公开(公告)号：US06593364B2

公开(公告)日：2003-07-15

申请号：US09921983

申请日：2001-08-06

申请人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

发明人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

IPC分类号： A61K31215

CPC分类号： C07J63/008 ,  C07J63/00 ,  Y10S514/893 ,  Y10S514/894

摘要： A triterpene derivative useful for the treatment of hepatic disorders is disclosed. This compound comprises as an active ingredient a triterpene derivative represented by the following formula (I) or a salt thereof: wherein R1 represents a hydroxyl group, arylmethyloxy, lower alkoxy, or lower alkanoyloxy, R2 represents lower alkyl, lower alkenyl, —CH2OR5, formyl, —COOR6, or —CH2N(R7)R8, or R1 and R2 may combine with each other to form —O—C(R9)R10—O—CH2—, R3 and R4, which may be the same or different represent a hydrogen atom, a hydroxyl group, lower alkyl, lower alkenyl, aryl, hydroxymethyl, —N(R11)R12, formyl, —COOR6, or —OR13, or R3 and R4 may combine with each other to form oxo, hydroxyimino, or alkylidene and X represents O, CH2, or NH.

摘要翻译： 公开了用于治疗肝脏疾病的三萜衍生物。 该化合物包含作为活性成分的下式（I）表示的三萜衍生物或其盐：其中R1表示羟基，芳基甲氧基，低级烷氧基或低级烷酰氧基，R2表示低级烷基，低级烯基，-CH2OR5， 甲酰基，-COOR 6或-CH 2 N（R 7）R 8，或R 1和R 2可以彼此结合形成-OC（R 9）R 10 -O-CH 2 - ，R 3和R 4，其可以相同或不同，表示氢 原子，羟基，低级烷基，低级烯基，芳基，羟甲基，-N（R 11）R 12，甲酰基，-COOR 6或-OR 13或R 3和R 4可以彼此结合形成氧代，羟基亚氨基或亚烷基， X表示O，CH 2或NH。

公开(公告)号：US06306862B1

公开(公告)日：2001-10-23

申请号：US08983127

申请日：1998-06-01

申请人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

发明人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

IPC分类号： A61K31495

CPC分类号： C07J63/008 ,  C07J71/0005

摘要： A pharmaceutical composition for treating a hepatic disorder, comprising a triterpene derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof is disclosed: wherein R1 represents a hydroxyl group, alkoxy, alkylcarbonyloxy, or aralkyloxy; R2 represents alkyl, —CH2OR5, wherein R5 represents a hydrogen atom, alkyl, aralkyl, or alkylcarbonyl, formyl, —COOR6, wherein R6 represents a hydrogen atom or alkyl, or —CH2N(R7)R8; or R1 and R2 combine with each other to form —O—CR9(R10)—OCH2—, wherein R9 and R10, which may be the same or different, represent a hydrogen atom, alkyl, or aryl; R3 and R4, which may be the same or different, represent a hydrogen atom, a hydroxyl group, alkyl, hydroxyalkyl, formyl, —COOR11, wherein R11 represents a hydrogen atom or alkyl, or —OR12, wherein R12 represents alkyl, aralkyl, C1-6 alkylcarbonyl, arylcarbonyl, alkenyl, alkenylcarbonyl, or arylalkenylcarbonyl which may be optionally substituted; or R3 and R4 combine with each other to form a methylene group; and — — — represents a single or double bond, provided that, when — — — represents a double bond, R4 is absent.

摘要翻译： 公开了一种治疗肝病的药物组合物，其包含由式（I）表示的三萜衍生物或其药学上可接受的盐：其中R1表示羟基，烷氧基，烷基羰氧基或芳烷氧基; R 2表示烷基，-CH 2 OR 5，其中R 5表示氢原子，烷基，芳烷基或烷基羰基，甲酰基，-COOR 6，其中R 6表示氢原子或烷基或-CH 2 N（R 7）R 8; 或R 1和R 2彼此结合形成-O-CR 9（R 10）-OCH 2 - ，其中R 9和R 10可以相同或不同，表示氢原子，烷基或芳基; R 3和R 4可以相同或不同，表示氢原子，羟基，烷基，羟基烷基，甲酰基，-COOR11，其中R11表示氢原子或烷基或-OR12，其中R12表示烷基，芳烷基， 可以任意取代的C 1-6烷基羰基，芳基羰基，烯基，烯基羰基或芳基烯基羰基; 或R 3和R 4彼此结合形成亚甲基; 和 - - 表示单键或双键，条件是当 - - 表示双键时，R4不存在。

公开(公告)号：US07153979B2

公开(公告)日：2006-12-26

申请号：US10370710

申请日：2003-02-24

申请人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

发明人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

IPC分类号： C07D203/26 ,  C07D303/06 ,  C07C35/00 ,  C07C35/18 ,  C07C49/83

CPC分类号： C07J63/008 ,  C07J63/00 ,  Y10S514/893 ,  Y10S514/894

摘要： A triterpene derivative useful for the treatment of hepatic disorders is disclosed. This compound comprises as an active ingredient a triterpene derivative represented by the following formula (I) or a salt thereof: wherein R1 represents a hydroxyl group, arylmethyloxy, lower alkoxy, or lower alkanoyloxy, R2 represents lower alkyl, lower alkenyl, —CH2OR5, formyl, —COOR6, or —CH2N(R7)R8, or R1 and R2 may combine with each other to form —O—C(R9)R10—O—CH2—, R3 and R4, which may be the same or different, represent a hydrogen atom, a hydroxyl group, lower alkyl, lower alkenyl, aryl, hydroxymethyl, —N(R11)R12, formyl, —COOR6, or —OR13, or R3 and R4 may combine with each other to form oxo, hydroxyimino, or alkylidene and X represents O, CH2, or NH.

摘要翻译： 公开了用于治疗肝脏疾病的三萜衍生物。 该化合物包含作为活性成分的由下式（I）表示的三萜衍生物或其盐：其中R 1表示羟基，芳基甲氧基，低级烷氧基或低级烷酰氧基，R SUP > 2代表低级烷基，低级烯基，-CH 2或OR 5，甲酰基，-COOR 6或-CH 3， N 2（R 7）R 8或R 1和R 2可以是 彼此结合形成-OC（R 9）R 10 -O-CH 2 - ，R 3 O， 和R 4可以相同或不同，表示氢原子，羟基，低级烷基，低级烯基，芳基，羟甲基，-N（R 11） R 12，R 12，R 12，R 12，R 12，R 12和R 12独立地选自氢， SUP> 4可以彼此结合形成氧代，羟基亚氨基或亚烷基，X代表O，CH 2或NH。

公开(公告)号：US06201018B1

公开(公告)日：2001-03-13

申请号：US09125776

申请日：1998-08-26

申请人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

发明人： Kazue Sasaki ,  Nobuto Minowa ,  Shoji Nishiyama ,  Hiroyuki Kuzuhara

IPC分类号： C07C6702

CPC分类号： C07J63/008 ,  C07J63/00 ,  Y10S514/893 ,  Y10S514/894

摘要： A triterpene derivative useful for the treatment of hepatic disorders is disclosed. This compound comprises as an active ingredient a triterpene derivative represented by the following formula (IV) or a salt thereof: Y represents a single bond to form a double bond in the ring with Y bonded thereto.

摘要翻译： 公开了用于治疗肝脏疾病的三萜衍生物。 该化合物作为活性成分包含由下式（Ⅳ）表示的三萜衍生物或其盐：Y表示在与Y键合的环中形成双键的单键。

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））。]。