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1. 发明申请

WO2011110859A1 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：WO2011110859A1
公开(公告)日：2011-09-15
申请号：PCT/GB2011/050478
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 and R 16 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-; 和R 1 -R 6，R 15和R 16如权利要求中所定义。

2. 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。

3. 发明申请

WO2010034996A1 CRYSTALLINE ACID ADDITION SALTS AND THEIR USE AS ENZYME INHIBITORS 审中-公开
标题翻译：水晶酸添加剂及其作为酶抑制剂使用
公开(公告)号：WO2010034996A1
公开(公告)日：2010-04-01
申请号：PCT/GB2009/002278
申请日：2009-09-23
申请人： ARGENTA DISCOVERY 2009 LIMITED , EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
发明人： EDWARDS, Christine , KULAGOWSKI, Janusz , FINCH, Harry
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P11/00
CPC分类号： C07D519/00 , C07D487/04
摘要： A crystalline acid addition salt of the compound of formula (I), said salt being selected from the hydrogen sulfate, p-toluene sulfonate, naphthalene-2-sulfonate, fumarate, and ethanesulfonate salts thereof. The said salts are inhibitors of human neutrophil elastase (HNE), and thus of use in the treatment of inflammatory conditions, including those of the respiratory tract, especially when administered by inhalation for pulmonary delivey.
摘要翻译：式（I）化合物的结晶酸加成盐，所述盐选自硫酸氢盐，对甲苯磺酸盐，萘-2-磺酸盐，富马酸盐及其乙磺酸盐。所述盐是人嗜中性粒细胞弹性蛋白酶（HNE）的抑制剂，因此可用于治疗炎性病症，包括呼吸道炎症状况，特别是当通过吸入用于肺动脉给药时。

4. 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。

5. 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，

6. 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。

7. 发明申请

WO2013007765A1 FUSED TRICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF JANUS KINASES 审中-公开
标题翻译：用作JANK KINASES的抑制剂的熔融三氯化合物
公开(公告)号：WO2013007765A1
公开(公告)日：2013-01-17
申请号：PCT/EP2012/063621
申请日：2012-07-12
申请人： F. HOFFMANN-LA ROCHE AG , BERGERON, Philippe , BODIL VAN NIEL, Monique , DRAGOVICH, Peter , HURLEY, Christopher , KULAGOWSKI, Janusz , LABADIE, Sharada , MCLEAN, Neville James , MENDONCA, Rohan , PULK, Rebecca , ZAK, Mark
发明人： BERGERON, Philippe , BODIL VAN NIEL, Monique , DRAGOVICH, Peter , HURLEY, Christopher , KULAGOWSKI, Janusz , LABADIE, Sharada , MCLEAN, Neville James , MENDONCA, Rohan , PULK, Rebecca , ZAK, Mark
IPC分类号： C07D471/04 , A61K31/437 , A61P37/00
CPC分类号： C07D471/04
摘要： The invention provides novel compounds of formula (I) having the general formula (I) wherein R 1 , V, W, X, Y and Z are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要翻译：本发明提供具有通式（I）的式（I）的新化合物，其中R 1，V，W，X，Y和Z如本文所述。因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

8. 发明申请

WO2013007768A1 TRICYCLIC HETEROCYCLIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF AS JAK INHIBITORS 审中-公开
标题翻译：三酮杂环化合物，其组合物及其作为JAK抑制剂的使用方法
公开(公告)号：WO2013007768A1
公开(公告)日：2013-01-17
申请号：PCT/EP2012/063632
申请日：2012-07-12
申请人： F. HOFFMANN-LA ROCHE AG , HURLEY, Christopher , KULAGOWSKI, Janusz , ZAK, Mark
发明人： HURLEY, Christopher , KULAGOWSKI, Janusz , ZAK, Mark
IPC分类号： C07D471/04 , C07D471/14 , A61K31/4375 , A61P35/00 , A61P37/00
CPC分类号： C07D471/14 , C07D471/04
摘要： The invention provides novel compounds of formula I having the general formula:(I) wherein R l s R 2 , R 3 , X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要翻译：本发明提供具有以下通式的新的式I化合物：其中R 1，R 2，R 3，X和Y如本文所述。因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

9. 发明申请

WO2012085176A1 TRICYCLIC PYRAZINONE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：三联吡嗪酮化合物，其组合物及其作为JANUS KINASE抑制剂的使用方法
公开(公告)号：WO2012085176A1
公开(公告)日：2012-06-28
申请号：PCT/EP2011/073734
申请日：2011-12-22
申请人： F. HOFFMANN-LA ROCHE AG , HURLEY, Christopher , KULAGOWSKI, Janusz , MAXEY, Robert , WARD, Stuart , ZAK, Mark
发明人： HURLEY, Christopher , KULAGOWSKI, Janusz , MAXEY, Robert , WARD, Stuart , ZAK, Mark
IPC分类号： C07D487/12 , A61K31/4985 , A61P11/00 , A61P29/00
CPC分类号： C07D487/12
摘要： The invention provides novel compounds of formula I having the general formula (I) wherein X, R 1 , R 2 , R 3 and R 5 are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要翻译：本发明提供具有通式（I）的式I的新化合物，其中X，R 1，R 2，R 3和R 5如本文所述。因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

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