公开(公告)号：US4709082A

公开(公告)日：1987-11-24

申请号：US789640

申请日：1985-10-21

申请人： Yasuhiro Takahashi ,  Kazutaka Arai ,  Yoshio Ohara ,  Hiroo Matsumoto ,  Syuuzi Tsuchiya

发明人： Yasuhiro Takahashi ,  Kazutaka Arai ,  Yoshio Ohara ,  Hiroo Matsumoto ,  Syuuzi Tsuchiya

IPC分类号： C07C51/487 ,  C07C201/16 ,  C07C205/43 ,  C07C69/76

CPC分类号： C07C201/12 ,  C07C201/16 ,  C07C51/487 ,  C07C67/14 ,  C07C67/52 ,  C07C69/612 ,  C07B2200/07

摘要： 2-Phenylpropoionic acid ester of Formula (I): ##STR1## wherein R represents p-nitrophenyl group, .beta.-naphthyl group or 2-(.beta.-naphthyl)ethyl group.Optical resolution of the above is carried out by preferential crystallization by seeding either one of the optical isomers into a super-saturated solution of a racemic modification thereof or a mixture of the optical isomers thereof. The efficiency of the optical resolution can be increased by optional addition of a recemizing agent comprising a strongly basic amine or an alcholate.

摘要翻译： 式（I）的2-苯基丙酸酯：其中R表示对硝基苯基，β-萘基或2-（β-萘基）乙基。 上述的光学拆分通过优选结晶通过将任一种光学异构体接种到其外消旋变体的超饱和溶液或其旋光异构体的混合物中进行。 通过任选地加入包含强碱性胺或醇酸盐的接收剂可以提高光学拆分的效率。

公开(公告)号：US06407298B1

公开(公告)日：2002-06-18

申请号：US09830555

申请日：2001-05-04

申请人： Hiroo Matsumoto ,  Minako Kamikawaji ,  Takashi Horiuchi

发明人： Hiroo Matsumoto ,  Minako Kamikawaji ,  Takashi Horiuchi

IPC分类号： C07C1716

CPC分类号： C07C17/16 ,  C07C29/14 ,  C07C45/512 ,  C07C25/02 ,  C07C47/24 ,  C07C33/46

摘要： A process for the preparation of an alcohol compound (1), characterized by subjecting p-iodochlorobenzene to Pd coupling with allyl alcohol in the presence of tetramethylammonium chloride, followed by reduction, and a process for the preparation of a compound (2), characterized by brominating the alcohol compound (1) obtainable by said process:

摘要翻译： 一种制备醇化合物（1）的方法，其特征在于在氯化四甲基铵存在下使对氯代苯与烯丙醇进行Pd偶联，然后还原，以及制备化合物（2）的方法，其特征在于 通过溴化由所述方法获得的醇化合物（1）：

公开(公告)号：US5079357A

公开(公告)日：1992-01-07

申请号：US449391

申请日：1989-12-07

申请人： Makoto Sato ,  Makoto Takemura ,  Kunio Higashi ,  Tsunehiko Soga ,  Hiroo Matsumoto ,  Toshiyuki Nishi

发明人： Makoto Sato ,  Makoto Takemura ,  Kunio Higashi ,  Tsunehiko Soga ,  Hiroo Matsumoto ,  Toshiyuki Nishi

IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D499/88 ,  C07D513/04 ,  C07D519/00 ,  C07D519/06

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D499/88 ,  C07D513/04 ,  Y02P20/55

摘要： New derivatives of penem and pharmacutically acceptable salt thereof are herein disclosed; these compounds being useful as an antibacterial agent which has an extremely wide antibacterial spectrum, exhibits a high sensitivity to bacteria resistant to conventional penicillins and cephalosporin antibiotics and is excellent in its physico-chemical stability, solubility to water and biological stability, in particular, stability to decomposition by enzyme such as dehydropeptidase I in kidney, .beta.-lactamase; these derivatives of penem being able to be prepared by reacting 2-substituted sulfinyl derivative of penem with a thiol compound and then optionally removing protective group(s) and further alkylating the reaction product or vice versa.

公开(公告)号：US4879400A

公开(公告)日：1989-11-07

申请号：US145042

申请日：1988-01-19

申请人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Ryozo Sakoda

发明人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Ryozo Sakoda

IPC分类号： C07F9/40 ,  C07F9/6571

CPC分类号： C07F9/657181 ,  C07F9/4015

摘要： A process for producing an .alpha.-(benzylidene)acetonylphosphonate of the formula: ##STR1## wherein Ar is phenyl substituted by at least one substituent selected from the group consisting of fluorine, chlorine, bromine, nitro, chloromethyl, dichloromethyl, trichloromethyl, trifluoromethyl, --CO.sub.2 R.sup.7 wherein R.sup.7 is C.sub.1 -C.sub.5 alkyl, --CONR.sup.7 R.sup.8 wherein R.sup.7 is as defined above and R.sup.8 is C.sub.1 -C.sub.5 alkyl, --C(O)R.sup.7 wherein R.sup.7 is as defined above, --OC(O)R.sup.7 wherein R.sup.7 is as defined above, --OSO.sub.3 R.sup.7 wherein R.sup.7 is as defined above, --OCF.sub.3, --S(.dbd.O).sub.2 R.sup.7 wherein R.sup.7 is as defined above, --CN and --SO.sub.3 R.sup.7 wherein R.sup.7 is as defined above, and each of R.sup.1 and R.sup.2 which may be the same or different is a saturated or unsaturated C.sub.1 -C.sub.12 aliphatic group, or R.sup.1 and R.sup.2 together form 1,2-ethylene, 1,3-propylene or 1,4-butylene, which is unsubstituted or substituted by from one to four C.sub.1 -C.sub.3 alkyl groups, which comprises:(a) reacting an aldehyde of the formula:ArCHO (I)wherein Ar is as defined above, with an acetonylphosphonate of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, in the presence of a secondary amine of the formula: ##STR3## wherein each of R.sup.3 and R.sup.4 which may be the same or different is C.sub.1 -C.sub.4 alkyl, or R.sub.3 and R.sub.4 together form 1,4-butylene or 1,5-pentylene, which is unsubstituted or substituted by from one to four C.sub.1 -C.sub.2 alkyl groups, --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 --, and an .alpha.-halogeno fatty acid of the formula: ##STR4## wherein X is fluorine, chlorine, bromine or iodine, and each of R.sup.5 and R.sup.6 which may be the same or different is hydrogen, fluorine, chlorine, bromine, iodine or C.sub.1 -C.sub.4 alkyl; or(b) reacting a compound of the formula ##STR5## wherein Ar, R.sup.1 and R.sup.2 are as defined above, with an acetonylphosphonate of the formula II as defined above, in the presence of an .alpha.-halogeno fatty acid of the formula V as defined above.

公开(公告)号：US20100105636A1

公开(公告)日：2010-04-29

申请号：US12651849

申请日：2010-01-04

申请人： Taiji FURUKAWA ,  Osamu Yamada ,  Hiroo Matsumoto ,  Toru Yamashita ,  Yukinori Masuda

发明人： Taiji FURUKAWA ,  Osamu Yamada ,  Hiroo Matsumoto ,  Toru Yamashita ,  Yukinori Masuda

IPC分类号： A61K31/675 ,  A61K31/551 ,  A61K31/4545

CPC分类号： A61K31/675

摘要： There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof: wherein Ar1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO2R2; Ra and Rb are independently of each other C1-6alkyl group, ANR8R9, CH2OANR8R9, or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R1 is C1-6alkyl group, ANR8R9, AN(CH2CH2)2NR8, AN(CH2CH2)2O, AOR8 or benzyl group; R3 is hydrogen atom, C1-20alkyl group, ANR8R9, a group of formula or the like.

摘要翻译： 提供了式（1）化合物，其药学上可接受的盐或其溶剂化物的T型钙通道阻断剂：其中Ar1是苯基，吡啶基，呋喃基或2,1,3-苯并恶二唑-2-基， 4-基; 含氮杂环部分为1,4-二氢吡啶环或吡啶环; Z是式（2）或CO 2 R 2的基团; R a和R b彼此独立地为C 1-6烷基，ANR 8 R 9，CH 2 OANR 8 R 9等; 在含氮杂环部分为1,4-二氢吡啶环的情况下，R 1为C 1-6烷基，ANR 8 R 9，AN（CH 2 CH 2）2 NR 8，AN（CH 2 CH 2）2 O，AOR 8或苄基; R3是氢原子，C1-20烷基，ANR8R9，式等基团。

公开(公告)号：US20070129335A1

公开(公告)日：2007-06-07

申请号：US10580532

申请日：2004-11-25

申请人： Taiji Furukawa ,  Osamu Yamada ,  Hiroo Matsumoto ,  Toru Yamashita ,  Yukinori Masuda

发明人： Taiji Furukawa ,  Osamu Yamada ,  Hiroo Matsumoto ,  Toru Yamashita ,  Yukinori Masuda

IPC分类号： A61K31/675 ,  A61K31/551 ,  A61K31/496 ,  A61K31/455 ,  A61K31/4439 ,  C07D403/02

CPC分类号： A61K31/675

摘要： There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof. wherein Ar1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO2R2; Ra and Rb are independently of each other C1-6alkyl group, ANR8R9, CH2OANR8R9, or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R1 is C1-6alkyl group, ANR8R9, AN(CH2CH2)2NR8, AN(CH2CH2)2O, AOR8 or benzyl group; R3 is hydrogen atom, C1-20alkyl group, ANR8R9, a group of formula or the like.

摘要翻译： 提供了一种T型钙通道阻断剂，其是式（1）的化合物，其药学上可接受的盐或其溶剂化物。 其中Ar 1是苯基，吡啶基，呋喃基或2,1,3-苯并二唑-4-基; 含氮杂环部分为1,4-二氢吡啶环或吡啶环; Z是式（2）或CO 2 R 2的基团; R a a和R b彼此独立地是C 1-6烷基，ANR 8 R 12 > 9 ，CH 2，OANR 8，9，9等等; 在含氮杂环部分为1,4-二氢吡啶环的情况下，R 1为C 1-6烷基，ANR 8 O AN（CH 2 CH 2 CH 2）2 NR 8，其中R 1，R 2， AN（CH 2 CH 2）2 O，AOR 8或苄基; R 3是氢原子，C 1-20烷基，ANR 8 R 9，式 或类似物。

公开(公告)号：US20060041031A1

公开(公告)日：2006-02-23

申请号：US10531458

申请日：2003-09-26

申请人： Osamu Yamada ,  Hiroo Matsumoto ,  Takanori Shimizu

发明人： Osamu Yamada ,  Hiroo Matsumoto ,  Takanori Shimizu

IPC分类号： C07C201/12

CPC分类号： C07C201/12 ,  C07C205/37

摘要： There is provided a process for producing an acetylene compound useful as an intermediate of pharmaceuticals, from 4-nitrofluorobenzene, in industrially and economically advantageous manner. Concretely, it is a method for producing an acetylene compound of formula (3) characterized by reacting 4-nitrofluorobenzene of formula (1) with an alkoxide of 2-methyl-3-butyn-2-ol of formula (2) at −20 to 10° C.

摘要翻译： 提供了从工业上和经济上有利的方式制备可用作4-硝基氟苯的药物中间体的乙炔化合物的方法。 具体地说，它是制备式（3）的炔属化合物的方法，其特征在于使式（1）的4​​-硝基氟苯与式（2）的2-甲基-3-丁炔-2-醇的醇盐在-20℃ 至10℃

公开(公告)号：US5361030A

公开(公告)日：1994-11-01

申请号：US928987

申请日：1992-08-12

申请人： Shigeyuki Akiyama ,  Hiroo Matsumoto

发明人： Shigeyuki Akiyama ,  Hiroo Matsumoto

IPC分类号： G01D5/20 ,  G01N27/02 ,  G01N27/28

CPC分类号： G01D5/204 ,  G01N27/023

摘要： An improved detector assembly of an electro-magnetic conduction-type conductivity meter includes a plastic housing member having a liquid sample flow path extending therethrough. An excitation transformer is mounted in a cavity of the housing member along with the detection transformer for respectively inducing a current flow and detecting a current flow in the liquid sample flow path. A porous electrode is positioned adjacent one of the transformers and insulated by hydrophilic paper so that the entrance of any fluid within the cavity can be detected.

摘要翻译： 电磁导电型电导率仪的改进的检测器组件包括具有延伸穿过其中的液体样品流动路径的塑料外壳构件。 励磁变压器与检测变压器一起安装在壳体构件的空腔中，用于分别引起电流并检测液体样品流动路径中的电流。 多孔电极位于一个变压器附近，并通过亲水纸绝缘，以便可以检测腔内任何流体的入口。

公开(公告)号：US5319089A

公开(公告)日：1994-06-07

申请号：US780357

申请日：1991-10-22

申请人： Hiroo Matsumoto ,  Kiyotomo Seto ,  Ryozo Sakoda

发明人： Hiroo Matsumoto ,  Kiyotomo Seto ,  Ryozo Sakoda

IPC分类号： C07D498/04

CPC分类号： C07D498/04

摘要： A process for the optical resolution of a pyranobenzoxadiazole compound represented by the formula [(.+-.)I]: ##STR1## which comprises reacting the compound [(.+-.)I] with an optically active carboxylic acid represented by the formula [II]: ##STR2## and separating the diastereomeric salt thus formed is disclosed.

摘要翻译： 用于光学拆分由式[（+/-）I]表示的吡喃并苯并恶二唑化合物的方法：包括使化合物[（+/-）I]与光学 公开了由式[II]表示的活性羧酸：＆lt; IMAGE＆gt;并分离如此形成的非对映体盐。

公开(公告)号：US4843076A

公开(公告)日：1989-06-27

申请号：US77220

申请日：1987-07-24

申请人： Kiyotomo Seto ,  Ryozo Sakoda ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Sakuya Tanaka

发明人： Kiyotomo Seto ,  Ryozo Sakoda ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Sakuya Tanaka

IPC分类号： C07F9/38 ,  A61K31/675 ,  A61P9/08 ,  C07F9/40 ,  C07F9/6571 ,  C07F9/6574

CPC分类号： C07F9/657181

摘要： An optical isomer of a compound having the formula: ##STR1## wherein the two methyl groups at 4- and 6-positions of the dioxaphosphorinane ring assume trans configurations to each other, which has a levo-rotatory angle of optical rotation attributable to the asymmetric carbon atom at 4-position of the dihydropyridine ring, and a pharmaceutically acceptable salt thereof.

摘要翻译： 具有下式的化合物的光学异构体：其中二氧杂磷杂环戊烷环的4位和6位上的两个甲基呈现相互构型，其具有归因于旋光的左旋旋角 到二氢吡啶环的4-位的不对称碳原子及其药学上可接受的盐。