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    Azoxy compound
    2.
    发明授权
    Azoxy compound 失效
    偶氮化合物

    公开(公告)号：US5541169A

    公开(公告)日：1996-07-30

    申请号：US232245

    申请日：1994-05-10

    Applicant: Takeo Deushi ,  Yoshio Takahashi ,  Hiroyuki Ishiwata ,  Yukihiro Okuno ,  Toshiaki Oda ,  Masami Shiratsuchi ,  Katsuhiro Yamamoto

    Inventor： Takeo Deushi ,  Yoshio Takahashi ,  Hiroyuki Ishiwata ,  Yukihiro Okuno ,  Toshiaki Oda ,  Masami Shiratsuchi ,  Katsuhiro Yamamoto

    IPC: A01N51/00 ,  C07C291/08 ,  A61K31/655

    CPC classification number: C07C291/08 ,  A01N51/00

    Abstract: An azoxy compound represented by the following general formula ##STR1## wherein R.sub.1 denotes a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkoxy group, a lower alkoxy-lower alkoxy group or a group of the formula X.sub.1 --C.tbd.C--CH.sub.2 O-- wherein X.sub.1 is a hydrogen atom or a halogen atom;R.sub.2 denotes a hydrogen atom or a lower alkyl group;R.sub.3 denotes a hydrogen atom or a lower alkyl group;R.sub.4 denotes a hydrogen atom or a group of the formula X.sub.2 --C.tbd.C--CH.sub.2 -- wherein X.sub.2 is a hydrogen atom or a halogen atom;R.sub.5 denotes a hydrogen atom or a lower alkyl group;andn is 0 or 1.This compound has an excellent antifungal activity against fungi infectious to warm-blooded animals and fungi infectious to agrohorticultural crops or fruit trees, and is useful as a medicine, a veterinary drug and an agrohorticultural antifungal agent.

    Abstract translation: PCT No.PCT / JP93 / 01295 Sec。 371日期1994年5月10日 102（e）日期1994年5月10日PCT提交1993年9月10日PCT公布。 出版物WO94 / 05629 日期：1994年3月17日由以下通式表示的氧化偶氮化合物（Ⅰ）其中R1表示氢原子，卤原子，羟基，低级烷氧基，低级烷氧基 - 低级烷氧基或基团 式X1-C3Bic C-CH2O-，其中X1是氢原子或卤素原子; R2表示氢原子或低级烷基; R3表示氢原子或低级烷基; R4表示氢原子或式X2-C 3BOND C-CH2-的基团，其中X2是氢原子或卤素原子; R5表示氢原子或低级烷基; 并且n为0或1.该化合物对感染了农作物或果树的温血动物和真菌感染真菌具有优异的抗真菌活性，并且可用作药物，兽药和农业园艺抗真菌剂。

    Thrombin-binding substance and process for preparing the same
    4.
    发明授权
    Thrombin-binding substance and process for preparing the same 失效
    凝血酶结合物质及其制备方法

    公开(公告)号：US4748156A

    公开(公告)日：1988-05-31

    申请号：US3465

    申请日：1987-01-15

    Applicant: Nobuo Aoki ,  Masami Shiratsuchi ,  Shigeru Kimura

    Inventor： Nobuo Aoki ,  Masami Shiratsuchi ,  Shigeru Kimura

    IPC: A61K35/50 ,  A61K38/16 ,  C07G99/00 ,  C07K3/20 ,  C07K3/28

    CPC classification number: A61K35/50

    Abstract: A novel thrombin-binding substance having the characteristics of (a) molecular weight: 47,000.+-.6,000 in reduced condition and 38,000.+-.6,000 in unreduced condition, (b) isoelectric point: pH 4.9-5.7, (c) affinity: strong affinity to thrombin, (d) activity: (1) capable of promoting the thrombin catalyzed activation of protein C, (2) prolongs clotting time; and (e) stability: stable to denaturing agents (urea sodium and dodecylsulfate), can be prepared from a human placenta by means of extraction, fractionation using ion exchange chromatography and affinity chromatography, and/or gel filtration, followed by electrophoresis. The substance is useful as a medicine for the treatment of thrombosis.

    Abstract translation: 一种具有以下特性的新型凝血酶结合物质：（a）分解质量为47,000 +/- 6,000，还原条件为38,000 +/- 6,000，（b）等电点：pH 4.9-5.7，（c）亲和力： （d）活性：（1）能促进凝血酶催化蛋白C的活化，（2）延长凝血时间; 和（e）稳定性：对变性剂（尿素钠和十二烷基硫酸盐）稳定，可以通过提取，使用离子交换层析和亲和层析分离，和/或凝胶过滤，然后电泳从人胎盘制备。 该物质可用作治疗血栓形成的药物。

    Tetrahydroxanthone derivatives
    7.
    发明授权
    Tetrahydroxanthone derivatives 失效
    四氢呫吨酮衍生物

    公开(公告)号：US4290954A

    公开(公告)日：1981-09-22

    申请号：US89403

    申请日：1979-10-30

    Applicant: Kazuhiro Onogi ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Masami Shiratsuchi ,  Masahiko Nagakura ,  Naoki Machida, deceased ,  by Takayasu Miwa, heir

    Inventor： Kazuhiro Onogi ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Masami Shiratsuchi ,  Masahiko Nagakura ,  Naoki Machida, deceased ,  by Takayasu Miwa, heir

    IPC: A61K31/35 ,  A61K31/352 ,  A61K31/41 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  C07D311/86 ,  C07D405/04 ,  C07D405/12 ,  C07D405/10 ,  C07D413/10

    CPC classification number: C07D311/86

    Abstract: A tetrahydroxanthone derivative represented by the general formula: ##STR1## wherein R is a hydrogen atom, a hydroxyl, cyano, lower alkyl, lower alkoxy, lower acyloxy, benzoyloxy or tetrazolyl group, or ##STR2## (R.sub.3 is a hydrogen atom, R.sub.4 is a hydrogen atom, a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.3 and R.sub.4 commonly form a ring together with the adjacent nitrogen atom and another nitrogen atom or an oxygen atom); R.sub.1 is a hydrogen or halogen atom, a lower alkyl, cyano, carboxyl or tetrazolyl group, or ##STR3## (R.sub.5 is a hydrogen atom, R.sub.6 is a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.5 and R.sub.6 commonly form a ring together with the adjacent nitrogen atom and an oxygen atom); and R.sub.2 is a hydrogen or halogen atom, or a lower alkyl group; with the proviso that neither R nor R.sub.1 is a hydrogen atom; when R is --CONH.sub.2, R.sub.1 and R.sub.2 are not respectively a hydrogen atom nor a hydrogen or halogen atom, or a lower alkyl group; and R.sub.2 and R.sub.1 are not respectively a hydrogen atom nor a halogen atom or a lower alkyl group. Exhibits anti-allergic, anti-inflammatory, analgesic, inhibitory and asthma-treating activities.

    Abstract translation: 其中R是氢原子，羟基，氰基，低级烷基，低级烷氧基，低级酰氧基，苯甲酰氧基或四唑基，或者是（R 3是氢原子，R 4 是氢原子，可以被任意取代的苯基或四唑基;或者R3和R4通常与相邻的氮原子和另一个氮原子或氧原子一起形成环）; R 1是氢或卤素原子，低级烷基，氰基，羧基或四唑基，或者R 5是氢原子，R 6是任选被取代的苯基或四唑基;或R 5和R 6 通常与相邻的氮原子和氧原子一起形成环）; 并且R 2是氢或卤原子或低级烷基; 条件是R和R1都不是氢原子; 当R为-CONH 2时，R 1和R 2不分别为氢原子或氢或卤素原子或低级烷基; R2和R1不分别为氢原子或卤素原子或低级烷基。 展示抗过敏，抗炎，镇痛，抑制和哮喘治疗活动。

    Anilide compounds and pharmaceutical compositions comprising them
    9.
    发明授权
    Anilide compounds and pharmaceutical compositions comprising them 失效
    酰苯胺化合物和包含它们的药物组合物

    公开(公告)号：US06825223B2

    公开(公告)日：2004-11-30

    申请号：US09789967

    申请日：2001-02-21

    Applicant: Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    Inventor： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    IPC: A61K31428

    CPC classification number: C07D263/58 ,  C07D235/28 ,  C07D277/70

    Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or an oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NR6—; R4 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

    Abstract translation: 本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基 基团或低级烷氧基; 并且R 4和R 5可以一起形成低级亚烷基，其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代; X是-NH-或氧或硫原子; Y是-NH-， 氧或硫原子，或亚砜或砜基; Z为单键或-NR 6 - ; R 4表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

    Pyrimidine derivatives as endothelin antagonists
    10.
    发明授权
    Pyrimidine derivatives as endothelin antagonists 失效
    嘧啶衍生物作为内皮素拮抗剂

    公开(公告)号：US5883092A

    公开(公告)日：1999-03-16

    申请号：US29244

    申请日：1998-03-04

    Applicant: Mitsuteru Hirata ,  Takeo Deushi ,  Yoshio Takahashi ,  Masahiro Tamura ,  Takeshi Ohshima ,  Toshiaki Oda ,  Tetsuya Ishikawa ,  Hiroyuki Sonoki ,  Masami Shiratsuchi

    Inventor： Mitsuteru Hirata ,  Takeo Deushi ,  Yoshio Takahashi ,  Masahiro Tamura ,  Takeshi Ohshima ,  Toshiaki Oda ,  Tetsuya Ishikawa ,  Hiroyuki Sonoki ,  Masami Shiratsuchi

    IPC: C07D403/04 ,  A61K31/506 ,  A61P9/00 ,  A61P9/12 ,  C07D213/00 ,  C07D239/52 ,  C07D239/545 ,  C07D295/00 ,  C07D401/14 ,  C07D413/04 ,  A61K31/505 ,  A61K31/535

    CPC classification number: C07D239/52

    Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## �wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

    Abstract translation: PCT No.PCT / JP96 / 02494 Sec。 371日期：1998年3月4日 102（e）1998年3月4日PCT PCT 1996年9月4日PCT公布。 公开号WO97 / 09318 日期1997年3月13日本发明涉及下式（1）的嘧啶衍生物或衍生物的盐：其中R1表示羟基，低级烷氧基，苯氧基 其可以具有取代基，可以具有取代基的芳烷氧基或-NR2R3; X表示氧原子或N-R4; m为2或3; n为1或2（式中，R2，R3各自相同或不同，表示氢原子，羟基，可具有取代基的低级烷基，可具有取代基的苯基， 取代基，可以具有取代基的芳烷基或可以具有取代基的杂环基; R4表示低级烷基，苯基，甲酰基或低级烷氧基羰基）]以及药物 含有衍生物或盐作为活性成分。 该化合物对具有强烈血管收缩作用的内皮素表现出强烈的结合抑制活性。 因此，该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。

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