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    • 1. 发明授权
    • Cephalosporins
    • 头孢菌素
    • US4436904A
    • 1984-03-13
    • US337380
    • 1982-01-06
    • Shigeo ShimizuHiroyuki TakanoShoji YoshimuraKinji Takada
    • Shigeo ShimizuHiroyuki TakanoShoji YoshimuraKinji Takada
    • C07D233/38C07D501/20C07D501/22C07D501/34C07D501/36C07D501/38C07D501/56
    • C07D233/38
    • Novel cephalosporin derivatives are described which have excellent antibiotic activity against pathogenic bacteria belonging to the Pseudomonas, Serratia and Enterobacter. The compounds have general formula ##STR1## in which R is hydrogen, acyloxy, carbamoyloxy, a substituted or unsubstituted pyridinium group or a group -S-Het in which Het represents a substituted or unsubstituted, hetero atom-containing, 5- or 6-membered heterocyclic ring, R' is hydrogen, alkali metal, an organic amine or an ester moiety, R.sub.1 and R.sub.2 are the same or different and are hydrogen or a lower alkyl and B stands for a 1,4-cyclohexadienyl group, a group ##STR2## in which Y is hydrogen, --OH or ##STR3## in which R.sub.5 is an alkyl of 1 to 5 carbon atoms, aryl or alkoxy having 1 to 4 carbon atoms, Z stands for hydrogen or halogen and p is an integer of 1 or 2, a furan group or a thiophene group. Methods of preparation are described.
    • 描述了对属于假单胞菌属,沙雷氏菌属和肠杆菌属的病原菌具有优异抗生素活性的新型头孢菌素衍生物。 所述化合物具有通式(I)其中R为氢,酰氧基,氨基甲酰氧基,取代或未取代的吡啶鎓基或-S-Het,其中Het表示取代或未取代的含杂原子的 5或6元杂环,R'是氢,碱金属,有机胺或酯部分,R 1和R 2相同或不同,为氢或低级烷基,B代表1,4- 环己二烯基,其中Y是氢的-OH基团,其中R 5是1到5个碳原子的烷基,R 1代表氢或卤素的芳基或烷氧基, p为1或2的整数,呋喃基或噻吩基。 描述制备方法。
    • 2. 发明授权
    • Cephalosporin derivatives
    • 头孢菌素衍生物
    • US4987129A
    • 1991-01-22
    • US222404
    • 1988-07-21
    • Shigeo ShimizuHiroyuki Takano
    • Shigeo ShimizuHiroyuki Takano
    • A63B69/02A61K31/545C07D487/04C07D519/00
    • C07D519/00Y02P20/55
    • There are disclosed a .beta.-lactam compound represented by the formula (I): ##STR1## wherein R.sub.1 represents an acyl group; M represents a hydrogen atom, a protective group or an eliminatable group which is easily hydrolyzable in a human body; B represents a group represented by the formula (b): ##STR2## where at least one of R.sub.2, R.sub.3 and R.sub.9 represent a group represented by the formula: --A--OR.sub.4 where R.sub.4 represents a hydrogen or a lower alkyl group; and A represents a straight or branched alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group or an eliminatable group which is easily hydrolyzable in a human body, and also when R.sub.9 is --A--OR.sub.4, and R.sub.3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; and Z represents a nitrogen atom or a group represented by the formula: C--R.sub.10 where R.sub.10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group,or its pharmaceutically acceptable salt, and a process for preparing the same, an intermediate for synthesis of the same and a medicinal composition for bacterially infectious disease therapy containing the same.
    • 公开了由式(I)表示的β-内酰胺化合物:其中R 1表示酰基; M表示氢原子,可在人体中容易水解的保护基或可消除基团; B表示由式(b)表示的基团:其中R 2,R 3和R 9中的至少一个表示由下式表示的基团:-A-OR 4,其中R 4表示氢或低级烷基; A表示碳原子数1〜6的直链或支链亚烷基。 剩余的基团各自独立地为氢原子; 氰基; 可被卤素原子取代的低级烷基; 可被低级烷基取代的氨基甲酰基; 环烷基; 或可以被保护基团取代的羧基或可在人体中容易水解的可消除基团,当R 9为-A-OR 4时,R 2和R 3可以相互结合形成亚烷基, 3至4个碳原子; Z表示氮原子或由式C-R 10表示的基团,其中R 10表示氢原子,可以被羟基或低级烷氧基取代的羧基或低级烷基,或其药学上可接受的 盐及其制备方法,其合成中间体和含有该盐的细菌感染性疾病治疗用药物组合物。
    • 3. 发明授权
    • Intermediates for synthesis of cephalosporin compounds
    • 用于合成头孢菌素化合物的中间体
    • US4958019A
    • 1990-09-18
    • US357172
    • 1989-05-26
    • Shigeo ShimizuHiroyuki Takano
    • Shigeo ShimizuHiroyuki Takano
    • A63B69/02A61K31/545C07D487/04C07D519/00
    • C07D519/00Y02P20/55
    • There are disclosed a .beta.-lactam compound represented by the formula (I): ##STR1## wherein R.sub.1 represents an acyl group; M represents a hydrogen atom, a protective group or an eliminatable group which is easily hydrolyzable in a human body; B represents a group represented by the formula (b): ##STR2## where at least one of R.sub.2, R.sub.3 and R.sub.9 represent a group represented by the formula: --A--OR.sub.4 where R.sub.4 represents a hydrogen or a lower alkyl group; and A represents a straight or branced alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group or an eliminatable group which is easily hydrolyzable in a human body, and also when R.sub.9 is --A--OR.sub.4, R.sub.2 and R.sub.3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; and Z represents a nitrogen atom or a group represented by the formula: C--R.sub.10 where R.sub.10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group,or its pharmaceutically acceptable salt, and a process for preparing the same, an intermediate for synthesis of the same and a medicinal composition for bacterially infectious disease therapy containing the same.
    • 公开了由式(I)表示的β-内酰胺化合物:其中R 1表示酰基; M表示氢原子,可在人体中容易水解的保护基或可消除基团; B表示由式(b)表示的基团:其中R 2,R 3和R 9中的至少一个表示由下式表示的基团:-A-OR 4,其中R 4表示氢或低级烷基; A表示碳原子数1〜6的直链或支链亚烷基。 剩余的基团各自独立地为氢原子; 氰基; 可被卤素原子取代的低级烷基; 可被低级烷基取代的氨基甲酰基; 环烷基; 或可以被保护基团取代的羧基或可在人体中容易水解的可消除基团,当R 9为-A-OR 4时,R 2和R 3可以相互结合形成亚烷基, 3至4个碳原子; Z表示氮原子或由式C-R 10表示的基团,其中R 10表示氢原子,可以被羟基或低级烷氧基取代的羧基或低级烷基,或其药学上可接受的 盐及其制备方法,其合成中间体和含有该盐的细菌感染性疾病治疗用药物组合物。
    • 4. 发明授权
    • “三唑并嘧啶中间体”
    • US4956462A
    • 1990-09-11
    • US357124
    • 1989-05-26
    • Shigeo ShimizuHiroyuki Takano
    • Shigeo ShimizuHiroyuki Takano
    • A63B69/02A61K31/545C07D487/04C07D519/00
    • C07D519/00Y02P20/55
    • There are disclosed a .beta.-lactam compound represented by the formula (I): ##STR1## wherein R.sub.1 represents an acyl group; M represents a hydrogen atom, a protective group of an eliminatable group which is easily hydrolyzable in a human body; B represents a group represented by the formula (b): ##STR2## where at least one of R.sub.2, R.sub.3 and R.sub.9 represent a group represented by the formula: -A-OR.sub.4 where R.sub.4 represents a hydrogen or a lower alkyl group; and A represents a straight or branched alkylene group having 1 to 6 carbon atoms; and a remaining group or groups are each independently a hydrogen atom; a cyano group; a lower alkyl group which may be substituted by a halogen atom; a carbamoyl group which may be substituted by a lower alkyl group; a cycloalkyl group; or a carboxyl group which may be substituted by a protective group of an eliminatable group which is easily hydrolyzable in a human body, and also when R.sub.9 is -A-OR.sub.4, R.sub.2 and R.sub.3 may be combined with each other to form an alkylene group having 3 to 4 carbon atoms; and Z represents a nitrogen atom or a group represented by the formula: C-R.sub.10 where R.sub.10 represents a hydrogen atom, a carboxyl group or a lower alkyl group which may be substituted by a hydroxy group or a lower alkoxy group,or its pharmaceutically acceptable salt, and a process for preparing the same, an intermediate for synthesis of the same and a medicinal composition for bacterially infectious disease therapy containing the same.
    • 公开了由式(I)表示的β-内酰胺化合物:其中R 1表示酰基; M表示氢原子,可在人体中容易水解的保护基或可消除基团; B表示由式(b)表示的基团:其中R 2,R 3和R 9中的至少一个表示由下式表示的基团:-A-OR 4,其中R 4表示氢或低级烷基; A表示碳原子数1〜6的直链或支链亚烷基。 剩余的基团各自独立地为氢原子; 氰基; 可被卤素原子取代的低级烷基; 可被低级烷基取代的氨基甲酰基; 环烷基; 或可以被保护基团取代的羧基或可在人体中容易水解的可消除基团,当R 9为-A-OR 4时,R 2和R 3可以相互结合形成亚烷基, 3至4个碳原子; Z表示氮原子或由式C-R 10表示的基团,其中R 10表示氢原子,可以被羟基或低级烷氧基取代的羧基或低级烷基,或其药学上可接受的 盐及其制备方法,其合成中间体和含有该盐的细菌感染性疾病治疗用药物组合物。
    • 5. 发明授权
    • Cephalosporin .beta.-lactam compound and medicinal composition
    • 头孢菌素β-内酰胺化合物和药物组合物
    • US4966900A
    • 1990-10-30
    • US75412
    • 1987-07-20
    • Shigeo ShimizuHiroyuki Takano
    • Shigeo ShimizuHiroyuki Takano
    • C07B20060101C07D20060101C07D277/38C07D501/34C07D519/00
    • C07D501/34C07D519/00Y02P20/55
    • There are disclosed a .beta.-lactam compound represented by the formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are independently a hydrogen atom or a lower alkyl group; M is a hydrogen atom, a protective group or an eliminatable group which is easily hydrolyzable in a human body; R' and R" are independently a hydrogen atom or a protective group; A is a mercapto group substituted by a substituted or unsubstituted polycyclic nitrogen-containing heterocyclic ring or a group represented by the following formula (a):--OOCNR.sub.3 R.sub.4 (a)where R.sub.3 and R.sub.4 are independently a hydrogen atom or a lower alkyl group, provided that R.sub.1 and R.sub.2 are both hydrogen atoms, both R.sub.3 and R.sub.4 being hydrogen atoms are excluded,or its pharmaceutically acceptable salt, and a method for preparing the same , medicinal composition for microbism therapy containing the same and intermediates for synthesis of the same.
    • 公开了由式(I)表示的β-内酰胺化合物:其中R 1和R 2独立地为氢原子或低级烷基; M是氢原子,在人体中容易水解的保护基或可消除基团; R'和R“独立地为氢原子或保护基; A是被取代或未取代的多环含氮杂环或由下式(a)表示的基团取代的巯基:其中R 3和R 4独立地为氢原子或低级烷基,取代的-OOCNR 3 R 4(a) R1和R2都是氢原子,R3和R4都是氢原子,不包括其中的药学上可接受的盐,及其制备方法,含有它们的微生物治疗用药物组合物和用于合成其的中间体。
    • 6. 发明授权
    • Cephalosporin derivatives
    • 头孢菌素衍生物
    • US4808711A
    • 1989-02-28
    • US819831
    • 1986-01-17
    • Shigeo ShimizuHiroyuki TakanoFujio Yagihashi
    • Shigeo ShimizuHiroyuki TakanoFujio Yagihashi
    • C07D501/20A61K31/43A61K31/545A61K31/546A61P31/04C07D277/20C07D499/00C07D499/64C07D499/70C07D501/24C07D501/34C07D501/36C07D501/46
    • C07D277/20C07D277/587C07D499/00Y02P20/55
    • There is disclosed a novel .beta.-lactam antibiotics represented by the formula: ##STR1## wherein A is a group represented by the formulae -NHCO--, --NHCONHCO--, --NHCOCH.dbd.CH-- or ##STR2## where R.sub.6 is a hydrogen atom or a lower alkyl group; R.sub.1 and R.sub.2 are independently a hydrogen atom or a protective group; R.sub.3 is a hydrogen atom or a methoxy group; X is a hydrogen atom, a hydroxyl group, a protected hydroxyl group, a halogen atom, a lower alkoxy group or a nitro group; n is an integer of 1 or 2; Y is a group represented by the formulae: ##STR3## provided that a carbon atom which is bonded by a carboxyl group being bonded to nitrogen atom; M is a hydrogen atom, a protective group or an easily hydrolyzable group in a human body; R.sub.7 is a hydrogen atom, a methyl group a lower alkoxy-methyl group or a group represented by the formula: --CH.sub.2 --T where T is an acyloxy group, a carbamoyloxy group, a quaternary ammonium, a substituted or unsubstituted heterocyclic ring or a formula: --S--R.sub.8 where R.sub.8 is an acyl group or a substituted or unsubstituted heterocyclic ring, R.sub.4 and R.sub.5 are each hydrogen atoms or combined with each other to form additional direct bond; Z is a direct bond or a carbonyl group when R.sub.4 and R.sub.5 are hydrogen atoms, or a formula: --O--B-- where the oxygen atom is bonded to nitrogen atom and B is a straight, branched or cyclic alkylene group when R.sub.4 and R.sub.5 are combined with each other to form additional direct bond, or its pharmaceutically acceptable salt.
    • 公开了一种新的β-内酰胺抗生素,其由下式表示:其中A是由式-NHCO-,-NHCONHCO-,-NHCOCH = CH-或者IMAGE表示的基团,其中R 6是 氢原子或低级烷基; R1和R2独立地为氢原子或保护基; R3是氢原子或甲氧基; X是氢原子,羟基,被保护的羟基,卤素原子,低级烷氧基或硝基; n为1或2的整数; Y是由下式表示的基团:,条件是通过与氮原子键合的羧基键合的碳原子; M是人体中的氢原子,保护基或易水解基团; R7是氢原子,甲基,低级烷氧基 - 甲基或由式-CH2-T表示的基团,其中T是酰氧基,氨基甲酰氧基,季铵,取代或未取代的杂环或 式-S-R8其中R8是酰基或取代或未取代的杂环,R4和R5各自为氢原子或彼此结合以形成额外的直接键; 当R4和R5是氢原子时,Z是直接键或羰基,或当R 4和R 5结合时,氧原子与氮原子连接并且B是直链,支链或环状亚烷基的式:-OB- 彼此形成另外的直接键合,或其药学上可接受的盐。
    • 7. 发明申请
    • THREE-PLATE TYPE OF LIQUID CRYSTAL PROJECTOR USING PROJECTION DISPLAY APPARATUS
    • 使用投影显示装置的三层液晶投影机
    • US20110032436A1
    • 2011-02-10
    • US12907318
    • 2010-10-19
    • Shigeo ShimizuTatsuya Mukouyama
    • Shigeo ShimizuTatsuya Mukouyama
    • G02F1/1335
    • G02F1/1393G02F1/133536G02F1/133553G02F2001/133531H04N9/3167
    • A projection display apparatus comprises a reflective LC display device and a polarizing beam splitter having a polarizing separative plane and wired grids. The LC molecules of the device are aligned such that i) a segment on a second subtracted, produced by projecting a major axis of each LC molecule perpendicularly onto the second substrate, makes an angle of 42 to 48 degrees counterclockwise or counterclockwise in relation to a direction of a straight line on the second substrate, formed by projecting each wire grid perpendicularly onto the second substrate and ii) of both ends of the segment, one end meeting an end of each LC molecule, which is positioned nearer to the second substrate than the other end, is positioned nearer to an intersection at which a plane including the polarizing separative plane and a plane including the second substrate mutually intersects, than the other end of the segment.
    • 投影显示装置包括反射LC显示装置和具有极化分离面和有线网格的偏振分束器。 将器件的LC分子对准,使得i)通过将每个LC分子的长轴垂直地投影到第二衬底上而产生的第二次减法部分,相对于第二衬底逆时针或逆时针的角度为42至48度 通过将每个线栅垂直地投影到第二基板上形成的直线的方向,以及ii)段的两端,一端满足每个LC分子的端部,其位于比第二基板更靠近第二基板的位置 另一端位于更靠近包括偏振分离面的平面和包括第二基板的平面彼此相交的交点处,比该段的另一端更靠近。
    • 8. 发明授权
    • Rolling machine element
    • 滚动机元件
    • US07645072B2
    • 2010-01-12
    • US11569032
    • 2004-05-12
    • Shigeo Shimizu
    • Shigeo Shimizu
    • F16C29/04
    • F16C29/0604F16C29/04F16C29/06F16C29/0609F16C33/585
    • The rolling machine element includes a first member in which a raceway surface is formed and a second member on which the first member is mounted through the rolling elements and which is formed to be able to guide the first member in a specified direction. The rolling machine element is characterized in that the first member can be moved in the guiding direction of the second member by allowing the rolling elements to move in an out of the raceway surface in an orderly arranged state, and the crowning based on the oval shape is formed at the end part of the raceway surface of the first member where an access point for the rolling elements is formed.
    • 滚动机构包括:第一构件,其中形成有滚道面;第二构件,第一构件通过滚动元件安装在该第二构件上,并且形成为能够沿指定方向引导第一构件。 滚动机构的特征在于,通过允许滚动元件以有序布置的状态在滚道表面内移动,第一构件可以在第二构件的引导方向上移动,并且基于椭圆形状的隆起 形成在形成有滚动体的接触点的第一部件的滚道面的端部。
    • 9. 发明授权
    • Method for driving an image displaying apparatus
    • 驱动图像显示装置的方法
    • US07429968B2
    • 2008-09-30
    • US11038429
    • 2005-01-21
    • Hideki AibaYutaka OchiShigeo Shimizu
    • Hideki AibaYutaka OchiShigeo Shimizu
    • G09G5/00G09G3/28
    • G09G3/204G09G3/2029G09G3/28G09G2320/0247G09G2320/0261G09G2320/0266
    • The present invention provides a technique of a method for driving an image displaying apparatus to suppress animated picture pseudo-contour, flicker disturbance and pseudo-contour disturbance by making weighting of light emission within a field is made equal to or almost equal to each other at all gradations. According to this technique, when an image signal of multiple gradation is expressed by dividing one field duration into a plurality of subfields with different relative ratios of luminance, a given number of subfields among a plurality of subfields are divided into “2n” subfields (SF1a to SF8b) wherein “n” represents an arbitrary integral number. Then, “2n” subfield groups (SF1a to SF8a, SF1b to SF8b) are formed so that one group divided into “2n” subfield belong to the groups different from each other. Subfield groups (A and B) are symmetrically arranged with respect to the center of one field duration, and the subfields (SFna, SFnb) divided into “2n” subfields are symmetrically arranged.
    • 本发明提供了一种用于驱动图像显示装置的方法的技术,该图像显示装置通过使场内的发光加权使彼此等于或几乎相等来抑制动画图像伪轮廓,闪烁干扰和伪轮廓干扰 所有等级。 根据该技术,当通过将一个场持续时间分成具有不同相对比率的多个子场来表示多个灰度的图像信号时,将多个子场中的给定数量的子场划分为“2n”个子场(SF 1 a至SF 8 b)其中“n”表示任意整数。 然后,形成“2n”个子场组(SF1a〜SF8a,SF1b〜SF8b),使得分成“2n”个子场的一组属于彼此不同的组。 子场组(A和B)相对于一个场持续时间的中心对称排列,并且被划分为“2n”个子场的子场(SFn,SFnb)被对称排列。