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1. 发明申请

WO2007057714A2 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2007057714A2
公开(公告)日：2007-05-24
申请号：PCT/GB2006/050397
申请日：2006-11-17
申请人： VECTURA GROUP PLC , RICHARDS, Andrew John McGlashan , STRONG, Peter , MIDDLEMISS, David , HAYES, Ann Gail , MORTON, David, Alexander, Vodden
发明人： RICHARDS, Andrew John McGlashan , STRONG, Peter , MIDDLEMISS, David , HAYES, Ann Gail , MORTON, David, Alexander, Vodden
IPC分类号： A61K31/519 , A61K45/06 , A61P11/06 , A61P11/12 , A61P11/00 , A61P29/00
CPC分类号： A61K45/06 , A61K9/0043 , A61K9/0075 , A61K9/0078 , A61K31/519
摘要： The present invention relates to pharmaceutical compositions and their uses in therapy. In particular, the invention relates to compositions comprising methotrexate, preferably wherein the compositions are for administration via the inhaled or intranasal route.
摘要翻译：本发明涉及药物组合物及其在治疗中的用途。特别地，本发明涉及包含甲氨蝶呤的组合物，优选其中所述组合物经由吸入或鼻内途径施用。

2. 发明公开

EP1951245A2 PHARMACEUTICAL COMPOSITIONS COMPRISING METHOTREXATE 审中-公开
标题翻译：用甲氨蝶呤药物组合物
公开(公告)号：EP1951245A2
公开(公告)日：2008-08-06
申请号：EP06808761.8
申请日：2006-11-17
申请人： Vectura Group PLC
发明人： RICHARDS, Andrew John McGlashan , STRONG, Peter , MIDDLEMISS, David , HAYES, Ann Gail , MORTON, David, Alexander, Vodden
IPC分类号： A61K31/519 , A61K45/06 , A61P11/06 , A61P11/12 , A61P11/00 , A61P29/00
CPC分类号： A61K45/06 , A61K9/0043 , A61K9/0075 , A61K9/0078 , A61K31/519
摘要： The present invention relates to pharmaceutical compositions and their uses in therapy. In particular, the invention relates to compositions comprising methotrexate, preferably wherein the compositions are for administration via the inhaled or intranasal route.

3. 发明申请

WO2010133534A1 BICYCLIC AMINO SUBSTITUTED COMPOUNDS AS PI3K INHIBITORS 审中-公开
标题翻译： BICYCLIC AMINO替代化合物作为PI3K抑制剂
公开(公告)号：WO2010133534A1
公开(公告)日：2010-11-25
申请号：PCT/EP2010/056706
申请日：2010-05-17
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , MIDDLEMISS, David , OLIVER, Kathryn , ELLARD, Katie , RATCLIFFE, Andrew
发明人： RAMSDEN, Nigel , MIDDLEMISS, David , OLIVER, Kathryn , ELLARD, Katie , RATCLIFFE, Andrew
IPC分类号： C07D417/04 , A61K31/44 , A61P35/00
CPC分类号： C07D417/04
摘要： The invention relates to compounds of formula (I) wherein X 1 to X 7 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PBK, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X 1至X 7具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是PBK抑制剂，用于治疗或预防免疫学，炎症性，自身免疫性或过敏性疾病。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及制备和用作药物。

4. 发明申请

WO2010007100A1 7-SUBSTITUTED AMINO TRIAZOLES AS PI3K INHIBITORS 审中-公开
标题翻译： 7-取代的氨基三唑作为PI3K抑制剂
公开(公告)号：WO2010007100A1
公开(公告)日：2010-01-21
申请号：PCT/EP2009/059076
申请日：2009-07-15
申请人： CELLZOME LTD , RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
发明人： RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein T 1 and R 1 to R 3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中T1和R1至R3具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及制备和用作药物。

5. 发明申请

WO2006136859A2 INDOLIZINE DERIVATIVES 审中-公开
标题翻译：吲哚衍生物
公开(公告)号：WO2006136859A2
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002341
申请日：2006-06-26
申请人： ARGENTA DISCOVERY LTD. , 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： C07D471/04
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 R 1 , R 2 , R 3 and R 4 each independently are hydrogen, C 1 C 6 alkyl, fully or partially fluorinated C 1 C 6 alkyl, halo, -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 or -OR 11 ; wherein each R 9 is independently C 1 C 6 alkyl, aryl, heteroaryl; R 10 is independently hydrogen, C 1 C 6 alkyl, aryl, or heteroaryl; R 11 is hydrogen, C 1 C 6 alkyl, fully or partially fluorinated C 1 C 6 alkyl or a group -SO 2 R 9 ; n is 0, 1 or 2; R5 is C 1 C 6 alkyl, fully or partially fluorinated C 1 C 6 alkyl , C 1 C 6 alkenyl , C 1 C 6 alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R 6 is hydrogen, C 1 C 6 alkyl or fully or partially fluorinated C 1 C 6 alkyl ; R 7 and R 8 are independently hydrogen or C 1 C 6 alkyl, or R 7 and R 8 together with the atom to which they are attached form a cycloalkyl group; and X is -CHR 6 -, -S(O) n -, -NR 6 SO 2 - or -SO 2 NR 6 - 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：式（I）其中R 1，R 2，R SUB > 3和R 4各自独立地是氢，C 1 -C 6烷基，完全或部分氟化的C 1 C 6烷基，卤素，-S（O）n R 10，-SO 2 N， N（R 10）2，-N（R 10）2 - ， - C（O）N（R 10） R 10，-NR 10 C（O）R 9，-CO 2， R 10，-C（O）R 9，-NO 2，-CN或-OR 11， SUB>; 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C 1 -C 6 烷基或基团-SO 2 R 9; 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烷基，C 1 -C 6烷基， 1个C 6链烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R 6是氢，C 1 -C 6烷基或完全或部分氟化的C 1 -C 6 烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或R 7， / SUB和R 8与它们所连接的原子一起形成环烷基; 并且X是-CHR 6 - ， - S（O）n - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

6. 发明申请

WO2005040112A1 COMPOUNDS WITH PGD2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有PGD2拮抗剂活性的化合物
公开(公告)号：WO2005040112A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004337
申请日：2004-10-13
申请人： OXAGEN LIMITED , MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
发明人： MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
IPC分类号： C07D209/18
CPC分类号： C07D403/12 , C07D209/18
摘要： Compounds of general formula (I); wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen, halo, -C 1 -C 6 alkyl, -O(C 1 -C 6 alkyl), -C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), -CON(R 9 ) 2 , -SOR 9 , -S0 2 R 9 . -S0 2 N(R 9 ) 2 , -N(R 9 ) 2 , -NR 9 OR 9 , -C0 2 R 9 , COR 9 , -SR 9 , -OH, -N0 2 or -CN; each R 9 independently hydrogen or C 1 -C 6 alkyl; R 5 and R 6 are each independently hydrogen, or C 1 -C 6 alkyl or together with the carbon atom to which they are attached form a C 3 -C 7 cycloalkyl. group; R 7 is hydrogen or C 1 -C 6 alkyl; R 8 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or an aromatic moiety, any of which may optionally be substituted with one or more substituents selected from halo, -SOR 13 -S0 2 R 13 , -R 14 , -OR 14 , -CON(R 14 )2 -SOR 14 , -S0 2 R 14 , -S0 2 N(R 14 ) -SO 2 N(R 14 ) 2 , -N(R 14 )2, NR 14 COR 14 , -CO 2 R 14 , COR 14 , -SR 14 , -N0 2 or -CN; wherein R 13 is a 5 to 7 membered heterocyclic ring; and each R 14 is independently hydrogen, alkyl or aryl, the aryl being optionally substituted by -R 9 , -OR 9 , -CON(R 9 ) 2 , -SOR 9 -S0 2 R 9 , -S0 2 N(R 9 ) 2 , -N(R 9 ) 2 , NR9COR 9 , -C0 2 R 9 , -COR 9 , -SR 9 , halo, -N0 2 or -CN; wherein R 9 is as defined above; provided that when R 1 , R 3 and R 4 are hydrogen and R 2 is hydrogen, halogen or -O(C 1 -C 6 )alkyl, R 8 is not unsubstituted phenyl or phenyl substituted by halo, C 1 -C 6 alkyl, -O(C 1 -C 6 )alkyl, -S(C 1 -C 6 )alkyl or -CO(C 1 -C 6 )alkyl; or pharmaceutically acceptable salts, hydrates, solvates, compexes or prodrugs therof are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物; 其中R 1，R 2，R 3和R 4独立地是氢，卤素，-C 1 -C 6烷基，-O（C 1 -C 6烷基），-C 1 -C 6烷基（C 3 -C 7 环烷基），-CON（R 9）2，-SOR 9，-SO 2 R 9。 -SO 2 N（R 9）2，-N（R 9）2，-NR 9 OR 9，-CO 2 R 9，COR 9，-SR 9，-OH， -NO 2或-CN; 每个R 9独立地是氢或C 1 -C 6烷基; R 5和R 6各自独立地为氢或C 1 -C 6烷基，或与它们所连接的碳原子一起形成C 3 -C 7环烷基。组; R 7是氢或C 1 -C 6烷基; R 8是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或芳族部分，其中任何一个可任选地被一个或多个选自卤素，-SOR 13 -SO 2 R 13，，-R 14，-OR 14，-CON（R 14）2 -SOR 14，-SO 2 R 14，-SO 2 N（R 14）-SO 2 N（R 14）2，-N（R COR 14，-C 14 R 14，COR 14，-SR 14，-NO 2或-CN; 其中R 13为5至7元杂环; 并且每个R 14独立地为氢，烷基或芳基，芳基任选被-R 9，-OR 9，-CON（R 9）2，-SOR 9 - （R 9）2，-N（R 9）2，NR 9 COR 9，-CO 2 R 9，-COR 9，-SR 9，卤素，-NO 2 或-CN; 其中R 9如上所定义; 条件是当R 1，R 3和R 4为氢且R 2为氢，卤素或-O（C 1 -C 6）烷基时，R 8为未取代的苯基或被卤素，C 1 -C 6烷基，-O（C 1 -C 6）烷基，-S（C 1 -C 6）烷基或-CO（C 1 -C 6）烷基; 或其药学上可接受的盐，水合物，溶剂合物，混合物或前药可用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

7. 发明申请

WO2010092041A1 [1, 2, 4] TRIAZOLO [1, 5 -A] PYRIDINES AS KINASE INHIBITORS 审中-公开
标题翻译： [1，2，4] TRIAZOLO [1,5-A]吡啶作为激酶抑制剂
公开(公告)号：WO2010092041A1
公开(公告)日：2010-08-19
申请号：PCT/EP2010/051556
申请日：2010-02-09
申请人： FOVEA PHARMACEUTICALS SA , LERICHE, Caroline , AUCLAIR, Eric , LE ROUX, Jacques , MIDDLEMISS, David
发明人： LERICHE, Caroline , AUCLAIR, Eric , LE ROUX, Jacques , MIDDLEMISS, David
IPC分类号： C07D471/04 , A61K31/437 , A61P27/02
CPC分类号： C07D471/04
摘要： The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted triazolopyridine compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder. In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.
摘要翻译：本发明涉及某些新化合物，其制备方法和用于治疗或改善激酶介导的病症的方法。更具体地，本发明涉及可用作选择性激酶抑制剂的取代的三唑并吡啶化合物，用于制备这些化合物的方法和用于治疗或改善激酶介导的病症的方法。特别地，所述方法涉及治疗或改善包括心血管疾病，糖尿病，糖尿病相关疾病，炎性疾病，免疫学疾病，癌症和眼睛疾病如视网膜病变或黄斑变性或其他玻璃体视网膜疾病的激酶介导的疾病，以及类似。

8. 发明申请

WO2010092015A1 UREA TRIAZOLOLO [1, 5-A] PYRIDINE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：尿素三唑醇[1,5-A]吡啶衍生物作为PI3K抑制剂
公开(公告)号：WO2010092015A1
公开(公告)日：2010-08-19
申请号：PCT/EP2010/051462
申请日：2010-02-08
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
发明人： RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P9/00 , A61P35/00 , A61P31/00 , A61P25/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein X 1 ,R and R 1 to R 4 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X 1，R 2和R 1至R 4具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及制备和用作药物。

9. 发明申请

WO2010057877A1 7-PYRIDINYL- OR PHENYL- SUBSTITUTED TRIAZOLO [1, 5 -A] PYRIDINES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的7-吡啶基或苯基取代的三唑并[1,5-A]吡啶
公开(公告)号：WO2010057877A1
公开(公告)日：2010-05-27
申请号：PCT/EP2009/065292
申请日：2009-11-17
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
发明人： RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
IPC分类号： C07D471/04 , A61P37/08 , A61P35/00 , A61P3/00 , A61P29/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I), wherein X, X 1 , R and R 1 to R 4 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X，X1，R和R1至R4具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及制备和用作药物。

10. 发明申请

WO2009098458A2 BIARYL AMIDES 审中-公开
公开(公告)号：WO2009098458A2
公开(公告)日：2009-08-13
申请号：PCT/GB2009/000317
申请日：2009-02-05
申请人： ASTERAND UK LIMITED , COLEMAN, Robert , MIDDLEMISS, David
发明人： COLEMAN, Robert , MIDDLEMISS, David
IPC分类号： C07C233/87 , C07C233/75 , C07D207/16 , A61K31/167
CPC分类号： C07D207/16 , C07C233/75 , C07C233/87 , C07C235/20
摘要： A compound of formula (1): or formula (2) for treating ocular hypertension.
摘要翻译：式（1）化合物或式（2）用于治疗高眼压症。

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