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1. 发明授权

US08741943B2 Bicyclic compound, production and use thereof 有权
标题翻译：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
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： C07D403/02 , A61K31/4178
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： 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.
摘要翻译：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。

2. 发明申请

US20060178359A1 Tricyclic compound, process for producing the same, and use 审中-公开
标题翻译：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
申请人： Mitsuru Shiraishi , Masaki Seto , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
发明人： Mitsuru Shiraishi , Masaki Seto , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
IPC分类号： A61K31/55 , A61K31/4745 , C07D487/14
CPC分类号： C07D471/04 , A61K31/4353 , A61K31/55
摘要： 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.
摘要翻译：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。

3. 发明申请

US20050154016A1 Preventives for hiv infection 审中-公开
标题翻译：预防HIV感染
公开(公告)号：US20050154016A1
公开(公告)日：2005-07-14
申请号：US10511531
申请日：2003-04-17
申请人： Katsunori Takashima , Yuji Iizawa , Mitsuru Shiraishi , Yoshihiro Sugihara , Masanori Baba
发明人： Katsunori Takashima , Yuji Iizawa , Mitsuru Shiraishi , Yoshihiro Sugihara , Masanori Baba
IPC分类号： A61K31/445 , A61K31/452 , A61K31/454 , A61K31/4545 , A61K31/55 , A61P31/18 , A61P37/04
CPC分类号： A61K31/445 , A61K31/452 , A61K31/454 , A61K31/4545 , A61K31/55
摘要： It is intended to provide a novel drug which exhibits an excellent effect of preventing HIV infection in transfusing blood and using a blood preparation. This object can be achieved by a preventive for HIV infection in transfusing blood and using a blood prepartion characterized by containing a compound having an antagonism to a CC chemokine receptor (preferably antagonism to CCR5 and/or CCR2).
摘要翻译：旨在提供一种在输血和使用血液制剂中具有优异的预防HIV感染效果的新型药物。该目的可以通过预防HIV感染来预防输血，并使用血液制剂，其特征在于含有对CC趋化因子受体具有拮抗作用的化合物（优选对CCR5和/或CCR2的拮抗作用）。

4. 发明授权

US06627651B1 Cyclic compounds and uses thereof 失效
标题翻译：环状化合物及其用途
公开(公告)号：US06627651B1
公开(公告)日：2003-09-30
申请号：US09980773
申请日：2001-11-02
申请人： Mitsuru Shiraishi , Masanori Baba , Masaki Seto , Naoyuki Kanzaki , Osamu Nishimura
发明人： Mitsuru Shiraishi , Masanori Baba , Masaki Seto , Naoyuki Kanzaki , Osamu Nishimura
IPC分类号： A61K3138
CPC分类号： C07D405/12 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/44 , A61K31/4709 , A61K31/4725 , A61K31/661 , C07D217/06 , C07D309/08 , C07D313/08 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07F9/65517
摘要： Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1 is an optionally substituted five- or six-membered ring group; X1 is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1 and E4 are each optionally substituted carbon or the like; E2 and E3 are each oxygen or the like; and a and b are each a single bond or a double bond); X2 is a divalent group constituting a straight chain moiety; Z1 is a divalent cyclic group or the like; Z2 is a free valency or the like; and R2 is optionally substituted amino or the like.
摘要翻译：通式（1）的化合物或其盐，表现出对HIV感染性疾病的预防和治疗作用，其中R 1为任选取代的五元或六元环基团; X 1是自由价或类似物; W是由e表示的二价基团。例如通式（2）（其中A和B各自为任选取代的五至七元环; E1和E4各自为任选取代的碳等; E2和E3各自为氧等; 和b各自为单键或双键）; X 2是构成直链部分的二价基团; Z 1是二价的环状基团等; Z 2是自由价或类似物; 和R 2是任选取代的氨基等。

5. 发明授权

US06172061B2 Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative 失效
公开(公告)号：US06172061B2
公开(公告)日：2001-01-09
申请号：US09213377
申请日：1998-12-17
申请人： Osamu Nishimura , Masanori Baba , Hidekazu Sawada , Naoyuki Kanzaki , Ken-ichi Kuroshima , Mitsuru Shiraishi , Yoshio Aramaki
发明人： Osamu Nishimura , Masanori Baba , Hidekazu Sawada , Naoyuki Kanzaki , Ken-ichi Kuroshima , Mitsuru Shiraishi , Yoshio Aramaki
IPC分类号： A62K31351
CPC分类号： C07D407/12 , A61K31/335 , A61K31/351 , A61K31/452 , A61K31/4523 , A61K31/5377 , A61K31/665 , A61K31/67 , A61K45/06 , C07C233/62 , C07C2602/12 , C07D309/14 , C07D313/08 , C07D337/08
摘要： This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof.

6. 发明授权

US5420363A Optically active phenol derivatives and preparation thereof 失效
标题翻译：光学活性酚衍生物及其制备方法
公开(公告)号：US5420363A
公开(公告)日：1995-05-30
申请号：US266494
申请日：1994-06-27
申请人： Mitsuru Shiraishi , Shoji Fukumoto
发明人： Mitsuru Shiraishi , Shoji Fukumoto
IPC分类号： C07C39/15 , C07C59/56 , C07C59/74 , C07C59/88 , C07C69/007 , C07C69/732 , C07C69/734 , C07C69/738 , C07C39/12 , C07C37/11 , C07C39/14
CPC分类号： C07C59/88 , C07C39/15 , C07C59/56 , C07C59/74 , C07C69/007 , C07C69/732 , C07C69/734 , C07C69/738 , C07B2200/07
摘要： 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.
摘要翻译：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。

7. 发明授权

US5354913A Optically active phenol derivatives and preparation thereof 失效
标题翻译：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
申请人： Mitsuru Shiraishi , Shoji Fukumoto
发明人： Mitsuru Shiraishi , Shoji Fukumoto
IPC分类号： C07C39/15 , C07C59/56 , C07C59/74 , C07C59/88 , C07C69/007 , C07C69/732 , C07C69/734 , C07C69/738 , C07C39/10 , C07C39/08
CPC分类号： C07C59/88 , C07C39/15 , C07C59/56 , C07C59/74 , C07C69/007 , C07C69/732 , C07C69/734 , C07C69/738 , C07B2200/07
摘要： 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.
摘要翻译：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。

8. 发明授权

US5156053A Measuring system using a robot 失效
标题翻译：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
申请人： Mitsuru Shiraishi , Hideo Kato
发明人： Mitsuru Shiraishi , Hideo Kato
IPC分类号： G01N3/02 , G01N3/06 , G01N3/08 , G01N3/20
CPC分类号： G01N3/20 , G01N3/08 , G01N2203/0218 , G01N2203/0682
摘要： 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.
摘要翻译： 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。

9. 发明授权

US4517361A Cephalosporin derivatives 失效
标题翻译：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
申请人： Mitsuo Numata , Isao Minamida , Masayoshi Yamaoka , Mitsuru Shiraishi , Toshio Miyawaki
发明人： Mitsuo Numata , Isao Minamida , Masayoshi Yamaoka , Mitsuru Shiraishi , Toshio Miyawaki
IPC分类号： C07D277/34 , C07D277/36 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/28
CPC分类号： C07D501/24 , C07D277/34 , C07D277/36
摘要： 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.
摘要翻译：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。

10. 发明授权

US4421912A Cephalosporin derivatives 失效
公开(公告)号：US4421912A
公开(公告)日：1983-12-20
申请号：US235609
申请日：1981-02-18
申请人： Mitsuo Numata , Isao Mimamida , Masayoshi Yamaoka , Mitsuru Shiraishi , Toshio Miyawaki
发明人： Mitsuo Numata , Isao Mimamida , Masayoshi Yamaoka , Mitsuru Shiraishi , Toshio Miyawaki
IPC分类号： C07D277/34 , C07D277/36 , C07D501/24 , C07D501/34 , C07D501/36
CPC分类号： C07D501/24 , C07D277/34 , C07D277/36
摘要： 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.

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