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71 条记录 (耗时 0.021 秒)

    Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and &agr;-1-blocking action
    12.
    发明授权
    Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and &agr;-1-blocking action 失效
    具有5-羟色胺受体拮抗作用和α-1-阻断作用的吡罗噻嗪和吡咯并噻吩类化合物

    公开(公告)号：US06743913B2

    公开(公告)日：2004-06-01

    申请号：US10421929

    申请日：2003-04-24

    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： C07D51304

    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。

    Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and alpha-1-blocking action
    13.
    发明授权
    Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and alpha-1-blocking action 失效
    具有5-羟色胺受体拮抗作用和α-1-阻断作用的吡罗噻嗪和吡咯并噻吩类化合物

    公开(公告)号：US06331623B1

    公开(公告)日：2001-12-18

    申请号：US09367842

    申请日：1999-08-26

    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： C07O51334

    CPC分类号： C07D513/04 ,  C07D207/36

    摘要： A pyrrolesulfonamide compound having formula (I) wherein the ring P represented by &agr; is a pyrrole ring having structure &bgr; or &psgr; wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group &dgr; 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 a &agr;1-blocking action and serotonin-2 receptor antagonistic action in combination.

    摘要翻译： 具有式（I）的吡咯磺酰胺化合物，其中由α表示的环P是具有β或psi结构的吡咯环，其中A表示亚烷基，亚烯基或亚炔基; 并且Y表示其中W表示CH，C =或N的组δ; 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）对于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，对5-羟色胺-2受体以外的受体的效力，选择性，毒性，副作用等改善， 结合。

    Herbicidally active phenoxyalkanecarboxylic acid derivatives
    15.
    发明授权
    Herbicidally active phenoxyalkanecarboxylic acid derivatives 失效
    除草活性苯氧亚硬脂酸衍生物

    公开(公告)号：US4976773A

    公开(公告)日：1990-12-11

    申请号：US230481

    申请日：1988-08-10

    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： A01N37/02 ,  A01N37/18 ,  A01N37/24 ,  A01N39/02 ,  A01N39/04 ,  A01N41/06 ,  A01N43/40 ,  A01N47/12 ,  A01N47/24 ,  C07C69/712 ,  C07C205/38 ,  C07C255/54 ,  C07C311/39 ,  C07D213/64 ,  C07D213/643 ,  C07D213/84 ,  C07D213/85

    CPC分类号： C07D213/643 ,  A01N39/02 ,  A01N39/04 ,  A01N41/06 ,  A01N43/40 ,  A01N47/12 ,  A01N47/24 ,  C07C205/38 ,  C07C255/54 ,  C07C311/39

    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 alkxoycarobnyl; 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 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Q 2和Q 3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 1 -C 5烷氧基羰基; R 3，R 4和R 5各自为H或C 1 -C 5烷基; R 6是H，卤素或C 1 -C 5烷基; R 7，R 8，R 9和R 1各自为H或C 1 -C 5烷基; R 1是H，C 1 -C 5烷基，C 1 -C 5烷氧基，C 2 -C 6烯基，C 6 -C 10芳基，C 7 -C 15芳氧基烷基或C 7 -C 15芳烷基; R 1，R 2和R 3各自为H或C 1 -C 5烷基; R 1为C 1 -C 5烷基，C 2 -C 6烯基，C 5 -C 10芳基或C 7 -C 15芳烷基; 或R 1 3和R 1 4。 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; V 3是卤素或CF 3; W 1是-O-或-NH-; W 2为 - （CH 2）n - ，其中n为0或1，或CO; X 1是作为除草剂有效的卤素或其盐。

    Phenylpiperazine derivatives and their acid addition salts
    16.
    发明授权
    Phenylpiperazine derivatives and their acid addition salts 失效
    苯基哌嗪衍生物及其酸加成盐

    公开(公告)号：US4716161A

    公开(公告)日：1987-12-29

    申请号：US719456

    申请日：1985-04-03

    申请人： Harukazu Fukami ,  Ryoji Kikumoto ,  Kenichiro Nakao ,  Issei Nitta ,  Shinya Inoue

    发明人： Harukazu Fukami ,  Ryoji Kikumoto ,  Kenichiro Nakao ,  Issei Nitta ,  Shinya Inoue

    IPC分类号： C07D239/96 ,  C07D285/32 ,  C07D491/04 ,  C07D491/056 ,  C07D513/04 ,  A61K31/54 ,  C07D417/06

    CPC分类号： C07D491/04 ,  C07D239/96 ,  C07D285/32 ,  C07D513/04

    摘要： A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention. The phenylpiperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.

    摘要翻译： 根据本发明的苯基哌嗪衍生物具有以下通式[I]：其中R 1，R 2和R 3独立地是氢或具有1至3个碳原子的烷氧基，或者R 1和R 2或R 2和R 3 与其连接的碳原子一起形成-O（CH 2）m O-，其中m是1至3的整数，或者R 1或R 2是选自-NH 2，-NHSO 2 CH 3，-NHCOCH 3和 -NHCONH 2，另一个是1或3个碳原子的氢或烷氧基，R 3是氢; R4和R5独立地是氢或1〜3个碳原子的烷基; Y是-CO-或-SO 2 - ，条件是当Y是-CO-时，R 1和R 2中的至少一个不是氢; n为2〜4的整数。本发明包括具有通式[I]的苯基哌嗪衍生物的酸加成盐。 根据本发明的苯基哌嗪衍生物及其酸加成盐具有降低血压的能力。

    2-O- (β-D-glucopyranosyl) ascorbic acid, process for its production, and foods and cosmetics containing compositions comprising it
    19.
    发明授权
    2-O- (β-D-glucopyranosyl) ascorbic acid, process for its production, and foods and cosmetics containing compositions comprising it 有权
    2-O-（＆bgr--D-吡喃葡萄糖基）抗坏血酸，其生产方法，以及含有组合物的组合物的食品和化妆品

    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。

    Process for producing powdered compositions containing highly unsaturated fatty acid esters of ascorbic acid and powdered compositions containing the esters
    20.
    发明授权
    Process for producing powdered compositions containing highly unsaturated fatty acid esters of ascorbic acid and powdered compositions containing the esters 有权
    制备含有抗坏血酸的高度不饱和脂肪酸酯的粉末状组合物和含有酯的粉末状组合物的方法

    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。