公开(公告)号：US08017587B2

公开(公告)日：2011-09-13

申请号：US11898121

申请日：2007-09-10

申请人： Mitsuru Maeda ,  Masahiro Nakao ,  Harukazu Fukami

发明人： Mitsuru Maeda ,  Masahiro Nakao ,  Harukazu Fukami

IPC分类号： A01N43/04 ,  A01N43/08

CPC分类号： A61K8/676 ,  A23L33/105 ,  A23L33/15 ,  A23V2002/00 ,  A61K8/602 ,  A61K31/375 ,  A61K2800/52 ,  A61Q17/04 ,  A61Q19/00 ,  A61Q19/02 ,  C07H1/08 ,  C07H17/04 ,  C12P19/60 ,  A23V2250/708

摘要： The present invention provides a novel ascorbic acid derivative as a provitamin C with improved stability in the body and prolonged life in the body compared to conventionally known 2-O-(α-D-glucopyranosyl)ascorbic acid.The composition comprising the novel compound 2-O-(β-D-glucopyranosyl)ascorbic acid has been extracted from plants such as from Ningxia Lycium barbarum L. and/or Lycium chinense Mill. The compositions comprising 2-O-(β-D-glucopyranosyl)ascorbic acid may be enzymatically synthesized using β-D-glucosyltransferase. Pure 2-O-(β-D-glucopyranosyl)ascorbic acid may be produced from such compositions. Alternatively, 2-O-(β-D-glucopyranosyl)ascorbic acid may be produced by chemical synthesis. The 2-O-(β-D-glucopyranosyl)ascorbic acid results in higher stability and a prolonged life of vitamin C when ingested in the body compared to the corresponding α-D-glucopyranosyl derivative, and is therefore highly suitable as a provitamin C to be used in cosmetics and foods.

摘要翻译： 与常规已知的2-O-（α-D-吡喃葡萄糖基）抗坏血酸相比，本发明提供了一种新型抗坏血酸衍生物作为维生素C，具有改善体内的稳定性和延长的身体寿命。 从宁夏枸杞子和/或枸杞子植物提取含有新化合物2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸的组合物。 可以使用β-葡萄糖基转移酶酶法合成包含2-O-（β-谷氨酰-D-吡喃葡萄糖基）抗坏血酸的组合物。 可以从这样的组合物制备纯2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸。 或者，可通过化学合成制备2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸。 与对应的α-D-吡喃葡萄糖基衍生物相比，2-O-（＆bgr-D-吡喃葡萄糖基）抗坏血酸在身体摄取时导致更高的稳定性和更长的维生素C的使用寿命，因此非常适合作为维生素 C用于化妆品和食品。

公开(公告)号：US07989642B2

公开(公告)日：2011-08-02

申请号：US10547259

申请日：2004-02-27

申请人： Harukazu Fukami

发明人： Harukazu Fukami

IPC分类号： C07D307/62 ,  C08K2/16

CPC分类号： C11C3/04 ,  A23D9/05

摘要： The invention provides a process for powdering highly unsaturated fatty acid esters of ascorbic acid which are pasty and problematic in physical properties by a simple and easy means; highly unsaturated fatty acid esters of ascorbic acid which are improved in stability by powdering; and compositions containing the powdered highly unsaturated fatty acid esters of ascorbic acid. Specifically, a process for powdering a highly unsaturated fatty acid ester of ascorbic acid as represented by the general formula (I): RCO-A [wherein RCO— is acyl derived from a highly unsaturated fatty acid; and A is an ascorbic acid residue bonded through an —O— linkage resulting from an hydroxyl group of ascorbic acid], characterized by mixing a highly unsaturated fatty acid ester of ascorbic acid as represented by the general formula (I) with an aqueous solution of a water-soluble filler to form an emulsion and dehydrating and drying the emulsion by a spray drying method.

摘要翻译： 本发明提供了一种通过简单方便的方法粉化糊状的高度不饱和脂肪酸的抗坏血酸和物理性质问题的方法; 通过粉化提高稳定性的抗坏血酸的高度不饱和脂肪酸酯; 以及含有抗坏血酸的粉末状高度不饱和脂肪酸酯的组合物。 具体而言，是将通式（I）表示的抗坏血酸高度不饱和脂肪酸酯粉末化的方法：RCO-A [其中，RCO-为高度不饱和脂肪酸衍生的酰基， A是通过由抗坏血酸的羟基产生的-O-键连接的抗坏血酸残基]，其特征在于将由通式（I）表示的抗坏血酸的高度不饱和脂肪酸酯与 水溶性填料以形成乳液，并通过喷雾干燥方法使乳液脱水和干燥。

公开(公告)号：US20080058409A1

公开(公告)日：2008-03-06

申请号：US11795959

申请日：2006-01-25

申请人： Harukazu Fukami ,  Masahiro Nakao ,  Koshi Namikawa ,  Mitsuru Maeda

发明人： Harukazu Fukami ,  Masahiro Nakao ,  Koshi Namikawa ,  Mitsuru Maeda

IPC分类号： A61K31/352 ,  A61P31/04 ,  C07D311/04 ,  C12P17/06

CPC分类号： C12P17/06 ,  A01N43/16 ,  A23L3/3472 ,  A23L3/3517 ,  A61K8/498 ,  A61Q17/005 ,  C07D311/62

摘要： The present invention provides substances having sufficiently antibacterial activity against heat-resistant spore-forming bacteria that they can be used to improve the shelf life of beverages and processed foods, as well as to control the growth of microorganisms in cosmetics. The present invention provides a catechin ester in which at least one of the hydroxyl groups of a catechin is esterified with a medium-chain fatty acid. This medium-chain fatty acid ester of a catechin, which may be used either alone or as a composition, shows a strong growth suppressing effect on heat-resistant spore-forming bacteria and, if added to foods or beverages, can prevent them from rotting or deterioration and, if added to cosmetics, can prevent their rotting or deterioration.

摘要翻译： 本发明提供对耐热孢子形成细菌具有足够抗菌活性的物质，它们可用于改善饮料和加工食品的保质期，以及控制化妆品中微生物的生长。 本发明提供一种儿茶素酯，其中儿茶素的至少一个羟基与中链脂肪酸酯化。 可以单独或作为组合物使用的儿茶素的该中链脂肪酸酯对耐热孢子形成细菌具有强烈的生长抑制作用，如果添加到食品或饮料中，可以防止它们的腐烂 或变质，如果添加到化妆品中，可以防止其腐烂或变质。

公开(公告)号：US06867214B1

公开(公告)日：2005-03-15

申请号：US09763213

申请日：1999-08-20

申请人： Harukazu Fukami ,  Akiko Ito ,  Seiichi Imajo

发明人： Harukazu Fukami ,  Akiko Ito ,  Seiichi Imajo

IPC分类号： A61K31/517 ,  A61K31/538 ,  A61P7/00 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P19/02 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C311/60 ,  C07D239/96 ,  C07D401/12 ,  C07D413/12

CPC分类号： C07D401/12 ,  C07C311/60 ,  C07D239/96 ,  C07D413/12

摘要： A quinazoline derivative having formula (1) and a pharmaceutically acceptable salt thereof: wherein the ring A represents an aryl group, which derivative has a chymase inhibitory activity and suppresses the exacerbation of vascular permeability induced by chymase, and a pharmaceutical composition containing the same as an essential ingredient. These compounds are useful for treatment of allergic diseases, rheumatic diseases, and cardiac and circulatory system diseases which are due to the abnormal exacerbation of Angiotensin II production.

摘要翻译： 具有式（1）的喹唑啉衍生物及其药学上可接受的盐：其中环A表示芳基，该衍生物具有糜酶抑制活性，并抑制由胃促胰酶诱导的血管通透性恶化，以及含有 一个必不可少的成分。 这些化合物可用于治疗由于血管紧张素II产生异常恶化而引起的过敏性疾病，风湿性疾病以及心脏和循环系统疾病。

公开(公告)号：US06583296B2

公开(公告)日：2003-06-24

申请号：US09939829

申请日：2001-08-28

申请人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

发明人： Akira Mizuno ,  Makoto Shibata ,  Tomoe Kamei ,  Harukazu Fukami ,  Norio Inomata

IPC分类号： C07D20736

CPC分类号： C07D513/04 ,  C07D207/36

摘要： A pyrrolesulfonamide compound having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with &agr;1-blocking action and serotonin-2 receptor antagonistic action in combination.

摘要翻译： 具有下式（I）的吡咯磺酰胺化合物：其中由具有以下结构的吡咯环表示的环P：其中A表示亚烷基，亚烯基或亚炔基; Y表示W表示CH，C =或N的基团; 当W为CH或N时，m代表0或1，当W为C =时，m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基; l代表0或1; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但当不存在键时，Z1表示H，Z2表示OH或Z1，Z2组合在一起表示O或NOR5基团，其中R5表示 H或烷基，芳烷基或芳基; R代表H，烷基，环烷基，环烷基 - 烷基或芳烷基。 化合物（1）对迄今为止报道的并且具有α1-阻断作用和5-羟色胺-2受体拮抗作用的药物的效力，对5-羟色胺2受体以外的受体的选择性，毒性，副作用等改善 组合。

公开(公告)号：US5205855A

公开(公告)日：1993-04-27

申请号：US578254

申请日：1990-09-06

申请人： Harukazu Fukami ,  Naoki Higuchi ,  Naoko Kawaguchi ,  Masaki Hashimoto ,  Kinya Ide ,  Toshio Takahashi

发明人： Harukazu Fukami ,  Naoki Higuchi ,  Naoko Kawaguchi ,  Masaki Hashimoto ,  Kinya Ide ,  Toshio Takahashi

IPC分类号： A01N39/02 ,  A01N39/04 ,  A01N41/06 ,  A01N43/40 ,  A01N47/12 ,  A01N47/24 ,  C07C69/712 ,  C07C205/38 ,  C07D213/64 ,  C07D213/643

CPC分类号： C07D213/643 ,  A01N39/02 ,  A01N39/04 ,  A01N41/06 ,  A01N43/40 ,  A01N47/12 ,  A01N47/24 ,  C07C205/38 ,  C07C69/712

摘要： A compound of the formula: ##STR1## wherein Q.sup.1 is CH or N; R is H or C.sub.1 -C.sub.5 alkyl; X is H, halogen, CF.sub.3, or NO.sub.2 ; Y is H or halogen; Z is --O-- or --NH--; A is ##STR2## wherein Q.sup.2, and Q.sup.3 are each CH or N; R.sup.1 and R.sup.2 are each H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, or C.sub.2 -C.sub.6 alkoxycarbonyl; R.sup.3, R.sup.4, and R.sup.5 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.6 is H, halogen, or C.sub.1 -C.sub.5 alkyl; R.sup.7, R.sup.8, R.sup.9, and R.sup.10 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.11 is H, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.2 -C.sub.6 alkenyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.15 aryloxyalkyl, or C.sub.7 -C.sub.15 aralkyl; R.sup.12 and R.sup.13 are each H or C.sub.1 -C.sub.5 alkyl; R.sup.14 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.5 -C.sub.10 aryl, or C.sub.7 -C.sub.15 aralkyl; or R.sup.13 and R.sup.14 taken together form C.sub.3 -C.sub.4 alkylene, V.sup.1 and V.sup.2 and are each H, halogen, NO.sub.2, CN, or CF.sub.3 ; V.sup.3 is halogen or CF.sub.3 ; W.sup.1 is --O-- or --NH--; W.sup.2 is --(CH.sub.2).sub.n -- wherein n is 0 or 1, or CO; X.sup.1 is halogen, or a salt thereof, which is effective as a herbicidal agent.

摘要翻译： 下式的化合物：其中Q 1是CH或N; R是H或C 1 -C 5烷基; X是H，卤素，CF 3或NO 2; Y为H或卤素; Z是-O-或-NH-; A是 其中Q2和Q3各自为CH或N; R 1和R 2各自为H，C 1 -C 5烷基，C 1 -C 5烷氧基或C 2 -C 6烷氧基羰基; R 3，R 4和R 5各自为H或C 1 -C 5烷基; R6是H，卤素或C1-C5烷基; R 7，R 8，R 9和R 10各自为H或C 1 -C 5烷基; R11是H，C1-C5烷基，C1-C5烷氧基，C2-C6烯基，C6-C10芳基，C7-C15芳氧基烷基或C7-C15芳烷基; R 12和R 13各自为H或C 1 -C 5烷基; R14是C1-C5烷基，C2-C6烯基，C5-C10芳基或C7-C15芳烷基; 或R 13和R 14一起形成C 3 -C 4亚烷基，V 1和V 2，各自为H，卤素，NO 2，CN或CF 3; V3是卤素或CF 3; W1是-O-或-NH-; W2是 - （CH2）n-，其中n是0或1，或CO; X1是作为除草剂有效的卤素或其盐。

公开(公告)号：US5039696A

公开(公告)日：1991-08-13

申请号：US473632

申请日：1990-02-01

申请人： Shinjiro Niwata ,  Harukazu Fukami ,  Masaki Hashimoto ,  Norio Ohtsuka ,  Fumio Fujita

发明人： Shinjiro Niwata ,  Harukazu Fukami ,  Masaki Hashimoto ,  Norio Ohtsuka ,  Fumio Fujita

IPC分类号： C07D207/452 ,  A01N37/46 ,  C07D207/44 ,  C07D207/456

CPC分类号： C07D207/456 ,  A01N37/46

摘要： A maleimide derivative useful as an active agent for a fungicide for agriculture and horticulture, having the formula (I): ##STR1## wherein X and Y each independently represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group or a trifluoromethyl group,Z represents a chlorine atom or bromine atom,and R represents a straight or branched alkyl group having 1 to 15 carbon atoms, an alkenyl group having 2 to 5 carbon atoms, an alkynyl group having 2 to 5 carbon atoms, an alkoxyalkyl group having 2 to 5 carbon atoms, an oxoalkyl group having 3 to 6 carbon atoms or a phenyl group or a phenyl alkyl group which may be substituted.

公开(公告)号：US4684739A

公开(公告)日：1987-08-04

申请号：US326417

申请日：1981-12-01

申请人： Ryoji Kikumoto ,  Harukazu Fukami ,  Kenichiro Nakao ,  Mamoru Sugano

发明人： Ryoji Kikumoto ,  Harukazu Fukami ,  Kenichiro Nakao ,  Mamoru Sugano

IPC分类号： C07D317/64 ,  C07D319/20 ,  C07D407/12 ,  C07D321/10

CPC分类号： C07D407/12 ,  C07D317/64 ,  C07D319/20

摘要： Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.

摘要翻译： 制备了亚烷基二氧基苯衍生物，发现其可用作药剂，特别是作为低渗剂。

公开(公告)号：US08383384B2

公开(公告)日：2013-02-26

申请号：US13530914

申请日：2012-06-22

申请人： Misa Ochiai ,  Harukazu Fukami ,  Masahiro Nakao ,  Akio Noguchi

发明人： Misa Ochiai ,  Harukazu Fukami ,  Masahiro Nakao ,  Akio Noguchi

IPC分类号： C12N9/28

CPC分类号： C12N9/1048

摘要： The present invention provides novel glycosyltransferase proteins produced by ascomycetous filamentous fungi (preferably species belonging to the genus Trichoderma, more preferably Trichoderma viride), as well as genes encoding the same. Among novel enzyme proteins provided by the present invention, particularly preferred is an enzyme protein obtained from the culture supernatant of Trichoderma viride strain IAM5141. The novel enzymes of the present invention allow glycosylation of flavonoid compounds to thereby improve their water solubility.

摘要翻译： 本发明提供了由Ascomycetoto丝状真菌（优选属于木霉属，更优选绿色木霉）的物质以及编码它们的基因产生的新的糖基转移酶蛋白质。 在本发明提供的新型酶蛋白中，特别优选从绿色木霉菌株IAM5141的培养物上清液获得的酶蛋白质。 本发明的新型酶可以使类黄酮化合物进行糖基化从而提高其水溶性。

公开(公告)号：US08278088B2

公开(公告)日：2012-10-02

申请号：US12523068

申请日：2008-01-18

申请人： Misa Ochiai ,  Harukazu Fukami ,  Masahiro Nakao ,  Akio Noguchi

发明人： Misa Ochiai ,  Harukazu Fukami ,  Masahiro Nakao ,  Akio Noguchi

IPC分类号： C12N1/20 ,  C12N1/00 ,  C12N1/12 ,  C12N5/04 ,  C12N5/00 ,  C12N15/00 ,  C07H21/04

CPC分类号： C12N9/1048

摘要： The present invention provides novel glycosyltransferase proteins produced by ascomycetous filamentous fungi (preferably species belonging to the genus Trichoderma, more preferably Trichoderma viride), as well as genes encoding the same. Among novel enzyme proteins provided by the present invention, particularly preferred is an enzyme protein obtained from the culture supernatant of Trichoderma viride strain IAM5141. The novel enzymes of the present invention allow glycosylation of flavonoid compounds to thereby improve their water solubility.

摘要翻译： 本发明提供了由Ascomycetoto丝状真菌（优选属于木霉属，更优选绿色木霉）的物质以及编码它们的基因产生的新的糖基转移酶蛋白质。 在本发明提供的新型酶蛋白中，特别优选从绿色木霉菌株IAM5141的培养物上清液获得的酶蛋白质。 本发明的新型酶可以使类黄酮化合物进行糖基化从而提高其水溶性。