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1. 发明申请

WO2006013359A1 MEDICAMENTS FOR TREATING CHRONIC RESPIRATORY DISEASE 审中-公开
标题翻译：治疗慢性呼吸道疾病的药物
公开(公告)号：WO2006013359A1
公开(公告)日：2006-02-09
申请号：PCT/GB2005/003039
申请日：2005-08-03
申请人： ARGENTA DISCOVERY LIMITED , FOX, Craig , FINCH, Harry , FITZGERALD, Mary
发明人： FOX, Craig , FINCH, Harry , FITZGERALD, Mary
IPC分类号： A61K31/52
CPC分类号： A61K31/52 , A61K31/573 , A61K2300/00
摘要： There is provided the use of a methylxanthine compound and a steroid in a synergistic combination for the treatment of a respiratory disease, wherein the methylxanthine compound is administered at a dose which, in isolation, is not effective to treat said disease.
摘要翻译：提供了用于治疗呼吸系统疾病的协同组合中的甲基黄嘌呤化合物和类固醇的用途，其中所述甲基黄嘌呤化合物以分离的方式以不能有效治疗所述疾病的剂量施用。

2. 发明申请

WO2006085102A1 COMBINATION OF METHYLXANTHINE COMPOUNDS AND STEROIDS TO TREAT CHRONIC RESPIRATORY DISEASES 审中-公开
标题翻译：甲基噻嗪化合物与异黄酮联合治疗慢性呼吸道疾病
公开(公告)号：WO2006085102A1
公开(公告)日：2006-08-17
申请号：PCT/GB2006/000482
申请日：2006-02-13
申请人： ARGENTA DISCOVERY LIMITED , FOX, Justian, Craig , FITZGERALD, Mary, Frances , FINCH, Harry
发明人： FOX, Justian, Craig , FITZGERALD, Mary, Frances , FINCH, Harry
IPC分类号： A61K31/52 , A61K31/58 , A61P11/00
CPC分类号： A61K31/58 , A61K31/52 , A61K2300/00
摘要： There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery.
摘要翻译：提供甲基黄嘌呤衍生物如茶碱和类固醇在协同组合中用于治疗慢性阻塞性肺疾病的用途，其中所述组合由吸入途径施用用于肺部递送。

3. 发明申请

WO2010015818A1 RESPIRATORY DISEASE TREATMENT 审中-公开
标题翻译：呼吸道疾病治疗
公开(公告)号：WO2010015818A1
公开(公告)日：2010-02-11
申请号：PCT/GB2009/001920
申请日：2009-08-05
申请人： ARGENTA DISCOVERY LIMITED , FINCH, Harry , FOX, Craig , SAJAD, Mohammed
发明人： FINCH, Harry , FOX, Craig , SAJAD, Mohammed
IPC分类号： A61K9/00 , A61K31/427 , A61P11/00
CPC分类号： A61K31/427 , A61K9/0073 , C07D413/12 , C07D417/12
摘要： There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and a kit.
摘要翻译：提供了适于通过吸入肺部给药的药物组合物，该组合物包含格列酮（如吡格列酮或罗格列酮）和一种或多种药学上可接受的载体和/或赋形剂，并且其中组合物的格列酮含量由至少95重量％的5R对映体和小于5重量％的5S对映异构体。还提供了一个使用和一个工具包。

4. 发明申请

WO2009013444A1 TETRAHYDROPYRROLOPYRIMIDINEDIONES AND THEIR USE AS HUMAN NEUTROPHIL ELASTASE INHIBITORS 审中-公开
标题翻译：四氢吡咯并嘧啶及其作为人类中性粒细胞抑制剂的用途
公开(公告)号：WO2009013444A1
公开(公告)日：2009-01-29
申请号：PCT/GB2007/002825
申请日：2007-07-25
申请人： ARGENTA DISCOVERY LIMITED , RAY, Nicholas, Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth
发明人： RAY, Nicholas, Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) and multimers thereof are inhibitors of human neutrophil elastase activity, and of utility in the treatment of, e.g., COPD : wherein all the substituents are as defined in claim 1.
摘要翻译：式（I）化合物及其多聚体是人中性粒细胞弹性蛋白酶活性的抑制剂，并且在治疗例如COPD中有用：其中所有取代基如权利要求1所定义。

5. 发明申请

WO2008099186A1 HETEROCYCLIC DERIVATIVES AS M3 MUSCARINIC RECEPTORS 审中-公开
标题翻译：杂环衍生物作为M3肌肉接受体
公开(公告)号：WO2008099186A1
公开(公告)日：2008-08-21
申请号：PCT/GB2008/000519
申请日：2008-02-14
申请人： ARGENTA DISCOVERY LIMITED , AVITABILE, Barbara, Giuseppina , FINCH, Harry , KNIGHT, Jamie, David , NADIN, Alan, John , RAY, Nicholas, Charles
发明人： AVITABILE, Barbara, Giuseppina , FINCH, Harry , KNIGHT, Jamie, David , NADIN, Alan, John , RAY, Nicholas, Charles
IPC分类号： C07D471/08 , A61K31/439 , A61P11/00 , A61P9/00 , A61P1/00
CPC分类号： C07D471/08
摘要： This invention relates to M3 antagonists of formula (I) wherein R 2 , R 4 , R 5 , R 6 , W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.
摘要翻译：本发明涉及式（I）的M3拮抗剂，其中R 2，R 4，R 5，R 5，R 5， R 6，W，V，A，D，X，t，u和v如本文所定义; 含有它们的药物组合物其制备方法; 以及它们在治疗与M3受体激活有关的疾病时的用途。

6. 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。

7. 发明申请

WO2008078069A1 INDOLIZINEACETIC ACIDS AND THEIR THERAPEUTIC USE AS LIGANDS OF THE CRTH2 RECEPTOR 审中-公开
标题翻译：吲哚啉酸及其作为CRTH2受体配体的治疗用途
公开(公告)号：WO2008078069A1
公开(公告)日：2008-07-03
申请号：PCT/GB2007/004789
申请日：2007-12-13
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John , FINCH, Harry , HARRISON, Trevor , KULAGOWSKI, Janusz
发明人： HYND, George , MONTANA, John , FINCH, Harry , HARRISON, Trevor , KULAGOWSKI, Janusz
IPC分类号： C07D471/04 , A61K31/437 , A61K31/5375 , A61K31/506 , A61K31/496 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, inter alia, respiratory diseases: wherein R 1 is fluoro, chloro, cyano or trifluoromethyl; R 2 is hydrogen, fluoro or chloro; R 3 is hydrogen, fluoro, chloro or trifluoromethyl; X is -CH 2 -, -S-, -S(=O)- or -S(=O) 2 -; one of Y and Y 1 is hydrogen and the other is -C(=O)R 4 , or -S(=O) 2 R 4 , or -CR 5 R 6 OR 7 or a heterocyclic group selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, furazanyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3- thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,2,4-triazinyl and 1,3,5-triazinyl any of which may be optionally substituted; R 4 is an optionally substituted cyclic amino group having 5, 6 or 7 ring atoms which is linked to the carbonyl or sulfonyl through a ring nitrogen; R 5 and R 6 are independently hydrogen, (C 1 C 3 )alkyl, cyclopropyl, or R 5 and R 6 taken together with the carbon atom to which they are attached form a 3-6 membered cycloalkyl ring; and R 7 is optionally substituted (C 1 -C 6 )alkyl or (C 3 - C 6 )cycloalkyl,
摘要翻译：式（I）化合物是CRTH2配体，可用于治疗呼吸系统疾病，其中R 1是氟，氯，氰基或三氟甲基; R 2是氢，氟或氯; R 3是氢，氟，氯或三氟甲基; X是-CH 2 - ， - S - ， - S（= O） - 或-S（= O）2 - 。 Y和Y 1中的一个是氢，另一个是-C（= O）R 4或-S（= O）2 R 4或-CR 5或6或7或选自呋喃基，噻吩基，吡咯基的杂环基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，1,2,3-恶二唑基，1,2,4-恶二唑基，1,3,4-恶二唑基，1,2,5-恶二唑基，呋咱基，1,2 ，3-三唑基，1,2,4-三唑基，1,2,3-噻二唑基，1,2,5-噻二唑基，1,3,4-噻二唑基，1,2,4-噻二唑基，四唑基，吡啶基，哒嗪基，嘧啶基，吡嗪基，1,2,4-三嗪基和1,3,5-三嗪基，其中任何一个可以任选被取代; R 4是具有5,6或7个环原子的任选取代的环状氨基，其通过环氮连接到羰基或磺酰基; R 5和R 6独立地是氢，（C 1 -C 3）3烷基，环丙基或R 5，与它们所连接的碳原子一起形成3-6元环烷基环的O 5+和R 6' 和R 7是任选被取代的（C 1 -C 6 -C 6）烷基或（C 3 -C 6 - C > 6 ）环烷基，

8. 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。

9. 发明申请

WO2009060158A1 4- (4-CYANOPHENYL) -1- (3-TRIFLUOROMETHYLPHENYL) -3,4, 6, 7-TETRAHYDRO-1H-PYRROLO [3, 4- D] PYRIMIDINE-2, 5-DIONE DERIVATIVES AND THEIR USE AS HUMAN NEUTROPHIL ELASTASE INHIBITORS 审中-公开
标题翻译： 4-（4-氰基苯基）-1-（3-三氟甲基苯基）-3,4，6,7-四氢-1H-吡咯并[3,4-D]嘧啶-2,5-二酮衍生物及其作为人中性粒细胞弹性抑制剂
公开(公告)号：WO2009060158A1
公开(公告)日：2009-05-14
申请号：PCT/GB2007/004238
申请日：2007-11-07
申请人： ARGENTA DISCOVERY LIMITED , RAY, Nicholas, Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth , KULAGOWSKI, Janusz
发明人： RAY, Nicholas, Charles , FINCH, Harry , EDWARDS, Christine , O'CONNOR, Elizabeth , KULAGOWSKI, Janusz
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519
CPC分类号： C07D487/04
摘要： Thirty six specific compounds having human neutrophil elastase inhibitory activity are disclosed, one of which has the structural formula (1). The compounds are useful inter alia for the treatment of inflammatory respiratory disease, and may be administered by inhalation.
摘要翻译：公开了具有人嗜中性粒细胞弹性蛋白酶抑制活性的三十六种具体化合物，其中之一具有结构式（1）。所述化合物尤其用于治疗炎性呼吸系统疾病，并且可以通过吸入给药。

10. 发明申请

WO2008074966A1 CRTH2 ANTAGONISTS 审中-公开
公开(公告)号：WO2008074966A1
公开(公告)日：2008-06-26
申请号：PCT/GB2006/004856
申请日：2006-12-21
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MIDDLEMISS, David , CRAMP, Michael, Colin , BLANEY, Paul, Matthew , WILLIAMS, Karen , GRIFFON, Yan , HARRISON, Trevor, Keith , CRACKETT, Peter
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MIDDLEMISS, David , CRAMP, Michael, Colin , BLANEY, Paul, Matthew , WILLIAMS, Karen , GRIFFON, Yan , HARRISON, Trevor, Keith , CRACKETT, Peter
IPC分类号： A61K31/437 , C07D471/04 , A61P37/08
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-ylmethyl)-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-溴苯基硫烷基）-6- -2-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。

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