公开(公告)号：US5268501A

公开(公告)日：1993-12-07

申请号：US988432

申请日：1992-12-09

申请人： Takaharu Ikeda ,  Seiichi Kai ,  Masayoshi Minai

发明人： Takaharu Ikeda ,  Seiichi Kai ,  Masayoshi Minai

IPC分类号： C07C67/313 ,  C07C67/343 ,  C07C69/716 ,  C07C251/38 ,  C07C229/06

CPC分类号： C07C251/38 ,  C07C67/313 ,  C07C67/343 ,  C07C69/716

摘要： Process for preparing haloketo acid derivatives [I]: ##STR1## wherein R is H or C.sub.1-6 alkyl, and X is chlorine or bromine, which comprises reacting .beta.-oxo-acid ester [II]: ##STR2## wherein R.sup.1 is H or C.sub.1-6 alkyl, R.sup.2 is C.sub.1-5 alkyl or OR.sup.3 (R.sup.3 is C.sub.1-6 alkyl), and X is the same as above, with nitrosating agent [IV]:ONOR.sup.4 [IV]wherein R.sup.4 is H, alkyl, halogen or SO.sub.3 H to give 7-halo-2-hydroxyminoheptanoic acid ester [III]: ##STR3## wherein R.sup.1 and X are the same as above, following by reacting the product with aldehyde or ketone; and intermediates therefor, and process for preparing said intermediates. Said haloketo acid derivatives are useful as intermediate for synthesis of cilastatin, which is useful as medicament, especially as dehydropeptidase inhibitor.

摘要翻译： 制备卤代羧酸衍生物的方法[I]：其中R是H或C 1-6烷基，X是氯或溴，其包括使β-氧代酸酯[II]： II]其中R 1是H或C 1-6烷基，R 2是C 1-5烷基或OR 3（R 3是C 1-6烷基），X与上述相同，与亚硝化剂[Ⅳ]：ONOR4 [Ⅳ]其中R4 是H，烷基，卤素或SO 3 H，得到7-卤代-2-羟基乙酸庚酯。[III]：其中R1和X与上述相同，然后使产物与醛或酮反应; 及其中间体，以及制备所述中间体的方法。 所述卤代酸衍生物可用作合成西司他丁的中间体，其可用作药物，特别是作为脱氢肽酶抑制剂。

公开(公告)号：US5202467A

公开(公告)日：1993-04-13

申请号：US651971

申请日：1991-02-07

申请人： Takaharu Ikeda ,  Seiichi Kai ,  Masayoshi Minai

发明人： Takaharu Ikeda ,  Seiichi Kai ,  Masayoshi Minai

IPC分类号： C07C67/313 ,  C07C67/343 ,  C07C69/716 ,  C07C251/38

CPC分类号： C07C69/716 ,  C07C251/38 ,  C07C67/313 ,  C07C67/343

摘要： Process for preparing haloketo acid derivatives [I]: ##STR1## wherein R is H or C.sub.1-6 alkyl, and X is chlorine or bromine, which comprises reacting .beta.-oxo-acid ester [II]: ##STR2## wherein R.sup.1 is C.sub.1-6 alkyl, R.sup.2 is C.sub.1-5 alkyl or OR.sup.3 (R.sup.3 is C.sub.1-6 alkyl), and X is the same as above, with nitrosating agent [IV]:ONOR.sup.4 [IV]wherein R.sup.4 is H, alkyl, halogen or SO.sub.3 H to give 7-halo-2-hydroxyiminoheptanoic acid ester [III]: ##STR3## wherein R.sup.1 and X are the same as above, followed by reacting the product with aldehyde or ketone; and intermediates therefor, and process for preparing said intermediates. Said haloketo acid derivatives are useful as intermediate for synthesis of cilastatin, which is useful as medicament, especially as dehydropeptidase inhibitor.

公开(公告)号：US5191109A

公开(公告)日：1993-03-02

申请号：US648893

申请日：1991-01-31

申请人： Masayoshi Minai ,  Sachiko Imazu ,  Seiichi Kai ,  Takaharu Ikeda ,  Hideyuki Ikehira

发明人： Masayoshi Minai ,  Sachiko Imazu ,  Seiichi Kai ,  Takaharu Ikeda ,  Hideyuki Ikehira

IPC分类号： C07C69/593 ,  C07C69/606 ,  C07C69/738 ,  C07D307/54 ,  C12P7/62 ,  C12P41/00

CPC分类号： C07C69/593 ,  C07C69/606 ,  C07C69/738 ,  C07D307/54 ,  C12P41/004 ,  C12P7/62

摘要： An improved process for preparing an optically active 4-hydroxycyclopentenone of the formula: ##STR1## wherein R is a lower alkyl, the symbol means double bond or triple bond, and the * marked carbon is an asymmetric carbon, and the corresponding racemic 4-hydroxycyclopentenone, which are useful as an intermediate for preparing medicinal or agricultural products, particularly pharmaceutically active prostaglandins, and intermediates for preparing the optically active and/or racemic 4-hydroxycyclopentenone.

摘要翻译： 制备下式的光学活性4-羟基环戊烯酮的改进方法：其中R是低级烷基，符号是指双键或三键，并且*标记的碳是不对称碳，相应的 可用作制备药用或农产品的中间体，特别是药学上可接受的前列腺素的外消旋4-羟基环戊烯酮和用于制备光学活性和/或外消旋4-羟基环戊烯酮的中间体。

公开(公告)号：US5144039A

公开(公告)日：1992-09-01

申请号：US471966

申请日：1990-01-29

申请人： Yukio Yoneyoshi ,  Gohfu Suzukamo ,  Naoto Konya ,  Takaharu Ikeda

发明人： Yukio Yoneyoshi ,  Gohfu Suzukamo ,  Naoto Konya ,  Takaharu Ikeda

IPC分类号： C07C29/143 ,  C07D249/08 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07C29/143 ,  C07D233/56 ,  C07D249/08 ,  C07B2200/07

摘要： The process for producing an optically active alcohol of the present invention comprises allowing(A) an optically active amino alcohol represented by the general formula (I) ##STR1## (R.sup.1 is an aryl group, R.sup.2 is a lower alkyl group, R.sup.3 is a hydrogen atom or a lower alkyl group, and the carbon atoms having a mark * are each an asymmetric carbon atom) and an acid, or a salt of the optically active amino alcohol (I) and an acid,(B) a metal borohydride, and(C) at least one member selected from the group consisting of water, sulfides, cyclic ethers, ethers of mono alcohol to react witha prochiral ketone represented by the general formula (II) ##STR2## [R.sup.4 and R.sup.5 are different and each a lower alkyl group, an aryl group, an aralkyl group or a 2-substituted-1-triazoleethylene group represented by the general formula (III) ##STR3## (R.sup.6 is a halogen- or haloalkyl-substituted or unsubstituted phenyl group or a cycloalkyl group)].According to the present invention, the optically active alcohol (IV) can be obtained with good efficiency and a high optical purity. Therefore, the present process is advantageous in industrial application, in particular.

公开(公告)号：US4544635A

公开(公告)日：1985-10-01

申请号：US579602

申请日：1984-02-13

申请人： Naohito Ohashi ,  Kozo Shimago ,  Takaharu Ikeda ,  Kikuo Ishizumi

发明人： Naohito Ohashi ,  Kozo Shimago ,  Takaharu Ikeda ,  Kikuo Ishizumi

IPC分类号： C07D233/32 ,  C07D491/04 ,  C07D491/048 ,  C12N9/18 ,  C12P17/10

CPC分类号： C07D491/04 ,  C07D233/32 ,  C12N9/18 ,  C12P17/10

摘要： A process for preparing an optically active cis-1,3-dibenzylhexahydro-1H-furo[3,4-d]imidazole-2,4-dione of the formula: ##STR1## wherein an asterisk (*) indicates an asymmetric carbon, Bzl represents a benzyl group and the 3a- and 6a-positions take the cis-configuration, which comprises reducing selectively an optically active cis-imidazolidinedicarboxylic acid monoester of the formula: ##STR2## wherein R is a C.sub.1 -C.sub.6 alkyl group and Bzl is as defined above with a reducing agent at either one of the carboxyl group and the alkoxycarbonyl group in the said monoester, followed by cyclization.

公开(公告)号：US20100261528A1

公开(公告)日：2010-10-14

申请号：US12678987

申请日：2008-08-11

申请人： Mitsuhiro Nomi ,  Fumiaki Oshita ,  Kazuto Nishimura ,  Kazuhiko Ninomiya ,  Takaharu Ikeda

发明人： Mitsuhiro Nomi ,  Fumiaki Oshita ,  Kazuto Nishimura ,  Kazuhiko Ninomiya ,  Takaharu Ikeda

IPC分类号： A63F9/24

CPC分类号： A63F13/55 ,  A63F13/10 ,  A63F13/5375 ,  A63F13/837 ,  A63F2300/305 ,  A63F2300/406 ,  A63F2300/64 ,  A63F2300/8076

摘要： To provide a game device capable of improving reality regarding an operation of a game in which an attack on one or more attack targets is performed. Remaining number-of-times information storage means (70) stores remaining number-of-times information that indicates a remaining number of times an attack on one or more attack targets can be performed. Display means (74) displays a screen that includes a first image, containing a plurality of reference regions, and a second image. Image moving means (72) moves at least one of the first image and the second image according to a direction instructing operation of a player. Remaining number-of-times information update means (76) increases the remaining number of times the attack on one or more attack target can be performed based on a number of one or more reference regions included in a superposition region in which the first image and the second image are superposed on each other.

摘要翻译： 提供能够改善对执行对一个或多个攻击目标的攻击的游戏的操作的现实的游戏装置。 剩余次数信息存储装置（70）存储指示可以执行对一个或多个攻击目标的攻击的剩余次数的剩余次数信息。 显示装置（74）显示包括包含多个参考区域的第一图像和第二图像的屏幕。 图像移动装置（72）根据指示玩家的操作的方向移动第一图像和第二图像中的至少一个。 剩余次数信息更新装置（76）基于包括在重叠区域中的一个或多个参考区域的数量增加对一个或多个攻击目标的攻击的剩余次数，其中第一图像和 第二图像彼此重叠。

公开(公告)号：US4814461A

公开(公告)日：1989-03-21

申请号：US7655

申请日：1987-01-28

申请人： Takaharu Ikeda ,  Kazuhiro Tada

发明人： Takaharu Ikeda ,  Kazuhiro Tada

IPC分类号： B01J21/00 ,  B01J27/06 ,  B01J31/00 ,  B01J31/04 ,  C07B61/00 ,  C07D249/08 ,  C07D521/00 ,  C07D249/12

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： A novel process for preparing E-isomer of a triazolyl styryl ketone derivative of the formula (I): ##STR1## which includes treating Z-isomer of the derivative (which may contain E-isomer of the derivative) with sulfuric acid and an isomerization catalyst in an organic solvent, precipitating and separating the resulting sulfuric acid salt of E-isomer from the solution, and decomposing the resulting precipitate to obtain E-isomer of the derivative free from sulfuric acid. The E-isomer is useful for preparing E-isomer of triazolyl styryl carbinol of the formula (II): ##STR2## which is useful as an antimicrobial agent, a herbicide, a plant growth regulator, or the like.

摘要翻译： 一种制备式（I）的三唑基苯乙烯基酮衍生物的E-异构体的新方法：其中包括用硫酸处理衍生物的Z-异构体（其可含有衍生物的E-异构体） 和有机溶剂中的异构化催化剂，从溶液中沉淀并分离得到的E-异构体的硫酸盐，并分解所得沉淀物，得到不含硫酸的衍生物的E-异构体。 E型异构体可用于制备式（II）的三唑基苯乙烯基甲醇的E-异构体：可用作抗微生物剂，除草剂，植物生长调节剂等的图像（II）。

公开(公告)号：US08602890B2

公开(公告)日：2013-12-10

申请号：US12678987

申请日：2008-08-11

申请人： Mitsuhiro Nomi ,  Fumiaki Oshita ,  Kazuto Nishimura ,  Kazuhiko Ninomiya ,  Takaharu Ikeda

发明人： Mitsuhiro Nomi ,  Fumiaki Oshita ,  Kazuto Nishimura ,  Kazuhiko Ninomiya ,  Takaharu Ikeda

IPC分类号： A63F13/04

CPC分类号： A63F13/55 ,  A63F13/10 ,  A63F13/5375 ,  A63F13/837 ,  A63F2300/305 ,  A63F2300/406 ,  A63F2300/64 ,  A63F2300/8076

摘要： To provide a game device capable of improving reality regarding an operation of a game in which an attack on one or more attack targets is performed. Remaining number-of-times information storage means (70) stores remaining number-of-times information that indicates a remaining number of times an attack on one or more attack targets can be performed. Display means (74) displays a screen that includes a first image, containing a plurality of reference regions, and a second image. Image moving means (72) moves at least one of the first image and the second image according to a direction instructing operation of a player. Remaining number-of-times information update means (76) increases the remaining number of times the attack on one or more attack target can be performed based on a number of one or more reference regions included in a superposition region in which the first image and the second image are superposed on each other.

摘要翻译： 提供能够改善对执行对一个或多个攻击目标的攻击的游戏的操作的现实的游戏装置。 剩余次数信息存储装置（70）存储指示可以执行对一个或多个攻击目标的攻击的剩余次数的剩余次数信息。 显示装置（74）显示包括包含多个参考区域的第一图像和第二图像的屏幕。 图像移动装置（72）根据指示玩家的操作的方向移动第一图像和第二图像中的至少一个。 剩余次数信息更新装置（76）基于包括在重叠区域中的一个或多个参考区域的数量增加对一个或多个攻击目标的攻击的剩余次数，其中第一图像和 第二图像彼此重叠。

公开(公告)号：US4983758A

公开(公告)日：1991-01-08

申请号：US279095

申请日：1988-12-02

申请人： Yoshiaki Oda ,  Takaharu Ikeda ,  Hiroshi Yamachika

发明人： Yoshiaki Oda ,  Takaharu Ikeda ,  Hiroshi Yamachika

IPC分类号： C07C51/09

CPC分类号： C07C51/09

摘要： A process for producing an optically active .alpha.-isopropyl-p-chlorophenylacetic acid (ICPA) of the formula: ##STR1## wherein the symbol * stands for an asymmetric carbon atom.

公开(公告)号：US4904793A

公开(公告)日：1990-02-27

申请号：US95833

申请日：1987-09-14

申请人： Takaharu Ikeda ,  Kazuhiro Tada

发明人： Takaharu Ikeda ,  Kazuhiro Tada

IPC分类号： C07D249/08 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： A triazole compound of the formula: ##STR1## wherein X is a hydrogen atom or a chlorine atom, which can be produced by subjecting an aromatic aldehyde of the formula: ##STR2## wherein X is as defined above, an alpha-halopinacolone of the formula: ##STR3## wherein Hal is a chlorine atom or a bromine atom and 1,2,4-triazole to condensation in the presence of an alkali, is useful as an intermediate in the synthesis of anti-microbial triazole-alcohols with high purity and high yield.

摘要翻译： 下式的三唑化合物：其中X是氢原子或氯原子，其可以通过使下式的芳族醛进行制备：其中X如上定义，其中X如上定义，α-卤代新戊酸钠 式：其中Hal是氯原子或溴原子和1,2,4-三唑在碱存在下缩合，可用作合成具有高纯度的抗微生物三唑醇的中间体 产量高。