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1. 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。

2. 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。

3. 发明申请

US20120107175A1 MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM 有权
标题翻译：模块化放射化学合成系统
公开(公告)号：US20120107175A1
公开(公告)日：2012-05-03
申请号：US13058526
申请日：2009-08-19
申请人： Nagichettiar Satyamurthy , Jorge R. Barrio , Bernard Amarasekera , R. Michael Van Dam , Sebastian Olma , Dirk Williams , Mark A. Eddings , Clifton Kwang-Fu Shen
发明人： Nagichettiar Satyamurthy , Jorge R. Barrio , Bernard Amarasekera , R. Michael Van Dam , Sebastian Olma , Dirk Williams , Mark A. Eddings , Clifton Kwang-Fu Shen
IPC分类号： G01N31/00 , G05B1/00
CPC分类号： C07H19/16 , B01J19/004 , B01J19/126 , B01J2219/00049 , B01J2219/24 , C07B59/001 , C07B59/002 , C07B59/005 , C07B2200/05 , C07C201/06 , C07D207/46 , C07H5/02 , C07H19/06 , Y10T436/115831 , Y10T436/12
摘要： A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures. The modular chemical production system is assembled from modules which can each include operating condition sensors and controllers configured for monitoring and controlling the individual modules and the assembled system from a remote position. Other modules include, but are not limited to a Reagent Storage and Delivery Module, a Cartridge Purification Module, a Microwave Reaction Module, an External QC/Analysis/Purification Interface Module, an Aliquotting Module, an F-18 Drying Module, a Concentration Module, a Radiation Counting Module, and a Capillary Reactor Module.
摘要翻译：模块化化学生产系统包括从远程位置进行化学反应，特别是放射化学化合物的多个模块。一个实施例包括一个包括可移动热源的反应容器，其相对于反应容器的位置可从远程位置控制。或者，热源可以固定在位置，并且反应小瓶可移动进入和离开热源。反应容器具有一个或多个密封塞，其与反应容器相关的定位可从远程位置控制。此外，一个或多个反应容器密封塞可以包括一个或多个导管，用于输送反应物，大气压或高压气体，惰性气体，抽真空和从反应小瓶中除去反应终产物，具有密封塞位置的反应小瓶可在升高的压力下操作。模块化化学生产系统由模块组装，每个模块可以包括操作状态传感器和配置成用于从远程位置监控和控制各个模块和组装系统的控制器。其他模块包括但不限于试剂储存和输送模块，滤芯净化模块，微波反应模块，外部QC /分析/纯化界面模块，等分模块，F-18干燥模块，浓缩模块，辐射计数模块和毛细管反应堆模块。

4. 发明申请

US20110178302A1 NUCLEOPHILIC FLUORINATION OF AROMATIC COMPOUNDS 有权
标题翻译：芳香化合物的核化学荧光
公开(公告)号：US20110178302A1
公开(公告)日：2011-07-21
申请号：US13054458
申请日：2009-07-13
申请人： Nagichettiar Satyamurthy , Jorge R. Barrio
发明人： Nagichettiar Satyamurthy , Jorge R. Barrio
IPC分类号： C07D241/08 , C07C17/20 , C07C45/63 , C07C67/307 , C07C253/30 , C07C201/12 , C07D213/61 , C07D277/66 , C07D263/18 , C07C227/16 , C07D233/32
CPC分类号： C07B59/00 , C07C17/093 , C07C45/63 , C07C201/12 , C07C223/02 , C07C229/36 , C07C251/24 , C07C253/30 , C07C271/22 , C07D233/32 , C07D263/14 , C07D263/18 , C07D277/66 , C07C25/18 , C07C25/13 , C07C47/55 , C07C49/807 , C07C255/50 , C07C205/12
摘要： Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.
摘要翻译：在芳香环上使用由电子给体取代的取代基和吸电子基团作为芳族亲核取代反应的前体。碘基（IO2）被亲核氟化物区域性取代，以提供相应的氟代芳基衍生物。 F-18]（F / Kryptofix，[F-18] CsF或季铵氟化物（如Me4NF，Et4NF，n-Bu4NF，（PhCH2））的无载体添加[F-18] 4NF）仅代替这些衍生物中的碘基部分，并提供高比活性F-18标记的氟代芳基类似物。苯并噻唑类似物和6-碘代-L-多巴衍生物的碘代衍生物已被合成为前体，并已用于制备无载体添加的[F-18]氟代苯并噻唑以及6- [F-18]氟-L-多巴。

5. 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.

6. 发明授权

US06262254B1 8-fluoropurine compounds 有权
标题翻译： 8-氟嘌呤化合物
公开(公告)号：US06262254B1
公开(公告)日：2001-07-17
申请号：US09199975
申请日：1998-11-25
申请人： Jorge R. Barrio , Nagichettiar Satyamurthy , Mohammad Namavari , Michael E. Phelps
发明人： Jorge R. Barrio , Nagichettiar Satyamurthy , Mohammad Namavari , Michael E. Phelps
IPC分类号： C07H19167
CPC分类号： C07D473/00
摘要： An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred embodiment, a purine compound is dissolved in a polar solvent and reacted with a dilute mixture of F2 in He or other inert gas.
摘要翻译：提供了通过用稀释的元素氟或乙酰基次氟酸直接氟化嘌呤来合成8-氟嘌呤的有效的区域控制方法。在一个优选的实施方案中，将嘌呤化合物溶解在极性溶剂中并与F 2在He或其它惰性气体中的稀混合物反应。

7. 发明申请

US20120123120A1 No-Carrier-Added Nucleophilic [F-18] Fluorination of Aromatic Compounds 有权
标题翻译：无载体添加的亲核[F-18]芳香族化合物的氟化
公开(公告)号：US20120123120A1
公开(公告)日：2012-05-17
申请号：US13263333
申请日：2010-04-01
申请人： Nagichettiar Satyamurthy , Jorge R. Barrio
发明人： Nagichettiar Satyamurthy , Jorge R. Barrio
IPC分类号： C07D233/38 , C07C41/22 , C07C201/12 , C07D405/12 , C07C227/16 , C07D413/12 , C07D263/18 , C07C17/361 , C07D319/06
CPC分类号： C07D319/06 , C07B59/00 , C07B2200/05 , C07C201/12 , C07C227/16 , C07C229/36 , C07D233/32 , C07D241/08 , C07D263/18 , C07D405/12 , C07D413/12 , C07C205/11
摘要： Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.
摘要翻译：显示了用芳族亲核取代反应的前体作为芳族环上的给电子基团和吸电子基团取代的苯基碘鎓衍生物衍生物。碘鎓叶立德基团被诸如卤素离子的亲核试剂取代，得到相应的卤代芳基衍生物。无载体添加的[F-18]氟化物离子专门代替这些衍生物中的碘鎓内鎓盐部分，并提供高比活性F-18标记的氟衍生物。已经合成了保护的左旋多巴-6-碘鎓叶立德衍生物作为制备无载体添加的6- [F-18]氟-L-多巴的前体。该L-多巴胺衍生物中的碘鎓叶立德碱通过无载体添加的[F-18]氟离子被亲核取代，得到[F-18]氟中间体，其在酸水解时产生6- [F-18]氟 -L-多巴

8. 发明授权

US5393908A Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[.sup.18 F]fluoro-L-dopa 失效
标题翻译：合成N-甲酰基-3,4-二叔丁氧羰基氧基-6-（三甲基甲锡烷基）-L-苯丙氨酸乙酯及其对6- [18 F]氟-L-多巴的区域选择性放射性氟代脱氨基
公开(公告)号：US5393908A
公开(公告)日：1995-02-28
申请号：US903915
申请日：1992-06-25
申请人： Nagichettiar Satyamurthy , Jorge R. Barrio , Allyson J. Bishop , Mohammad Namavari
发明人： Nagichettiar Satyamurthy , Jorge R. Barrio , Allyson J. Bishop , Mohammad Namavari
IPC分类号： C07B59/00 , C07C227/16 , C07F7/22 , C07C229/00
CPC分类号： C07B59/001 , C07C227/16 , C07F7/2212
摘要： A protected 6-trimethylstannyl dopa derivative has been synthesized for the as a precursor for the preparation of 6-[.sup.18 F]fluoro-L-dopa. The tin derivative readily reacts with electrophilic radiofluorinating agents such as [.sup.18 F]F.sub.2, [.sup.18 F]OF.sub.2 and [.sup.18 F]AcOF. The [.sup.18 F]fluoro intermediate was easily hydrolyzed with HBr and the product 6-[.sup.18 F]fluoro-L-dopa was isolated after HPLC purification in a maximum radiochemical yield of 23%, ready for human use.
摘要翻译：受保护的6-三甲基甲锡巴衍生物已被合成为作为6- [18 F]氟-L-多巴的制备前体。锡衍生物容易与亲电子radiofluorinating剂如[18 F] F 2，[18 F] OF2和[18 F] ACOF反应。的[18 F]氟中间体很容易用HBr和产物水解6- [18 F]氟-L-多巴被HPLC纯化之后，分离在23％的最大放射化学产率，准备用于人体。

9. 发明授权

US08742139B2 No-carrier-added nucleophilic [F-18] fluorination of aromatic compounds 有权
标题翻译：芳香族化合物的无载体添加亲核[F-18]氟化
公开(公告)号：US08742139B2
公开(公告)日：2014-06-03
申请号：US13263333
申请日：2010-04-01
申请人： Nagichettiar Satyamurthy , Jorge R. Barrio
发明人： Nagichettiar Satyamurthy , Jorge R. Barrio
IPC分类号： C07D319/06
CPC分类号： C07D319/06 , C07B59/00 , C07B2200/05 , C07C201/12 , C07C227/16 , C07C229/36 , C07D233/32 , C07D241/08 , C07D263/18 , C07D405/12 , C07D413/12 , C07C205/11
摘要： Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.
摘要翻译：显示了用芳族亲核取代反应的前体作为芳族环上的给电子基团和吸电子基团取代的苯基碘鎓衍生物衍生物。碘鎓叶立德基团被诸如卤素离子的亲核试剂取代，得到相应的卤代芳基衍生物。无载体添加的[F-18]氟化物离子专门代替这些衍生物中的碘鎓内鎓盐部分，并提供高比活性F-18标记的氟衍生物。已经合成了保护的左旋多巴-6-碘鎓叶立德衍生物作为制备无载体添加的6- [F-18]氟-L-多巴的前体。该L-多巴胺衍生物中的碘鎓叶立德碱通过无载体添加的[F-18]氟离子被亲核取代，得到[F-18]氟中间体，其在酸水解时产生6- [F-18]氟 -L-多巴

10. 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。

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