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1. 发明申请

US20100010034A1 CRTH2 ANTAGONISTS 审中-公开
公开(公告)号：US20100010034A1
公开(公告)日：2010-01-14
申请号：US12519979
申请日：2006-12-21
申请人： George Hynd , Nicholas Charles Ray , Harry Finch , David Middlemiss , Michael Colin Cramp , Paul Matthew Blaney , Karen Williams , Yann Griffon , Trevor Keith Harrison , Peter Crackett
发明人： George Hynd , Nicholas Charles Ray , Harry Finch , David Middlemiss , Michael Colin Cramp , Paul Matthew Blaney , Karen Williams , Yann Griffon , Trevor Keith Harrison , Peter Crackett
IPC分类号： A61K31/44 , C07D471/04 , A61P11/00 , A61P1/00
CPC分类号： C07D471/04
摘要： The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: [3-(2,4-dichlorophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(2-fluoro-4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methanesulfonyl-2-trifluoromethylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, (R)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, [3-(4-ethanesulfonylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, (S)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, ethanesulfonylaminobenzenesulfonyl)-6-fluoro-2-methyiindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(2-chloro-4-methanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(4-methanesulfonylbenzyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-chlorobenzyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(6-fluoroquinolin-2-yl-methyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-bromophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, and [3-(4-cyclopropylsulfamoylphenylsulfanyl)-6-fluoro-2-methylindolizin-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-（2,4-二氯苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸[6-氟-3-（2- （4-甲基磺酰基-2-三氟甲基苯基硫烷基）-2-甲基吲哚哩啶-1-基]乙酸，（R） - （4-氟-4-甲磺酰基苯基硫烷基）-2-甲基吲哚啉-1-基] 2- [6-氟-3-（4-甲磺酰基苯基硫基）-2-甲基吲哚啉-1-基]丙酸，[3-（4-乙磺酰基苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸，（S）-2- [6-氟-3-（4-甲磺酰基苯基硫烷基）-2-甲基吲哚啉-1-基]丙酸，乙磺酰氨基苯磺酰基）-6-氟-2-甲基吲哚啉-1-基]乙酸[7 （4-甲磺酰基苯基硫烷基）-2-甲基吲哚哩啶-1-基]乙酸[3-（2-氯-4-甲磺酰基苯基硫烷基）-7-氰基-2-甲基吲哚啉-1-基] ]乙酸[6-氰基-3-（4-甲磺酰基苄基）-2-甲基吲哚啉-1-基]乙酸[3-（4-氯苄基）-7-氰基-2-甲基吲哚吡啶-1-基]乙酸[6-氰基-3-（6-氟喹啉-2-基 - 甲基）-2-甲基吲哚啉-1-基]乙酸[6-氟-3-（4-甲氧基苯基硫烷基）-2-甲基吲哚啉-1-基]乙酸[7-氯-6-氟-3-（4-甲氧基苯基硫烷基）-2-甲基吲哚啉-1-基]乙酸[3-（4-溴苯基硫基） - 6-氟-2-甲基吲哚啉-1-基]乙酸和[3-（4-环丙基氨磺酰基苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸。

2. 发明申请

US20090163534A1 Indolizine Derivatives 审中-公开
标题翻译：中氮衍生物
公开(公告)号：US20090163534A1
公开(公告)日：2009-06-25
申请号：US11993412
申请日：2006-06-26
申请人： George Hynd , Nicholas Charles Ray , Harry Finch , David Middlemiss , Michael Colin Cramp , Paul Matthew Blaney , Karen Williams , Yan Griffon , Trevor Keith Harrison , Peter Crackett
发明人： George Hynd , Nicholas Charles Ray , Harry Finch , David Middlemiss , Michael Colin Cramp , Paul Matthew Blaney , Karen Williams , Yan Griffon , Trevor Keith Harrison , Peter Crackett
IPC分类号： A61K31/437 , C07D221/04 , A61P29/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R1, R2, R3 and R4 each independently are hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl, 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 C1C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl or a group —SO2R9; n is 0, 1 or 2; R5 is C1C6alkyl, fully or partially fluorinated C1C6alkyl. C1C6alkenyl, C1C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1C6alkyl or fully or partially fluorinated C1C6alkyl; R7 and R5 are independently hydrogen or C1C6alkyl, or R7 and R5 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —NR6SO2— or —SO2NR6— wherein n is 0, 1 or 2.
摘要翻译：式（I）化合物是CRTH2受体的配体，可用于治疗呼吸系统疾病：其中R 1，R 2，R 3和R 4各自独立地为氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，卤素， S（O）nR10，-SO2N（R10）2，-N（R10）2，-C（O）N（R10）2，-NR10C（O）R9，-CO2R10，-C（O），-CN或-OR11; 其中每个R 9独立地为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 9; n为0,1或2; R5是C1C6烷基，完全或部分氟化的C1C6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，C1C6烷基或完全或部分氟化的C 1 -C 6烷基; R 7和R 5独立地为氢或C 1 -C 6烷基，或者R 7和R 5与它们所连接的原子一起形成环烷基; 且X为-CHR 6 - ， - S（O）n - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

3. 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。

4. 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。

5. 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。

6. 发明申请

US20100137300A1 Indolizine Acetic Acid Derivatives as CRTH2 Antagonists 审中-公开
标题翻译： Indolizine乙酸衍生物作为CRTH2拮抗剂
公开(公告)号：US20100137300A1
公开(公告)日：2010-06-03
申请号：US12530929
申请日：2007-03-21
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： A61K31/5377 , A61K31/435 , A61K31/4709 , C07D413/12 , C07D221/04 , C07D215/14 , A61P1/00 , A61P11/06 , A61P11/00 , A61P1/04
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-ylmethyl)-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。

7. 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。

8. 发明申请

US20120184579A1 Quinolines and Their Therapeutic Use 有权
标题翻译：喹啉及其治疗用途
公开(公告)号：US20120184579A1
公开(公告)日：2012-07-19
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： A61K31/4709 , C07D413/10 , C07D215/22 , C07D417/10 , A61P37/08 , A61P11/06 , A61P11/00 , A61P17/06 , A61P1/00 , A61P17/00 , C07D401/10 , A61K31/47
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。

9. 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。

10. 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。

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