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1. 发明申请

WO2010067131A1 P38 MAP KINASE INHIBITORS 审中-公开
标题翻译： P38 MAP激酶抑制剂
公开(公告)号：WO2010067131A1
公开(公告)日：2010-06-17
申请号：PCT/GB2009/051703
申请日：2009-12-11
申请人： RESPIVERT LIMITED , ITO, Kazuhiro , STRONG, Peter , RAPEPORT, William, Garth , MURRAY, Peter, John , KING-UNDERWOOD, John , WILLIAMS, Jonathan, Gareth , ONIONS, Stuart, Thomas , HIRST, Simon Christopher , TADDEI, David, Michel, Adrien , CHARRON, Catherine, Elisabeth
发明人： ITO, Kazuhiro , STRONG, Peter , RAPEPORT, William, Garth , MURRAY, Peter, John , KING-UNDERWOOD, John , WILLIAMS, Jonathan, Gareth , ONIONS, Stuart, Thomas , HIRST, Simon Christopher , TADDEI, David, Michel, Adrien , CHARRON, Catherine, Elisabeth
IPC分类号： C07D401/12 , C07D401/14 , A61K31/415 , A61P11/00 , A61P29/00
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，包括其所有的立体异构体，互变异构体和同位素衍生物，它们是p38丝裂原活化蛋白激酶的抑制剂（本文称为p38 MAP激酶抑制剂），特别是其α和γ激酶亚型，以及它们在治疗中的用途，包括药物组合，特别是治疗炎症性疾病，包括肺炎性疾病如COPD。

2. 发明申请

WO2008053185A1 INHIBITORS OF IKK-β SERINE-THREONINE PROTEIN KINASE 审中-公开
标题翻译： IKK-ß丝氨酸蛋白激酶激酶的抑制剂
公开(公告)号：WO2008053185A1
公开(公告)日：2008-05-08
申请号：PCT/GB2007/004117
申请日：2007-10-29
申请人： CHROMA THERAPEUTICS LTD. , MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
发明人： MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
IPC分类号： C07D333/38 , A61K31/381
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases wherein R 7 is hydrogen or optionally substituted (C 1 C 6 )alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L 1 -Y 1 -(CH 2 ) z -, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R 6 is hydrogen, or optionally substituted C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, aryl or heteroaryl or -(C=O)R 3 , -(C=O)OR 3 , Or -(C=O)NR 3 wherein R 3 is hydrogen.or optionally substituted (C 1 -C 6 )alkyl; Y 1 is a bond, -(C=O)-, -S(O 2 )-, -C(=O)O-, -OC(=O)-, -(C=O)NR 3 -, -NR 3 (C=O)-, -S(O 2 )NR 3 -, -NR 3 S(O 2 )-, or -NR 3 (C=O)NR 4 -, wherein R 3 and R 4 are independently hydrogen or optionally substituted (CrC6)alkyl, L 1 is a divalent linker radical of formula -(Alk 1 ) m (Q) n (Alk 2 ) p - wherein m, n, p, Q, Alk 1 and AIk 2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗其中R 7为氢或任选取代的自身免疫性和炎性疾病（C _{1 C _{6 ）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式RL的基团，其中：z（Z 2）z 是0或1; R是式（X）或（Y）的基团，R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R 6是氢或任选取代的C 1 -C 6烷基，C 3 -C 3 - 芳基或杂芳基或 - （C = O）R 3， - （C = O）OR 3或 - （C = O）其中R 3为氢或任选取代的（C 1 -C 6 -C 6）烷基; - （C = O） - ， - S（O）2 - ， - C（= O）O-，-OC（= O ） - ， - （C = O）NR 3 - ， - NR 3（C = O） - ， - S（O NR 3 - ， - NR 3 S（O 2 - ） - 或-NR 3（C = O ）NR 4 - ，其中R 3和R 4独立地是氢或任选取代的（C 1 -C 6）烷基，L 1， SUP>是二价连接基团，式 - （Alk 1）2（Q）n（Alk 2））其中m，n，p，Q，Alk 1和Alk 2如权利要求中所定义。}}

3. 发明申请

WO1998009969A1 NOVEL ARYL-PYRIDAZINES 审中-公开
标题翻译：新亚美尼亚
公开(公告)号：WO1998009969A1
公开(公告)日：1998-03-12
申请号：PCT/SE1997001359
申请日：1997-08-19
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , HIRST, Simon , PERRY, Matthew , PHILLIPS, Eifion
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D491/052
CPC分类号： C07D495/04 , C07D231/54 , C07D237/26 , C07D237/36 , C07D471/04 , C07D491/04 , C07D491/14 , C07D495/14
摘要： Use of a compound of formula (I) wherein, A, A , A and A are all CH or CR or one of A, A , A or A is nitrogen and the others are all CH or CR ; Ar and Ar are independently phenyl, pyridyl, benzothiazolyl, quinolyl or quinoxalinyl all of which are optionally substituted by one or more substituents, X, Y, Z, R , R , R , R are as described in the specification or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of an allergic or an inflammatory condition.
摘要翻译：其中A，A 1，A 2和A 3的式（I）化合物均为CH或CR 4或A，A 1，A 2或 A 3为氮，其余为CH或CR 4; Ar 1和Ar 2独立地是苯基，吡啶基，苯并噻唑基，喹啉基或喹喔啉基，它们全部被一个或多个取代基X，Y，Z，R 1，R 2， 3>，R 4如说明书或其药学上可接受的衍生物所述，用于制备用于治疗过敏或炎性疾病的药物。

4. 发明申请

WO2010038086A8 P38 MAP KINASE INHIBITORS 审中-公开
标题翻译： P38 MAP激酶抑制剂
公开(公告)号：WO2010038086A8
公开(公告)日：2011-04-28
申请号：PCT/GB2009051304
申请日：2009-10-02
申请人： RESPIVERT LTD , ITO KAZUHIRO , STRONG PETER , RAPEPORT WILLIAM GARTH , MURRAY PETER JOHN , KING-UNDERWOOD JOHN , WILLIAMS JONATHAN GARETH , ONIONS STUART THOMAS , HIRST SIMON CHRISTOPHER , TADDEI DAVID MICHEL ADRIEN , CHARRON CATHERINE ELISABETH
发明人： ITO KAZUHIRO , STRONG PETER , RAPEPORT WILLIAM GARTH , MURRAY PETER JOHN , KING-UNDERWOOD JOHN , WILLIAMS JONATHAN GARETH , ONIONS STUART THOMAS , HIRST SIMON CHRISTOPHER , TADDEI DAVID MICHEL ADRIEN , CHARRON CATHERINE ELISABETH
IPC分类号： C07D401/12 , A61K31/415 , A61P11/00 , A61P29/00 , C07D403/12
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12
摘要： There are provided inter aliacompoundsof formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
摘要翻译：提供了式（I）的中间体化合物，其中R 1，Ar，L，X，R 3和Q如在说明书中用于治疗，特别是治疗炎性疾病中所定义。

5. 发明申请

WO1997045428A1 NOVEL PYRIDAZINE COMPOUNDS 审中-公开
标题翻译：新颖的吡咯烷酮化合物
公开(公告)号：WO1997045428A1
公开(公告)日：1997-12-04
申请号：PCT/SE1997000818
申请日：1997-05-20
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , HIRST, Simon , PERRY, Matthew
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to fused pyridazine compounds, in particular pyrido[h]cinnoline, pyrido[h]cinnolinone, pyridocyclopenta[1,2-c]pyridazine, pyridocyclopenta[1,2-c]pyridazinone, pyridocyclohepta[1,2-c]pyridazine and pyridocyclohepta[1,2-c]pyridazinone derivatives, their use as medicaments and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及稠合的哒嗪化合物，特别是吡啶并[h]噌啉，吡啶并[h]噌啉酮，吡啶并环戊[1,2-c]哒嗪，吡啶并环戊[1,2-c]哒嗪酮，吡啶并杂庚环[1,2-c] 哒嗪和吡啶并环庚三烯并[1,2-c]哒嗪酮衍生物，它们用作药物和包含它们的药物组合物。

6. 发明申请

WO1997034893A1 PHARMACEUTICALLY USEFUL COMPOUNDS 审中-公开
标题翻译：药物有用的化合物
公开(公告)号：WO1997034893A1
公开(公告)日：1997-09-25
申请号：PCT/SE1997000471
申请日：1997-03-20
申请人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG , BANTICK, John , BONNERT, Roger , CAGE, Peter , DONALD, David , FURBER, Mark , HIRST, Simon , PERRY, Matthew , PHILLIPS, Eifion
发明人： ASTRA PHARMACEUTICALS LTD. , ASTRA AKTIEBOLAG
IPC分类号： C07D471/04
CPC分类号： C07D231/56 , C07D401/04 , C07D471/04 , C07D487/04
摘要： The invention relates to 2-arylpyrazolisoquinoline and cinnolinone derivatives, methods for their preparation, their use as medicaments, and pharmaceutical formulations including them.
摘要翻译：本发明涉及2-芳基吡唑并喹啉和噌啉酮衍生物，其制备方法，它们作为药物的用途，以及包括它们的药物制剂。

7. 发明申请

WO2008053182A1 IKK-β SERINE-THREONINE PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： IKK-ß丝氨酸蛋白激酶激酶抑制剂
公开(公告)号：WO2008053182A1
公开(公告)日：2008-05-08
申请号：PCT/GB2007/004114
申请日：2007-10-29
申请人： CHROMA THERAPEUTICS LTD. , MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
发明人： MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
IPC分类号： C07D333/38 , A61K31/381
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R 7 is hydrogen or optionally substituted (C 1 -C 6 )alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R 1 R 2 CHNH-Y-L 1 -X 1 -(CH 2 ) Z - wherein: z is 0 or 1; R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non- natural alpha amino acid; Y is a bond, -C(=O)-, -S(=O)2-, -C(=O)O-, -C(=O)NR3-, - C(=S)-NR 3 , -C(=NH)-NR 3 or -S(=O) 2 NR 3 - wherein R 3 is hydrogen or optionally substituted C 1 -C 6 alkyl; L 1 is a divalent linker radical of formula -(Alk 1 ) m (Q) n (Alk 2 ) p - wherein m, n, p, Q, AIk 1 and AIk 2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：式（A）和（B）其中R 7 是氢或任选取代的（C 1 -C 6 -C 6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是（a）式R 1的基团R 2 R 2 CHNH-YL 1 - （O） - 1 - （ Z 2 - 其中：z为0或1; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链; Y是-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR 3 - ， - C（= S） > 3，-C（= NH）-NR 3或-S（= O）2 NR 3 - 其中R 3是氢或任选取代的C 1 -C 6烷基; L 1是式（II）的二价连接基团（Q）n（Alk）其中m，n，p，Q，Alk 1和Alk 2定义如下：其中m，n，p，Q，索赔。

8. 发明申请

WO2008053157A1 AMINOHETEROARYL COMPOUNDS AS FOR THE TREATMENT OF DISEASES MEDIATED BY C-MET KINASE ACTIVITY 审中-公开
标题翻译：用于治疗由C-MET激酶活性介导的疾病的氨基酸化合物
公开(公告)号：WO2008053157A1
公开(公告)日：2008-05-08
申请号：PCT/GB2007/004013
申请日：2007-10-19
申请人： CHROMA THERAPEUTICS LTD. , DRUMMOND, Alan, Hastings , KING-UNDERWOOD, John , ONIONS, Stuart, Thomas , WILLIAMS, Johathan, Gareth , HIRST, Simon, Christopher
发明人： DRUMMOND, Alan, Hastings , KING-UNDERWOOD, John , ONIONS, Stuart, Thomas , WILLIAMS, Johathan, Gareth , HIRST, Simon, Christopher
IPC分类号： C07D401/04 , C07D401/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/14 , C07D401/04
摘要： Compounds of formula (I), are inhibitors of c-Met kinase activity, useful inter alia in the treatment of hyperproliferative diseases: wherein X is -N= or -CH=; ring A is optionally substituted mono- or bi-cyclic aryl or heteroaryl having from 5 to 12 ring atoms; ring B is (i) optionally substituted phenyl, (ii) optionally substituted monocyclic heterocyclic having 5 or 6 ring atoms and having one or two nitrogens as the sole ring heteroatoms, (iii) optionally substituted bicyclic ring system of 9 or 10 ring atoms having one two or three ring nitrogens and optionally a ring oxygen as the sole ring heteroatoms; R 2 is selected from hydrogen, halogen, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 3 -C 6 )cycloalkyl, and mono- or bi-cyclic heterocyclic having from 5 to 12 ring atoms, R 3 and R 4 are (a) independently selected from hydrogen, halogen, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 3 -C 6 )cycloalkyl, and mono- or bi-cyclic heterocyclic having from 5 to 12 ring atoms; or (b) R 3 and R 4 taken together with the carbon to which they are attached form a (C 3 -C 6 )cycloalkyl ring; or (c) one of R 3 and R 4 is as defined in case (a) while the other is a divalent radical selected from -(CH 2 ) 3 - or -(CH 2 ) 4 - in which one or two non-adjacent carbons are replaced by oxygen, sulfur or -NR 3 - wherein Ra is hydrogen or (C 1 -C 3 ) alkyl; R 5 is hydrogen and R 6 is a radical of formula (IA), or R 6 is hydrogen and R 5 is a radical of formula -(Z 1 ) w -(CH 2 ) Z -L 1 -Y 1 -CH(R 7 )-NHR 8 wherein R 7 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; and R 8 is hydrogen; or optionally substituted (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, aryl or heteroaryl Or -(C=O)R 9 , -(C=O)OR 9 , Or -(C=O)NR 9 wherein R 9 is hydrogen or optionally substituted (C 1 -C 6 )alkyl; and -(Z 1 ) w -(CH 2 ) Z -L 1 -Y 1 - is a linker radical as defined in the claims.
摘要翻译：式（I）化合物是c-Met激酶活性的抑制剂，尤其用于治疗过度增殖性疾病：其中X是-N =或-CH =; 环A是具有5至12个环原子的任选取代的单环或双环芳基或杂芳基; 环B是（i）任选取代的苯基，（ii）具有5或6个环原子并具有一个或两个氮原子作为唯一环杂原子的任选取代的单环杂环，（iii）具有9或10个环原子的任选取代的双环体系，其具有一个二或三环氮和任选的环氧作为唯一的环杂原子; R 2选自氢，卤素，（C 1 -C 6 -C 6）烷基，（C 2 -C 6 - C 6 -C 6烯基，（C 3 -C 6）环烷基和具有5至12个环原子的单环或双环杂环 R 3和R 4是（a）独立地选自氢，卤素，（C 1 -C 6 - （C 1 -C 6）烷基，（C 2 -C 6 -C 6）链烯基，（C 3 -C 6 -C 6）环烷基，和具有5至12个环原子的单环或双环杂环; 或（b）R 3和R 4与它们所连接的碳一起形成（C 3 -C 3）烷基， 6个）环烷基环; 或（c）R 3和R 4中的一个如情况（a）中所定义，而另一个是选自以下的二价基团： - （CH 2）其中一个或两个不相邻的碳被氧，硫取代，或者 - （CH 2）3 - 或-NR 3 - ，其中R a是氢或（C 1 -C 3 -C 3）烷基; R 5是氢，R 6是式（IA）的基团，或者R 6是氢，R 5是氢， SUB>是式的基团 - （Z 1）Z - （CH 2）2 Z - 其中R 7是（CH 3）NHR 8，其中R 7是氢，是羧酸基团（-COOH）或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; 并且R 8是氢; 或任选取代的（C 1 -C 6 -C 6）烷基，（C 3 -C 7 -C 7）环烷基，芳基或杂芳基或 - （C = O）R 9， - （C = O）或9或 - （C = O）NR 9 其中R 9是氢或任选取代的（C 1 -C 6 -C 6）烷基; 和 - （Z 1） - - - - （CH 2） - Z - L - 1 - 如权利要求中所定义的连接基团。

9. 发明申请

WO2010038086A3 P38 MAP KINASE INHIBITORS 审中-公开
公开(公告)号：WO2010038086A3
公开(公告)日：2010-04-08
申请号：PCT/GB2009/051304
申请日：2009-10-02
申请人： RESPIVERT LIMITED , ITO, Kazuhiro , STRONG, Peter , RAPEPORT, William, Garth , MURRAY, Peter, John , KING-UNDERWOOD, John , WILLIAMS, Jonathan, Gareth , ONIONS, Stuart ,Thomas , HIRST, Simon, Christopher , TADDEI, David, Michel, Adrien , CHARRON, Catherine, Elizabeth
发明人： ITO, Kazuhiro , STRONG, Peter , RAPEPORT, William, Garth , MURRAY, Peter, John , KING-UNDERWOOD, John , WILLIAMS, Jonathan, Gareth , ONIONS, Stuart ,Thomas , HIRST, Simon, Christopher , TADDEI, David, Michel, Adrien , CHARRON, Catherine, Elizabeth
IPC分类号： C07D401/12 , C07D403/12 , A61K31/415 , A61P11/00 , A61P29/00
摘要： There are provided inter aliacompoundsof formula (I) wherein R 1 , Ar, L, X, R 3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.

10. 发明申请

WO2010038086A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2010038086A2
公开(公告)日：2010-04-08
申请号：PCT/GB2009051304
申请日：2009-10-02
申请人： RESPIVERT LTD , ITO KAZUHIRO , STRONG PETER , RAPEPORT WILLIAM GARTH , MURRAY PETER JOHN , KING-UNDERWOOD JOHN , WILLIAMS JONATHAN GARETH , ONIONS STUART THOMAS , HIRST SIMON CHRISTOPHER , TADDEI DAVID MICHEL ADRIEN , CHARRON CATHERINE ELIZABETH
发明人： ITO KAZUHIRO , STRONG PETER , RAPEPORT WILLIAM GARTH , MURRAY PETER JOHN , KING-UNDERWOOD JOHN , WILLIAMS JONATHAN GARETH , ONIONS STUART THOMAS , HIRST SIMON CHRISTOPHER , TADDEI DAVID MICHEL ADRIEN , CHARRON CATHERINE ELIZABETH
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12
摘要： There are provided inter aliacompoundsof formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
摘要翻译：提供了式（I）化合物，其中R 1，Ar，L，X，R 3和Q如用于治疗，特别是治疗炎性疾病的说明书中所定义。

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