Pyrimidine derivatives
    3.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号:US6008224A

    公开(公告)日:1999-12-28

    申请号:US849725

    申请日:1997-06-27

    CPC分类号: C07D239/69

    摘要: 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 lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

    摘要翻译: PCT No.PCT / JP95 / 02605 Sec。 371日期:1997年6月27日 102(e)日期1997年6月27日PCT 1995年12月19日PCT公布。 公开号WO96 / 20177 PCT 日期:1996年7月4日本发明涉及下述式(1)所示的嘧啶衍生物或其衍生物的盐:其中R1表示低级烷基; R 2和R 3各自表示H,烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基,-OR 7或-NR 8 R 9; 并且n是0和3之间的数字(其中R7,R8和R9各自表示H,烷基,芳基,芳烷基,氨基,杂环等)],以及含有该衍生物或 盐作为活性成分。 本发明化合物对内皮素具有强烈的结合抑制活性,具有强烈的血管收缩作用和细胞增殖作用。 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。

    Pyrimidine derivatives as endothelin antagonists
    4.
    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

    CPC分类号: C07D239/52

    摘要: 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.

    摘要翻译: 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。

    Pyrimidine derivatives
    5.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号:US06337334B1

    公开(公告)日:2002-01-08

    申请号:US09434474

    申请日:1999-11-05

    IPC分类号: A61K31505

    CPC分类号: C07D239/69

    摘要: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: [wherein R1 represents a lower alkyl group; each of R2 and R3 represents H, alkyl, or alkoxy; each of R4 and R5 represents H or alkyl; R6 represents alkyl, —OR7, or —NR8R9; and n is a number between 0 and 3 inclusive (wherein each of R7, R8, and R9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

    摘要翻译: 本发明涉及下式(1)的嘧啶衍生物或其衍生物的盐:其中R 1表示低级烷基; R 2和R 3各自表示H,烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基,-OR 7或-NR 8 R 9; 并且n是0和3之间的数字(其中R7,R8和R9各自表示H,烷基,芳基,芳烷基,氨基,杂环等)],以及含有该衍生物或 盐作为活性成分。 本发明化合物对内皮素具有强烈的结合抑制活性,具有强烈的血管收缩作用和细胞增殖作用。 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。

    Process for producing toluidine compound
    6.
    发明授权
    Process for producing toluidine compound 有权
    甲苯胺化合物的制备方法

    公开(公告)号:US08338612B2

    公开(公告)日:2012-12-25

    申请号:US12671050

    申请日:2008-07-29

    IPC分类号: C07D213/74

    CPC分类号: C07D213/72

    摘要: Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.

    摘要翻译: 由于氟啶胺作为农药的有效成分是优异的,而且是非常有用的,因此希望能以低成本的环境友好的方式以简单的操作以适当的形式有效地生产。 通过使用工业上有利的反应体系,通过使用包括(1)在碱组分,选自酮,腈的溶剂存在下使ACTF和DCDNBTF反应的步骤,以简单的操作获得所需产物 ,醚和酯和足够量的水以基本上溶解碱组分,(2)用酸中和或酸化反应混合物的步骤和(3)通过蒸馏从包含氟啶胺的混合物中除去溶剂的步骤为 反应产物和反应溶剂使产物析出晶体。

    PROCESS FOR PRODUCING TOLUIDINE COMPOUND
    7.
    发明申请
    PROCESS FOR PRODUCING TOLUIDINE COMPOUND 有权
    生产托洛芬化合物的方法

    公开(公告)号:US20100197930A1

    公开(公告)日:2010-08-05

    申请号:US12671050

    申请日:2008-07-29

    IPC分类号: C07D213/36

    CPC分类号: C07D213/72

    摘要: Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.

    摘要翻译: 由于氟啶胺作为农药的有效成分是优异的,而且是非常有用的,因此希望能以低成本的环境友好的方式以简单的操作以适当的形式有效地生产。 通过使用工业上有利的反应体系,通过使用包括(1)在碱组分,选自酮,腈的溶剂存在下使ACTF和DCDNBTF反应的步骤,以简单的操作获得所需产物 ,醚和酯和足够量的水以基本上溶解碱组分,(2)用酸中和或酸化反应混合物的步骤和(3)通过蒸馏从包含氟啶胺的混合物中除去溶剂的步骤为 反应产物和反应溶剂使产物析出晶体。

    Surface treating agent for ligneous floorings and process for manufacturing the same
    9.
    发明授权
    Surface treating agent for ligneous floorings and process for manufacturing the same 有权
    木质地板用表面处理剂及其制造方法

    公开(公告)号:US06730147B2

    公开(公告)日:2004-05-04

    申请号:US10016104

    申请日:2001-12-17

    IPC分类号: C09G108

    CPC分类号: C09G1/08

    摘要: There is provided a surface treating agent for ligneous floorings that makes the surface of a treated floor resistant to slipping and thus is capable of preventing tumbling. The surface treating agent for ligneous floorings contains a drying oil, Japan wax, candelilla wax, and powdery carnauba wax.

    摘要翻译: 提供了一种用于木质地板的表面处理剂,其使处理后的地板的表面具有滑动性,因此能够防止翻滚。 用于木质地板的表面处理剂含有干性油,日本蜡,小烛树蜡和粉状巴西棕榈蜡。

    Imidazole compound and process for preparing the same
    10.
    发明授权
    Imidazole compound and process for preparing the same 失效
    咪唑化合物及其制备方法

    公开(公告)号:US5023336A

    公开(公告)日:1991-06-11

    申请号:US424630

    申请日:1989-10-20

    IPC分类号: A01N43/50 C07D233/90 C07F7/08

    CPC分类号: C07D233/90 C07F7/0812

    摘要: An imidazole compound is disclosed, which is represented by formula (I): ##STR1## wherein: X represents a --COOT group, in which T represents a hydrogen atom, an alkyl group, a benzyl group, or a phenyl group; or a --CONH.sub.2 group,Y represents a hydrogen atom, a chlorine atom, or a bromine atom,Z represents an alkyl group containing from 2 to 6 carbon atoms, which may be substituted with one or more halogen atoms; or a phenyl group which may be substituted with one or more halogen atoms or alkyl groups, andQ represents a hydrogen atom; an --SO.sub.2 R.sup.1 group, in which R.sup.1 represents an alkyl group, a dialkylamino group, or a phenyl group which may be substituted with one or more alkyl groups; or a --CH(R.sup.2)(R.sup.3) group, in which R.sup.2 represents a hydrogen atom, a methyl group, or an alkoxy group, and R.sup.3 represents an alkoxy group, an --OCH.sub.2 CH.sub.2 Si (CH.sub.3) group, or a phenyl group which may be substituted with one or more alkyl groups or alkoxy groups,provided that when Y and Q each represents a hydrogen atom and Z represents a phenyl group, X represents a group other than a --COOH-phenyl group, and a --CONH.sub.2 group; and that when Y and Q each represents a hydrogen atom and Z represents an n--C.sub.5 H.sub.11 group, X represents a group other than a --COOH group and a --COOC.sub.2 H.sub.5 group.Processes for preparing imidazole compounds are also disclosed.The imidazole compounds are useful as an intermediate for production of biocides for controlling harmful organisms in the agricultural and horticultural areas, or medical and pharmaceutical fungicides.