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1. 发明申请

WO2006092584A2 BIOLOGICAL COMPOSITIONS LABELLED WITH RADIOISOTOPE 审中-公开
标题翻译：用放射性标记标记的生物组合物
公开(公告)号：WO2006092584A2
公开(公告)日：2006-09-08
申请号：PCT/GB2006000713
申请日：2006-02-28
申请人： XCELERON LTD , GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： A61K51/08 , G01N33/60
CPC分类号： A61K51/081 , G01N33/60
摘要： The invention provides a biological composition comprising a biological compound of formula I (I) B-A* alone or together with B wherein B-A* is a biological compound or a derivative thereof formed as the product of reaction of the biological compound to introduce A*, A* is a radioisotopic moiety having MW in the range 10 to 500 comprising an AMS radioisotope * wherein the composition is characterised by a value for the percent incorporation of radioisotope which is a measure of maximum specific activity, wherein 100% incorporation is defined as the incorporation of one radioisotope per molecule, and wherein the percent incorporation is in the range from in excess of zero to 100%, wherein the quantity of organic radioisotope A* labelled molecules in a population of one thousand molecules is so low as to not alter the biological activity of the drag; a process for the preparation thereof; a method for AMS detection of one or more biological compositions as defined in any of claims 1 to 17 comprising B of same or different origin, comprising providing one or more biological compositions and optionally one or more control compositions comprising biological compound B, for dosing to at least one subject, obtaining metabolic samples from the subject(s) having been dosed with said biological(s) as hereinbefore defined and conducting AMS detection and obtaining AMS results for the or each biological; and the use of a biological composition or compound of formula I in AMS detection providing in vitro or in vivo metabolism characteristics thereof.
摘要翻译：本发明提供一种生物组合物，其包含式I（I）的生物化合物单独或与B一起的BA *，其中BA *是生物化合物或其衍生物，其作为生物化合物引入A *，A *是放射性同位素部分，其具有10至500范围内的MW，包括AMS放射性同位素*，其中组合物的特征在于放射性同位素掺入百分比的值，其是最大比活性的量度，其中100％掺入被定义为掺入每个分子具有一种放射性同位素，并且其中掺入百分比在超过零至100％的范围内，其中在一千个分子的群体中的有机放射性同位素A *标记分子的量如此低以至于不改变生物拖动的活动; 其制备方法; 一种用于AMS检测如权利要求1至17中任一项所定义的一种或多种生物组合物的方法，其包含相同或不同来源的B，包括提供一种或多种生物组合物和任选的一种或多种包含生物化合物B的对照组合物，至少一个受试者，从已经给予所述生物体的受试者获得如上文所定义的代谢样品，并进行AMS检测并获得所述或每种生物的AMS结果; 并且在AMS检测中使用生物学组合物或式I化合物提供其体外或体内代谢特征。

2. 发明专利

CA2517349A1 LIBRARY OF COMPOUNDS LABELLED WITH RADIOISOTOPE 未知
公开(公告)号：CA2517349A1
公开(公告)日：2004-09-10
申请号：CA2517349
申请日：2004-02-27
申请人： XCELERON LTD
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： G01N33/60 , G01N33/58 , C07B61/00 , G01N33/68
摘要： Library of compounds or their pharmaceutically acceptable salts, each compound being associated with information on its chemical identity and structure, wherein at least two of the compounds is labelled with radioisotope characterised in that the radioisotope is an AMS active radioisotope; A solid support having a compound or its pharmaceutically acceptable salt as hereindefined bound thereto, the compound being associated with information on its chemical identity and structure and comprising a radioisotope, characterised in that the radioisotope is an AMS active radioisotope as hereinbefore defined; Process for the preparation of a library of compounds as claimed in any of claims 1 to 19 comprising radioisotope labelling a plurality of compounds, each compound being associated with information on its chemical identity and structure characterised in that labelling is with an AMS active radioisotope; A kit therefor; Method for selecting one or more candidate compounds comprising screening a library of the invention comprising AMS active radioisotope labelled compounds as hereinbefore defined and obtaining a sample from the screen or submitting a compound identified for metabolic studies and obtaining a sample therefrom, and performing AMS detection of the sample; and Use of the library, a solid support comprising radioisotope labelled compound or a method as hereinbefore defined in (bio)medical, agrochemical, environmental and like screening for further study by AMS detection.

3. 发明专利

GB2428676B Library of compounds labelled with radioisotope 未知
公开(公告)号：GB2428676B
公开(公告)日：2007-06-06
申请号：GB0622381
申请日：2004-02-27
申请人： XCELERON LTD
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： C40B40/04 , C40B20/08 , C40B70/00 , G01N33/60
摘要： Library of compounds or their pharmaceutically acceptable salts, each compound being associated with information on its chemical identity and structure, wherein at least two of the compounds is labelled with radioisotope characterised in that the radioisotope is an AMS active radioisotope; A solid support having a compound or its pharmaceutically acceptable salt as hereindefined bound thereto, the compound being associated with information on its chemical identity and structure and comprising a radioisotope, characterised in that the radioisotope is an AMS active radioisotope as hereinbefore defined; Process for the preparation of a library of compounds as claimed in any of claims 1 to 19 comprising radioisotope labelling a plurality of compounds, each compound being associated with information on its chemical identity and structure characterised in that labelling is with an AMS active radioisotope; A kit therefor; Method for selecting one or more candidate compounds comprising screening a library of the invention comprising AMS active radioisotope labelled compounds as hereinbefore defined and obtaining a sample from the screen or submitting a compound identified for metabolic studies and obtaining a sample therefrom, and performing AMS detection of the sample; and Use of the library, a solid support comprising radioisotope labelled compound or a method as hereinbefore defined in (bio)medical, agrochemical, environmental and like screening for further study by AMS detection.

4. 发明专利

CA2599520A1 RADIOISOTOPE LABELLED BIOLOGICAL COMPOSITIONS, AND THEIR USEIN ACCELERATOR MASS SPECTROMETRY 未知
公开(公告)号：CA2599520A1
公开(公告)日：2006-09-08
申请号：CA2599520
申请日：2006-02-28
申请人： XCELERON LTD
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： A61K49/00 , A61K51/00 , A61K51/08 , G01N33/60 , G01N33/66

5. 发明专利

HK1096711A1 Library of compounds labelled with radioisotope 未知
公开(公告)号：HK1096711A1
公开(公告)日：2007-06-08
申请号：HK07102260
申请日：2007-02-28
申请人： XCELERON LTD
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： C40B20060101 , G01N33/60
摘要： Library of compounds or their pharmaceutically acceptable salts, each compound being associated with information on its chemical identity and structure, wherein at least two of the compounds is labelled with radioisotope characterised in that the radioisotope is an AMS active radioisotope; A solid support having a compound or its pharmaceutically acceptable salt as hereindefined bound thereto, the compound being associated with information on its chemical identity and structure and comprising a radioisotope, characterised in that the radioisotope is an AMS active radioisotope as hereinbefore defined; Process for the preparation of a library of compounds as claimed in any of claims 1 to 19 comprising radioisotope labelling a plurality of compounds, each compound being associated with information on its chemical identity and structure characterised in that labelling is with an AMS active radioisotope; A kit therefor; Method for selecting one or more candidate compounds comprising screening a library of the invention comprising AMS active radioisotope labelled compounds as hereinbefore defined and obtaining a sample from the screen or submitting a compound identified for metabolic studies and obtaining a sample therefrom, and performing AMS detection of the sample; and Use of the library, a solid support comprising radioisotope labelled compound or a method as hereinbefore defined in (bio)medical, agrochemical, environmental and like screening for further study by AMS detection.

6. 发明专利

GB2428676A Library of compounds labelled with a radioisotope 未知
公开(公告)号：GB2428676A
公开(公告)日：2007-02-07
申请号：GB0622381
申请日：2004-02-27
申请人： XCELERON LTD
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： C40B40/04 , C40B20/08 , C40B70/00 , G01N33/60
摘要： A library of compounds or their pharmaceutically acceptable salts, provided as an array of compounds suitable for use in high throughput screening by means of accelerator mass spectrometry (AMS), each compound being associated with information on its chemical identity and structure. Each compound comprises an AMS active radioisotope and a tag associated with information on the compounds chemical identity and structure. A process for the preparation of such a library, wherein labelling the compound with an AMS active radioisotope comprises labelling a synthetic precursor or intermediate, determining the specific activty thereof, determining the desired specific activty and combining with a sufficient amount of corresponding unlabelled synthetic precursor or intermediate and isolating a product having desired percent incorporation.

7. 发明专利

GB2414989A Library of compounds labelled with radioisotope 未知
公开(公告)号：GB2414989A
公开(公告)日：2005-12-14
申请号：GB0518710
申请日：2004-02-27
申请人： XCELERON LTD
发明人： GARNER RONALD COLIN , LAPPIN GRAHAM JOHN
IPC分类号： G01N33/60 , G01N33/58
摘要： Library of compounds or their pharmaceutically acceptable salts, each compound being associated with information on its chemical identity and structure, wherein at least two of the compounds is labelled with radioisotope characterised in that the radioisotope is an AMS active radioisotope; a solid support having a compound or its pharmaceutically acceptable salt as herein-defined bound thereto, the compound being associated with information on its chemical identity and structure and comprising a radioisotope, characterised in that the radioisotope is an AMS active radioisotope as hereinbefore defined; process for the preparation of a library of compounds as claimed in any of Claims 1 to 19 comprising radioisotope labelling a plurality of compounds, each compound being associated with information on its chemical identity and structure characterised in that labelling is with an AMS active radioisotope; a kit therefor; Method for selecting one or more candidate compounds comprising screening a library of the invention comprising AMS active radioisotope labelled compounds as hereinbefore defined and obtaining a sample from the screen or submitting a compound identified for metabolic studies and obtaining a sample therefrom, and performing, AMS detection of the sample; and use of the library, a solid support comprising radioisotope labelled compound or a method as hereinbefore defined in (bio)medical,agrochemical, environmental and like screening for further study by AMS detection.

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