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1. 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。

2. 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。

3. 发明申请

WO2007129060A1 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：WO2007129060A1
公开(公告)日：2007-11-15
申请号：PCT/GB2007/001638
申请日：2007-05-03
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 , A61K47/55 , C07D519/00
摘要： Compounds of formula (I) and multimers thereof are inhibitors of human neutrophil elastase activity, and 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。

4. 发明申请

WO2009060203A1 3,4,6,7-TETRAHYDRO-1 H-PYRROLO[3,4-D]PYRIMIDINE-2,5-DIONES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： 3,4,6,7-四氢-1H-吡咯并[3,4-D]嘧啶-2,5-二酮及其治疗用途
公开(公告)号：WO2009060203A1
公开(公告)日：2009-05-14
申请号：PCT/GB2008/003752
申请日：2008-11-07
申请人： ARGENTA DISCOVERY LIMITED , FINCH, Harry , RAY, Nicholas, Charles , EDWARDS, Christine
发明人： FINCH, Harry , RAY, Nicholas, Charles , EDWARDS, Christine
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00
CPC分类号： C07D487/04
摘要： A compound of formula (IA) or (IB): wherein A is aryl or heteroaryl; D is oxygen or sulphur; R 1 , R 2 , R 3 and R 5 are independently each hydrogen, halogen, nitro, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, hydroxy or C 1 -C 6 -alkoxy or C 2 -C 6 - alkenyloxy,, wherein C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy can be further substituted with one to three identical or different radicals selected from the group consisting of halogen, hydroxy and C 1 -C 4 -alkoxy; R 4 is hydrogen CrC6-alkyl, formyl, aminocarbonyl, mono- or di-C 1 -C 4 - alkylaminocarbonyl, C 3 -C 8 -cycloalkylcarbonyl, C 1 -C 6 -alkylcarbonyl, C 1 -C 6 - alkoxycarbonyl, N-(C 1 -C 4 -alkylsulfonyl)-aminocarbonyl, N-(C 1 -C 4 -alkylsulfonyl)-N-(C 1 -C 4 -alkyl)-aminocarbonyl, heteroaryl, heterocycloalkyl, heteroarylcarbonyl or heterocycloalkylcarbonyl; wherein C 1 -C 6 -alkyl, mono- and di-C 1 -C 4 - alkylaminocarbonyl, C 1 -C 6 -alkylcarbonyl, C 1 -C 2 -alkoxycarbonyl, heteroaryl and heterocycloalkyl can be substituted with one to three identical or different radicals selected from the group consisting of aryl, heteroaryl, hydroxyl, C 1 -C 4 -alkoxy, hydroxycarbonyl, C 1 -C 6 -alkoxycarbonyl, aminocarbonyl, mono and di-C 1 -C 4 - alkylaminocarbonyl, amino, mono- and di-C 1 -C 4 -alkylamino, C 1 -C 4 - alkylcarbonylamino, cyano, N-(mono- and di-Ci-C4-alkylamino-d-C4-alkyl)- aminocarbonyl, N-(C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl)-aminocarbonyl or halogen; -[Linker]- is a divalent linker radical; and M is a moiety having M3 receptor antagonist activity.
摘要翻译：式（IA）或（IB）的化合物：其中A是芳基或杂芳基; D是氧或硫; R1，R2，R3和R5各自独立地为氢，卤素，硝基，氰基，C1-C6-烷基，C2-C6-烯基，C2-C6-炔基，羟基或C1-C6-烷氧基或C2-C6-烯氧基，其中C 1 -C 6 - 烷基和C 1 -C 6 - 烷氧基可以被一至三个相同或不同的选自卤素，羟基和C 1 -C 4 - 烷氧基的基团取代; R4是氢C 1 -C 6烷基，甲酰基，氨基羰基，单或二-C 1 -C 4烷基氨基羰基，C 3 -C 8环烷基羰基，C 1 -C 6烷基羰基，C 1 -C 6烷氧基羰基，N-（C 1 -C 4烷基磺酰基）氨基羰基，N-（C 1 -C 4 - 烷基磺酰基）-N-（C 1 -C 4 - 烷基） - 氨基羰基，杂芳基，杂环烷基，杂芳基羰基或杂环烷基羰基; 其中C 1 -C 6烷基，单 - 和二-C 1 -C 4 - 烷基氨基羰基，C 1 -C 6 - 烷基羰基，C 1 -C 2 - 烷氧基羰基，杂芳基和杂环烷基可以被一至三个相同或不同的基团取代，所述基团选自芳基，杂芳基，羟基，C 1 -C 4 - 烷氧基，羟基羰基，C 1 -C 6 - 烷氧基羰基，氨基羰基，单和二-C 1 -C 4烷基氨基羰基，氨基，单 - 和二-C 1 -C 4烷基氨基，C 1 -C 4烷基羰基氨基氰基，N-（单和二-C 1 -C 4烷基氨基 - C 1 -C 4 - 烷基） - 氨基羰基，N-（C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基） - 氨基羰基或卤素; - [连接子] - 是二价连接基团; M为具有M3受体拮抗剂活性的部分。

5. 发明申请

WO2007107706A2 MULTIMERS QF HETEROCYCLIC COMPOUNDS AND THEIR USE 审中-公开
标题翻译：多元QF杂环化合物及其用途
公开(公告)号：WO2007107706A2
公开(公告)日：2007-09-27
申请号：PCT/GB2007/000919
申请日：2007-03-16
申请人： ARGENTA DISCOVERY LIMITED , FINCH, Harry , EDWARDS, Christine , RAY, Nicholas, Charles
发明人： FINCH, Harry , EDWARDS, Christine , RAY, Nicholas, Charles
IPC分类号： A61K47/48
CPC分类号： C07D401/12 , A61K47/55 , C07D213/82 , C07D213/85 , C07D401/14 , C07D413/14
摘要： Covalent conjugates of two or more compounds, each having a structure as defined in any of WO2004/043924, WO2005/021509, WO2005/021512, WO2005/026123, WO2005/026124, WO2006/098683 and WO2006/098684, are inhibitors of human neutrophil elastase, useful in treatment of, for example, chronic obstructive pulmonary disease. Dimers of formula (IA) or (IB): wherein LINKER and the variable substituents are particular types of such multimers.
摘要翻译：任何具有如WO2004 / 043924，WO2005 / 021509，WO2005 / 021512，WO2005 / 026123，WO2005 / 026124，WO2006 / 098683和WO2006 / 098684中任一项所定义的结构的两种或更多种化合物的共价缀合物是人嗜中性粒细胞抑制剂弹性蛋白酶，可用于治疗例如慢性阻塞性肺疾病。式（IA）或（IB）的二聚体：其中LINKER和可变取代基是这种多聚体的特定类型。

6. 发明申请

WO2009037413A1 DIMERS OF 5- [ (4-CYANOPHENYL) SULFINYL] -6-METHYL-2-OXO-1- [3- (TRIFLUOROMETHYL)PHENYL] -1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE AS INHIBITORS OF HUMAN NEUTROPHIL ELASTASE FOR TREATING RESPIRATORY DISEASES 审中-公开
标题翻译： 5- [（4-氰基苯基）磺酰基] -6-甲基-2-氧代-1- [3-（三氟甲基）苯基] -1,2-二氢吡啶-3-羧酰胺作为人类中性粒细胞酶抑制剂治疗呼吸道疾病
公开(公告)号：WO2009037413A1
公开(公告)日：2009-03-26
申请号：PCT/GB2007/003537
申请日：2007-09-19
申请人： ARGENTA DISCOVERY LIMITED , FINCH, Harry , RAY, Nicholas, Charles , EDWARDS, Christine
发明人： FINCH, Harry , RAY, Nicholas, Charles , EDWARDS, Christine
IPC分类号： C07D213/82 , A61K31/444 , A61P11/00
CPC分类号： C07D213/82
摘要： Six specific compounds having human neutrophil elastase inhibitory activity are disclosed, one of which has the structural formula wherein A - is a pharmaceutically acceptable anion. 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六种具体化合物，其中一种具有结构式，其中A-是药学上可接受的阴离子。所述化合物特别用于治疗炎性呼吸系统疾病，并且可以通过吸入给药。

7. 发明申请

WO2006082412A2 MULTIMERS OF HETEROCYCLIC COMPOUNDS AND THEIR USE 审中-公开
标题翻译：多元醇的杂环化合物及其用途
公开(公告)号：WO2006082412A2
公开(公告)日：2006-08-10
申请号：PCT/GB2006/000361
申请日：2006-02-03
申请人： ARGENTA DISCOVERY LTD , FINCH, Harry , EDWARDS, Christine , RAY, Nicholas, Charles , O'CONNOR, Elizabeth, Anne , FITZGERALD, Mary, F.
发明人： FINCH, Harry , EDWARDS, Christine , RAY, Nicholas, Charles , O'CONNOR, Elizabeth, Anne , FITZGERALD, Mary, F.
IPC分类号： C07D239/22 , C07D401/12 , C07D403/14 , A61K31/513 , A61P9/00
CPC分类号： C07D239/22 , A61K31/513 , A61K47/55 , C07D401/12 , C07D403/14
摘要： A compound of formula (I): M-L-M, wherein L is a linker and each M is independently a group of formula (II): is useful in therapy, e.g. of respiratory diseases.
摘要翻译：式（I）的化合物：M-L-M，其中L是连接体，每个M独立地是式（II）的基团：可用于治疗，例如，的呼吸系统疾病。

8. 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。

9. 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。

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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