公开(公告)号：US20100136188A1

公开(公告)日：2010-06-03

申请号：US12700900

申请日：2010-02-05

申请人： Toru Mizuguchi ,  Takaaki Okita ,  Takashi Mori ,  Hiroyuki Onuki

发明人： Toru Mizuguchi ,  Takaaki Okita ,  Takashi Mori ,  Hiroyuki Onuki

IPC分类号： A23L1/325

CPC分类号： A23B4/20 ,  A23B4/08 ,  A23L17/00 ,  A23L17/70

摘要： Providing a frozen non-water-washed or water-washed at low level fish meat with suppressed freezing denaturation, from a fish species generally never used without water-wash. Biological iron, iron-containing substances and/or biological reducing substances in the fish meat are oxidized. A frozen non-water-washed or water-washed at low level fish meat made from minced fish meat or the dehydrated minced fish meat, where one or more cryoprotectants have been added and the decomposition of trimethylamine-N-oxide is suppressed through oxidation. Preferably, the fish meat is put in contact to oxygen under agitation of the fish meat, to thereby suppress trimethylamine-N-oxide decomposition, to which are added cryoprotectants for freezing. A frozen product of non-water-washed or water-washed at low level fish meat, where salts have been added for such agitation, followed by agitation. A fish paste product from the frozen product as the raw material.

摘要翻译： 提供冷冻非水洗或水洗的低级鱼肉，抑制冻结变性，从一般从未使用过没有水洗的鱼类。 鱼肉中的生物铁，含铁物质和/或生物还原物质被氧化。 将由切碎的鱼肉制成的低级鱼肉或经脱水的切碎的鱼肉进行冷冻非水洗或水洗，其中加入一种或多种冷冻保护剂并通过氧化抑制三甲胺-N-氧化物的分解。 优选地，在鱼肉搅拌下将鱼肉与氧气接触，从而抑制加入用于冷冻的冷冻保护剂的三甲胺-N-氧化物分解。 在低级鱼肉中非水洗或水洗的冷冻产品，其中已经加入盐进行搅拌，随后搅拌。 以冷冻产品为原料的鱼糊产品。

公开(公告)号：US20060204640A1

公开(公告)日：2006-09-14

申请号：US10485948

申请日：2002-08-01

申请人： Toru Mizuguchi ,  Takaaki Okita ,  Takashi Mori ,  Hiroyuki Onuki

发明人： Toru Mizuguchi ,  Takaaki Okita ,  Takashi Mori ,  Hiroyuki Onuki

IPC分类号： A23L1/325

CPC分类号： A23B4/20 ,  A23B4/08 ,  A23L17/00 ,  A23L17/70

摘要： Providing a frozen non-water-washed or water-washed at low level fish meat with suppressed freezing denaturation, from a fish species generally never used without water-wash. Biological iron, iron-containing substances and/or biological reducing substances in the fish meat are oxidized. A frozen non-water-washed or water-washed at low level fish meat made from minced fish meat or the dehydrated minced fish meat, where one or more cryoprotectants have been added and the decomposition of trimethylamine-N-oxide is suppressed through oxidation. Preferably, the fish meat is put in contact to oxygen under agitation of the fish meat, to thereby suppress trimethylamine-N-oxide decomposition, to which are added cryoprotectants for freezing. A frozen product of non-water-washed or water-washed at low level fish meat, where salts have been added for such agitation, followed by agitation. A fish paste product from the frozen product as the raw material.

摘要翻译： 提供冷冻非水洗或水洗的低级鱼肉，抑制冻结变性，从一般从未使用过没有水洗的鱼类。 鱼肉中的生物铁，含铁物质和/或生物还原物质被氧化。 将由切碎的鱼肉制成的低级鱼肉或经脱水的切碎的鱼肉进行冷冻非水洗或水洗，其中加入一种或多种冷冻保护剂并通过氧化抑制三甲胺-N-氧化物的分解。 优选地，在鱼肉搅拌下将鱼肉与氧气接触，从而抑制加入用于冷冻的冷冻保护剂的三甲胺-N-氧化物分解。 在低级鱼肉中非水洗或水洗的冷冻产品，其中已经加入盐进行搅拌，随后搅拌。 以冷冻产品为原料的鱼糊产品。

公开(公告)号：US06180659B2

公开(公告)日：2001-01-30

申请号：US09101842

申请日：1998-08-31

申请人： Shinya Yamashita ,  Jiro Takeo ,  Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita ,  Junichiro Hata ,  Yasuhiro Fukuda ,  Naomi Ohtsuka

发明人： Shinya Yamashita ,  Jiro Takeo ,  Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita ,  Junichiro Hata ,  Yasuhiro Fukuda ,  Naomi Ohtsuka

IPC分类号： A61K3138

CPC分类号： C07D337/14 ,  A61K31/352 ,  A61K31/382 ,  C07D313/14 ,  Y10S514/826

摘要： The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient. [In the formula, X and Y each is any group selected from a group consisting of CH2, CHW1 (where W1 is halogen atom, hydroxyl group or lower alkoxy group) and C═O when the bond of X and Y is a single bond while, when it is a double bond, X and Y each is any group selected from a group consisting of CH and COW2 (where W2 is lower alkyl group or lower alkylcarbonyl group); Z is O, S, S═O or SO2; and R1˜R8 each is selected from a group consisting of hydrogen atom, VR9 (where V is O, S, S═O or SO2; and R9 is hydrogen atom, lower alkyl group, hydroxy lower alkyl group, lower acyl group, trihalomethyl group or carboxyl lower alkyl group), carboxyl lower alkyl group, hydroxy lower alkyl group, hydroxy lower alkenyl group, hydroxy lower alkynyl group, halogen atom, lower alkyl group, lower alkyl ketone, trihalomethyl group, trimethylsilylethynyl, nitro group, amino group, N-carbonyl lower alkyl group, lower alkylphenyl group and phenyl group].

摘要翻译： 本发明提供含有下述式（1）表示的化合物或其药理学上可接受的盐作为有效成分的气管平滑肌松弛剂。[式中，X和Y各自为选自CH 2， CHW1（其中W1为卤原子，羟基或低级烷氧基），当X和Y的键为单键时为C = O，而当为双键时，X和Y各自为选自 由CH和COW 2组成（其中W2是低级烷基或低级烷基羰基）; Z是O，S，S = O或SO 2; R1〜R8各自选自氢原子，VR9（其中V为O，S，S = O或SO2; R9为氢原子，低级烷基，羟基低级烷基，低级酰基，三卤甲基 羧基低级烷基，羟基低级烷基，羟基低级烯基，羟基低级炔基，卤素原子，低级烷基，低级烷基酮，三卤代甲基，三甲基甲硅烷基乙炔基，硝基，氨基， N-羰基低级烷基，低级烷基苯基和苯基]。

公开(公告)号：US06495592B1

公开(公告)日：2002-12-17

申请号：US09609310

申请日：2000-06-30

申请人： Shinya Yamashita ,  Jiro Takeo ,  Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita ,  Junichiro Hata ,  Yasuhiro Fukuda ,  Naomi Ohtsuka

发明人： Shinya Yamashita ,  Jiro Takeo ,  Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita ,  Junichiro Hata ,  Yasuhiro Fukuda ,  Naomi Ohtsuka

IPC分类号： A61K31335

CPC分类号： C07D337/14 ,  A61K31/352 ,  A61K31/382 ,  C07D313/14 ,  Y10S514/826

摘要： The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.

摘要翻译： 本发明提供含有下述式（1）表示的化合物或其药理学可接受的盐作为有效成分的气管平滑肌松弛剂。

公开(公告)号：US5734067A

公开(公告)日：1998-03-31

申请号：US809001

申请日：1997-03-04

申请人： Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita

发明人： Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita

IPC分类号： C07D313/14 ,  C07D337/14 ,  C07D493/04

CPC分类号： C07D493/04 ,  C07D313/14 ,  C07D337/14

摘要： Providing a novel tricyclic, condensed heterocyclic compound having an anti-oxidative action and being promising for use in pharmaceutical agents, cosmetics, chemical products and the like. By chemical synthesis, a novel anti-oxidative, tricyclic, condensed heterocyclic compound represented by the following formula: ##STR1## (wherein X--Y represents CH.sub.2 --C.dbd.O, CH.sub.2 --CH.sub.2 or CH.dbd.CH; Z represents O, S, or S.dbd.O; R.sub.1 to R.sub.8 represent independently those selected from the group consisting of hydrogen atom, a hydroxyl group, a halogen group, a lower alkyl group, a lower alkoxyl group, a lower alkyl ketone group and CF.sub.3 ; and at least two of R.sub.1 to R.sub.4 are hydroxyl groups); and the salts thereof are provided. The compound has an anti-oxidative activity at the same degree as or higher than the activity of .alpha.-tocopherol, so the compound is promising as a therapeutic drug for a variety of diseases, such as cancer, arteriosclerosis, or liver diseases, in which it is believed that biological lipid peroxides may be involved.

摘要翻译： PCT No.PCT / JP95 / 01975 Sec。 371日期1997年3月4日 102（e）1997年3月4日PCT PCT 1995年9月28日PCT公布。 WO96 / 10021 PCT出版物 日期1996年4月4日提供具有抗氧化作用的新型三环稠合杂环化合物，并且有希望用于药剂，化妆品，化学产品等。 通过化学合成，由下式表示的新型抗氧化三环稠合杂环化合物：其中XY表示CH 2 -C = O，CH 2 -CH 2或CH = CH; Z表示O，S或S = O; R 1〜R 8分别独立地表示选自氢原子，羟基，卤素基，低级烷基，低级烷氧基，低级烷基酮基和CF 3的化合物; R 1〜 R4为羟基）; 并提供其盐。 该化合物具有与α-生育酚活性相同或更高的抗氧化活性，因此该化合物作为各种疾病如癌症，动脉硬化或肝脏疾病的治疗药物是有希望的，其中 相信可能涉及生物脂质过氧化物。

公开(公告)号：US5360585A

公开(公告)日：1994-11-01

申请号：US83568

申请日：1993-06-30

申请人： Yasuhiko Ishida ,  Minoru Yoshida ,  Hideki Mizuguchi ,  Takaaki Okita ,  Tetsuo Makida

发明人： Yasuhiko Ishida ,  Minoru Yoshida ,  Hideki Mizuguchi ,  Takaaki Okita ,  Tetsuo Makida

IPC分类号： B26D1/29 ,  B26D7/26 ,  B29B9/06 ,  B28B11/16

CPC分类号： B26D7/265 ,  B26D1/29 ,  B26D7/2614 ,  B29B9/065

摘要： A plastics granulating process wherein a cutter holder having cutter knives is driven to rotate along a die surface of a die and a housing is provided with a cutter drive shaft for driving the cutter holder to rotate in a manner so that plastics particles are obtained by cutting resin extruded from the die. A sleeve is axially movably provided in the housing so as to coaxially rotatably hold the cutter drive shaft, and a pressure medium is supplied into space chambers formed between the sleeve and the housing so that the cutter drive shaft moves axially with axial movement of the sleeve and the cutter knives presses against the die surface with a controlled thrust force.

摘要翻译： 一种塑料造粒方法，其中具有切割刀的切割器保持器被驱动沿着模具的模具表面旋转，并且壳体设置有切割器驱动轴，用于驱动切割器保持器旋转，使得通过切割获得塑料颗粒 从模头挤出的树脂。 套筒可轴向移动地设置在壳体中以同轴地可旋转地保持切割器驱动轴，并且压力介质被供应到形成在套筒和壳体之间的空间室中，使得切割器驱动轴随着套筒的轴向运动而轴向移动 并且切割刀以受控的推力压靠在模具表面上。

公开(公告)号：US20050203061A1

公开(公告)日：2005-09-15

申请号：US10505961

申请日：2003-06-20

申请人： Shinya Yamashita ,  Jiro Takeo ,  Takaaki Okita

发明人： Shinya Yamashita ,  Jiro Takeo ,  Takaaki Okita

IPC分类号： A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P43/00 ,  C07H15/18 ,  C07H15/203 ,  A61K31/715 ,  C07H5/04

CPC分类号： C07H15/203 ,  C07H15/18

摘要： A prodrug utilizes an enzyme whose enzymatic activity is different in between the target site of the drug and the site to express side effects, the prodrug having a substituent cleavable with the enzyme and being activated by cleaving the substituent with the enzyme. As the target site of the drug, for example, a respiratory organ can be mentioned and as the site to express side effects, for example, the heart can be mentioned. As the example of the drug, a bronchodilator can be mentioned and as the example of the enzyme, a glycosidase (for example, β-glucuronidase) can be mentioned. Furthermore, the substituent is, for example, a glycosyl group composed of a monosaccharide or an oligosaccharide. Use of the enzyme enables reducing the side effects of a drug of the type whose target site is different from the site to express side effects.

摘要翻译： 前体药物利用酶的活性在药物的靶位点和表达副作用的位点之间的酶活性不同的酶，前药具有可与酶切割的取代基并通过用酶切割取代基来活化。 作为药物的靶位，例如可以提及呼吸器官，作为表达副作用的部位，例如可以提及心脏。 作为药物的实例，可以提及支气管扩张剂，作为酶的实例，可以提及糖苷酶（例如β-葡糖苷酸酶）。 此外，取代基是例如由单糖或寡糖构成的糖基。 使用该酶能够减少目标部位不同于该部位的药物的副作用，以表现副作用。

公开(公告)号：US5326867A

公开(公告)日：1994-07-05

申请号：US914908

申请日：1992-07-16

申请人： Satsuki Okuyama ,  Takaaki Okita ,  Hajime Kamachi

发明人： Satsuki Okuyama ,  Takaaki Okita ,  Hajime Kamachi

IPC分类号： C07C65/40 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P31/04 ,  C07C235/84 ,  C07H15/24 ,  C07H15/244 ,  C07C13/00

CPC分类号： C07C235/84 ,  C07H15/244 ,  C07C2103/52 ,  Y02P20/55

摘要： The present invention relates to intermediates, pradimic acids and pradimic acid amides of the formula (II) ##STR1## wherein R is OH or NH.sub.2 ; R.sup.1 is hydrogen or a group of the formula ##STR2## with the proviso that when R is OH, R.sup.1 is not hydrogen; Y is OH or NR.sup.2 R.sup.3 ; R.sup.2 is hydrogen or methyl; R.sup.3 is hydrogen, C.sub.1-5 alkyl, or an amino protecting group; R.sup.4 is hydrogen, hydroxy protecting group, or .beta.-D-xylosyl. The invention relates also to novel processes for the preparation of pradimic acids and pradimic acid amides, as well as novel pradimicin derivatives prepared therefrom.

摘要翻译： 本发明涉及式（II）其中R是OH或NH 2的式（II）的中间体pradimic acid和pradimic acid酰胺; R 1是氢或式（IV）的基团： Y是OH或NR2R3; R2是氢或甲基; R3是氢，C1-5烷基或氨基保护基; R4是氢，羟基保护基或β-D-木糖基。 本发明还涉及用于制备偏二酸和游离酰胺的新方法，以及由其制备的新的普拉明霉素衍生物。

公开(公告)号：US06700013B2

公开(公告)日：2004-03-02

申请号：US10291429

申请日：2002-11-12

申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

IPC分类号： C07C53134

CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S═O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述定义相同 Y）为例如CH，CH 2或C = O; Z为例如O，S，S = O或SO 2; U为C或N; R 1至R 4各自独立地为例如 氢原子，OR，SR（其中R与上述定义相同）或芳环，取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，剩余的R 5和R 8 各自独立地，例如，氢原子或OH，其旋光异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

公开(公告)号：US06602898B1

公开(公告)日：2003-08-05

申请号：US09980581

申请日：2002-02-26

申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

IPC分类号： A61K3138

CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S=O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述定义相同 Y）为例如CH，CH 2或C = O; Z为例如O，S，S = O或SO 2; U为C或N; R 1至R 4各自独立地为例如 氢原子，OR，SR（其中R与上述定义相同）或芳环，取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，剩余的R 5和R 8 各自独立地，例如，氢原子或OH，其旋光异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。