公开(公告)号：US5190952A

公开(公告)日：1993-03-02

申请号：US549136

申请日：1990-07-05

申请人： Nobuto Minowa ,  Tomoya Machinami ,  Seiji Shibahara ,  Keiichi Imamura ,  Michiaki Iwata ,  Masaru Shimura ,  Shigeharu Inouye

发明人： Nobuto Minowa ,  Tomoya Machinami ,  Seiji Shibahara ,  Keiichi Imamura ,  Michiaki Iwata ,  Masaru Shimura ,  Shigeharu Inouye

IPC分类号： C07D215/22 ,  A01N43/42 ,  A01N47/06 ,  A01N53/00 ,  C07D215/233 ,  C07D215/56 ,  C07D219/06 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D215/233 ,  A01N43/42 ,  A01N47/06 ,  A01N53/00 ,  C07D215/56 ,  C07D219/06 ,  C07D405/12 ,  C07D409/12

摘要： A 4-acyloxyquinoline derivative represented by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.3 -C.sub.10 cycloalkyl which may be optionally substituted, phenylloweralkyl, phenoxyloweralkyl, aryl group, a group OR.sup.4, where R.sup.4 represents a lower alkyl or aryl group, or a group ##STR2## where X represents an oxygen or a sulphur atom; R.sup.2 represents a hydrogen atom, a lower alkyl alkyl group or a group --COOR.sup.5 where R.sup.5 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl or C.sub.2 -C.sub.10 alkenyl group, provided that R.sup.1 does not represent OR.sup.4 when R.sup.2 is a hydrogen atom and R.sup.3 is methyl; R.sup.2 and R.sup.3 together represent a group (CH.sub.2).sub.m, wherein m is 3 or 4, and W represents a hydrogen atom, 1 to 4 halogen atoms, a lower alkyl or lower alkoxy group which may be the same or different and with which the left-hand nucleus is substituted, provided that the compound wherein R.sup.1 represents methyl, R.sup.2, R.sup.3 and W each represent a hydrogen atom is excluded.

公开(公告)号：US5194617A

公开(公告)日：1993-03-16

申请号：US807946

申请日：1991-12-10

申请人： Nobuto Minowa ,  Tomoya Machinami ,  Takashi Shomura ,  Masaji Sezaki ,  Toru Sasaki ,  Seiji Shibahara ,  Shigeharu Inouye

发明人： Nobuto Minowa ,  Tomoya Machinami ,  Takashi Shomura ,  Masaji Sezaki ,  Toru Sasaki ,  Seiji Shibahara ,  Shigeharu Inouye

IPC分类号： C07D215/22 ,  C07D215/233

CPC分类号： C07D215/233

摘要： 2,3-disubstituted-4-hydroxyquinoline derivatives of the general formula (I): ##STR1## [wherein R.sup.1 represents a hydrogen atom or R.sup.3 CO-- (wherein R.sup.3 is a lower alkyl group); R.sup.2 represents a hydrogen atom, --CH.sub.3 or --C.sub.2 H.sub.5 ; A represents ##STR2## and W represents a hydrogen atom, or 1- 4 halogen atoms or alkyl groups which are substituted at the nucleus and may be the same or different] have a strong antagonistic action on leukotriene D.sub.4.

摘要翻译： （I）的2,3-二取代-4-羟基喹啉衍生物：其中R1表示氢原子或R3CO-（其中R3是低级烷基）; R 2表示氢原子，-CH 3或-C 2 H 5; A表示 ，W表示氢原子或1-4个卤原子或在核上被取代且可相同或不同的烷基对白三烯D4具有强拮抗作用。

公开(公告)号：US08648195B2

公开(公告)日：2014-02-11

申请号：US13580550

申请日：2011-02-22

申请人： Kouki Tanigakiuchi ,  Mikio Sekiguchi ,  Hiroki Hotta ,  Shizuo Shimano ,  Akinori Morikawa ,  Kazumi Yamamoto ,  Nozomu Nakanishi ,  Nobuto Minowa ,  Takashi Watanabe

发明人： Kouki Tanigakiuchi ,  Mikio Sekiguchi ,  Hiroki Hotta ,  Shizuo Shimano ,  Akinori Morikawa ,  Kazumi Yamamoto ,  Nozomu Nakanishi ,  Nobuto Minowa ,  Takashi Watanabe

IPC分类号： C07D215/38

CPC分类号： C07D215/233 ,  A01N43/42 ,  A01N47/06 ,  C07D215/20 ,  A01N25/12

摘要： An objective of the present invention is to provide a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate having stable physicochemical properties. The objective is attained by a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate that exhibits a diffraction peak pattern shown in FIG. 1 as determined by powder X-ray diffractometry.

摘要翻译： 本发明的目的是提供具有稳定物理化学性质的2-乙基-3,7-二甲基-6-（4-（三氟甲氧基）苯氧基）喹啉-4-基甲基碳酸酯的结晶。 目的是通过图2所示的衍射峰图案的2-乙基-3,7-二甲基-6-（4-（三氟甲氧基）苯氧基）喹啉-4-基甲基碳酸酯的晶体得到。 1，通过粉末X射线衍射测定。

公开(公告)号：US20120316358A1

公开(公告)日：2012-12-13

申请号：US13579135

申请日：2011-06-14

申请人： Takashi Ando ,  Nobuto Minowa ,  Masaaki Mitomi

发明人： Takashi Ando ,  Nobuto Minowa ,  Masaaki Mitomi

IPC分类号： C07F9/30

CPC分类号： C07F9/302 ,  C07F9/301

摘要： Provided is a method for producing a compound expressed by the following formula (3): [where R1 represents a hydrogen atom or C1-4 alkyl group, and R2 represents C1-4 alkyl group, C1-4 alkoxy group, aryl group, aryloxy group or benzyloxy group], the method comprising a reaction of dehydro-condensing a compound expressed by the following formula (1) and a compound expressed by the following formula (2): while being converted to a desired geometric isomer in the presence or absence of an acid catalyst, under a condition that an organic solvent to be used for the reaction is a mixed solvent of acetic acid and a solvent selected from the group consisting of toluene, xylene and chlorobenzene.

摘要翻译： 本发明提供由下式（3）表示的化合物的制造方法：[式中，R1表示氢原子或C1-4烷基，R2表示C1-4烷基，C1-4烷氧基，芳基，芳氧基 基团或苄氧基]，该方法包括使由下式（1）表示的化合物与下式（2）表示的化合物脱氢缩合的反应：在存在或不存在下转化为所需的几何异构体 的酸催化剂，在用于反应的有机溶剂是乙酸和选自甲苯，二甲苯和氯苯的溶剂的混合溶剂的条件下进行。

公开(公告)号：US08148504B2

公开(公告)日：2012-04-03

申请号：US12227861

申请日：2007-06-01

申请人： Yoshihiko Kobayashi ,  Yoshihisa Akiyama ,  Takeshi Murakami ,  Nobuto Minowa ,  Masaki Tsushima ,  Yukiko Hiraiwa ,  Shoichi Murakami ,  Mitsuhiro Abe ,  Kazushige Sasaki ,  Shigeru Hoshiko ,  Toshiaki Miyake ,  Yoshiaki Takahashi ,  Daishiro Ikeda

发明人： Yoshihiko Kobayashi ,  Yoshihisa Akiyama ,  Takeshi Murakami ,  Nobuto Minowa ,  Masaki Tsushima ,  Yukiko Hiraiwa ,  Shoichi Murakami ,  Mitsuhiro Abe ,  Kazushige Sasaki ,  Shigeru Hoshiko ,  Toshiaki Miyake ,  Yoshiaki Takahashi ,  Daishiro Ikeda

IPC分类号： C07H13/02

CPC分类号： C07H15/234 ,  C07H15/224

摘要： This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.

摘要翻译： 本发明涉及对细菌具有强力抗微生物活性的新型氨基糖苷类抗生素，其诱导感染性疾病，特别是MRSA，并且没有显着的肾毒性，以及生产它们的方法。 更具体地，本发明涉及由式（Ia）表示的化合物或其药理学上可接受的盐或溶剂合物或其非对映体混合物，包含它们的抗微生物剂及其制备方法。

公开(公告)号：US08017797B2

公开(公告)日：2011-09-13

申请号：US12530022

申请日：2008-03-21

申请人： Nobuto Minowa ,  Nozomu Nakanishi ,  Masaaki Mitomi

发明人： Nobuto Minowa ,  Nozomu Nakanishi ,  Masaaki Mitomi

IPC分类号： C07C67/00

CPC分类号： C07F9/301

摘要： A method for efficiently producing 4-(hydroxymethylphosphinyl)-2-oxobutanoic acid, useful as a production intermediate of herbicide L-AMPB. The method comprises using a compound represented by the below formula (4): (4) where R1 represents a C1-4 alkyl group, arylmethyl group, or substituted arylmethyl group.

摘要翻译： 一种有效生产4-（羟甲基氧膦基）-2-氧代丁酸的方法，可用作除草剂L-AMPB的生产中间体。 该方法包括使用由下式（4）表示的化合物：（4）其中R1表示C1-4烷基，芳基甲基或取代的芳基甲基。

公开(公告)号：US20090186841A1

公开(公告)日：2009-07-23

申请号：US12227861

申请日：2007-06-01

申请人： Yoshihiko Kobayashi ,  Yoshihisa Akiyama ,  Takeshi Murakami ,  Nobuto Minowa ,  Masaki Tsushima ,  Yukiko Hiraiwa ,  Shoichi Murakami ,  Mitsuhiro Abe ,  Kazushige Sasaki ,  Shigeru Hoshiko ,  Toshiaki Miyake ,  Yoshiaki Takahashi ,  Daishiro Ikeda

发明人： Yoshihiko Kobayashi ,  Yoshihisa Akiyama ,  Takeshi Murakami ,  Nobuto Minowa ,  Masaki Tsushima ,  Yukiko Hiraiwa ,  Shoichi Murakami ,  Mitsuhiro Abe ,  Kazushige Sasaki ,  Shigeru Hoshiko ,  Toshiaki Miyake ,  Yoshiaki Takahashi ,  Daishiro Ikeda

IPC分类号： A61K31/7036 ,  C07H15/234 ,  A61P31/04

CPC分类号： C07H15/234 ,  C07H15/224

摘要： This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.

摘要翻译： 本发明涉及对细菌具有强力抗微生物活性的新型氨基糖苷类抗生素，其诱导感染性疾病，特别是MRSA，并且没有显着的肾毒性，以及生产它们的方法。 更具体地，本发明涉及由式（Ia）表示的化合物或其药理学上可接受的盐或溶剂合物或其非对映体混合物，包含它们的抗微生物剂及其制备方法。

公开(公告)号：US20080146837A1

公开(公告)日：2008-06-19

申请号：US11909839

申请日：2006-03-28

申请人： Nobuto Minowa ,  Nozomu Nakanishi ,  Masaaki Mitomi

发明人： Nobuto Minowa ,  Nozomu Nakanishi ,  Masaaki Mitomi

IPC分类号： C07F9/36

CPC分类号： C07B53/00 ,  C07F9/301 ,  C07F9/65683

摘要： Disclosed is a method for efficiently and highly selectively producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid, which is useful as a herbicide, through a catalytic asymmetric synthesis reaction. Specifically disclosed is a method for producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid which is characterized in that a dehydroamino acid is subjected to an asymmetric hydrogenation by using a rhodium catalyst represented by the formula (2) below and having an optically active cyclic phosphine ligand, and then the resulting product is subjected to hydrolysis: [Rh(R4)(L)]X   (2) [where R4 represents 1,5-cyclooctadien or norbornadien; L represents a substance represented by the following formula (6): (wherein R5 and R8 respectively represent a C1-4 alkyl group; R6 and R7 respectively represent hydrogen atom or hydroxyl group; and Y represents a group selected from groups represented by the following formula (7): (where Me represents methyl group)).].

摘要翻译： 公开了通过催化不对称合成反应有效和高选择性地生产可用作除草剂的L-2-氨基-4-（羟甲基氧膦基） - 丁酸的方法。 具体公开了一种生产L-2-氨基-4-（羟甲基氧膦基） - 丁酸的方法，其特征在于，使用下式（2）表示的铑催化剂对脱氢氨基酸进行不对称氢化， 光学活性环膦配体，然后将所得产物进行水解：<？in-line-formula description =“In-line Formulas”end =“lead”→> [Rh（R 4） >）（L）] X（2）<？in-line-formula description =“In-line Formulas”end =“tail”？> [其中R 4表示1,5-环辛二烯或 降血统 L表示由下式（6）表示的物质：（其中R 5和R 8分别表示C 1-4烷基） ; R 6和R 7分别表示氢原子或羟基; Y表示选自下式（7）表示的基团：（其中Me表示甲基 组））。]。

公开(公告)号：US20130060042A1

公开(公告)日：2013-03-07

申请号：US13581857

申请日：2010-11-10

申请人： Yoshimasa Fukuda ,  Takashi Ando ,  Kimihiko Goto ,  Nozomu Nakanishi ,  Takashi Watanabe ,  Kenichi Kurihara ,  Nobuto Minowa ,  Masaaki Mitomi

发明人： Yoshimasa Fukuda ,  Takashi Ando ,  Kimihiko Goto ,  Nozomu Nakanishi ,  Takashi Watanabe ,  Kenichi Kurihara ,  Nobuto Minowa ,  Masaaki Mitomi

IPC分类号： C07D493/04

CPC分类号： C07D493/04

摘要： Disclosed is a process for efficiently producing pyripyropene derivatives having acyloxy at the 1-position and 11-position and hydroxyl at the 7-position. The process comprises selectively acylating hydroxyl at the 1-position and 11-position of a compound represented by formula B1 through one to three steps with an acylating agent in the presence or absence of a base.

摘要翻译： 公开了一种有效生产在1-位和11位上具有酰氧基并在7-位具有羟基的吡啶并苯衍生物的方法。 该方法包括在存在或不存在碱的情况下用酰化剂选择性地将式B1化合物的1位和11位羟基选择性酰化1-3步。

公开(公告)号：US20110009662A1

公开(公告)日：2011-01-13

申请号：US12529953

申请日：2008-03-19

申请人： Kenichi Kurihara ,  Nobuto Minowa ,  Nozomu Nakanishi ,  Masaaki Mitomi

发明人： Kenichi Kurihara ,  Nobuto Minowa ,  Nozomu Nakanishi ,  Masaaki Mitomi

IPC分类号： C07C227/14

CPC分类号： C07F9/4006 ,  C07F9/3217

摘要： A process for efficiently producing through a small number of steps an N-substituted 2-amino-4-(substituted-oxymethylphosphinyl)-2-butenoic ester which is an intermediate for herbicide L-AMPB. The process comprises reacting a compound represented by the following formula (1): (where R1 represents C1-4 alkyl group) with a compound represented by the following formula (2): (wherein R2, R2′, and R3 each represents C1-4 alkyl and R4 represents benzyloxycarbonyl) in the presence of a base.

摘要翻译： 通过少量步骤有效地制备作为除草剂L-AMPB的中间体的N-取代的2-氨基-4-（取代的 - 氧甲基氧膦基）-2-丁烯酸酯的方法。 该方法包括使由下式（1）表示的化合物（其中R 1表示C 1-4烷基）与下式（2）表示的化合物反应：（其中R2，R2'和R3各自表示C1- 4烷基，R 4表示苄氧基羰基）。