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1. 发明申请

WO2005016934A1 3H-PHENOXAZINE DERIVATIVES SUITABLE AS NEAR-INFRARED IMAGING AGENTS, PREPARATION AN USE THEREOF 审中-公开
标题翻译：适用于近红外成像剂的3H-苯并恶嗪衍生物，其制备方法
公开(公告)号：WO2005016934A1
公开(公告)日：2005-02-24
申请号：PCT/EP2004/009225
申请日：2004-08-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
发明人： AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
IPC分类号： C07D498/22
CPC分类号： C07D513/14
摘要： The present invention provides compounds of formula (I) wherein X and Y represent CH, CH 2 or a divalent or trivalent heteroatom under the proviso that X and Y are not simultaneously CH or CH 2 ; m and o represent independently of each other 0 or 1, with the proviso that if m is 0 then the dotted line between Y and the neighboring C atom represents a bond and Y is CH or a trivalent heteroatom, if m is 1 then the dotted line between Y and the neighboring C atom is absent and Y is CH 2 or a divalent heteroatom, if o is 0 then the dotted line between X and the neighboring C atom represents a bond and X is CH or a trivalent heteroatom, if o is 1 then the dotted line between X and the neighboring C atom is absent and X is CH 2 or a divalent heteroatom; A represents (CH 3 CR 4 ) p and Q represents (CR 9 R 10 ) n ; n and p represent independently of each other 0 or 1; R 6 , R 7 , R 13 and R 14 denote independently of each other hydrogen, halogen, (C 1-4 )alkyl, (C 1-4 )alkylSO 2 , SO 3 H, carboxy, (C 1-4 )alkoxy carbonyl, (C 1-4 )alkoxy, OH or NR 15 R 16 ; R 1 , R 2 , R 3 , R 4 , R 9 , R 10 , R 11 and R 12 denote independently of each other hydrogen, (C 1-4 )alkyl, carboxy, (C 1-4 )alkoxy carbonyl or (C 1-4 )alkoxy, or, when X is CH or CH 2 then R 1 and R 2 can also be OH or NR 15 R 16 , or when Y is CH or CH 2 then R 11 , R 12 can also be OH or NR 15 R 16 ; R 5 , R 8 , R 15 and R 16 are independently of each other hydrogen, (C 1-4 )alkyl, (C 1-4 )alkoxy, R 17 O-C(O)-(C 1-4 )alkyl or (reactive group)-(C 1-4 )alkyl; and R 17 represents hydrogen or (C 1-4 )alkyl; compositions comprising such compounds, a process for the production of such compounds of formula (I), a method of labeling target structures, especially amyloid plaques, in the brain, a method for identifying Alzheimer's disease, use of a compound of formula I as a near-infrared imaging agent and a conjugate comprising a compound of formula (I) covalently linked to a biomolecule through a reactive group.
摘要翻译：本发明提供式（I）化合物，其中X和Y表示CH，CH 2或二价或三价杂原子，条件是X和Y不同时为CH或CH 2; m和o彼此独立地表示0或1，条件是如果m是0，则Y和相邻C原子之间的虚线表示键，Y是CH或三价杂原子，如果m是1，则虚线 Y与相邻C原子之间的直线不存在且Y为CH 2或二价杂原子，如果o为0，则X与相邻C原子之间的虚线表示键，X为CH或三价杂原子，如果o为1 则X与相邻C原子之间的虚线不存在，X为CH 2或二价杂原子; A表示（CH 3 CR 4）p且Q表示（CR 9 R 10）n; n和p彼此独立地表示0或1; R6，R7，R13和R14彼此独立地表示氢，卤素，（C1-4）烷基，（C1-4）烷基SO2，SO3H，羧基，（C1-4）烷氧基羰基，（C1-4）烷氧基，OH 或NR15R16; R1，R2，R3，R4，R9，R10，R11和R12彼此独立地表示氢，（C1-4）烷基，羧基，（C1-4）烷氧基羰基或（C1-4）烷氧基，或当X 那么R1和R2也可以是OH或NR15R16，或当Y是CH或CH2时R11，R12也可以是OH或NR15R16; R5，R8，R15和R16彼此独立地为氢，（C1-4）烷基，（C1-4）烷氧基，R17O-C（O） - （C1-4）烷基或（反应性基团） - （C1- 4）烷基; R 17表示氢或（C 1-4）烷基; 包含这种化合物的组合物，制备式（I）化合物的方法，在脑中标记靶结构，特别是淀粉样蛋白斑的方法，用于鉴定阿尔茨海默氏病的方法，式I化合物作为近红外显影剂和包含通过反应性基团与生物分子共价连接的式（I）化合物的共轭物。

2. 发明申请

WO2006094688A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2006094688A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/001866
申请日：2006-03-01
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUER, Manfred , MEISNER, Nicole-Claudia , HINTERSTEINER, Martin , SCHINDLER, Torsten , GSTACH, Hubert
发明人： AUER, Manfred , MEISNER, Nicole-Claudia , HINTERSTEINER, Martin , SCHINDLER, Torsten , GSTACH, Hubert
IPC分类号： G01N33/53 , G01N33/542
CPC分类号： G01N33/542 , G01N33/5308 , G01N2500/02
摘要： The invention relates to an assay for identifying an agent that modulates the interaction of a mRNA with a target protein, e.g. HuR and to organic compounds of formula (I); wherein R 1 , R 2 and R 3 are as defined above, and their use, e.g. as an inhibitor on the complex-formation of an ARE-containing mRNA and a target protein.
摘要翻译：本发明涉及用于鉴定调节mRNA与靶蛋白的相互作用的试剂的测定法，例如。 HuR和式（I）的有机化合物; 其中R 1，R 2和R 3 3如上所定义，并且它们的用途，例如，作为含有ARE的mRNA和靶蛋白复合物形成的抑制剂。

3. 发明申请

WO2009000775A1 POST-SCREENING LABELING OF ON-BEAD COMPOUNDS 审中-公开
标题翻译：珠粒化合物的后验标签
公开(公告)号：WO2009000775A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/057878
申请日：2008-06-20
申请人： NOVARTIS AG , AUER, Manfred , HINTERSTEINER, Martin , KIMMERLIN, Thierry
发明人： AUER, Manfred , HINTERSTEINER, Martin , KIMMERLIN, Thierry
IPC分类号： C40B20/00 , C40B40/10 , C07C271/18 , C07D249/04 , C07D311/88
CPC分类号： C07D311/88 , B01J2219/00454 , B01J2219/005 , B01J2219/00576 , B01J2219/00596 , B01J2219/0072 , C07B2200/11 , C07C271/22 , C07C2603/18 , C07D209/12 , C07D209/14 , C07D249/04 , C40B40/04 , C40B50/18 , C40B80/00
摘要： The present invention relates to new on bead chemistry to produce compound libraries used in improved screening methods, allowing the direct solution confirmation of on-bead screening hits without compound decoding and resynthesis. More specifically, the invention relates to on-bead compounds having the formula B - L - C - S, wherein - represents a bond or any stable covalent spacer, B is a solid support to which a plurality of L-C-S molecules are covalently attached, L is a cleavable linker for covalently linking C to the solid support, C is a covalent linking core comprising at least one protected labeling functional group for covalently linking of a label or a detection molecule, S is a spacer comprising at least one protected or unprotected functional group for on-bead compound derivatization, and wherein L and C are selected so that (i) the linker L and the protected labeling functional group are not affected by side chain deprotection during on-bead compound derivatization, (ii) the linker L and any synthetic molecule attached to S are not affected by deprotection of labeling functional group and labeling reaction step, (iii) covalent linkage of the label or the detection molecule or any synthetic molecule attached to S are not affected by cleavage of the linker L.
摘要翻译：本发明涉及新的珠粒化学制备用于改进筛选方法的化合物文库，允许直接溶液确认珠粒筛选命中而无需复合解码和再合成。更具体地，本发明涉及具有式B-L-C-S的珠珠化合物，其中 - 表示键或任何稳定的共价间隔基，B是多个LCS分子共价连接的固体载体，L C是共价连接C与固体支持物的可切割接头，C是包含至少一个用于共价连接标记或检测分子的保护标记官能团的共价连接核心，S是包含至少一个被保护或未被保护的官能团用于珠珠化合物衍生化的组，并且其中选择L和C，使得（i）接头L和受保护的标记官能团在珠粒化合物衍生化期间不受侧链脱保护的影响，（ii）接头L和与S连接的任何合成分子不受标记官能团的脱保护和标记反应步骤的影响，（iii）标记或检测分子或任何合成分子的共价连接连接于S不受连接体L切割的影响。

4. 发明申请

WO2008145609A1 METHOD OF MAKING COVALENT CONJUGATES WITH HIS-TAGGED PROTEINS 审中-公开
标题翻译：用标记的蛋白质制备共价物的方法
公开(公告)号：WO2008145609A1
公开(公告)日：2008-12-04
申请号：PCT/EP2008/056361
申请日：2008-05-23
申请人： NOVARTIS AG , AUER, Manfred , HINTERSTEINER, Martin , KIMMERLIN, Thierry
发明人： AUER, Manfred , HINTERSTEINER, Martin , KIMMERLIN, Thierry
IPC分类号： A61K41/00 , A61K47/48 , A61K49/00 , C07C237/10 , C07C257/02
CPC分类号： C07C237/10 , A61K41/0042 , A61K47/542 , A61K49/0041 , A61K49/0056 , C07D233/26 , C07D257/02 , C07D311/82
摘要： The present invention refers to novel agents for covalently conjugating His-tagged proteins, to covalent conjugates of His-tagged proteins and to methods of making such conjugates.
摘要翻译：本发明涉及用于共价结合His-标记的蛋白质与His-标签蛋白质的共价缀合物和制备这种缀合物的方法的新型试剂。

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