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1. 发明申请

WO2011012269A3 METHOD AND SUBSTANCES FOR PREPARATION OF N-SUBSTITUTED PYRIDINIUM COMPOUNDS 审中-公开
标题翻译：制备N-取代的吡啶鎓化合物的方法和物质
公开(公告)号：WO2011012269A3
公开(公告)日：2011-08-11
申请号：PCT/EP2010004522
申请日：2010-07-23
申请人： ROCHE DIAGNOSTICS GMBH , HOFFMANN LA ROCHE , HEINDL DIETER , MAERZ HERIBERT , SCHMIDT AXEL
发明人： HEINDL DIETER , MAERZ HERIBERT , SCHMIDT AXEL
IPC分类号： C07D213/82 , C07D401/04 , C07D473/16
CPC分类号： C07D401/04 , C07D213/82 , C07D473/16
摘要： The present invention relates to a method for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine. In this reaction the pyridinium ring of the Zincke salt reacts with the amine which induces ring opening followed by ring closing, whereby the nitrogen of the amine becomes part of the N-substituted pyridinium ring. Preferably the amine is a primary amine. Novel purine-substituted pyridyl compounds, which can e.g. used in the above reaction, are also disclosed.
摘要翻译：本发明涉及通过使用N-杂芳基取代的吡啶鎓盐（Zincke盐）并使其与亲核胺反应来合成N-取代的吡啶鎓化合物的方法。在该反应中，Zincke盐的吡啶鎓环与引起开环然后闭环的胺反应，其中胺的氮成为N-取代的吡啶鎓环的一部分。优选胺是伯胺。新的嘌呤取代的吡啶基化合物，其可以例如也用于上述反应中。

2. 发明专利

ES2276733T3 NUEVOS REACTIVOS PARA MARCAR ACIDOS NUCLEICOS. 未知
公开(公告)号：ES2276733T3
公开(公告)日：2007-07-01
申请号：ES01121139
申请日：2001-09-04
申请人： ROCHE DIAGNOSTICS GMBH , HOFFMANN LA ROCHE
发明人： HEINDL DIETER DR , SAGNER GREGOR DR , MAERZ HERIBERT , VON DER ELTZ HERBERT DR
IPC分类号： C07H21/00 , G01N33/58 , C07B61/00 , C07C217/10 , C07C233/18 , C07H21/04 , C08G69/08 , C09B11/28 , C09B69/10 , C12N15/09
摘要： Reactivo marcador que tiene la estructura M-NH-CO-L-Z-(CH2)n-O-S ¿ (CH2)m-O-K en la que - M es un colorante fluorescente, - L significa un engarce de estructura -(CH2)p o de la estructura -(CH2)p-CO-NH-, - Z es CH o N, - S es un grupo protector eliminable, - n, m y p con independencia entre sí son números enteros de 1 a 15, - O-K es una fosforamidita.

3. 发明专利

DE60124637D1 未知
公开(公告)号：DE60124637D1
公开(公告)日：2007-01-04
申请号：DE60124637
申请日：2001-09-04
申请人： ROCHE DIAGNOSTICS GMBH , HOFFMANN LA ROCHE
发明人： HEINDL DIETER DR , SAGNER GREGOR DR , MAERZ HERIBERT , VON DER ELTZ HERBERT DR
IPC分类号： C07H21/00 , G01N33/58 , C07B61/00 , C07C217/10 , C07C233/18 , C07H21/04 , C08G69/08 , C09B11/28 , C09B69/10 , C12N15/09

4. 发明专利

JP2003012951A Novel reagent for labelling nucleic acid 有权
标题翻译：用于标记核酸的新试剂
公开(公告)号：JP2003012951A
公开(公告)日：2003-01-15
申请号：JP2001272569
申请日：2001-09-07
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲー
发明人： HEINDL DIETER DR , SAGNER GREGOR DR , MAERZ HERIBERT , VON DER ELTZ HERBERT
IPC分类号： G01N33/58 , C07B61/00 , C07C217/10 , C07C233/18 , C07H21/00 , C07H21/04 , C08G69/08 , C09B11/28 , C09B69/10 , C12N15/09
CPC分类号： C07H21/00 , C07B2200/11 , C40B40/00 , Y02P20/55 , Y10T428/2996
摘要： PROBLEM TO BE SOLVED: To provide a labelling reagent which is used for synthesizing a labelled oligonucleotide, gives a label free from strong electron acceptor effects, and is stable during the synthesis of an oligonucleotide. SOLUTION: This reagent is represented by the structural formula [wherein M is a detectable label; L is a linker represented by -(CH2 )p - or -(CH2 )p -CO-NH-; Z is CH or N; S is a removable protective group; n and m are each independently a natural number of 1-15; and K is a phosphoamidite or K=-V-T (wherein T is a solid-phase carrier substance; and V is a linking group containing a cleavable bond)].
摘要翻译：要解决的问题：为了提供用于合成标记的寡核苷酸的标记试剂，给出没有强电子受体效应的标记，并且在寡核苷酸的合成期间是稳定的。解决方案：该试剂由结构式[其中M是可检测标记; L是由 - （CH 2）p - 或 - （CH 2）p -CO-NH-表示的连接体。 Z是CH或N; S是可拆卸的保护组; n和m各自独立地为1-15的自然数; 并且K是亚磷酰胺或K = -V-T（其中T是固相载体物质; V是含有可切割键的连接基团）]。

5. 发明专利

ES2529385T3 Métodos y sustancias para la obtención de compuestos de piridinio sustituidos sobre N 未知
公开(公告)号：ES2529385T3
公开(公告)日：2015-02-19
申请号：ES10740156
申请日：2010-07-23
申请人： HOFFMANN LA ROCHE
发明人： HEINDL DIETER , MAERZ HERIBERT , SCHMIDT AXEL
IPC分类号： C07D213/82 , C07D401/04 , C07D473/16
摘要： Un método para la síntesis de un compuesto de piridinio sustituido sobre N que consta de los pasos de a) proporcionar una sal de Zincke de la fórmula I**Fórmula** que tiene un contraión, en la que R1 se elige entre H, alquilo, arilo, 2-metil-1,3-dioxolan-2-ilo, ariloxi, alquiloxi, hidroxialquilo, arilalquilo, aminoalquilo protegido sobre N, alquenilo, alquinilo, arilalquenilo, arilalquinilo C>=XNH2, C>=XNH-alquilo, C>=XN(alquilo)2 C>=XNH-arilo, C>=XN(arilo)2, C>=X-arilo, C>=X-alquilo, COO-alquilo, en la que R2 se elige entre H, alquilo, arilo, pirid-4-ilo, alquilpiridinio-4-ilo, 2-metil-1,3-dioxolan-2-ilo, ariloxi, alquiloxi, hidroxialquilo, arilalquilo, aminoalquilo protegido, alquenilo, alquinilo, arilalquenilo, arilalquinilo, C>=XNH2, C>=XNHalquilo, C>=XN(alquilo)2, C>=XNH-arilo, C>=XN(arilo)2, C>=X-arilo, C>=X-alquilo, COO-alquilo, alquilsulfanilo y**Fórmula** en la que por lo menos uno de R1 o R2 es H o alquilo o los restos R1 y R2 juntos son un resto butano-1,4-diilo o butadieno-1,4-diilo que están unidos entre para formar un ciclo de 6 eslabones, en la que con independencia en R1 o R2 alquilo es alquilo C1-C6 lineal o ramificado o cicloalquilo C5-C6, alquenilo es alquenilo C2-C6 lineal o ramificado, alquinilo es alquinilo C2-C6 lineal o ramificado y arilo es fenilo o naftilo, en la que X >= S u O, en la que Y es N o C; en el caso de que Y sea N, no está presente ningún R3 y en el caso de que Y sea C, entonces R3 es H, alquilo C1-C3 o junto con R4 y los dos átomos de carbono sp2, a los que están unidos R3 y R4, forman un sistema de anillo aromático de 5 ó 6 eslabones, que contiene opcionalmente 1 ó 2 átomos de nitrógeno, en la que R4 es H, alquilo C1-C3, hidroxi, O-alquilo C1-C3, amino, (alquil C1-C3)-amino, fenilamino, fenilo o junto con R3 y los dos átomos de carbono sp2, a los que están unidos R3 y R4, forman un sistema de anillo aromático de 5 ó 6 eslabones, que contiene opcionalmente 1 ó 2 átomos de nitrógeno, en la que R5 es H, alquilo C1-C3, hidroxi, O-alquilo C1-C3, amino, (alquil C1-C3)-amino, fenilamino, fenilo o halógeno, y en la que en el caso de que la fórmula I represente a un compuesto bipiridilo, cada uno de Y', R1', R3', R4' y R5', tienen los mismos significados que los restos Y, R1, R3, R4 y R5 correspondientes, (b) hacer reaccionar la sal de Zincke del paso (a) con una amina primaria de la fórmula II:**Fórmula** en la que R6 forma parte de una amina orgánica primaria, que contiene un átomo de carbono sp2 o sp3 que está unido al resto -NH2, o en la que R6 es un resto, que junto con -NH2, es una hidrazina, una hidroxilamina, una sulfonil-hidrazida o una carbohidrazida, (c) con lo cual se obtiene un compuesto de piridinio sustituido sobre N de la fórmula III:**Fórmula** que tiene un contraión y en la que R1, R2, y R6 tienen los significados definidos antes.

6. 发明专利

CA2769154C METHOD AND SUBSTANCES FOR PREPARATION OF N-SUBSTITUTED PYRIDINIUM COMPOUNDS 未知
公开(公告)号：CA2769154C
公开(公告)日：2015-10-27
申请号：CA2769154
申请日：2010-07-23
申请人： HOFFMANN LA ROCHE
发明人： HEINDL DIETER , MAERZ HERIBERT , SCHMIDT AXEL
IPC分类号： C07D213/82 , C07D401/04 , C07D473/16
摘要： The present invention relates to a method for the synthesis of N-substituted pyridinium compounds of the Formula III: (See formula III) having a counterion, where R1, R2 and R3 are as defined herein. The compounds are synthesized by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine. In this reaction the pyridinium ring of the Zincke salt reacts with the amine which induces ring opening followed by ring closing, whereby the nitrogen of the amine becomes part of the N-substituted pyridinium ring. Preferably the amine is a primary amine. Purine-substituted pyridyl compounds, which can be used in the above reaction, are also disclosed.

7. 发明专利

CA2356552C NEW REAGENT FOR LABELLING NUCLEIC ACIDS 未知
公开(公告)号：CA2356552C
公开(公告)日：2009-07-28
申请号：CA2356552
申请日：2001-09-04
申请人： HOFFMANN LA ROCHE
发明人： VON DER ELTZ HERBERT , SAGNER GREGOR , HEINDL DIETER , MAERZ HERIBERT
IPC分类号： C07H21/00 , G01N33/58 , C07B61/00 , C07C217/10 , C07C233/18 , C07H21/04 , C08G69/08 , C09B11/28 , C09B69/10 , C12N15/09 , C12Q1/68 , C40B70/00
摘要： The present invention concerns a labelling reagent in which the label is bound via an amide bond and a linker to a residue of the molecule which is essentially characterized in that the N atom of the amide bond and the label are linked together directly by a covalent bond. In particular these are phosphoramidites or reactive supports suitable for nucleic acid synthesis. The invention also concerns processes for the production of such supports from suitable precursors.

8. 发明专利

AT346079T 未知
公开(公告)号：AT346079T
公开(公告)日：2006-12-15
申请号：AT01121139
申请日：2001-09-04
申请人： ROCHE DIAGNOSTICS GMBH
发明人： HEINDL DIETER DR , SAGNER GREGOR DR , MAERZ HERIBERT , VON DER ELTZ HERBERT DR
IPC分类号： G01N33/58 , C07B61/00 , C07C217/10 , C07C233/18 , C07H21/00 , C07H21/04 , C08G69/08 , C09B11/28 , C09B69/10 , C12N15/09

9. 发明专利

CA2769154A1 METHOD AND SUBSTANCES FOR PREPARATION OF N-SUBSTITUTED PYRIDINIUM COMPOUNDS 未知
公开(公告)号：CA2769154A1
公开(公告)日：2011-02-03
申请号：CA2769154
申请日：2010-07-23
申请人： HOFFMANN LA ROCHE
发明人： HEINDL DIETER , MAERZ HERIBERT , SCHMIDT AXEL
IPC分类号： C07D213/82 , C07D401/04 , C07D473/16
摘要： The present invention relates to a method for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine. In this reaction the pyridinium ring of the Zincke salt reacts with the amine which induces ring opening followed by ring closing, whereby the nitrogen of the amine becomes part of the N-substituted pyridinium ring. Preferably the amine is a primary amine. Novel purine-substituted pyridyl compounds, which can e.g. used in the above reaction, are also disclosed.

10. 发明专利

CA2356552A1 NEW REAGENT FOR LABELLING NUCLEIC ACIDS 未知
公开(公告)号：CA2356552A1
公开(公告)日：2002-03-08
申请号：CA2356552
申请日：2001-09-04
申请人： HOFFMANN LA ROCHE
发明人： MAERZ HERIBERT , HEINDL DIETER , VON DER ELTZ HERBERT , SAGNER GREGOR
IPC分类号： G01N33/58 , C07B61/00 , C07C217/10 , C07C233/18 , C07H21/00 , C07H21/04 , C08G69/08 , C09B11/28 , C09B69/10 , C12N15/09
摘要： The present invention concerns a labelling reagent in which the label is bound via an amide bond and a linker to a residue of the molecule which is essentially characterized in that the N atom of the amide bond and the label are linked together directly by a covalent bond. In particular these are phosphoramidites or reactive supports suitable for nucleic acid synthesis. The invention also concerns processes for the production of such supports from suitable precursors.

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