公开(公告)号：US5155259A

公开(公告)日：1992-10-13

申请号：US742352

申请日：1991-08-08

申请人： Yukio Suzuki ,  Kouichi Kuno ,  Motoshi Shoda ,  Masao Yaso ,  Satoshi Yaginuma ,  Akira Asahi

发明人： Yukio Suzuki ,  Kouichi Kuno ,  Motoshi Shoda ,  Masao Yaso ,  Satoshi Yaginuma ,  Akira Asahi

IPC分类号： C12N9/99 ,  A61K31/19 ,  A61P3/08 ,  A61P3/10 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  A61P27/12 ,  A61P43/00 ,  C07C59/64 ,  C07C59/72

CPC分类号： C07C59/72 ,  C07C59/64

摘要： An aldose reductase inhibitor, comprising a compound of the formula (I) ##STR1## or a pharmaceutically acceptable salt thereof as the effective component, in which R is lower alkyl or cyclohexylmethyl and n is 2 or 3. The compounds of formula (I) and salts thereof according to the invention exhibit a superior aldose reductase inhibiting activity with simultaneous high stability, so that they are useful for the prevention and therapy of diabetic complications.

公开(公告)号：US5089393A

公开(公告)日：1992-02-18

申请号：US176235

申请日：1988-03-31

申请人： Shigeyuki Imamura ,  Hideo Misaki

发明人： Shigeyuki Imamura ,  Hideo Misaki

IPC分类号： G01N33/92 ,  C12Q1/26 ,  C12Q1/44

CPC分类号： C12Q1/44 ,  C12Q1/26 ,  C12Q2326/96 ,  G01N2333/906 ,  G01N2333/916 ,  G01N2405/04 ,  Y10S435/832

摘要： Ethanolamine in a sample can be assayed by treating the sample with ethanolamine oxidase, thereby to catalyze a reaction-consuming ethanolamine, oxygen and water, and forming glycolaldehyde, ammonia and hydrogen peroxide. The amount of consumed oxygen or the amount of generated ammonia or hydrogen peroxide is then determined, as a measure of the ethanolamine that was originally the sample. The ethanolamine can appear in the sample as such, or can be liberated simultaneously with or prior to the catalysis reaction, from an ethanolamine derivative, e.g. phosphatidyl ethanolamine by the action of phospholipase D. Ethanolamine oxidase can be produced from Bacillus sp. B-0783 FERM-P No. 5798 in a conventional culture medium, preferably by submerged aeration liquid culturation.

公开(公告)号：US5051499A

公开(公告)日：1991-09-24

申请号：US445965

申请日：1989-11-28

申请人： Satoshi Shuto ,  Hiromichi Itoh ,  Kiyofumi Fukukawa ,  Masatoshi Tsujino

发明人： Satoshi Shuto ,  Hiromichi Itoh ,  Kiyofumi Fukukawa ,  Masatoshi Tsujino

IPC分类号： C07D473/00 ,  C07H19/10

CPC分类号： C07D473/00 ,  C07H19/10

摘要： Novel nucleoside-phospholipid conjugates of the formula ##STR1## wherein R.sub.1 is C.sub.14-24 long chain aliphatic acyl or C.sub.1-24 aliphatic alkyl, R.sub.2 is C.sub.2-10 aliphatic acyl or C.sub.1-24 aliphatic alkyl and N.sub.s is a nucleoside residue; and pharmacologically acceptable salts thereof are prepared in a one-step reaction by reacting the corresponding nucleoside and glycerophospholipid derivative in the presence of phospholipase D-P.

公开(公告)号：US4877877A

公开(公告)日：1989-10-31

申请号：US260904

申请日：1988-10-19

申请人： Masao Yaso ,  Yukio Suzuki ,  Kensuke Shibata ,  Eiichi Hayashi

发明人： Masao Yaso ,  Yukio Suzuki ,  Kensuke Shibata ,  Eiichi Hayashi

IPC分类号： C07D243/00 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61P3/06 ,  A61P7/02 ,  A61P9/08 ,  C07D241/18 ,  C07D241/44 ,  C07D247/00 ,  C07D333/00 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D409/12 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/18 ,  C07D241/44 ,  C07D249/08 ,  C07D403/06 ,  C07D409/12

摘要： 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of hydroxyl, halogen, lower alkanocyloxy, R.sub.4 -carbamoyloxy and arylthio, in which R.sub.4 is lower alkyl or aryl; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

公开(公告)号：US4877733A

公开(公告)日：1989-10-31

申请号：US42655

申请日：1987-04-28

申请人： Mamoru Takahashi ,  Shigeyuki Imamura ,  Masaki Takada

发明人： Mamoru Takahashi ,  Shigeyuki Imamura ,  Masaki Takada

IPC分类号： C12N9/04

CPC分类号： C12N9/0006 ,  Y10S435/911

摘要： Glucose dehydrogenase having the following biochemial properties:(a) enzymatic action: catalyzes a reaction which generates glucono-.delta.-lactone and reduced NADP from glucose and NADP;(b) substrate specificity: has substrate specificity on glucose and no substrate specificity on 2-deoxyglucose;(c) optimum pH: pH 6-8,(d) optimum temperature: approximately 55.degree. C.,(e) pH-stability: stable at pH 6.0-7.5,(f) molecular weight: 11.times.10.sup.4 .+-.11000,(g) Km-value: 2.6.times.10.sup.-3 .+-.2.6.times.10.sup.-4 M(glucose) 4.2.times.10.sup.-6 35 4.2.times.10.sup.-7 M(NADP) and(h) isoelectric point: 4.9.+-.0.5,comprises culturing a glucose dehydrogenase-producing microorganism Cryptococcus uniguttulatus Y 0033 FERM P-8709, now FERM BP-1352 in a nutrient medium and isolating glucose dehydrogenase thus produced from the cultured medium.

摘要翻译： 具有以下生物化学性质的葡萄糖脱氢酶：（a）酶促作用：催化从葡萄糖和NADP产生葡萄糖酸-δ-内酯和还原的NADP的反应; （b）底物特异性：对葡萄糖具有底物特异性，对2-脱氧葡萄糖没有底物特异性; （c）最适pH：pH 6-8，（d）最适温度：约55℃，（e）pH稳定性：pH 6.0-7.5稳定，（f）分子量：11×10 4 +/- 11000，（g ）Km值：2.6×10 -3 +/- 2.6×10 -4 M（葡萄糖）4.2×10-635 4.2×10-7M（NADP）和（h）等电点：4.9 +/- 0.5，包括培养产生葡萄糖脱氢酶 微生物隐球酵母Y 0033 FERM P-8709，现在是营养培养基中的FERM BP-1352，并从培养基中分离出葡萄糖脱氢酶。

公开(公告)号：US4845028A

公开(公告)日：1989-07-04

申请号：US244513

申请日：1988-09-09

申请人： Shigeyuki Imamura ,  Hideo Misaki

发明人： Shigeyuki Imamura ,  Hideo Misaki

IPC分类号： C12Q1/44 ,  C12Q1/34 ,  C12Q1/61

CPC分类号： C12Q1/34 ,  G01N2333/918

摘要： A composition and method for lipase assay, comprising the use of an aqueous solution of a 1,2-diglyceride of a higher fatty acid, and a nonionic surface active agent. The higher fatty acid is a higher fatty acid of 8 or more and preferably 12 or more carbons, most preferably a higher unsaturated fatty acid of more than 16 carbons. The concentration of 1,2-diglyceride is more than 0.5 g per liter of solution. The nonionic surface active agent is a polyoxyethylene-type nonionic surface active agent, a polyhydric-alcohol-type nonionic surface active agent or a block-polymer-type nonionic surface active agent, whose concentration is more than 0.1% by weight in the composition and which has an HLB more than 10. The composition preferably contains 0.5-10 g of 1,2-diglyceride and 10-50 g of nonionic surface active agent per liter of solution.

摘要翻译： 脂肪酶测定的组合物和方法，包括使用高级脂肪酸的1,2-二甘油酯的水溶液和非离子表面活性剂。 高级脂肪酸是8个以上且优选12个或更多个碳的高级脂肪酸，最优选高于16个碳的较高不饱和脂肪酸。 1,2-二甘油酯的浓度高于每升溶液0.5g。 非离子表面活性剂是组合物中浓度大于0.1重量％的聚氧乙烯型非离子表面活性剂，多元醇型非离子表面活性剂或嵌段聚合物型非离子表面活性剂， 其HLB大于10.该组合物优选每升溶液含有0.5-10g的1,2-二甘油酯和10-50g的非离子表面活性剂。

公开(公告)号：US4837319A

公开(公告)日：1989-06-06

申请号：US20012

申请日：1987-02-25

申请人： Masao Yaso ,  Yukio Suzuki ,  Kensuke Shibata ,  Eiichi Hayashi

发明人： Masao Yaso ,  Yukio Suzuki ,  Kensuke Shibata ,  Eiichi Hayashi

IPC分类号： C07D243/00 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61P3/06 ,  A61P7/02 ,  A61P9/08 ,  C07D241/18 ,  C07D241/44 ,  C07D247/00 ,  C07D333/00 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D409/12 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/18 ,  C07D241/44 ,  C07D249/08 ,  C07D403/06 ,  C07D409/12

摘要： 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

公开(公告)号：US4816575A

公开(公告)日：1989-03-28

申请号：US877758

申请日：1986-06-24

申请人： Kiyofumi Fukukawa ,  Takao Hirano ,  Masatoshi Tsujino ,  Tooru Ueda

发明人： Kiyofumi Fukukawa ,  Takao Hirano ,  Masatoshi Tsujino ,  Tooru Ueda

IPC分类号： C07D473/34 ,  A61K31/52 ,  A61P35/00 ,  C07D473/00 ,  C07F9/6561 ,  C07H19/20 ,  C07D473/30

CPC分类号： C07D473/00 ,  C07F9/65616 ,  C07H19/20 ,  Y02P20/55

摘要： Neplanocin A derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen or benzoyl, R.sub.4 is hydrogen or halogen, hydroxy, acetoxy, acetylthio, amino or azide, R.sub.5 is hydrogen or acetyl, and R.sub.6 is hydrogen or acetyl. The compounds of the present invention have inhibitory action for the growth of L 5178 Y cells and have the same or superior activity as neplanocin A.

摘要翻译： 其中R 1为氢或苯甲酰基，R 4为氢或卤素，羟基，乙酰氧基，乙酰硫基，氨基或叠氮基，R 5为氢或乙酰基，且R 6为氢或乙酰基的萘普鲁星A衍生物。 本发明化合物对L 5178 Y细胞的生长具有抑制作用，具有与奈普洛诺菌素A相同或优异的活性。

公开(公告)号：US4788147A

公开(公告)日：1988-11-29

申请号：US865584

申请日：1986-05-21

申请人： Shigeyuki Imamura ,  Hideo Misaki

发明人： Shigeyuki Imamura ,  Hideo Misaki

IPC分类号： G01N33/92 ,  C12Q1/26 ,  C12Q1/44 ,  C12N9/06

CPC分类号： C12Q1/44 ,  C12Q1/26 ,  C12Q2326/96 ,  G01N2333/906 ,  G01N2333/916 ,  G01N2405/04 ,  Y10S435/832

摘要： Ethanolamine in a sample can be assayed by treating the sample with ethanolamine oxidase, thereby to catalyze a reaction-consuming ethanolamine, oxygen and water, and forming glycolaldehyde, ammonia and hydrogen peroxide. The amount of consumed oxygen or the amount of generated ammonia or hydrogen peroxide is then determined, as a measure of the ethanolamine that was originally the sample. The ethanolamine can appear in the sample as such, or can be liberated simultaneously with or prior to the catalysis reaction, from an ethanolamine derivative, e.g. phosphatidyl ethanolamine by the action of phospholipase D. Ethanolamine oxidase can be produced from Bacillus sp. B-0783 FERM-P No. 5798 in a conventional culture medium, preferably by submerged aeration liquid culturation.

摘要翻译： 通过用乙醇胺氧化酶处理样品可以测定样品中的乙醇胺，从而催化消耗反应的乙醇胺，氧和水，并形成乙二醇，氨和过氧化氢。 然后测定消耗的氧气的量或产生的氨或过氧化氢的量，作为最初为样品的乙醇胺的量度。 乙醇胺可以如此出现在样品中，或者可以与催化反应同时或之前从乙醇胺衍生物例如乙醇胺衍生物中释放出来。 磷脂酰乙醇胺通过磷脂酶D的作用。乙醇胺氧化酶可以从芽孢杆菌sp。 B-0783 FERM-P No.5798，优选通过浸没曝气液体培养。

公开(公告)号：US4556634A

公开(公告)日：1985-12-03

申请号：US506844

申请日：1983-06-22

申请人： Hideo Misaki ,  Masahiko Taniuchi

发明人： Hideo Misaki ,  Masahiko Taniuchi

IPC分类号： C12Q1/00 ,  C12Q1/26 ,  C12Q1/32

CPC分类号： C12Q1/008

摘要： A high sensitivity assay method of the coenzyme cyclic assay type, eliminates the need for a separate indication reaction, by using the cycling reaction itself as the indication reaction, according to the following steps: ##STR1## the thus-formed formazan is then colorimetrically measured, to give a highly sensitive determination of the quantity of the substance to be assayed, e.g. NAD.sup.+, NADP.sup.+, malic acid or .gamma.-aminobutyric acid in human serum.

摘要翻译： 根据以下步骤，通过使用循环反应本身作为指示反应，辅酶循环测定型的高灵敏度测定方法不需要单独的指示反应：（1）主反应体系：其中AH2 或A：要测定的物质; NAD（P）+：NAD +或NADP +; NAD（P）H：还原形式的NAD +或NADP +; （2）分解反应：中和：碱中和：其中M：碱金属和R：低级烷基; （3）循环反应：然后比色测定如此形成的甲，，以测定待测物质的量的高灵敏度。 NAD +，NADP +，苹果酸或γ-氨基丁酸。