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1. 发明申请

WO2006015870A1 TETRAHYDRO-NAPHTHALENE DERIVATIVES AS GLUCOCORTICOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为葡萄糖激素受体调节剂的四氢萘衍生物
公开(公告)号：WO2006015870A1
公开(公告)日：2006-02-16
申请号：PCT/EP2005/008763
申请日：2005-08-10
申请人： GLAXO GROUP LIMITED , EDWARDS, Christine , FENTON, Garry , MACDONALD, Simon, John, Fawcett , WEINGARTEN, Gordon, Gad
发明人： EDWARDS, Christine , FENTON, Garry , MACDONALD, Simon, John, Fawcett , WEINGARTEN, Gordon, Gad
IPC分类号： A61K31/47 , C07D215/04 , C07D217/04 , A61K31/472 , A61P17/00 , A61P29/00
CPC分类号： C07C255/34 , C07C17/2635 , C07C25/24 , C07C45/29 , C07C45/30 , C07C45/69 , C07C47/273 , C07C49/233 , C07C49/237 , C07C57/50 , C07C255/33 , C07C2602/10 , C07D215/38 , C07D217/02 , C07D303/08
摘要： The present invention is directed to compounds of formula (I): wherein R represents a methyl or an ethyl group X represents N, C-H or C-CH 3 when X represents C-H or C-CH 3 , Y represents N when X represents N, Y represents C-H and physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.
摘要翻译：本发明涉及式（I）的化合物：其中R表示甲基或乙基，X表示N，C-H或C-CH

2. 发明申请

WO2009060206A1 3,4,6,7-TETRAHYDRO-1H-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：WO2009060206A1
公开(公告)日：2009-05-14
申请号：PCT/GB2008/003755
申请日：2008-11-07
申请人： ARGENTA DISCOVERY LIMITED , KULAGOWSKI, Janusz , EDWARDS, Christine
发明人： KULAGOWSKI, Janusz , EDWARDS, Christine
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Compounds in which two substituted 3,4,6,7-tetrahydro-1 H-pyrrolo[3,4-d]pyrimidine-2,5- dione molecules are covalently linked via a linker radical which has contains a betaine or zwitterionic motif are inhibitors of human neutrophil elastase activity, for the treatment of respiratory diseases, especially by inhalation.
摘要翻译：其中两个取代的3,4,6,7-四氢-1H-吡咯并[3,4-d]嘧啶-2,5-二酮分子通过含有甜菜碱或两性离子基序的连接基团共价连接的化合物是人嗜中性粒细胞弹性蛋白酶活性抑制剂，用于治疗呼吸道疾病，特别是通过吸入。

3. 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。

4. 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。

5. 发明申请

WO2013037809A1 TETRAHYDROTRIAZOLOPYRIMIDINE DERIVATIVES AS HUMAN NEUTROPHIL ELASTASE INHIBITORS 审中-公开
标题翻译：四氢叶酸嘧啶衍生物作为人类中性粒细胞抑制剂
公开(公告)号：WO2013037809A1
公开(公告)日：2013-03-21
申请号：PCT/EP2012/067810
申请日：2012-09-12
申请人： CHIESI FARMACEUTICI S.p.A. , BLENCH, Toby Jonathan , EDWARDS, Christine , HEALD, Robert Andrew , KULAGOWSKI, Janusz Jozef , SUTTON, Jonathan Mark , CAPALDI, Carmelida
发明人： BLENCH, Toby Jonathan , EDWARDS, Christine , HEALD, Robert Andrew , KULAGOWSKI, Janusz Jozef , SUTTON, Jonathan Mark , CAPALDI, Carmelida
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) are inhibitors of human neutrophil elastase.
摘要翻译：式（I）化合物是人嗜中性粒细胞弹性蛋白酶的抑制剂。

6. 发明申请

WO2010086638A1 DIMERIC PYRROLOPYRIMIDINEDIONE AND ITS USE IN THERAPY OF RESPIRATORY DISEASES 审中-公开
标题翻译：二甲基吡咯啉二酮及其在呼吸道疾病治疗中的应用
公开(公告)号：WO2010086638A1
公开(公告)日：2010-08-05
申请号：PCT/GB2010/050092
申请日：2010-01-22
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , EDWARDS, Christine , KULAGOWSKI, Janus , FINCH, Harry
发明人： EDWARDS, Christine , KULAGOWSKI, Janus , FINCH, Harry
IPC分类号： C07D519/00 , A61K31/519 , A61P11/00
CPC分类号： C07D519/00
摘要： The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation.
摘要翻译：式（I）化合物是人嗜中性粒细胞弹性蛋白酶抑制剂，可用于肺部炎症的吸入治疗。

7. 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。

8. 发明申请

WO2006002434A2 NOVEL INDAZOLE CARBOXAMIDES AND THEIR USE 审中-公开
标题翻译：新型吲唑羧酰胺及其用途
公开(公告)号：WO2006002434A2
公开(公告)日：2006-01-05
申请号：PCT/US2005/022870
申请日：2005-06-24
申请人： SMITHKLINE BEECHAM CORPORATION , KERNS, Jeffrey, K. , EDWARDS, Christine
发明人： KERNS, Jeffrey, K. , EDWARDS, Christine
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14
摘要： The invention is directed to novel indazole carboxamide derivatives. Specifically, the invention is directed to compounds according to Formula (I), wherein R1 and Z are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKß) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新型吲唑甲酰胺衍生物。具体而言，本发明涉及式（I）的化合物及其药学上可接受的盐，其中R 1和Z如下定义。本发明的化合物是IKK2的抑制剂，并且可用于治疗与不适当的IKK2（也称为IKK＆szlig;）活性相关的病症，例如类风湿性关节炎，哮喘和COPD（慢性阻塞性肺病）。因此，本发明还涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制IKK2活性和治疗与之相关的病症的方法。

9. 发明申请

WO2011110858A1 PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF RESPIRATORY DISEASES SUCH AS COPD 审中-公开
标题翻译：吡嗪衍生物及其在治疗呼吸道疾病如COPD中的应用
公开(公告)号：WO2011110858A1
公开(公告)日：2011-09-15
申请号：PCT/GB2011/050477
申请日：2011-03-10
申请人： PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED , EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
发明人： EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
IPC分类号： C07D487/04 , A61K31/519 , A61P1/00 , A61P11/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C-R 1 or N; -X 1 -X 2 - is CR 15 =N- or -NR 19 -CO-; and R 1 -R 6 , R 15 , R 15 and R 19 are as defined in the claims.
摘要翻译：式（I）化合物是中性粒细胞弹性蛋白酶抑制剂，其中A是C-R1或N; -X1-X2-是CR15 = N-或-NR19-CO-; 并且R 1 -R 6，R 15，R 15和R 19如权利要求中所定义。

10. 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。

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