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11 条记录 (耗时 0.008 秒)

    CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE
    1.
    发明公开
    CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE 有权
    氨乙基苯氧基的衍生物的KRISTAL-多态性

    公开(公告)号：EP1146035A9

    公开(公告)日：2001-12-05

    申请号：EP00900407

    申请日：2000-01-17

    申请人： KISSEI PHARMACEUTICAL

    发明人： TODA MICHIO ,  TAMAI TETSURO ,  TANAKA NOBUYUKI ,  KASAI KIYOSHI ,  SONEHARA JUNICHI ,  TSURU EIJI

    IPC分类号： A61K31/19 ,  A61P13/04 ,  A61P29/00 ,  C07C213/10 ,  C07C217/60

    CPC分类号： C07C217/60 ,  C07C213/10

    摘要： The present invention relates to a crystalline polymorph of 2-[4-[2-[[(1
    S ,2
    R )-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]phenoxy]acetic acid having strong diffraction peaks (diffraction angle: 2 ± 0.1°) at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0° in powder x-ray diffraction pattern, which has potent β
    2 - and β
    3 - adrenoceptor stimulating effects and is useful as an agent for relieving pain and promoting the removal of calculi in urolithiasis, and the like. For example, the crystalline polymorph can be prepared by hydrolyzing ethyl 2-[4-[2-[[1
    S ,2
    R )-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]phenoxy]acetate phosphate by sodium hydroxide, adding an aqueous phosphoric acid solution at 40 °C and over, adding a mixed solvent of water and methanol or methanol to the resulting compound, and stirring the suspension at 40 °C to reflux temperature for 30 minutes to several hours.

    PHENYLETHANOLAMINOTETRALINCARBOXAMIDE DERIVATIVES
    4.
    发明公开
    PHENYLETHANOLAMINOTETRALINCARBOXAMIDE DERIVATIVES 失效
    PHENYLETHANOLAMINOTETRALINCARBOXAMID衍

    公开(公告)号：EP0893432A4

    公开(公告)日：2002-01-02

    申请号：EP97914598

    申请日：1997-04-04

    申请人： KISSEI PHARMACEUTICAL

    发明人： KITAZAWA MAKIO ,  OKAZAKI KOSUKE ,  TAMAI TETSURO ,  SAITO MASARU ,  TANAKA NOBUYUKI ,  KOBAYASHI HIROAKI ,  KIKUCHI KEN ,  MURANAKA HIDEYUKI

    IPC分类号： A61K31/165 ,  A61K31/445 ,  A61K31/535 ,  C07C235/06 ,  C07D295/16 ,  C07D295/185 ,  A61K31/495 ,  C07D295/18

    CPC分类号： C07D295/185 ,  C07C235/06 ,  C07C2602/10

    摘要： Phenylethanolaminotetralincarboxamide derivative represented by general formula (I) and pharmacologically acceptable salts thereof, wherein A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino which may bear oxygen on the ring; the asterisked carbon atom represents a carbon atom with an R- or S-configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective β2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.

    摘要翻译： 由通式（I）表示的苯乙醇氨基四氢吡喃甲酰胺衍生物及其药理学上可接受的盐，其中A代表低级亚烷基; B表示氨基，二（低级烷基）氨基或在环上可以带有氧的3-7元脂环族氨基; 带星号的碳原子表示具有R-或S-构型的碳原子或这些原子的混合物; 并且用（S）标记的碳原子表示具有S-构型的碳原子。 这些化合物具有选择性β2 - 肾上腺素能受体刺激作用，同时减轻心脏负担，例如心动过速，并且可用作预先堕胎和早产的预防剂，支气管扩张剂和用于缓解泌尿系结石的药物。

    3,4-DISUBSTITUTED PHENYLETHANOLAMINOTETRALINCARBOXYLATE DERIVATIVES
    9.
    发明公开
    3,4-DISUBSTITUTED PHENYLETHANOLAMINOTETRALINCARBOXYLATE DERIVATIVES 失效
    3,4-二氟苯乙烯苯乙醇胺缩氨基羧酸酯衍生物

    公开(公告)号：EP0894787A4

    公开(公告)日：2000-09-20

    申请号：EP97914541

    申请日：1997-03-26

    申请人： KISSEI PHARMACEUTICAL

    发明人： KITAZAWA MAKIO ,  OKAZAKI KOSUKE ,  TAMAI TETSURO ,  SAITO MASARU ,  TANAKA NOBUYUKI ,  KOBAYASHI HIROAKI ,  KIKUCHI KEN ,  MURANAKA HIDEYUKI

    IPC分类号： C07C217/74 ,  C07C229/46 ,  C07C229/50 ,  A61K31/195 ,  A61K31/215

    CPC分类号： C07C229/50 ,  C07C217/74 ,  C07C2602/10 ,  Y02P20/55

    摘要： 3,4-Disubstituted phenylethanolaminotetralincarboxylate derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, wherein Q represents vinylene or a group represented by the general formula -A-(CH2)m- (wherein A represents oxygen or methylene, and m represents an integer of 1 to 6); R represents hydrogen or lower alkyl; n represents an integer of 1 or 2; the asterisked carbon atom represents a carbon atom with an R- or S- configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective beta 2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.

    摘要翻译： 3,4-二取代的通式（I）及其药理学上可接受的盐，其中Q代表亚乙烯基或亚由通式-A-（CH 2）间 - 表示的基团表示phenylethanolaminotetralincarboxylate衍生物（其中A代表氧或亚甲基，且m 表示1至6的整数）; R代表氢或低级烷基; n表示1或2的整数; 带星号的碳原子表示具有R-或S-构型的碳原子或这些原子的混合物; 并且用（S）标记的碳原子表示具有S-构型的碳原子。 这些化合物具有选择性β2肾上腺素能受体刺激作用，同时减少对心脏的负担如心动过速，并可用作预防剂用于先兆流产和早产，支气管扩张药，和剂缓解和排石尿结石是有用的。