专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

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

US20120277275A1 AZOLE AND THIAZOLE DERIVATIVES AND THEIR USE 审中-公开
标题翻译：偶氮和噻唑衍生物及其用途
公开(公告)号：US20120277275A1
公开(公告)日：2012-11-01
申请号：US13454159
申请日：2012-04-24
申请人： Nicholas Charles Ray , Richard James Bull , Harry Finch , Marco van den Heuvel , Jose Antonio Bravo
发明人： Nicholas Charles Ray , Richard James Bull , Harry Finch , Marco van den Heuvel , Jose Antonio Bravo
IPC分类号： A61K31/421 , A61P37/08 , A61P11/06 , A61P11/02 , C07D263/32 , A61P11/00
CPC分类号： C07D263/32 , C07D277/28 , C07D413/06 , C07D413/12
摘要： Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases:
摘要翻译：式（I）化合物可用于治疗涉及增强的M3受体活化的疾病，例如呼吸道疾病：

9. 发明授权

US08198288B2 Tetrahydropyrrolopyrimidinediones and their use in therapy 有权
标题翻译：四氢吡咯并嘧啶二酮及其在治疗中的应用
公开(公告)号：US08198288B2
公开(公告)日：2012-06-12
申请号：US12264621
申请日：2008-11-04
申请人： Nicholas Charles Ray , Harry Finch , Christine Edwards , Elizabeth O'Connor
发明人： Nicholas Charles Ray , Harry Finch , Christine Edwards , Elizabeth O'Connor
IPC分类号： C07D487/04 , A61K31/519 , A61P11/08 , A61P17/06
CPC分类号： C07D487/04
摘要： The subject invention provides compounds of formula (1): including monomers and multimers thereof that are inhibitors of human neutrophil elastase (HNE) activity and are useful in the treatment of diseases or conditions in which HNE plays a part.
摘要翻译：本发明提供式（1）化合物：包括作为人中性粒细胞弹性蛋白酶（HNE）活性抑制剂的单体和多聚体，并且可用于治疗HNE起作用的疾病或病症。

10. 发明申请

US20100144852A1 Bicyclo[2.2.1]hept-7-ylamine Derivatives and Their Uses 失效
标题翻译：双环[2.2.1]庚-7-基胺衍生物及其用途
公开(公告)号：US20100144852A1
公开(公告)日：2010-06-10
申请号：US12063212
申请日：2006-08-08
申请人： Harry Finch , Nicholas Charles Ray , Richard James Bull , Monique Bodil van Niel , Andrew Stephen Robert Jennings
发明人： Harry Finch , Nicholas Charles Ray , Richard James Bull , Monique Bodil van Niel , Andrew Stephen Robert Jennings
IPC分类号： A61K31/381 , C07C269/00 , C07D409/06 , A61K31/24 , A61P11/06 , A61P1/00 , A61P9/10
CPC分类号： C07C271/38 , C07C219/24 , C07C235/36 , C07C2602/42 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/06 , C07D409/14
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula (I) wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5—Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R4 is a group of formula (a), (b), (c) or (d); is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中A是氧原子或基团-N（R12） - ; （ⅰ）R 1是C 1 -C 6 - 烷基或氢原子; 并且R 2是氢原子或基团-R 5，-Z-Y-R 5 -Z-NR 9 R 10; -Z-CO-NR9R10; -Z-NR 9 -CO-R 5; 或-Z-CO 2 H; 并且R 3是孤对的，或者是C 1 -C 6烷基，在这种情况下，与其连接的氮原子是季氮并携带正电荷; 或（ii）R 1和R 3与它们所连接的氮一起形成杂环烷基环，并且R 2是氢原子; 或基团-R5，-Z-Y-R5，-Z-NR9R10，-Z-CO-NR9R10，-Z-NR9-CO-R5或-Z-CO2H，其中，附着是季氮并带正电荷; 或（iii）R 1和R 2与它们所连接的氮一起形成杂环烷基环，所述环被基团-Y-R 5，-Z-Y-R 5，-Z-NR 9 R 10取代; -Z-CO-NR9R10; -Z-NR9-CO-R5; 或-Z-CO 2 H，并且R 3是孤对的，或者C 1 -C 6 - 烷基，在这种情况下，与其连接的氮原子是季氮并带正电荷; R4是式（a），（b），（c）或（d）的基团; 是C 1 -C 6烷基，芳基，芳基稠合环烷基，芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C 1 -C 8 - 烷基） - ，杂芳基（C 1 -C 8 - 烷基） - ，环烷基或杂环烷基，剩余的变量如规范中所定义。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式