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1. 发明申请

WO2009060209A1 6,6-FUSED BICYCLIC AROMATIC COMPOUNDS AND THEIR THERAPEUTI USE 审中-公开
标题翻译： 6,6-双金属化合物及其治疗用途
公开(公告)号：WO2009060209A1
公开(公告)日：2009-05-14
申请号：PCT/GB2008/003758
申请日：2008-11-07
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John Gary , FINCH, Harry , AHMED, Shahadat , DOMOSTOJ, Mathias , MOISE, JOELLE , ARIENZO, Rosa
发明人： HYND, George , MONTANA, John Gary , FINCH, Harry , AHMED, Shahadat , DOMOSTOJ, Mathias , MOISE, JOELLE , ARIENZO, Rosa
IPC分类号： C07D215/28 , C07D217/24 , C07D239/74 , C07D401/10 , C07D215/233 , A61K31/47 , A61K31/4725 , A61K31/517 , A61P11/00 , C07C59/66
CPC分类号： C07D215/233 , C07C45/50 , C07C2601/14 , C07D215/28 , C07D217/24 , C07D239/74 , C07D401/10 , C07C47/02 , C07C47/11
摘要： This invention relates to a class of 6,6-fused bicyclic aromatic compounds which are ligands of the CRTH2 receptor (Chemoattractant Receptor-homologous molecule expressed on T Helper cells type 2), and their use in the treatment of diseases responsive to modulation of CRTH2 receptor activity, principally diseases having a sgnificant inflammatory component. the invention also relates to novel members of that class of ligands and pharmaceutical compositions containing them.
摘要翻译：本发明涉及一类作为CRTH2受体的配体的6,6-稠合双环芳族化合物（在2型T辅助细胞上表达的化学受体受体同源分子），以及它们在治疗对CRTH2的调节作用的疾病中的应用受体活性，主要是具有明显炎症成分的疾病。本发明还涉及该类配体的新成员和含有它们的药物组合物。

2. 发明申请

WO2009077728A1 INDOLES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：吲哚及其治疗用途
公开(公告)号：WO2009077728A1
公开(公告)日：2009-06-25
申请号：PCT/GB2008/004107
申请日：2008-12-12
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John, Gary , FINCH, Harry , ARIENZO, Rosa , AVITABILE-WOO, Barbara , DOMOSTOJ, Mathias
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry , ARIENZO, Rosa , AVITABILE-WOO, Barbara , DOMOSTOJ, Mathias
IPC分类号： C07D209/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/14 , C07D417/06 , A61K31/404
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 are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is -SO 2 - or *-SO 2 NR 3 - wherein the bond marked with an asterisk is attached to Ar 1 ; R 1 is hydrogen, fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; R 3 is hydrogen, C 1 C 8 alkyl or C 3 -C 7 cycloalkyl; Ar 1 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, C 3 - C 7 cycloalkyl, -O(C 1 -C 4 alkyl) or C 1 C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar 2 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, C 3 - C 3 - C 7 cycloalkyl, -O(C 1 -C 4 alkyl) or C 1 C 6 alkyl, 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。

3. 发明申请

WO2008119917A1 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：WO2008119917A1
公开(公告)日：2008-10-09
申请号：PCT/GB2007/001138
申请日：2007-03-29
申请人： ARGENTA DISCOVERY LIMITED , RAY, Nicholas, Charles , FINCH, Harry , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , MONTANA, John, Gary
发明人： RAY, Nicholas, Charles , FINCH, Harry , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , MONTANA, John, Gary
IPC分类号： C07D215/20 , C07D215/22 , A61K31/47 , A61P11/00 , A61P29/00
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。

4. 发明申请

WO2008113965A1 INDOLIZINE ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS 审中-公开
标题翻译：将醋酸衍生物作为CRTH2拮抗剂
公开(公告)号：WO2008113965A1
公开(公告)日：2008-09-25
申请号：PCT/GB2007/000996
申请日：2007-03-21
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
IPC分类号： A61K31/437 , C07D471/04 , A61P11/00
CPC分类号： C07D471/04
摘要： The specific compounds of this list : {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1 -(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro-4-(morpholine-4-sutfonyl)phenylsutfanyl]-7-cyano-2-methylindolizin-3- yl}acetic acid, {7-cyano-1 -(6-fluoroquinolin-2-y1methyl)-2-methylindolizin-3-yl}acetic acid are ligands of the CRTH2 receptor and are useful in the treatment of respiratory diseases.
摘要翻译：该列表的具体化合物：{7-氰基-2-甲基-1- [4-（吗啉-4-磺酰基）苄基]中氮茚-3-基}乙酸，{1-（3-氯-4-乙磺酰基苄基）-7-氰基-2-甲基吲哚啉-3-基}乙酸{1- [3-氯-4-（吗啉-4-磺酰基）苄基] -7-氰基-2-甲基吲哚啉-3-基}乙酸， {1-（3-氯-4-乙磺酰基苯基硫烷基）-7-氰基-2-甲基吲哚啉-3-基}乙酸{1- [3-氯-4-（吗啉-4-磺基）苯基f烷基] 氰基-2-甲基吲哚啉-3-基}乙酸，{7-氰基-1-（6-氟喹啉-2-基甲基）-2-甲基吲哚啉-3-基}乙酸是CRTH2受体的配体，可用于治疗呼吸系统疾病。

5. 发明申请

WO2008122784A1 QUINOLINES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：喹啉及其治疗用途
公开(公告)号：WO2008122784A1
公开(公告)日：2008-10-16
申请号：PCT/GB2008/001201
申请日：2008-04-03
申请人： ARGENTA DISCOVERY LIMITED , MONTANA, John, Gary , FINCH, Harry , HYND, George , CRAMP, Michael, Colin , ARIENZO, Rosa , MCLEAN, Neville
发明人： MONTANA, John, Gary , FINCH, Harry , HYND, George , CRAMP, Michael, Colin , ARIENZO, Rosa , MCLEAN, Neville
IPC分类号： C07D401/10 , C07D413/10 , C07D417/10 , C07D215/227 , C07D215/233 , A61K31/4709 , A61P11/00
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: R 1 is halogen or cyano; R 2 is hydrogen or methyl; R 3 and R 4 are independently -OR 6 , C 1 -C 6 alkyl or C 3 -C 6 cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R 5 is hydrogen or halogen; R 6 is C 1 C 6 alkyl or C 3 -C 6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is -CH 2 -, -S-, or -O-; one of Y and Y 1 is hydrogen and the other is OR 6 , -C(=O)R 7 , NR 8 SO 2 R 6 or a heterocyclic group selected from those referred to in the specification; and R 6 , R 7 and R 8 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：R 1是卤素或氰基; R 2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，后两个基团任选地被一个或多个卤素原子取代; R 5是氢或卤素; R 6是C 1 -C 6烷基或C 3 -C 6 - 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Y 1之一是氢，另一个是OR 6，-C（= O）R 7，NR 8 或者选自本说明书中提及的那些的杂环基;和/或和R 6，R 7和R 8是如说明书中所定义的。

6. 发明申请

WO2010142934A1 INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS 审中-公开
标题翻译：作为CRTH2受体配体的衍生物
公开(公告)号：WO2010142934A1
公开(公告)日：2010-12-16
申请号：PCT/GB2009/050671
申请日：2009-06-12
申请人： PULMAGEN THERAPEUTICS (ASTHMA) LIMITED , HYND, George , MONTANA, John Gary , FINCH, Harry , ARIENZO, Rosa , AHMED, Shahadat
发明人： HYND, George , MONTANA, John Gary , FINCH, Harry , ARIENZO, Rosa , AHMED, Shahadat
IPC分类号： C07D209/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , A61P37/00 , A61K31/4439 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , A61K31/4178 , A61K31/422 , A61K31/404
CPC分类号： C07D417/14 , C07D209/10 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid, [3-(5-benzenesulfonyloxazol-4-ylmethyl)-5-fluoro-2-methylindol-1-yl]acetic acid, [3-(3-benzenesulfonyl-4-met ylthiophen-2-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {5-fluoro-2-methyl-3-[2-(pyridin-2-ylsulfamoyl)benzyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[4-methyl-3-(pyridine-2-sulfonyl)thiophen-2- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[3-methyl-5-(pyridine-2-sulfonyl)-3H-imidazol-4- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-3-[2-(3-fluorophenylsulfamoyl)pyridin-3-ylmethyl]-2-methylindol-1- yl}acetic acid, [3-(4-benzenesulfonyloxazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {3-[2-(3-cyanophenylsulfamoyl)benzyl]-5-fluoro-2-methylindol-1-yl}acetic acid, [3-(4-benzenesulfonylthiazol-5-ylmethyl)-5-chloro-2-methyl-indol-1-yl]acetic acid, [3-(4-benzenesulfonyl-2-methylthiazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, and [3-(4-benzenesulfonyl-3-methylisothiazol-5-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid.
摘要翻译：以下化合物是可用于治疗呼吸系统疾病的CRTH2拮抗剂：{3- [3-氯-4-（吡啶-2-磺酰基）异噻唑-5-基甲基] -5-氟-2-甲基吲哚-1-基} 乙酸，[3-（5-苯磺酰基-3-甲基-3H-咪唑-4-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸[3-（5-苯磺酰基恶唑-4-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸，[3-（3-苯磺酰基-4-甲基噻吩-2-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸， {5-氟-2-甲基-3- [2-（吡啶-2-基氨磺酰基）苄基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [4-甲基-3- （吡啶-2-磺酰基）噻吩-2-基甲基]吲哚-1-基}乙酸{5-氟-2-甲基-3- [3-甲基-5-（吡啶-2-磺酰基）咪唑-4-基甲基]吲哚-1-基}乙酸，{5-氟-3- [2-（3-氟苯基氨磺酰基）吡啶-3-基甲基] -2-甲基吲哚-1-基}乙酸[3 - （4-苯磺酰氧基-5-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸{3- [2-（3-氰基苯基氨磺酰基）苄基] -5-氟-2-甲基吲哚-1-基] 乙酸，[3- （4-苯磺酰基噻唑-5-基甲基）-5-氯-2-甲基 - 吲哚-1-基]乙酸[3-（4-苯磺酰基-2-甲基噻唑-5-基甲基）-5-氟-2- 甲基吲哚-1-基]乙酸和[3-（4-苯磺酰基-3-甲基异噻唑-5-基甲基）-5-氟-2-甲基吲哚-1-基]乙酸。

7. 发明申请

WO2009044134A1 INDOLIZINE DERIVATIVES WITH CRTH2 RECEPTOR AFFINITY FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：具有CRTH2受体亲和力的吲哚美辛衍生物用于治疗炎症性疾病
公开(公告)号：WO2009044134A1
公开(公告)日：2009-04-09
申请号：PCT/GB2008/003328
申请日：2008-10-02
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John, Gary , FINCH, Harry
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are ligands of the CRTH2 receptor useful in the treatment of, for example, inflammatory respiratory diseases: R 1 is fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; X is -CH 2 -, or - S(O) n -; Ar 1 is phenyl or 5- or 6-membered heteroaryl, wherein the phenyl or heteroaryl rings are optionally substituted with one substituent selected from fluoro, chloro, CN, -O(C 1 C 3 alkyl) or C 1 -C 3 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; Y is -CR 3 R 4 -, -C(O)-, -O-, -S(O) n - or -NR 3 -; R 3 and R 4 independently represent hydrogen or C 1 C 3 alkyl; Ar 2 is phenyl or 5- or 6- membered heteroaryl, wherein the phenyl or heteroaryl rings are optionally substituted by one or more substituents independently selected from halogen, - CN, -S(O) n R 5 , -S(O) 2 NR 6 R 7 , -NR 6 S(O) 2 R 5 -NR 6 R 7 , -NR 6 COR 5 , -CONR 6 R 7 , - COR 5 , -OR 6 , C 1 C 6 alkyl or C 3 -C 7 cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; R 5 is C 1 C 6 alkyl or C 3 -C 7 cycloalkyl, optionally substituted by one or more fluoro atoms; R 6 and R 7 independently represent hydrogen, C 1 C 6 alkyl or C 3 -C 7 cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and n is O, 1 or 2.
摘要翻译：式（I）化合物是可用于治疗例如炎症性呼吸道疾病的CRTH2受体的配体：R 1是氟，氯，CN或CF 3; R2是氢，氟或氯; X是-CH 2 - 或-S（O）n - ; Ar1为苯基或5-或6-元杂芳基，其中苯基或杂芳基环任选被一个选自氟，氯，CN，-O（C 1 -C 3烷基）或C 1 -C 3烷基的取代基取代，后两个基团任选被一个或多个氟原子; Y是-CR 3 R 4 - ， - C（O） - ， - O - ， - S（O）n - 或-NR 3 - ; R3和R4独立地表示氢或C1C3烷基; Ar 2是苯基或5-或6-元杂芳基，其中苯基或杂芳基环任选地被一个或多个独立地选自卤素，-CN，-S（O）nR 5，-S（O）2 NR 6 R 7，-NR 6 S （O）2R5 -NR6R7，-NR6COR5，-CONR6R7，-COR5，-OR6，C1C6烷基或C3-C7环烷基，后两个基团任选被一个或多个氟原子取代; R5是任选被一个或多个氟原子取代的C 1 -C 6烷基或C 3 -C 7环烷基; R6和R7独立地表示氢，C1C6烷基或C3-C7环烷基，后两个基团任选被一个或多个氟原子取代; 并且n为O，1或2。

8. 发明申请

WO2007036743A3 QUINOLINES AND THEIR THERAPEUTIC USE 审中-公开
公开(公告)号：WO2007036743A3
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003644
申请日：2006-09-29
申请人： ARGENTA DISCOVERY LTD. , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
发明人： CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
IPC分类号： A61K31/47 , A61P11/00 , A61P43/00 , C07D215/00
摘要： Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R 1 , R 2 , R 3 , R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl, C 1 - C 6 fluoroalkyl, cyclopropyl, halo, -S(O) n R 6 , -SO 2 NR 7 R 8 , -NR 7 R 8 , -NR 7 C(O)R 6 , -CO 2 R 7 , -C(O)NR 7 R 8 , -C(O)R 6 , -NO 2 , -CN or a group -OR 9 ; wherein each R 6 is independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R 7 , R 8 are independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, cycloalkyl-(C 1 -C 6 alkyl)-, aryl, heteroaryl or hydrogen; R 9 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, cylcoalkyl-(C 1 -C 6 alkyl)-, or a group -SO 2 R 6 ; A is -CHR 10 -, -C(O)-, -S(O) n -, -0-, or -NR 10 - wherein n is an integer from 0-2 and R 10 is hydrogen, C 1 -C 3 alkyl, or C 1 -C 6 fluoroalkyl group; B is a direct bond, or a divalent radical selected from -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 -, and divalent radicals of formula -(CR 11 R 12 ) P -Z- wherein Z is attached to the ring carrying R 1 , R 2 and R 3 ; wherein R 11 is C 1 -C 3 alkyl, cyclopropyl, C 1 -C 6 fluoroalkyl; R 12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is -0-, -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)NHSO 2 R 6 or SO 2 NHC(=O)R 6 ; and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.

9. 发明申请

WO2009090399A1 INDOLES ACTIVE ON CRTH2 RECEPTOR 审中-公开
标题翻译：在CRTH2受体上有活性的
公开(公告)号：WO2009090399A1
公开(公告)日：2009-07-23
申请号：PCT/GB2009/000124
申请日：2009-01-16
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John, Gary , FINCH, Harry
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry
IPC分类号： C07D209/22 , A61K31/405 , A61P29/00
CPC分类号： C07D209/22
摘要： Indole derivatives having therapeutic utility are of formula (I): X is -SO 2 - or *-SO 2 NR 3 - wherein the bond marked with an asterisk is attached to Ar 1 ; R 1 and R 2 are, independently, hydrogen, fluoro, chloro, CN or CF 3 ; R 3 is hydrogen, C 1 -C 8 alkyl or C 3 -C 7 cycloalkyl; and Ar 1 and Ar 2 are, independently, phenyl or a 5- or 6-membered heteroaryl group, wherein the phenyl or heteroaryl group is optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C 3 -C 7 cycloalkyl, -O(C 1 -C 4 alkyl) or C 1 -C 6 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.
摘要翻译：具有治疗用途的吲哚衍生物具有式（I）：X是-SO 2 - 或* -SO 2 NR 3 - ，其中用星号标记的键连接到Ar1; R 1和R 2独立地是氢，氟，氯，CN或CF 3; R3是氢，C1-C8烷基或C3-C7环烷基; 并且Ar 1和Ar 2独立地是苯基或5或6元杂芳基，其中苯基或杂芳基任选被一个或多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（ C1-C4烷基）或C1-C6烷基，后两个基团任选被一个或多个氟原子取代。

10. 发明申请

WO2009044147A1 INDOLIZINE DERIVATIVES WITH CRTH2 RECEPTOR AFFINITY FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：具有CRTH2受体亲和力的吲哚美辛衍生物用于治疗炎症性疾病
公开(公告)号：WO2009044147A1
公开(公告)日：2009-04-09
申请号：PCT/GB2008/003345
申请日：2008-10-02
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John, Gary , FINCH, Harry , CRAMP, Michael, Colin , GOLD, Johan , CARNEVALE, Gennaro
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry , CRAMP, Michael, Colin , GOLD, Johan , CARNEVALE, Gennaro
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are ligands of the CRTH2 receptor, useful in the treatment of, for example, inflammatory respiratory disease: R 1 is fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; X is -CH 2 -, or - S(O) n -; Ar 1 is phenyl or 5- or 6-membered heteroaryl, wherein the phenyl or heteroaryl rings are optionally substituted with one substituent selected from fluoro, chloro, CN, -O(C 1 -C 3 alkyi) or C 1 -C 3 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; Y is -CR 3 R 4 -, -C(O)-, -O-, -S(O) 2 - or -NR 3 -; R 3 and R 4 independently represent hydrogen or C 1 -C 3 alkyl; Ar 2 is phenyl or 5- or 6- membered heteroaryl, wherein the phenyl or heteroaryl rings are optionally substituted by one or more substituents independently selected from halogen, - CN, -S(O) n R 5 , -S(O) 2 NR 6 R 7 , -NR 6 S(O) 2 R 5 -NR 6 R 7 , -NR 6 COR 5 , -CONR 6 R 7 , -COR 5 , -OR 6 , C 1 - C 6 alkyl or C 3 -C 7 cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; R 5 is C 1 -C 6 alkyl or C 3 -C 7 cycloalkyl, optionally substituted by one or more fluoro atoms; R 6 and R 7 independently represent hydrogen, C 1 -C 6 alkyl or C 3 -C 7 cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and n is O, 1 or 2.
摘要翻译：式（I）化合物是CRTH2受体的配体，可用于治疗例如炎性呼吸系统疾病：R1是氟，氯，CN或CF3; R2是氢，氟或氯; X是-CH 2 - 或-S（O）n - ; Ar1为苯基或5-或6-元杂芳基，其中苯基或杂芳基环任选被一个选自氟，氯，CN，-O（C 1 -C 3烷基）或C 1 -C 3烷基的取代基取代，后两个基团任选被一个或多个氟原子取代; Y是-CR 3 R 4 - ， - C（O） - ， - O - ， - S（O）2 - 或-NR 3 - ; R3和R4独立地表示氢或C1-C3烷基; Ar 2是苯基或5-或6-元杂芳基，其中苯基或杂芳基环任选地被一个或多个独立地选自卤素，-CN，-S（O）nR 5，-S（O）2 NR 6 R 7，-NR 6 S （O）2R5 -NR6R7，-NR6COR5，-CONR6R7，-COR5，-OR6，C1- C6烷基或C3-C7环烷基，后两个基团任选被一个或多个氟原子取代; R5是任选被一个或多个氟原子取代的C 1 -C 6烷基或C 3 -C 7环烷基; R6和R7独立地表示氢，C1-C6烷基或C3-C7环烷基，后两个基团任选被一个或多个氟原子取代; 并且n为O，1或2。

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