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1.发明授权Indole derivatives having cPLA2 inhibiting activity and applications and production methods of the same 失效具有cPLA2抑制活性的吲哚衍生物及其应用及其制备方法公开(公告)号：US08293781B2
公开(公告)日：2012-10-23
申请号：US12532738
申请日：2008-03-28
IPC分类号： A61K31/402 , C07D209/04
CPC分类号： C07D209/08 , C07D209/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12
摘要： A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.
摘要翻译： 具有式（I）的具有cPLA2抑制活性的化合物或其盐或其溶剂化物：或药物组合物cPLA2抑制剂和含有与活性成分相同的各种脂质介体生产抑制剂。
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2.发明申请INDOLE DERIVATIVES HAVING cPLA2 INHIBITING ACTIVITY AND APPLICATIONS AND PRODUCTION METHODS OF THE SAME 失效具有cPLA2抑制活性和应用的吲哚衍生物及其生产方法公开(公告)号：US20100113777A1
公开(公告)日：2010-05-06
申请号：US12532738
申请日：2008-03-28
IPC分类号： C07D209/08 , C07D209/12 , C07D403/12 , C07D403/06 , C07D401/04 , C07D405/12 , C07D405/10 , C07D413/10
CPC分类号： C07D209/08 , C07D209/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12
摘要： A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.
摘要翻译： 具有式（I）的具有cPLA2抑制活性的化合物或其盐或其溶剂化物：或药物组合物cPLA2抑制剂和含有与活性成分相同的各种脂质介体生产抑制剂。
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公开(公告)号：US06867297B1
公开(公告)日：2005-03-15
申请号：US09178594
申请日：1998-10-26
IPC分类号： C07D205/08
CPC分类号： C07D205/08
摘要： An azetidinone derivative represented by the general formula (1) (wherein OR1 is a protected hydroxyl group; R2 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group or a substituted or unsubstituted aromatic group) is reacted with an ester compound represented by the formula (2) (wherein CO2R3 is an esterified carboxyl group; X and Y are the same or different and represent individually a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted alkyloxy group, a substituted or unsubstituted alkenyloxy group, a substituted or unsubstituted aralkyloxy group, a substituted or unsubstituted aryloxy group, a substituted or unsubstituted silyloxy group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic-thio group, a substituted or unsubstituted heterocyclic-oxy group, a substituted or unsubstituted acyl group, a substituted or unsubstituted ester group, a substituted or unsubstituted thio ester group, a substituted or unsubstituted amide group, a substituted or unsubstituted amino group, a hydrogen atom or halogen atom, or are taken together with each other to form a substituted or unsubstituted cycloalkan-2-on-1-yl group) in the presence of zinc and copper compounds to synthesis a 4-substituted azetidinone derivative represented by the formula (3) (wherein OR1, CO2R3, X and Y are as defined above).
摘要翻译： 由通式（1）表示的氮杂环丁酮衍生物（其中OR 1为保护的羟基; R2为取代或未取代的烷基，取代或未取代的烯基或取代或未取代的芳族基团）与表示的酯化合物 通式（2）（其中CO 2 R 3是酯化的羧基; X和Y相同或不同，分别代表取代或未取代的烷基，取代或未取代的烯基，取代或未取代的芳烷基，取代或未取代的芳烷基， 未取代的芳基，取代或未取代的烷硫基，取代或未取代的链烯硫基，取代或未取代的芳烷硫基，取代或未取代的芳硫基，取代或未取代的烷氧基，取代或未取代的烯氧基，取代或未取代的 芳烷氧基，取代或未取代的芳氧基，取代基 取代或未取代的杂环基，取代或未取代的杂环硫基，取代或未取代的杂环氧基，取代或未取代的酰基，取代或未取代的酯基，取代或未取代的硫代 酯基，取代或未取代的酰胺基，取代或未取代的氨基，氢原子或卤素原子，或彼此一起形成取代或未取代的环烷烃-2-基-1-基） 存在锌和铜化合物以合成由式（3）表示的4-取代的氮杂环丁酮衍生物（其中OR1，CO2R3，X和Y如上定义）。
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公开(公告)号：US5506225A
公开(公告)日：1996-04-09
申请号：US971828
申请日：1993-02-19
IPC分类号： A61K31/43 , A61K31/431 , A61P31/04 , C07D499/88 , C07D499/897 , C07D499/00
CPC分类号： C07D499/88
摘要： Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a physiological-hydrolyzable, ester-forming group. The physiologically hydrolyzable, ester-forming group useful in the penem compound of the present invention means a group which can be removed easily by in vivo hydrolysis, such as an acetyloxymethyl, 1-(acetyloxy)ethyl, pivaloyloxymethyl, 1-(ethoxycarbonyloxy)ethyl, 1-(isopropyloxycarbonyloxy)ethyl, 1-(cyclohexyloxycarbonyloxy)ethyl or 3-phthalidyl group. Antibiotic compositions for oral administration are also described.
摘要翻译： PCT No.PCT / JP91 / 01099 Sec。 371日期：1993年2月19日 102（e）日期1993年2月19日PCT 1991年8月16日PCT PCT。 出版物WO92 / 03443 日期：1992年3月5日。抗生素penem化合物由下式表示：其中R表示生理水解性酯形成基团。 可用于本发明青霉烯化合物的生理上可水解的酯形成基是指通过体内水解容易除去的基团，例如乙酰氧基甲基，1-（乙酰氧基）乙基，新戊酰氧基甲基，1-（乙氧基羰基氧基）乙基 ，1-（异丙氧基羰基氧基）乙基，1-（环己氧基羰基氧基）乙基或3-苯二酰基。 还描述了用于口服给药的抗生素组合物。
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公开(公告)号：US06570355B2
公开(公告)日：2003-05-27
申请号：US09822483
申请日：2001-04-02
IPC分类号： B25J1906
CPC分类号： B25J9/1674 , G05B9/02 , G05B2219/40217
摘要： An object of the present invention is to provide a control apparatus for a robot in which the work efficiency is improved in the whole robot peripheral system including the robot, and in which considering the increase in the consciousness of safety such as the standardization of safety apparatuses, both the reliability of the safety circuit of the control apparatus for a robot and the ensuring of the safety are improved. By connecting, to peripheral devices outside the robot, each intermediate output signal line for extracting the operation signal or the emergency stop signal of each of the plurality of switches each assigned to a factor causing the stop of the robot, a factor to cause the stop of the robot body alone can be distinguished from a factor to cause the stop of both the robot body and the peripheral devices.
摘要翻译： 本发明的目的是提供一种机器人的控制装置，其中在包括机器人的整个机器人外围系统中提高了工作效率，并且考虑到诸如安全装置的标准化等安全意识的增加 机器人控制装置的安全电路的可靠性和安全性的确保都得到改善。通过将机器人外部的外围设备连接到用于提取操作信号或紧急停止信号的中间输出信号线 多个开关中的每一个分配给导致机器人停止的因素，可以将导致机器人主体单独停止的因素与导致机器人主体和外围设备的停止的因素区分开。
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公开(公告)号：US4997829A
公开(公告)日：1991-03-05
申请号：US496145
申请日：1990-03-09
IPC分类号： C07D499/897 , A61K31/425 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/06 , C07D499/88
CPC分类号： C07D499/88 , Y02P20/55
摘要： A penem compound represented by the general formula: ##STR1## (wherein R denotes hydrogen or allyl group, A denotes oxygen atom or methylene group and B denotes methylene, ethylene or carbonyl group) or a pharmacologically acceptable salt is produced through several processes.The compound exhibits stronger activities against wide variety of gram-positive and gram-negative bacteria as compared with known penem compounds.
摘要翻译： 通过几个方法制备由以下通式表示的青霉烯化合物：其中R表示氢或烯丙基，A表示氧原子或亚甲基，B表示亚甲基，亚乙基或羰基）或药理学上可接受的盐。 与已知的penem化合物相比，该化合物对各种革兰氏阳性和革兰氏阴性细菌表现出更强的活性。
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公开(公告)号：US20050004092A1
公开(公告)日：2005-01-06
申请号：US10831694
申请日：2004-04-26
IPC分类号： C07D499/74 , C07D499/88 , A61K31/43
CPC分类号： C07D499/88 , Y02P20/55
摘要： A penem derivative represented by the following formula (I): wherein R1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof. The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA. It is therefore useful not only as a general antibacterial agent but also as an antibacterial agent for MRSA against which no general antibacterial agents are recognized to be-effective.
摘要翻译： 由下式（I）表示的pen嗪衍生物：其中R1表示取代或未取代的烷基，取代或未取代的烯基，取代或未取代的芳烷基，取代或未取代的芳基，取代或未取代的烷硫基， 取代或未取代的链烯硫基，取代或未取代的芳烷硫基，取代或未取代的芳硫基，取代或未取代的杂环基，取代或未取代的杂环硫基，取代或未取代的酰硫基，巯基或氢原子 R 2表示氢原子或羧基保护基; 或其药理学上可接受的盐。 化合物（I）表现出强烈的抗菌活性，特别是对MRSA具有较强的活性。 因此，不仅可以作为一般的抗菌剂，而且作为MRSA的抗菌剂也是有用的，其中没有一般的抗菌剂被认为是有效的。
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公开(公告)号：US6084374A
公开(公告)日：2000-07-04
申请号：US159624
申请日：1998-09-24
IPC分类号： G05B13/02 , B25J9/10 , G05B20060101 , G05B19/19 , G05B19/416 , G05D3/12
CPC分类号： G05B19/416 , B25J9/1638 , G05B2219/41151 , G05B2219/43099
摘要： The controller comprises (a) an interpolation calculator for dividing move data of a robot arm tip position into each sample period, the data fed from a position teaching section, (b) a load inertia calculator, (c) a gravity torque calculator, (d) acceleration and deceleration (A & D) time calculator for calculating an optimum A & D time by using the load inertia calculated by the load inertia calculator and the gravity torque calculated by the gravity torque calculator, (e) an A & D processor for providing an A & D process to move data of each sample time calculated by the interpolation calculator based on the A & D time calculated by the A & D time calculator, and (f) position controllers for controlling each motor based on the move data processed by the A & D processor. The A & D time is calculated with the following equation:T=.alpha..multidot.(J.sub.m +J.sub.L)/(T.sub.m -T.sub.L).multidot.Vwhere: V=desirable speed, J.sub.m =motor inertia, J.sub.L =load inertia, T.sub.m =motor torque, T.sub.L =disturbance torque including gravity torque, .alpha.=proportional coefficient and T=A & D time. The robot having the above construction can figure out an optimum A & D time by considering change of load inertia and also that of gravity torque produced by a posture change of the robot, whereby A & D time can be varied. As a result, the robot can be operated at a higher speed.
摘要翻译： 控制器包括：（a）插入计算器，用于将机器人臂尖位置的移动数据分割成每个采样周期，从位置示教部分馈送的数据，（b）负载惯量计算器，（c）重力矩计算器， d）加速和减速（A＆D）时间计算器，用于通过使用由负载惯量计算器计算的负载惯量和由重力矩计算器计算的重力矩来计算最佳A＆D时间，（e）A＆D处理器 用于提供A＆D处理以基于由A＆D时间计算器计算的A＆D时间来计算由插值计算器计算的每个采样时间的数据，以及（f）基于移动数据控制每个电动机的位置控制器 由A＆D处理器处理。 A＆D时间用以下公式计算：T =αx（Jm + JL）/（Tm-TL）xV其中：V =期望速度，Jm =电机惯量，JL =负载惯量，Tm =电机转矩，TL =干扰转矩，包括重力矩，α=比例系数，T = A＆D时间。 具有上述结构的机器人可以通过考虑负载惯量的变化以及由机器人的姿势变化产生的重力矩的变化来确定最佳的A＆D时间，从而可以改变A＆D时间。 结果，机器人可以以更高的速度运行。
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9.发明授权1'S, 5R, 6R-carbapenem derivatives and antimicrobial agents comprising the same 失效1'S，5R，6R-碳青霉烯衍生物和包含其的抗微生物剂
公开(公告)号：US6051569A
公开(公告)日：2000-04-18
申请号：US911937
申请日：1997-08-15
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/08 , C07D477/20
CPC分类号： C07D477/08 , C07D477/20 , Y02P20/55
摘要： A carbapenem derivative represented by the following formula (I), ##STR1## wherein R.sub.1 represents a hydrogen atom, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, R.sub.2 indicates a hydrogen atom or a protective group for a carboxyl group, and R.sub.3 is a methyl group or an ethyl group; or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising this carbapenem derivative or a salt thereof as an active ingredient. The carbapenem derivative exhibits a wide and strong antimicrobial activity, particularly a strong antimicrobial activity against MRSA. An intermediate compound for preparing the carbapenem derivative is also disclosed.
摘要翻译： 由下式（I）表示的碳青霉烯衍生物，其中R1表示氢原子，取代或未取代的芳基或取代或未取代的杂环基，R2表示氢原子或羧基保护基，R3 是甲基或乙基; 或其药学上可接受的盐，以及包含该碳青霉烯衍生物或其盐作为活性成分的药物组合物。 碳青霉烯衍生物具有广泛而强的抗微生物活性，特别是抗MRSA的强抗微生物活性。 还公开了用于制备碳青霉烯衍生物的中间体化合物。
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公开(公告)号：US4985575A
公开(公告)日：1991-01-15
申请号：US475801
申请日：1990-02-06
申请人： Masaji Ishiguro , Hiromitsu Iwata , Takashi Nakatsuka , Kiyoharu Nakayama , Osamu Miyahara , Kenichi Noguchi
发明人： Masaji Ishiguro , Hiromitsu Iwata , Takashi Nakatsuka , Kiyoharu Nakayama , Osamu Miyahara , Kenichi Noguchi
IPC分类号： C07B57/00 , C07D307/24
CPC分类号： C07D307/24
摘要： A process for preparing an optically active tetrahydro-2-furoic acid is disclosed. The process comprises (i) reacting (.+-.)-tetrahydro-2-furoic acid with an optically active amine resolver of the following formula (I): ##STR1## wherein R.sub.1 is a lower alkyl group and R.sub.2 represents an alkyl group or ar aryl group, provided that R.sub.1 and R.sub.2 are different from each other, thus producing an optically active diastereomer salt, and (ii) decomposing the diastereomer salt. According to the process, a high purity, optically active tetrahydro-2-furoic acid can be prepared at a high yield using an amine resolver. The amine resolver can be recovered at a high yield and high purity.
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