECEPTOR LIGANDS 审中-公开
标题翻译：喹啉衍生物作为CRTH2受体配体
公开(公告)号：US20100144786A1
公开(公告)日：2010-06-10
申请号：US12531367
申请日：2007-03-29
申请人： Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
发明人： Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
IPC分类号： A61K31/47 , C07D215/233 , A61P17/02 , A61P11/06 , A61P37/06 , A61P17/06
CPC分类号： C07D215/233 , C07D215/20 , C07D215/227
摘要： Specific quinoline derivatives are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component.
摘要翻译：特定的喹啉衍生物是可用于治疗具有炎性成分的病症的CRTH2拮抗剂。

23. 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。

24. 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

25. 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).

26. 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。

27. 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。

28. 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。

29. 发明授权

US08173812B2 Quinolines and their therapeutic use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US08173812B2
公开(公告)日：2012-05-08
申请号：US12531935
申请日：2008-04-03
申请人： John Gary Montana , Harry Finch , George Hynd , Michael Colin Cramp , Rosa Arienzo , Neville McLean
发明人： John Gary Montana , Harry Finch , George Hynd , Michael Colin Cramp , Rosa Arienzo , Neville McLean
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D401/10 , C07D215/227 , C07D215/233 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1-C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(═O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.
摘要翻译：式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R1是卤素或氰基; R2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6烷基或C 3 -C 6环烷基，后两个基团任选被一个或多个卤素原子取代; R5是氢或卤素; R6是C1-C6烷基或C3-C6环烷基，其任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y1中的一个是氢，另一个是选自本说明书中提到的那些的OR 6，-C（= O）R 7，NR 8 SO 2 R 6或杂环基; R6，R7和R8如说明书中所定义。

30. 发明申请

US20090156600A1 Quinolines and Their Therapeutic Use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US20090156600A1
公开(公告)日：2009-06-18
申请号：US12066603
申请日：2006-09-29
申请人： Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
发明人： Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
IPC分类号： A61K31/5377 , C07D215/233 , A61P11/06 , C07D413/14 , A61K31/47
CPC分类号： C07D215/233 , A61K31/47 , C07D215/12 , C07D215/18 , C07D215/20 , C07D215/227 , C07D215/36 , C07D215/48 , C07D401/04 , C07D401/10 , C07D401/12
摘要： Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6alkyl, C1-C6-fluoroalkyl, cyclopropyl, halo, —S(O)nR6, —SO2NR7R8, —NR7R8, —NR7C(O)R6, —CO2R7, —C(O)NR7R8, —C(O)R76, —NO2, —CN or a group —OR9; wherein each R6 is independently C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R7, R8 are independently C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl, heteroaryl or hydrogen; R9 is hydrogen, C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group —SO2R6; A is —CHR10—, —C(O)—, —S(O)n—, —O—, or —NR10— wherein n is an integer from 0-2 and R10 is hydrogen C1-C3alkyl, or C1-C6-fluoroalkyl group; B is a direct bond, or a divalent radical selected from —CH2—, —CH2CH2—, —CHR11—, —CR11R12—, —CH2CHR11—, CH2CR11R12—, —CHR11CHR12—, and divalent radicals of formula —(CR11R12)p-Z- wherein Z is attached to the ring carrying R1, R2 and R3; wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6-fluoroalkyl; R12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is —O—, —NH—, or —S(O)n—, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(═O)NHSO2R6 or SO2NHC(═O)R6; and Y is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.
摘要翻译：式[1]化合物是CRTH2拮抗剂，可用于治疗具有炎性成分的病症; 其中：R1，R2，R3，R4和R5独立地是氢，C1-C6烷基，C1-C6-氟烷基，环丙基，卤素，-S（O）nR6，-SO2NR7R8，-NR7R8，-NR7C（O） -C（O）NR 7 R 8，-C（O）R 76，-NO 2，-CN或-OR 9基团; 其中每个R 6独立地为C 1 -C 6烷基，C 1 -C 6 - 氟烷基，环烷基，芳基或杂芳基; R 7，R 8独立地是C 1 -C 6烷基，C 1 -C 6氟代烷基，环烷基，环烷基 - （C 1 -C 6烷基） - ，芳基，杂芳基或氢; R 9是氢，C 1 -C 6烷基，C 1 -C 6 - 氟代烷基，环烷基，环烷基 - （C 1 -C 6烷基） - 或-SO 2 R 6基团; A是-CHR 10 - ， - C（O） - ， - S（O）n - ， - O-或-NR 10 - ，其中n是0-2的整数，R 10是氢C1-C3烷基或C1-C6 氟烷基或选自-CH 2 - ， - CH 2 CH 2 - ， - CHR 11 - ， - CR 11 R 12 - ， - CH 2 CHR 11 - ，CH 2 CR 11 R 12 - ， - CHR 11 CHR 12 - - 的二价基团和式 - （CR11R12）pZ- 其中Z连接到携带R1，R2和R3的环上; 其中R11是C1-C3烷基，环丙基，C1-C6-氟代烷基; R12是甲基或氟甲基; p独立地为1或2; 和Z是-O - ， - NH-或-S（O）n - ，其中n是0-2的整数; X是羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸盐，膦酸盐，膦酰胺或磺酸基，或式C（-O）NHSO 2 R 6或SO 2 NHC（-O）R 6的基团; 并且Y是芳基，杂芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基稠合 - 环烷基。

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