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1. 发明授权

US08372380B2 In vivo imaging of sulfotransferases 失效
标题翻译：磺酰转移酶的体内成像
公开(公告)号：US08372380B2
公开(公告)日：2013-02-12
申请号：US12594197
申请日：2008-03-31
申请人： Jorge R. Barrio , Vladimir Kepe , Gary W. Small , Nagichettiar Satyamurthy
发明人： Jorge R. Barrio , Vladimir Kepe , Gary W. Small , Nagichettiar Satyamurthy
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61B5/055 , A61B5/4088 , A61B5/411 , A61B6/481 , A61K31/57 , A61K51/04 , G01N2333/91194
摘要： Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18F, 123I, 124I, 125I, or 11C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.
摘要翻译：提供了用于磺基转移酶（SULTs）的放射标记示踪剂，其合成及其用途。包括用18F，123I，124I，125I或11C放射性标记的取代苯酚，萘酚，香豆素和黄酮。还提供了使用这些和其他示踪剂作为研究磺基转移酶分布和活性，在健康和疾病中并用于评估治疗干预的分析和诊断工具的体内技术。

2. 发明授权

US06274119B1 Methods for labeling &bgr;-amyloid plaques and neurofibrillary tangles 有权
标题翻译： β-淀粉样蛋白斑和神经原纤维缠结的标记方法
公开(公告)号：US06274119B1
公开(公告)日：2001-08-14
申请号：US09378662
申请日：1999-08-20
申请人： Jorge R. Barrio , Andrej Petric , Nagichettiar Satyamurthy , Gary W. Small , Gregory M. Cole , Sung-Cheng Huang
发明人： Jorge R. Barrio , Andrej Petric , Nagichettiar Satyamurthy , Gary W. Small , Gregory M. Cole , Sung-Cheng Huang
IPC分类号： A61K5100
CPC分类号： A61K51/0406 , A61K51/0455 , A61K51/0459
摘要： A method for labeling &bgr;-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): with mammalian tissue. In formula (I), R1 is selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C═C(CN)2-alkyl, —C═C(CN)2-alkylenyl-R4 , R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5, is a radical selected from the group consisting of —NH2, —OH, —SH, —NH-alkyl, —NHR4, —NH-alkylenyl-R4, —O-alkyl, —O-alkylenyl-R4, —S-alkyl, and —S-alkylenyl-R4; R6 is a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)-halogen, —C(O)NH , —C(O)NH-alkyl, —C(O)NH-alkylenyl-R4; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S. R2 and R3 are each independently selected from the group consisting of alkyl and alkylenyl-R10, wherein R10 is selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal and spiperone-3-yl. Alternatively, R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkylenyl-R10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl. In the compounds of formula (I), one or more of the hydrogen, halogen or carbon atoms can, optionally, be replaced with a radiolabel.
摘要翻译：一种用于在体内和体外标记β-淀粉样蛋白斑和神经原纤维缠结的方法，包括使式（I）化合物与哺乳动物组织接触。在式（I）中，R 1选自-C（O） - 烷基，-C（O） - 亚烷基基-R 4，-C（O）O-烷基，-C（O）O-亚烷基 - R4，-C = C（CN）2-烷基，-C = C（CN）2 - 亚烷基-R4，R4为选自烷基，取代烷基，芳基和取代芳基的基团; R5是选自-NH 2，-OH，-SH，-NH-烷基，-NHR 4，-NH-亚烷基-R 4，-O-烷基，-O-亚烷基基-R 4，-S- 烷基和-S-亚烷基基-R4; R6是选自-CN，-COOH，-C（O）O-烷基，-C（O）O-亚烷基-R4，-C（O） - 烷基，-C（O） - 亚烷基-R4，-C（O） - 卤素，-C（O）NH，-C（O）NH-烷基，-C（O）NH-亚烷基基-R4; R7是选自O，NH和S的基团; 并且R 8是N，O或S.R 2和R 3各自独立地选自烷基和亚烷基-R 10，其中R 10选自-OH，-OT，卤素，螺哌
酮，螺哌酮缩酮和螺哌隆 -3-基。或者，R2和R3一起形成杂环，任选被至少一个选自烷基，烷氧基，OH，OT，卤素，亚烷基-R 10，羰基，螺哌
酮，螺哌酮缩酮和螺哌酮-3-基。在式（I）的化合物中，氢，卤素或碳原子中的一个或多个可以任选地被放射性标记代替。

3. 发明授权

US07341709B2 Compositions for labeling β-amyloid plaques and neurofibrillary tangles 有权
公开(公告)号：US07341709B2
公开(公告)日：2008-03-11
申请号：US10680818
申请日：2003-10-07
申请人： Jorge R. Barrio , Andrej Petric , Nagichettiar Satyamurthy , Gary W. Small , Gregory M. Cole , Sung-Cheng Huang
发明人： Jorge R. Barrio , Andrej Petric , Nagichettiar Satyamurthy , Gary W. Small , Gregory M. Cole , Sung-Cheng Huang
IPC分类号： A61K51/00
CPC分类号： A61K51/0406 , A61K51/0455 , A61K51/0459
摘要： Compositions useful for labeling β-amyloid plaques and neurofibrillary tangles are provided. The compositions comprises compounds of formula (I): wherein R1 is selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C═C(CN)2-alkyl, —C═C(CN)2-alkylenyl-R4, wherein R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5 is a radical selected from the group consisting of —NH2, —OH, —SH, —NH-alkyl, —NHR4, —NH-alkylenyl-R4, —O-alkyl, —O-alkylenyl-R4, —S-alkyl, and —S-alkylenyl-R4; R6 is a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)-halogen, —C(O)NH-alkyl, —C(O)NH-alkylenyl-R4 and —C(O)NH2; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S; and R2 is selected from the group consisting of alkyl and alkylenyl-R10 and R3 is alkylenyl-R10, wherein R10 is selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal, and spiperone-3-yl, or R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkyl-R10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl, and further wherein one or more of the hydrogen, halogen or carbon atoms are optionally replaced with a radiolabel.

4. 发明授权

US06660530B2 Methods for labeling &bgr;-amyloid plaques and neurofibrillary tangles 有权
标题翻译： β-淀粉样蛋白斑和神经原纤维缠结的标记方法
公开(公告)号：US06660530B2
公开(公告)日：2003-12-09
申请号：US09891883
申请日：2001-06-26
申请人： Jorge R. Barrio , Andrej Petric , Nagichettiar Satyamurthy , Gary W. Small , Gregory M. Cole , Sung-Cheng Huang
发明人： Jorge R. Barrio , Andrej Petric , Nagichettiar Satyamurthy , Gary W. Small , Gregory M. Cole , Sung-Cheng Huang
IPC分类号： G01N33567
CPC分类号： A61K51/0406 , A61K51/0455 , A61K51/0459
摘要： A method for labeling &bgr;-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): with mammalian tissue. In formula (I), R1 is selected from the group consisting of —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C═C(CN)2-alkyl, —C═C(CN)2-alkylenyl-R4, R4 is a radical selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl; R5 is a radical selected from the group consisting of —NH2, —OH, —SH, —NH-alkyl, —NHR4, —NH-alkylenyl-R4, —O-alkyl, —O-alkylenyl-R4, —S-alkyl, and —S-alkylenyl-R4; R6 is a radical selected from the group consisting of —CN, —COOH, —C(O)O-alkyl, —C(O)O-alkylenyl-R4, —C(O)-alkyl, —C(O)-alkylenyl-R4, —C(O)-halogen, —C(O)NH, —C(O)NH-alkyl, —C(O)NH-alkylenyl-R4; R7 is a radical selected from the group consisting of O, NH, and S; and R8 is N, O or S. R2 and R3 are each independently selected from the group consisting of alkyl and alkylenyl-R10, wherein R10 is selected from the group consisting of —OH, —OTs, halogen, spiperone, spiperone ketal and spiperone-3-yl. Alternatively, R2 and R3 together form a heterocyclic ring, optionally substituted with at least one radical selected from the group consisting of alkyl, alkoxy, OH, OTs, halogen, alkylenyl-R10, carbonyl, spiperone, spiperone ketal and spiperone-3-yl. In the compounds of formula (I), one or more of the hydrogen, halogen or carbon atoms can, optionally, be replaced with a radiolabel.
摘要翻译：一种用于在体内和体外标记β-淀粉样蛋白斑和神经原纤维缠结的方法，包括使式（I）化合物与哺乳动物组织接触。在式（I）中，R 1选自-C（O） - 烷基，-C（O） - 亚烷基基-R 4，-C（O）O-烷基，-C（O）O-亚烷基 - R4，-C = C（CN）2-烷基，-C = C（CN）2 - 亚烷基-R4，R4为选自烷基，取代烷基，芳基和取代芳基的基团; R5是选自-NH2，-OH，-SH，-NH-烷基，-NHR4，-NH-亚烷基-R4，-O-烷基，-O-亚烷基-R4，-S-烷基的基团和-S-亚烷基基-R4; R6是选自-CN，-COOH，-C（O）O-烷基，-C（O）O-亚烷基-R4，-C（O） - 烷基，-C（O） - 亚烷基-R4，-C（O） - 卤素，-C（O）NH，-C（O）NH-烷基，-C（O）NH-亚烷基基-R4; R7是选自O，NH和S的基团; 并且R 8是N，O或S.R 2和R 3各自独立地选自烷基和亚烷基-R 10，其中R 10选自-OH，-OT，卤素，螺哌
酮，螺哌酮缩酮和螺哌隆 -3-基。或者，R2和R3一起形成杂环，任选被至少一个选自烷基，烷氧基，OH，OT，卤素，亚烷基-R 10，羰基，螺哌
酮，螺哌酮缩酮和螺哌酮-3-基。在式（I）的化合物中，氢，卤素或碳原子中的一个或多个可以任选地被放射性标记代替。

5. 发明授权

US5459317A Method and apparatus for non-invasive detection of physiological chemicals, particularly glucose 失效
标题翻译：用于非侵入性检测生理化学品，特别是葡萄糖的方法和装置
公开(公告)号：US5459317A
公开(公告)日：1995-10-17
申请号：US195709
申请日：1994-02-14
申请人： Gary W. Small , Mark Arnold
发明人： Gary W. Small , Mark Arnold
IPC分类号： A61B5/00 , A61B5/145 , A61B5/1455 , G01J3/45 , G01N21/35 , G01J3/28
CPC分类号： G01J3/45 , A61B5/14532 , A61B5/1455 , A61B5/7257 , G01N21/35 , G01N21/359
摘要： Non-invasive measurements of physiological chemicals such as glucose are made using infrared radiation and a signal processing system that permits the construction of a device suited for home use. The level of a selected physiological chemical in a test subject is determined in a non-invasive and quantitative manner by a method comprising the steps of: (a) irradiating a portion of the test subject with near-infrared radiation such that the radiation is transmitted through or reflected from the test subject; (b) collecting data concerning the transmitted or reflected infrared radiation using a detector; (c) digitally filtering the collected data to isolate a portion of the data indicative of the physiological chemical; and (d) determining the amount of physiological chemical in the test subject by applying a defined mathematical model to the digitally filtered data. The data collected may be in the form of an absorbance spectrum, i.e., a representation of the variation in absorbance as a function of wavelength; or in the form of an interferogram, i.e., a representation of infrared light intensity as a function of the retardation of the moving mirror in the interferometer, and thus of time.
摘要翻译：使用红外辐射和信号处理系统制造生物化学品如葡萄糖的非侵入性测量，其允许构造适于家庭使用的装置。通过包括以下步骤的方法以非侵入性和定量的方式测定受检对象中所选择的生理化学物质的水平：（a）用近红外辐射照射被测物体的一部分，使得辐射被传输通过或反映在考试科目; （b）使用检测器收集关于发射或反射的红外辐射的数据; （c）对所收集的数据进行数字滤波以分离指示生理化学品的数据的一部分; 和（d）通过将定义的数学模型应用于数字滤波数据来确定测试对象中生理化学物质的量。收集的数据可以是吸收光谱的形式，即作为波长的函数的吸光度变化的表示; 或者以干涉图的形式，即作为干涉仪中的移动镜的延迟的函数的红外光强度的表示，以及因此的时间。

6. 发明授权

US6061582A Method and apparatus for non-invasive determination of physiological chemicals, particularly glucose 失效
标题翻译：用于非侵入性测定生理化学品，特别是葡萄糖的方法和装置
公开(公告)号：US6061582A
公开(公告)日：2000-05-09
申请号：US860850
申请日：1997-06-11
申请人： Gary W. Small , Mark Arnold
发明人： Gary W. Small , Mark Arnold
IPC分类号： A61B5/00 , A61B5/145 , A61B5/1455 , G01J3/45 , G01N21/35
CPC分类号： G01J3/45 , A61B5/14532 , A61B5/1455 , A61B5/7257 , G01N21/35 , G01N21/359
摘要： Non-invasive measurements of physiological chemicals such as glucose in a test subject are made using infrared radiation and a signal processing system. The level of a selected physiological chemical in the test subject is determined in a non-invasive and quantitative manner by a method comprising the steps of: (a) irradiating a portion of the test subject with near infrared radiation; (b) collecting data concerning the irradiated light on the test subject; (c) digitally filtering the collected data to isolate a portion of the data indicative of the physiological chemical; and (d) determining the amount of physiolgocial chemical in the test subject by applying a defined mathematical model to the digitally filtered data. The collected data is in the form of either an absorbance spectrum or an interferogram.
摘要翻译： PCT No.PCT / US95 / 01556 Sec。 371日期：1997年6月11日 102（e）日期1997年6月11日PCT提交1995年2月7日PCT公布。公开号WO95 / 22046 日期1995年8月17日使用红外辐射和信号处理系统对测试对象中生理化学物质（如葡萄糖）进行非侵入性测量。通过包括以下步骤的方法以非侵入性和定量的方式确定测试对象中所选择的生理化学品的水平：（a）用近红外辐射照射测试对象的一部分; （b）收集关于受试对象的照射光的数据; （c）对所收集的数据进行数字滤波以分离指示生理化学品的数据的一部分; 和（d）通过将定义的数学模型应用于数字滤波数据来确定测试对象中的生物化学物质的量。收集的数据是吸收光谱或干涉图的形式。

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