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41. 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。

42. 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。

43. 发明授权

US08394836B2 Indoles and their therapeutic use 有权
标题翻译：吲哚及其治疗用途
公开(公告)号：US08394836B2
公开(公告)日：2013-03-12
申请号：US12746104
申请日：2008-12-12
申请人： George Hynd , John Gary Montana , Harry Finch , Rosa Arienzo , Barbara Avitabile-Woo , Mathias Domostoj
发明人： George Hynd , John Gary Montana , Harry Finch , Rosa Arienzo , Barbara Avitabile-Woo , Mathias Domostoj
IPC分类号： A61K31/4439 , C07D409/12 , C07D401/12
CPC分类号： C07D209/12 , C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is —SO2— or *—SO2NR3— wherein the bond marked with an asterisk is attached to Ar1; R1 is hydrogen, fluoro, chloro, CN or CF3; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, C1C8alkyl or C3-C7cycloalkyl; Ar1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.
摘要翻译：式（I）的化合物是CRTH2受体的配体，特别用于治疗炎性病症。其中X是-SO 2 - 或* -SO 2 NR 3 - ，其中用星号附着的键连接到Ar1上; R1是氢，氟，氯，CN或CF3; R2是氢，氟或氯; R3是氢，C1C8烷基或C3-C7环烷基; Ar 1是苯基或选自呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基的5-或6-元杂芳基，其中苯基或杂芳基任选被一个或更多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代; 并且Ar 2是苯基或选自吡咯基，呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基中的5-或6-元杂芳基，其中苯基或杂芳基任选被取代通过一个或多个独立地选自氟，氯，CN，C 3 -C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代。

44. 发明授权

US08394830B2 Quinolines and their therapeutic use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US08394830B2
公开(公告)日：2013-03-12
申请号：US13435242
申请日：2012-03-30
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： A61K31/04
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 C1C6alkyl or C3-C6cycloalkyl, 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，其中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。

45. 发明申请

US20110071175A1 Indoles and Their Therapeutic Use 有权
标题翻译：吲哚及其治疗用途
公开(公告)号：US20110071175A1
公开(公告)日：2011-03-24
申请号：US12746104
申请日：2008-12-12
申请人： George Hynd , John Gary Montana , Harry Finch , Rosa Arienzo , Barbara A. Vitabile-Woo , Mathias Domostoj
发明人： George Hynd , John Gary Montana , Harry Finch , Rosa Arienzo , Barbara A. Vitabile-Woo , Mathias Domostoj
IPC分类号： A61K31/506 , C07D403/06 , A61K31/4178 , C07D417/06 , A61K31/427 , A61K31/405 , C07D417/14 , A61K31/4439 , C07D209/42 , C07D403/12 , A61P11/06 , A61P1/04
CPC分类号： C07D209/12 , C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14
摘要： Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is —SO2— or *—SO2NR3— wherein the bond marked with an asterisk is attached to Ar1; R1 is hydrogen, fluoro, chloro, CN or CF3; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, C1C8alkyl or C3-C7cycloalkyl; Ar1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.
摘要翻译：式（I）的化合物是CRTH2受体的配体，特别用于治疗炎性病症。其中X是-SO 2 - 或* -SO 2 NR 3 - ，其中用星号附着的键连接到Ar1上; R1是氢，氟，氯，CN或CF3; R2是氢，氟或氯; R3是氢，C1C8烷基或C3-C7环烷基; Ar 1是苯基或选自呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基的5-或6-元杂芳基，其中苯基或杂芳基任选被一个或更多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代; 并且Ar 2是苯基或选自吡咯基，呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基中的5-或6-元杂芳基，其中苯基或杂芳基任选被取代通过一个或多个独立地选自氟，氯，CN，C 3 -C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代。

46. 发明授权

US07858640B2 Quinolines and their therapeutic use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US07858640B2
公开(公告)日：2010-12-28
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： A01N43/42 , A61K31/47 , C07D215/00 , C07D215/38
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 components; in which: R1-R9 are various substituents; A is —CHR10—, —C(O)—, —S(O)n—, —O—, or —NR10— wherein n is an integer from 0-1 and R10 is selected from various substituents; B is a direct bond or a divalent radical; R11 and R12 are selected from cvarious substituents; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, 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：R 1 -R 9是各种取代基; A是-CHR 10 - ， - C（O） - ， - S（O）n - ， - O-或-NR 10 - ，其中n是0-1的整数，R 10选自各种取代基; B是直接键或二价基团; R 11和R 12选自多个取代基; 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，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。

47. 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。

48. 发明申请

US20080306109A1 Indolizine Derivatives as Ligands of the Crth2 Receptor 审中-公开
标题翻译：吲哚啉衍生物作为Crth2受体的配体
公开(公告)号：US20080306109A1
公开(公告)日：2008-12-11
申请号：US12065963
申请日：2006-09-14
申请人： George Hynd , Nicholas Charles Ray , Harry Finch , John Gary Montana , Michael Colin Cramp , Trevor Keith Harrison , Rosa Arienzo , Paul Blaney , Yann Griffon , David Middlemiss
发明人： George Hynd , Nicholas Charles Ray , Harry Finch , John Gary Montana , Michael Colin Cramp , Trevor Keith Harrison , Rosa Arienzo , Paul Blaney , Yann Griffon , David Middlemiss
IPC分类号： A61K31/44 , C07D455/02 , A61P43/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R1, R2. R3 and R4 each independently are hydrogen, C1-C6alkyl, fully or partially fluorinated C1-C6alkyl, halo, —S(O)nR10, —SO2N(R10)2, —N(R10)2, —C(O)N(R10)2, —NR10C(O)R9, —CO2R10, —C(O)R9, —NO2, —CN or —OR11; wherein each R9 is independently C1-C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1-C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1-C6alkyl, fully or partially fluorinated C1-C6alkyl or a group —SO2R10; n is 0, 1 or 2; R5 is C1-C6alkyl, fully or partially fluorinated C1-C6alkyl, C1-C6alkenyl, C1-C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1-C6alkyl or fully or partially fluorinated C1-C6alkyl; R7 and R8 are independently hydrogen or C1-C6alkyl, or R7 and R8 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —C(O)—, —NR6SO2— or —SO2NR6- wherein n is 0, 1 or 2.
摘要翻译：式（I）化合物是CRTH2拮抗剂，可用于治疗例如哮喘，慢性阻塞性肺病，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎。式（I）其中R1，R2。完全或部分氟化的C 1 -C 6烷基，卤素，-S（O）n R 10，-SO 2 N（R 10）2，-N（R 10）2，-C（O）N（ R 10）2，-NR 10 C（O）R 9，-CO 2 R 10，-C（O）R 9，-NO 2，-CN或-OR 11; 其中每个R 9独立地是C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基或基团-SO 2 R 10; n为0,1或2; R 5是C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，C 1 -C 6烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R6是氢，C1-C6烷基或完全或部分氟化的C1-C6烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或者R 7和R 8与它们所连接的原子一起形成环烷基; 且X为-CHR 6 - ， - S（O）n - ， - C（O） - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

49. 发明授权

US06566384B1 Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity 失效
标题翻译：具有MMP和TNF抑制活性的羟肟酸和羧酸衍生物
公开(公告)号：US06566384B1
公开(公告)日：2003-05-20
申请号：US10011031
申请日：2001-11-13
申请人： David Alan Owen , John Gary Montana , John Fraser Keily , Robert John Watson , Andrew Douglas Baxter
发明人： David Alan Owen , John Gary Montana , John Fraser Keily , Robert John Watson , Andrew Douglas Baxter
IPC分类号： A61K3116
CPC分类号： C07D207/48 , C07C317/44 , C07C2601/08
摘要： Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.
摘要翻译：具有MMP和TNF抑制活性的羟肟酸和羧酸衍生物

50. 发明授权

US06506764B1 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：US06506764B1
公开(公告)日：2003-01-14
申请号：US09623669
申请日：2000-09-06
申请人： Andrew Douglas Baxter , David Alan Owen , Duncan Hannah , John Gary Montana
发明人： Andrew Douglas Baxter , David Alan Owen , Duncan Hannah , John Gary Montana
IPC分类号： A61K31438
CPC分类号： C07D221/20 , C07D211/96
摘要： Compounds of the formula B—X—(CH2)m—CR1R2—(CH2)n—CO—Y (I) have therapeutic utility as inhibitors of metalloproteinases etc.
摘要翻译：具有治疗作用的化合物作为金属蛋白酶抑制剂等

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