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1. 发明申请

WO2003046577A1 A SYSTEM AND METHOD FOR AUTOMATIC PROTEIN SEQUENCING BY MASS SPECTROMETRY 审中-公开
标题翻译：一种通过质谱分析自动蛋白质测序的系统和方法
公开(公告)号：WO2003046577A1
公开(公告)日：2003-06-05
申请号：PCT/EP2001/014041
申请日：2001-11-30
申请人： THE EUROPEAN MOLECULAR BIOLOGY LABORATORY , WILM, Matthias , NEUBAUER, Gitte, Jackie
发明人： WILM, Matthias , NEUBAUER, Gitte, Jackie
IPC分类号： G01N33/68
CPC分类号： G01N33/6848 , G01N2458/15 , H01J49/04
摘要： A method of deducing the sequence of a protein by analysing tandem mass spectrometry data. The protein is subjected to partial isotopic labelling by enzymatic digestion in a water mixture comprising a non-natural abundance of H 2 1s O. Differential scanning mass spectrometry is applied to the peptide fragments obtained from the digestion. Peaks in the spectra are analyzed to ascertain whether they arise from isotopically labeled fragments or not. A filtered spectrum is calculated that just comprises peaks from the y-ions. The sequence of the peptide is deduced by computing the difference in the mass between adjacent y-ion peaks.
摘要翻译：通过分析串联质谱数据推导蛋白质序列的方法。蛋白质通过在包含非天然丰度的H2 <1s> O的水混合物中通过酶消化进行部分同位素标记。差示扫描质谱法应用于从消化获得的肽片段。分析光谱中的峰，以确定它们是否来自同位素标记的片段。计算出仅包含来自y离子的峰的滤波光谱。通过计算相邻y离子峰之间的质量差异来推导肽的序列。

2. 发明申请

WO2002092626A2 CLEAVAGE AND POLYADENYLATION COMPLEX OF PRECURSOR MRNA 审中-公开
标题翻译：前列腺MRNA的清除和聚合复合物
公开(公告)号：WO2002092626A2
公开(公告)日：2002-11-21
申请号：PCT/EP2002/005359
申请日：2002-05-15
申请人： CELLZOME AG , NEUBAUER, Gitte
发明人： NEUBAUER, Gitte
IPC分类号： C07K14/34
CPC分类号： C12N15/62 , A61K38/00 , A61K39/00 , A61K48/00 , C07K14/39 , C07K14/47 , C07K2319/00 , C07K2319/02 , C07K2319/50
摘要： The present invention relates to novel components of the cleavage/polyadenylation machinery of precursor mRNA as well as to the complex containing the new components and its use. The complex is obtained by using one component thereof as a bait and isolating a highly organised complex consisting of at least 13 distinct proteins.
摘要翻译：本发明涉及前体mRNA的切割/多聚腺苷酸化机理的新组分以及含有新成分的复合物及其用途。通过使用其一种组分作为诱饵并分离由至少13种不同蛋白质组成的高度组织的复合物来获得复合物。

3. 发明申请

WO2010133318A1 METHODS FOR THE IDENTIFICATION OF PHOSPHATIDYLINOSITOL KINASE INTERACTING MOLECULES AND FOR THE PURIFICATION OF PHOSPHATIDYLINOSITOL KINASE PROTEINS 审中-公开
标题翻译：磷脂酰肌氨酸激酶相互作用分子鉴定方法和磷脂酰肌氨酸激酶蛋白的纯化方法
公开(公告)号：WO2010133318A1
公开(公告)日：2010-11-25
申请号：PCT/EP2010/002987
申请日：2010-05-14
申请人： CELLZOME AG , BELL, Kathryn , RAMSDEN, Nigel , BERGAMINI, Giovanna , NEUBAUER, Gitte
发明人： BELL, Kathryn , RAMSDEN, Nigel , BERGAMINI, Giovanna , NEUBAUER, Gitte
IPC分类号： C07D471/04 , C12N11/06 , C12Q1/48
CPC分类号： C07D471/04 , B01J20/3212 , B01J20/3255 , C12N9/1205 , C12N11/06 , C12Q1/485 , G01N2500/02
摘要： The present invention relates to immobilization compounds of formula (I), immobilization products and preparations thereof as well as methods and uses for the identification of phosphatidylinositol kinase interacting compounds or for the purification or identification of phosphatidylinositol kinase proteins.
摘要翻译：本发明涉及式（I）的固定化合物，其固定产物及其制备方法以及用于鉴定磷脂酰肌醇激酶相互作用化合物或用于纯化或鉴定磷脂酰肌醇激酶蛋白的方法和用途。

4. 发明申请

WO2004099774A3 PROCESSES FOR THE IDENTIFICATION OF MEDICAL TARGETS BY SCREENING AN ACTIVE AGENT FOR BINDING INTERACTIONS 审中-公开
标题翻译：通过筛选用于结合相互作用的活性剂来鉴定医疗目标的过程
公开(公告)号：WO2004099774A3
公开(公告)日：2006-01-12
申请号：PCT/EP2004004883
申请日：2004-05-07
申请人： CELLZOME AG , SUPERTI-FUGA GIULIO , KRUSE ULRICH , RYBIN VLADIMIR , NEUBAUER GITTE
发明人： SUPERTI-FUGA GIULIO , KRUSE ULRICH , RYBIN VLADIMIR , NEUBAUER GITTE
IPC分类号： G01N33/543 , G01N33/68 , G01N33/94 , G01N33/53
CPC分类号： G01N33/543 , G01N33/6803 , G01N33/94 , G01N2333/525 , G01N2500/04
摘要： The present invention relates to a process for the isolation and identification of pharmaceutically relevant target compounds (TC) from a sample, said sample being derived from a living organism, wherein said target compound(s) bind(s) to a compound of interest (COI) under physiological conditions, said compound of interest (COI) being associated with a given impaired condition or disease. This process involves the isolation and the purification of the complex(es) formed by the compound. The present invention also relates to a process for the identification of a pharmaceutically effective compound useful for preventing and/or treating a given impaired condition or disease, wherein said compound is identified by its binding to a relevant target compound (TC) that has been identified and isolated according to the above mentioned process. Furthermore, the present application concerns a process for the identification of new uses (i.e. medical indications) of an active agent involving identifying diseases associated with the binding partner(s) of the active agent.
摘要翻译：本发明涉及从样品中分离和鉴定药学上相关的目标化合物（TC）的方法，所述样品衍生自活生物体，其中所述目标化合物与感兴趣的化合物结合（ COI），所述感兴趣的化合物（COI）与给定的受损条件或疾病相关。该方法涉及由化合物形成的络合物的分离和纯化。本发明还涉及用于鉴定可用于预防和/或治疗给定的受损病症或疾病的药学有效化合物的方法，其中所述化合物通过与已鉴定的相关目标化合物（TC）的结合来鉴定并根据上述方法分离。此外，本申请涉及用于鉴定涉及鉴定与活性剂的结合配偶体相关的疾病的活性剂的新用途（即医学适应症）的方法。

5. 发明申请

WO2009098021A1 SELECTIVITY PROFILING OF PI3K INTERACTING MOLECULES AGAINST MULTIPLE TARGETS 审中-公开
标题翻译： PI3K交互分子对多种目标的选择性分析
公开(公告)号：WO2009098021A1
公开(公告)日：2009-08-13
申请号：PCT/EP2009/000692
申请日：2009-02-03
申请人： CELLZOME AG , CANSFIELD, Andrew , BERGAMINI MOORE, Giovanna , NEUBAUER, Gitte
发明人： CANSFIELD, Andrew , BERGAMINI MOORE, Giovanna , NEUBAUER, Gitte
IPC分类号： C12Q1/48 , G01N33/573
CPC分类号： G01N33/573 , G01N2333/91215 , G01N2500/02
摘要： The present invention relates to methods wherein a PI3K interacting compound is identified by incubating a PI3K containing protein preparation with phenyl thiazole ligand 1.
摘要翻译：本发明涉及通过将含PI3K的蛋白质制剂与苯基噻唑配体1孵育来鉴定PI3K相互作用化合物的方法。

6. 发明申请

WO2009068482A1 AMINO TRIAZOLES AS PI3K INHIBITORS 审中-公开
标题翻译： AMINO TRIAZOLES作为PI3K抑制剂
公开(公告)号：WO2009068482A1
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066001
申请日：2008-11-21
申请人： Cellzome Limited , RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , NEUBAUER, Gitte
发明人： RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , NEUBAUER, Gitte
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) Said compounds are useful as protein kinase inhibitors, especially inhibitors of P13K, 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。所述化合物可用作蛋白激酶抑制剂，特别是P13K抑制剂，用于治疗或预防免疫学，炎症，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。

7. 发明申请

WO2009068482A8 AMINO TRIAZOLES AS PI3K INHIBITORS 审中-公开
标题翻译： AMINO TRIAZOLES作为PI3K抑制剂
公开(公告)号：WO2009068482A8
公开(公告)日：2010-07-29
申请号：PCT/EP2008066001
申请日：2008-11-21
申请人： CELLZOME LTD , RAMSDEN NIGEL , BELL KATHRYN , CANSFIELD ANDREW , TAYLOR JESS , SUNOSE MIHIRO , MIDDLEMISS DAVID , NEUBAUER GITTE
发明人： RAMSDEN NIGEL , BELL KATHRYN , CANSFIELD ANDREW , TAYLOR JESS , SUNOSE MIHIRO , MIDDLEMISS DAVID , NEUBAUER GITTE
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) Said compounds are useful as protein kinase inhibitors, especially inhibitors of P13K, 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。所述化合物可用作蛋白激酶抑制剂，特别是P13K抑制剂，用于治疗或预防免疫学，炎症，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。

8. 发明申请

WO2012010240A1 IN VIVO METHOD FOR THE EVALUATION OF A COMPOUND-TARGET INTERACTION 审中-公开
标题翻译：用于评估化合物 - 目标相互作用的体内方法
公开(公告)号：WO2012010240A1
公开(公告)日：2012-01-26
申请号：PCT/EP2011/003055
申请日：2011-06-20
申请人： CELLZOME AG , DREWES, Gerard , HOPF, Carsten , KRUSE, Ulrich , NEUBAUER, Gitte
发明人： DREWES, Gerard , HOPF, Carsten , KRUSE, Ulrich , NEUBAUER, Gitte
IPC分类号： C12Q1/48 , G01N33/50
CPC分类号： G01N33/573 , G01N33/5088 , G01N2333/91215 , G01N2500/00
摘要： The invention relates to a method for evaluation of a compound-target interaction in vivo, comprising the steps of administering the compound to an animal, taking a body fluid sample of the animal, determining the concentration of the compound in the body fluid sample, taking a cellular sample of the animal containing the target, preparing a protein preparation of said cellular sample, providing an immobilised ligand capable of binding to the target, contacting the protein preparation with the immobilised ligand under conditions allowing the formation of a complex between the immobilised ligand and the target, determining the amount of complexes formed in step, and correlating the amount of complexes with the concentration of the compound in the body fluid sample.
摘要翻译：本发明涉及一种用于评价体内化合物 - 靶相互作用的方法，包括以下步骤：向动物施用化合物，服用动物的体液样品，测定体液样品中化合物的浓度，取制备含有该靶标的动物的细胞样品，制备所述细胞样品的蛋白质制剂，提供能够结合靶标的固定化配体，使蛋白质制剂与固定的配体在允许在固定化配体之间形成复合物的条件下接触和靶标，确定步骤中形成的络合物的量，并且将复合物的量与体液样品中化合物的浓度相关联。

9. 发明申请

WO2008015013A1 METHODS FOR THE IDENTIFICATION OF PI3K INTERACTING MOLECULES AND FOR THE PURIFICATION OF PI3K 审中-公开
标题翻译： PI3K相互作用分子鉴定方法和PI3K纯化方法
公开(公告)号：WO2008015013A1
公开(公告)日：2008-02-07
申请号：PCT/EP2007/006887
申请日：2007-08-03
申请人： CELLZOME AG , BERGAMINI MOORE, Giovanna , CANSFIELD, Andrew , RAMSDEN, Nigel , NEUBAUER, Gitte
发明人： BERGAMINI MOORE, Giovanna , CANSFIELD, Andrew , RAMSDEN, Nigel , NEUBAUER, Gitte
IPC分类号： G01N33/573 , C12Q1/48
CPC分类号： C12Q1/485 , G01N2500/02
摘要： The present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing a protein preparation containing PI3K, b) contacting the protein preparation with phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1 - PI3K complex, c) incubating the phenylthiazole ligand 1 - PI3K complex with a given compound, and d) determining whether the compound is able to separate PI3K from the immobilized phenylthiazole ligand 1. Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing a protein preparation containing PI3K, b) contacting the protein preparation with phenylthiazole ligand 1 immobilized on a solid support and with a given compound under conditions allowing the formation of a phenylthiazole ligand 1 - PI3K complex, and c) detecting the phenylthiazole ligand 1 - PI3K complex formed in step b). Furthermore, the present invention relates to a method for the identification of a PI3 K interacting compound, comprising the steps of a) providing two aliquots of a protein preparation containing PI3K, b) contacting one aliquot with the phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1 - PI3K complex, c) contacting the other aliquot with the phenylthiazole ligand 1 immobilized on a solid support and with a given compound under conditions allowing the formation of a phenylthiazole ligand 1 - PI3K complex, and d) determining the amount of the phenylthiazole ligand 1 - PI3K complex formed in steps b) and c). Furthermore, the present invention realtes to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing two aliquots comprising each at least one cell containing PI3K, b) incubating one aliquot with a given compound, c) harvesting the cells of each aliquot, d) lysing the cells in order to obtain protein preparations, e) contacting the protein preparations with the phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1 - PI3K complex, and f) determining the amount of the phenylthiazole ligand 1 - PI3K complex formed in each aliquot in step e).
摘要翻译：本发明涉及一种鉴定PI3K相互作用化合物的方法，包括以下步骤：a）提供含有PI3K的蛋白质制剂，b）使蛋白制备物与固定在固相载体上的苯基噻唑配体1接触，苯基噻唑配体1-PI3K复合物，c）将苯基噻唑配体1-PI3K复合物与给定化合物一起孵育，以及d）测定该化合物是否能够从固定的苯基噻唑配体1分离PI3K。此外，本发明涉及用于鉴定PI3K相互作用化合物的方法，包括以下步骤：a）提供含有PI3K的蛋白质制剂，b）使所述蛋白质制剂与固定在固体支持物上的苯基噻唑配体1和给定化合物在允许形成苯基噻唑配体1-PI3K复合物，和c）检测苯基噻唑配体1-PI3K互补 x在步骤b）中形成。此外，本发明涉及用于鉴定PI3K相互作用化合物的方法，包括以下步骤：a）提供含有PI3K的蛋白质制剂的两个等分试样，b）使一个等分试样与固定在固体支持物上的苯基噻唑配体1接触在允许形成苯基噻唑配体1-PI3K复合物的条件下，c）使其他等分试样与固定在固体载体上的苯基噻唑配体1和允许形成苯基噻唑配体1-PI3K复合物的条件下与给定化合物接触，以及 d）测定步骤b）和c）中形成的苯基噻唑配体1-PI3K复合物的量。此外，本发明涉及用于鉴定PI3K相互作用化合物的方法，其包括以下步骤：a）提供两个等分试样，其包含每个至少一个含有PI3K的细胞，b）将一个等分试样与给定化合物一起孵育，c）每个等分试样的细胞，d）裂解细胞以获得蛋白质制剂，e）在允许形成苯基噻唑配体1-PI3K复合物的条件下，使蛋白质制剂与固定在固体支持物上的苯基噻唑配体1接触，以及f）测定在步骤e）中在每个等分试样中形成的苯基噻唑配体1-PI3K复合物的量。

10. 发明申请

WO2004099774A2 PROCESS FOR THE IDENTIFICATION OF NEW MEDICAL TARGETS 审中-公开
标题翻译：鉴定新医疗目标的过程
公开(公告)号：WO2004099774A2
公开(公告)日：2004-11-18
申请号：PCT/EP2004/004883
申请日：2004-05-07
申请人： CELLZOME AG , SUPERTI-FUGA, Giulio , KRUSE, Ulrich , RYBIN, Vladimir , NEUBAUER, Gitte
发明人： SUPERTI-FUGA, Giulio , KRUSE, Ulrich , RYBIN, Vladimir , NEUBAUER, Gitte
IPC分类号： G01N33/53
CPC分类号： G01N33/543 , G01N33/6803 , G01N33/94 , G01N2333/525 , G01N2500/04
摘要： The present invention relates to a process for the isolation and identification of pharmaceutically relevant target compounds (TC) from a sample, said sample being derived from a living organism, wherein said target compound(s) bind(s) to a compound of interest (COI) under physiological conditions, said compound of interest (COI) being associated with a given impaired condition or disease. Furthermore, the present invention relates to a process for the identification of a pharmaceutically effective compound useful for preventing and/or treating a given impaired condition or disease, wherein said compound is identified by its binding to a relevant target compound (TC) that has been identified and isolated according to the above mentioned process.
摘要翻译：本发明涉及从样品中分离和鉴定药学上相关的目标化合物（TC）的方法，所述样品衍生自活生物体，其中所述目标化合物与感兴趣的化合物结合（ COI），所述感兴趣的化合物（COI）与给定的受损条件或疾病相关。此外，本发明涉及用于鉴定可用于预防和/或治疗给定的受损病症或疾病的药学上有效的化合物的方法，其中所述化合物通过与已经经过的相关目标化合物（TC）的结合来鉴定根据上述过程鉴定和分离。

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