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    Bicyclic compound, production and use thereof
    1.
    发明授权
    Bicyclic compound, production and use thereof 有权
    双环化合物，其生产和使用

    公开(公告)号：US08741943B2

    公开(公告)日：2014-06-03

    申请号：US13476454

    申请日：2012-05-21

    Applicant: Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Iizawa

    Inventor： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Iizawa

    IPC: C07D403/02 ,  A61K31/4178

    CPC classification number: A61K31/4196 ,  A61K31/395 ,  A61K31/4178 ,  C07D225/06 ,  C07D313/20 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12

    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

    Abstract translation: 本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。 本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

    Tricyclic compound, process for producing the same, and use
    2.
    发明申请
    Tricyclic compound, process for producing the same, and use 审中-公开
    三环化合物，其制备方法和用途

    公开(公告)号：US20060178359A1

    公开(公告)日：2006-08-10

    申请号：US10544470

    申请日：2004-02-05

    Applicant: Mitsuru Shiraishi ,  Masaki Seto ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    Inventor： Mitsuru Shiraishi ,  Masaki Seto ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    IPC: A61K31/55 ,  A61K31/4745 ,  C07D487/14

    CPC classification number: C07D471/04 ,  A61K31/4353 ,  A61K31/55

    Abstract: A compound of the formula: wherein R1 is a 5- or 6-membered ring; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain; W is a group represented by wherein R3 and R3′ are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n′ are each an integer of 0 or 1 to 4; m and m′ are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide; or a salt thereof. The compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.

    Abstract translation: 下式的化合物：其中R 1是5或6元环; Z 1是5或6元芳环; Z 2是基团-Z 2 O 2 -W 2 -Z 2b 2，其中Z 2a 和/或O 2各自为O，S（O）q q（其中q为0,1或2），亚氨基或键; 和W 2是亚烷基链; W是由R 3和R 3'表示的基团各自为氢原子，低级烷基或低级烷氧基; X是CH或N; n和n'各自为0或1〜4的整数; m和m'分别为1或2; Y是O，S（O）p（其中p是0,1或2），CH 2或NR 4（其中R' SUP> 4 是氢原子，低级烷基或低级酰基）; R 2是（1）可以将氮原子转化为季铵或氧化物的氨基，或者（2）可含有硫原子的含氮杂环基 或氧原子作为构成环的原子，其中氮原子可以转化为季铵或氧化物; 或其盐。 该化合物对CCR5表现出优异的CCR拮抗剂活性，并且可用作人外周血单核细胞（特别是AIDS）中HIV感染的预防和/或治疗剂。

    Optically active phenol derivatives and preparation thereof
    7.
    发明授权
    Optically active phenol derivatives and preparation thereof 失效
    光学活性酚衍生物及其制备方法

    公开(公告)号：US5354913A

    公开(公告)日：1994-10-11

    申请号：US85166

    申请日：1993-07-02

    Applicant: Mitsuru Shiraishi ,  Shoji Fukumoto

    Inventor： Mitsuru Shiraishi ,  Shoji Fukumoto

    IPC: C07C39/15 ,  C07C59/56 ,  C07C59/74 ,  C07C59/88 ,  C07C69/007 ,  C07C69/732 ,  C07C69/734 ,  C07C69/738 ,  C07C39/10 ,  C07C39/08

    CPC classification number: C07C59/88 ,  C07C39/15 ,  C07C59/56 ,  C07C59/74 ,  C07C69/007 ,  C07C69/732 ,  C07C69/734 ,  C07C69/738 ,  C07B2200/07

    Abstract: An optically active tri-substituted methane compound having, as substituents, an aromatic ring group and a phenyl group having hydroxyl group at ortho or para position can be obtained by allowing a phenol compound unsubstituted at the ortho- or/and para-position to react with an optically active secondary carbinol compound having an aromatic ring group at the alpha-position in the presence of tri-substituted phosphine and diazodicarboxylate or diazodicarboxamide. These and other optically active tri-substituted methane compounds are useful as active ingredients for medicines or as intermediate compounds for preparing medicines.

    Abstract translation: 通过使在邻位或/或对位未取代的酚化合物反应，可以得到在邻位或对位具有芳环基和具有羟基的苯基作为取代基的光学活性三取代甲烷化合物 在三取代的膦和重氮二羧酸酯或重氮二甲酰胺的存在下，在α-位上具有芳环基的光学活性的仲甲醇化合物。 这些和其它光学活性三取代的甲烷化合物可用作药物的活性成分或用作制备药物的中间体化合物。

    Measuring system using a robot
    8.
    发明授权
    Measuring system using a robot 失效
    使用机器人的测量系统

    公开(公告)号：US5156053A

    公开(公告)日：1992-10-20

    申请号：US656060

    申请日：1991-02-19

    Applicant: Mitsuru Shiraishi ,  Hideo Kato

    Inventor： Mitsuru Shiraishi ,  Hideo Kato

    IPC: G01N3/02 ,  G01N3/06 ,  G01N3/08 ,  G01N3/20

    CPC classification number: G01N3/20 ,  G01N3/08 ,  G01N2203/0218 ,  G01N2203/0682

    Abstract: A robot measuring system automatically measures a mechanical characteristics of an object to be measured. The system includes a pressing robot for adding a predetermined pressing force to the object to be measured. An inner force sensor is mounted to one end of the pressing robot and detects strength of the pressing force through a pressing rod. A displacement gauge touches the object and detects a mechanical distortion caused in the object by the pressing force, a sensing robot supports the displacement gauge and moves the displacement gauge to a measuring position. A microprocessor inputs a detection result of the inner force sensor, controls a motion of the pressing robot based on the detection result, and calculates various mechanical characteristics based on a detection result input from the displacement gauge. A memory stores the various mechanical characteristics calculated from the microprocessor. Calculation of the mechanical characteristics of the plastic article is performed by the microprocessor by using a spline smoothing method.

    Abstract translation: PCT No.PCT / JP90 / 00800 Sec。 371日期1991年2月19日 102（e）1991年2月19日PCT申请1990年6月19日PCT公布。 公开号WO90 / 15982 日期1990年12月27日。机器人测量系统自动测量待测物体的机械特性。 该系统包括用于向待测量对象添加预定按压力的按压机器人。 内力传感器安装在按压机器人的一端，并通过按压杆检测按压力的强度。 位移计接触物体，通过按压力检测物体中引起的机械变形，感测机器人支撑位移计并将位移计移动到测量位置。 微处理器输入内力传感器的检测结果，根据检测结果控制按压机器人的运动，并根据从位移计输入的检测结果计算各种机械特性。 存储器存储从微处理器计算的各种机械特性。 通过使用花键平滑法由微处理器执行塑料制品的机械特性的计算。

    Cephalosporin derivatives
    9.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4517361A

    公开(公告)日：1985-05-14

    申请号：US480791

    申请日：1983-03-31

    Applicant: Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

    Inventor： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

    IPC: C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/28

    CPC classification number: C07D501/24 ,  C07D277/34 ,  C07D277/36

    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula -NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula -SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

    Abstract translation: 下式的化合物：其中R 1表示氢或烷基，X表示氧或硫或式-NR 2基团（其中R 2是氢或烷基，在烷基的情况下可以形成 环与R 1连接），Y表示乙酰氧基或式-SR 3（其中R 3为含氮杂环基）基团或其药学上可接受的盐具有宽的抗菌谱，特别是， 对革兰氏阴性菌有效，包括大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，变形杆菌，以及革兰氏阳性菌。 因此，这些化合物可用于治疗目的的抗微生物剂。

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