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公开(公告)号：US5202318A
公开(公告)日：1993-04-13
申请号：US708260
申请日：1991-05-28
IPC分类号： C07D401/04 , C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08
CPC分类号： C07D401/04 , C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08 , Y10S514/872
摘要： Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.3 is independently selected from hydrogen, hydroxy, alkyl and alkoxy;each R.sup.4 is independently hydrogen or alkyl; andR.sup.5 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, alkenyl, alkynyl or a group R.sup.7 -C.sub.1-3 alkyl in which R.sup.7 is phenyl or phenoxy optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
摘要翻译： 式I化合物：其中Z为CH 2或C = O; X和Y独立地选自氢，卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二（低级烷基）氨基和（低级烷酰基）氨基; （a），（b），（c）（d）和（e）所示的基团：（a） （e）其中p为0或1; n为1,2或3; R 2是氢，低级烷基，C 3-8环烷基，C 3-8环烷基-C 12烷基或其中R 6是噻吩基的R6-C 1-2烷基，任选地被一个或两个选自下列的取代基取代的吡咯基或呋喃基：低级烷基， 低级烷氧基，三氟甲基或卤素，或者是被一个或两个选自C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基和任选进一步被羟基，C 1-4烷氧基取代的C 1-4烷基取代的苯基 ，羧基，酯化羧基或体内可水解酰氧基; 每个R 3独立地选自氢，羟基，烷基和烷氧基; 每个R 4独立地是氢或烷基; R 5是氢，低级烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基，链烯基，炔基或其中R 7是任选被一个或两个取代基所取代的苯基或苯氧基的基团 由C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基和任选进一步被羟基，C 1-4烷氧基，羧基，酯化羧基或体内可水解酰氧基进一步取代的C 1-4烷基; 和其药学上可接受的盐，各异构体，异构体的混合物，制备方法，组合物及其使用方法。
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公开(公告)号：US5202333A
公开(公告)日：1993-04-13
申请号：US704565
申请日：1991-05-22
IPC分类号： C07D487/08 , A61K31/47 , A61K31/55 , A61P1/00 , A61P1/08 , A61P1/14 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D205/12 , C07D209/52 , C07D221/22 , C07D401/04 , C07D403/04 , C07D451/02 , C07D451/04 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/06 , C07D471/08
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/06 , C07D471/08 , Y10S514/872
摘要： The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
摘要翻译： 本发明涉及式I的5-HT 3受体拮抗剂化合物：其中虚线表示任选的双键; n为1,2或3; p为0,1,2或3; q是0,1或2; 每个R 1独立地选自卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二（低级烷基）氨基和（低级烷酰基）氨基; 每个R 2是低级烷基; （a），（b），（c）和（d）所示的基团：其中，（a），（c） 你是0或1; z为1,2或3; 和R 4是C 1-7烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基或基团（CH 2）t R 5，其中t是1或2，R 5是噻吩基，吡咯基或呋喃基， 选自C 1-6烷基，C 1-6烷氧基，三氟甲基或卤素的一个或两个取代基，或被任选被一个或两个选自C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基的取代基取代的苯基和 任选被羟基，C 1-4烷氧基，羧基，酯化羧基或体内可水解酰氧基取代的C 1-4烷基; 和其药学上可接受的盐，各异构体，异构体的混合物，制备方法，组合物及其使用方法。
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公开(公告)号：US5192770A
公开(公告)日：1993-03-09
申请号：US624028
申请日：1990-12-07
申请人： Robin D. Clark , Richard M. Eglen , Joseph M. Muchowski , William L. Smith , Klaus K. Weinhardt
发明人： Robin D. Clark , Richard M. Eglen , Joseph M. Muchowski , William L. Smith , Klaus K. Weinhardt
IPC分类号： A61K31/435 , A61K31/46 , A61P1/00 , A61P1/08 , A61P9/00 , A61P25/00 , A61P25/04 , C07D451/04 , C07D451/08 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08
CPC分类号： C07D451/04 , C07D451/14 , C07D453/02 , C07D471/08 , C07D487/08
摘要： .alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
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公开(公告)号：US07479377B2
公开(公告)日：2009-01-20
申请号：US10229747
申请日：2002-08-27
申请人： Sharon Zhao , Inna Vainshtein , Richard M. Eglen
发明人： Sharon Zhao , Inna Vainshtein , Richard M. Eglen
CPC分类号： C40B30/04 , C07K2319/60 , C07K2319/80 , C12N15/62 , C12Q1/34 , G01N33/5005 , G01N33/542 , G01N33/6845 , G01N2333/924 , G01N2500/20 , G01N2800/52
摘要： A system is provided an enzyme donor (“ED”) fused a surrogate of a mammalian protein of interest, where the fusion protein has the function of the natural protein. A vector is provided comprising a regulatory region functional in a mammalian host cell, a sequence encoding the ED joined to a multiple cloning site, an enzyme acceptor (“EA”) protein or enzyme acceptor sequence encoding such protein, and substrate for the enzyme formed by ED and EA.
摘要翻译： 提供一种系统，其融合了目标哺乳动物蛋白质的替代物，其中融合蛋白具有天然蛋白质的功能的酶供体（“ED”）。 提供载体，其包含哺乳动物宿主细胞中功能的调节区，编码与多克隆位点连接的ED的序列，编码该蛋白的酶受体（“EA”）蛋白或酶受体序列，以及形成的酶的底物 由ED和EA。
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公开(公告)号：US07410755B2
公开(公告)日：2008-08-12
申请号：US11357325
申请日：2006-02-17
CPC分类号： C12Q1/42
摘要： Methods and compositions are provided for determining ADP in the presence of ATP. These comprise including among the assay reagents at least one of the correcting components creatine phosphokinase and phosphocreatine, pyruvate kinase and phosphoenolpyruvate, peroxidase and a non-interfering peroxidase substrate, and catalase. One aspect of the method employs formation of hydrogen peroxide from the ADP by pyruvate kinase, phosphoenolpyruvate and pyruvate oxidase. The hydrogen peroxide is then determined. A combined reagent having all of the reagents may optionally include a peroxidase when the hydrogen peroxide is to be enzymatically determined. A peroxidase substrate is added to the sample in conjunction with the peroxidase substrate reagent, the mixture incubated and depending on whether the peroxidase substrate is a fluorescer or chemiluminescer, the mixture may be illuminated with excitation light and the emitted light determined as a measure of the ADP in the sample.
摘要翻译： 提供了在ATP存在下测定ADP的方法和组合物。 这些包括测定试剂中的至少一种校正组分肌酸磷酸激酶和磷酸肌酸，丙酮酸激酶和磷酸烯醇丙酮酸，过氧化物酶和非干扰性过氧化物酶底物，以及过氧化氢酶。 该方法的一个方面是通过丙酮酸激酶，磷酸烯醇丙酮酸和丙酮酸氧化酶从ADP形成过氧化氢。 然后测定过氧化氢。 当要酶法测定过氧化氢时，具有所有试剂的组合试剂可以任选地包括过氧化物酶。 将过氧化物酶底物与过氧化物酶底物试剂一起加入到样品中，混合物孵育，并且取决于过氧化物酶底物是荧光剂还是化学发光剂，可以用激发光照射混合物，并且将测定的发射光作为 ADP在样品中。
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公开(公告)号：US07608415B2
公开(公告)日：2009-10-27
申请号：US11170123
申请日：2005-06-29
申请人： Joseph Horecka , Peter Fung , Richard M. Eglen
发明人： Joseph Horecka , Peter Fung , Richard M. Eglen
CPC分类号： G01N33/6803 , C12Q1/24 , G01N33/5002 , G01N33/5008 , G01N33/502 , G01N33/5023 , G01N33/542 , G01N33/573 , G01N33/6872 , G01N2333/924
摘要： Improved methods of determining the intracellular state of a protein as well as modifications of the protein are provided by introducing a surrogate fusion protein comprising a member of an enzyme fragment complementation complex and a target protein. After exposing cells transformed with the surrogate fusion protein to a change in environment, e.g. a candidate drug, the cells are lysed, the lysate separated into fractions or bands, conveniently by gel electrophoresis and transferring the proteins by Western blot to a membrane. The bands on the membrane are developed using the other member of the enzyme fragment complementation complex and a substrate providing a detectable signal. The method is found to provide high sensitivity and the ability to observe modifications of the target protein.
摘要翻译： 通过引入包含酶片段互补复合物和靶蛋白的成员的替代融合蛋白来提供确定蛋白质的细胞内状态和蛋白质修饰的改进方法。 将用替代融合蛋白转化的细胞暴露于环境变化之后，例如， 候选药物，细胞被裂解，裂解物分离成部分或条带，方便地通过凝胶电泳并通过蛋白质印迹将蛋白转移到膜上。 使用酶片段互补复合体的其他成员和提供可检测信号的底物来开发膜上的条带。 发现该方法提供高灵敏度和观察靶蛋白修饰的能力。
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