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1. 发明申请

WO2008155556A1 A METHOD FOR ASSAYING FTO (2-OXOGLUTARATE DEPENDENT OXYGENASE) ACTIVITY 审中-公开
标题翻译：一种测定FTO（2-OXOGLUTARATE相关氧化）活性的方法
公开(公告)号：WO2008155556A1
公开(公告)日：2008-12-24
申请号：PCT/GB2008/002119
申请日：2008-06-20
申请人： ISIS INNOVATION LIMITED , ASHCROFT, Frances, Mary , PONTING, Christopher, Paul , GERKEN, Thomas , SCHOFIELD, Christopher, Joseph
发明人： ASHCROFT, Frances, Mary , PONTING, Christopher, Paul , GERKEN, Thomas , SCHOFIELD, Christopher, Joseph
IPC分类号： G01N33/50
CPC分类号： C12Q1/26 , G01N2333/90245
摘要： The present invention provides a method for assaying oxygenase activity, the method comprising monitoring oxygenase activity of FTO.
摘要翻译：本发明提供了检测加氧酶活性的方法，该方法包括监测FTO的加氧酶活性。

2. 发明申请

WO2003080566A2 HIF HYDROXYLASE INHIBITORS 审中-公开
标题翻译： HIF羟基酶抑制剂
公开(公告)号：WO2003080566A2
公开(公告)日：2003-10-02
申请号：PCT/GB2003/001239
申请日：2003-03-21
申请人： ISIS INNOVATION LIMITED , SCHOFIELD, Christopher, Joseph , MAXWELL, Patrick, Henry , PUGH, Christopher, William , RATCLIFFE, Peter, John
发明人： SCHOFIELD, Christopher, Joseph , MAXWELL, Patrick, Henry , PUGH, Christopher, William , RATCLIFFE, Peter, John
IPC分类号： C07C259/06
CPC分类号： C07D207/46 , C07F5/025
摘要： The invention provides a compound of one of the formulae (A), (B), (C), (D), (E), (F) as herein defined, or a salt thereof, for use in the treatment of a condition associated with increased or decreased HIF levels or activity, or a condition in which an increase or decrease in HIF levels or activity may be beneficial.
摘要翻译：本发明提供本文定义的式（A），（B），（C），（D），（E），（F）或其盐之一的化合物，与HIF水平或活动增加或降低相关联，或HIF水平或活动增加或减少可能有益的情况。

3. 发明申请

WO2005019468A1 MODIFIED DACS/DAOC ENZYMES 审中-公开
标题翻译：改良DACS / DAOC酶
公开(公告)号：WO2005019468A1
公开(公告)日：2005-03-03
申请号：PCT/GB2004/003563
申请日：2004-08-19
申请人： ISIS INNOVATION LIMITED , LLOYD, Matthew, David , SCHOFIELD, Christopher, Joseph , HEWITSON, Kirsty, Sarah , LIPSCOMB, Sarah
发明人： LLOYD, Matthew, David , SCHOFIELD, Christopher, Joseph , HEWITSON, Kirsty, Sarah , LIPSCOMB, Sarah
IPC分类号： C12P35/00
CPC分类号： C12N9/0071 , C12P35/00
摘要： Deacetoxy/deacetylcephalosporin C synthase (DAOC/DACS) modified to reduce the hydroxylation activity and in particular DAOC/DACS modified to reduce the hydroxylation activity and further modified to improve the ring expanding activity.
摘要翻译：脱乙酰氧基/脱乙酰头孢菌素C合成酶（DAOC / DACS）被修饰以降低羟基化活性，特别是改性的DAOC / DACS以降低羟基化活性并进一步改进以改善环扩展活性。

4. 发明申请

WO2003080566A3 HIF HYDROXYLASE INHIBITORS 审中-公开
公开(公告)号：WO2003080566A3
公开(公告)日：2003-10-02
申请号：PCT/GB2003/001239
申请日：2003-03-21
申请人： ISIS INNOVATION LIMITED , SCHOFIELD, Christopher, Joseph , MAXWELL, Patrick, Henry , PUGH, Christopher, William , RATCLIFFE, Peter, John
发明人： SCHOFIELD, Christopher, Joseph , MAXWELL, Patrick, Henry , PUGH, Christopher, William , RATCLIFFE, Peter, John
IPC分类号： C07C259/06
摘要： The invention provides a compound of one of the formulae (A), (B), (C), (D), (E), (F) as herein defined, or a salt thereof, for use in the treatment of a condition associated with increased or decreased HIF levels or activity, or a condition in which an increase or decrease in HIF levels or activity may be beneficial.

5. 发明申请

WO2010043866A2 HISTONE LYSINE DEMETHYLASE INHIBITORS 审中-公开
标题翻译： HISTONE赖氨酸二甲基酶抑制剂
公开(公告)号：WO2010043866A2
公开(公告)日：2010-04-22
申请号：PCT/GB2009/002465
申请日：2009-10-15
申请人： ISIS INNOVATION LIMITED , SCHOFIELD, Christopher, Joseph , MCDONOUGH, Michael , ROSE, Nathan , THALHAMMER, Armin
发明人： SCHOFIELD, Christopher, Joseph , MCDONOUGH, Michael , ROSE, Nathan , THALHAMMER, Armin
IPC分类号： C07C235/72 , C07D213/79 , C07D307/68 , A61K31/235 , A61K31/341 , A61K31/44 , A61P25/24 , A61P35/00
CPC分类号： C07D213/79 , C07C233/56 , C07C255/57 , C07C259/10 , C07C2601/14 , C07D307/68
摘要： The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z 1; Z 2 ; Y 1 ; Y 2 ; A; p; X 1 ; X 2 ; m; R 4 ; B; R 5 ; R 6 ; R 7 ; R 8 ; R 9 ; X 3 ; R 10 ; R 11 and R 12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression.
摘要翻译：本发明提供了式（I）的N-草酰甘氨酸衍生物：式（II）的异羟肟酸衍生物或式（III）的杂芳基衍生物的化合物：其中n; Z ^{1 Z ^{2 ; ÿ^{1 ; ÿ^{2 ; 一个; 磷; X ^{1 ; X ^{2 ; 米; [R ^{4 ; B; [R ^{5 ; [R ^{6 ; [R ^{7 ; [R ^{8 ; [R ^{9 ; X ^{3 ; [R ^{10 ; R 11和R 12如本文所定义，或其药学上可接受的盐。这些化合物是组蛋白去甲基化酶的人2-氧戊二酸依赖性JMJD2亚家族的抑制剂，特别是JMJD2E。这些抑制剂可用于改变细胞的表观遗传状态，导致染色质重塑的抑制/激活，多基因激活/失活，并用于治疗以不希望的细胞增殖为特征的癌症和其他病症以及包括抑郁症在内的精神病症。}}}}}}}}}}}}}}

6. 发明申请

WO2006010920A1 SOLUBLE POLYPEPTIDE 审中-公开
标题翻译：可溶多糖
公开(公告)号：WO2006010920A1
公开(公告)日：2006-02-02
申请号：PCT/GB2005/002929
申请日：2005-07-26
申请人： ISIS INNOVATION LIMITED , SCHOFIELD, Christopher, Joseph , HEWITSON, Kirsty, Sarah , MCNEILL, Luke, Alexander
发明人： SCHOFIELD, Christopher, Joseph , HEWITSON, Kirsty, Sarah , MCNEILL, Luke, Alexander
IPC分类号： C12N9/02
CPC分类号： C12N9/0071 , C12Q1/26
摘要： A polypeptide comprising an N-terminal truncated form of 2-OG dependent oxygenase, which retains hydroxylase activity.
摘要翻译：包含保留羟化酶活性的N-末端截短形式的2-OG依赖性加氧酶的多肽。

7. 发明申请

WO2004058252A2 ANTI-CANCER AGENTS 审中-公开
标题翻译：抗癌药剂
公开(公告)号：WO2004058252A2
公开(公告)日：2004-07-15
申请号：PCT/GB2003/005689
申请日：2003-12-30
申请人： ISIS INNOVATION LIMITED , WELFORD, Richard, William, David , HEWITSON, Kirsty, Sarah , MCNEILL, Luke, Alexander , SCHOFIELD, Christopher, Joseph , SCHLEMMINGER, Imre
发明人： WELFORD, Richard, William, David , HEWITSON, Kirsty, Sarah , MCNEILL, Luke, Alexander , SCHOFIELD, Christopher, Joseph , SCHLEMMINGER, Imre
IPC分类号： A61K31/4188
CPC分类号： A61K31/352 , A61K31/195 , A61K31/4164 , A61K31/4188 , A61K2300/00
摘要： A pharmaceutical combination which comprises: (a) a compound of one of the formulae: formula (I) wherein each of R I and R II , which max be the same or different, represents hydrogen, fluorine or alkyl of 1 to 6 carbon atoms, X represents CR I R II , NR III or O wherein R III is hydrogen or alkyl of 1 to 6 carbon atoms, each of Y and Z, which may be the same or different, represents hydrogen, NR III , OH or SH, or Y and Z together represents =O or =S, or formula (II) where R 1 to R 11 may independently be H, a branched or straight C 1 to C 6 alkyl chain, OH, O-alkyl having a branched or straight C 1 to C 6 alkyl chain optionally containing 1 or 2 N, O or S atoms, COOH, a branched or straight C 1 to C 6 alkyl ester (alkoxycarbonyl), a 4 to 7 membered heterocyclic ring optionally containing 1 or 2 N, S, O or P atoms or a 5 or 6 membered aromatic ring, optionally containing 1 or more N, O or S atoms, which can be fused to another ring, or a said alkyl chain substituted by a said aromatic ring, and formula (A) represents formula (B) or formula (C) or a pharmaceutically acceptable salt of a said compound; and (b) an anti-cancer alkylating agent. This combination is useful in the treatment of cancer.
摘要翻译：一种药物组合，其包含：（a）式（I）之一的化合物，其中R和R II各自相同或不同，表示氢，氟或1至6个碳的烷基 X表示CR R II，NR III或O，其中R III是氢或1至6个碳原子的烷基，Y和Z各自可以相同或不同，表示氢，NR 或者Y和Z一起代表= O或= S，或式（II）其中R 1至R 11可以独立地为H，支链或直链C1至C6烷基链，具有任选含有1或2个N，O或S原子的支链或直链C 1至C 6烷基链的OH，O-烷基，COOH，支链或直链C1至C6烷基酯（烷氧基羰基），可选地为4至7元杂环含有1或2个N，S，O或P原子或5或6元芳族环，任选地含有1个或更多个N，O或S原子，其可以与另一个环稠合，或所述烷基链被所述芳香环，和式（A）代表式（B）或式（C）或所述化合物的药学上可接受的盐; 和（b）抗癌烷化剂。这种组合可用于治疗癌症。

8. 发明申请

WO2003100438A1 ASSAYS FOR MODULATORS OF ASPARAGINYL HYDROXYLASE 审中-公开
标题翻译：阿糖胞苷羟化酶调节剂的测定
公开(公告)号：WO2003100438A1
公开(公告)日：2003-12-04
申请号：PCT/GB2003/002257
申请日：2003-05-23
申请人： ISIS INNOVATION LIMITED , PUGH, Christopher, William , GLEADLE, Jonathan, Mark , RATCLIFFE, Peter, John , SCHOFIELD, Christopher, Joseph , McNEILL, Luke, Alexander
发明人： PUGH, Christopher, William , GLEADLE, Jonathan, Mark , RATCLIFFE, Peter, John , SCHOFIELD, Christopher, Joseph , McNEILL, Luke, Alexander
IPC分类号： G01N33/68
CPC分类号： C12N9/0071 , C12Q1/26 , G01N33/6893 , G01N2333/4703 , G01N2500/04
摘要： A method of identifying an agent which modulates hydroxylation of hypoxia inducible factor (HIF), comprises contacting a HIF asparagine hydroxylase and a test substance in the presence of a substrate of the hydroxylase under conditions in which asparagine in the substrate is hydroxylated in the absence of the test substance; and determining hydroxylation of the substrate. Preferably the substrate is a HIF polypeptide comprising HIF-lα, a fragment thereof comprising Asn 803 of HIF-lα or a peptide analogue of HIF-lα or fragment thereof comprising an asparagine equivalent to Asn 803 of HIF-lα and wherein hydroxylation of Asn 803 or of a said equivalent asparagine is determined.
摘要翻译：一种鉴定调节缺氧诱导因子（HIF）的羟基化的试剂的方法包括在不存在羟基化酶的基质中的天冬酰胺被羟基化的条件下，在羟化酶底物的存在下使HIF天冬酰胺羟化酶和测试物质接触测试物质; 并测定底物的羟基化。优选地，底物是包含HIF-1α的HIF多肽，其包含HIF-1α的Asn 803的片段或HIF-1α的肽类似物或其片段，其包含与HIF-1α的Asn 803相当的天冬酰胺，并且其中Asn 803的羟基化或所述等同的天冬酰胺。

9. 发明申请

WO2003052113A1 CYCLISATION PROCESS FOR THE PREPARATION OF C-2 BETA-LACTAM COMPOUNDS 审中-公开
标题翻译：用于制备C-2 BETA-LACTAM化合物的循环方法
公开(公告)号：WO2003052113A1
公开(公告)日：2003-06-26
申请号：PCT/GB2002/005804
申请日：2002-12-19
申请人： ISIS INNOVATION LIMITED , SCHOFIELD, Christopher, Joseph , HEWITSON, Kirsty, Sarah , SLEEMAN, Mark, Christopher
发明人： SCHOFIELD, Christopher, Joseph , HEWITSON, Kirsty, Sarah , SLEEMAN, Mark, Christopher
IPC分类号： C12P17/10
CPC分类号： C12P17/10 , C07D205/08 , C07D477/04 , C07D503/00
摘要： A process for the preparation of a substituted C-2 β-lactam comprises incubating a 2-substituted 3-aminocarboxylic acid with a β-lactam synthetase under conditions such that the 2-substituted 3-aminocarboxylic acid is cyclised to produce a substituted C-2 β-lactam. The process can be used to produce an antibiotic or β-lactamase inhibitor.
摘要翻译：制备取代的C-2和β-内酰胺的方法包括在2-取代的3-氨基羧酸环化以产生取代的3-氨基羧酸的条件下，将2-取代的3-氨基羧酸与β-内酰胺合成酶进行温育 C-2＆bgr; - 内酰胺该方法可用于生产抗生素或β-内酰胺酶抑制剂。

10. 发明申请

WO2009141609A1 ASSAY FOR MONITORING ACTIVITY OF JMJD6 审中-公开
标题翻译：测定JMJD6的活动
公开(公告)号：WO2009141609A1
公开(公告)日：2009-11-26
申请号：PCT/GB2009/001270
申请日：2009-05-21
申请人： ISIS INNOVATION LIMITED , LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN , SCHOFIELD, Christopher, Joseph , WEBBY, Celia, Jane , BOETTGER, Angelika , WOLF, Alexander
发明人： SCHOFIELD, Christopher, Joseph , WEBBY, Celia, Jane , BOETTGER, Angelika , WOLF, Alexander
IPC分类号： C12Q1/26
CPC分类号： C12Q1/26
摘要： The invention provides a method for assaying Jmjd6 activity.
摘要翻译：本发明提供了测定Jmjd6活性的方法。

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