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    CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE
    5.
    发明授权
    CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE 有权
    多晶型氨乙基苯氧基的衍生物的

    公开(公告)号：EP1146035B1

    公开(公告)日：2005-11-16

    申请号：EP00900407.8

    申请日：2000-01-17

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： TODA, Michio ,  TAMAI, Tetsuro ,  TANAKA, Nobuyuki ,  KASAI, Kiyoshi ,  SONEHARA, Junichi ,  TSURU, Eiji

    IPC分类号： C07C217/60 ,  A61K31/195 ,  A61P13/04

    CPC分类号： C07C217/60 ,  C07C213/10

    摘要： Crystal polymorphism of 2-[4-[2-[[1s,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl ethyl]amino]ethyl]phenoxy]acetic acid which has potent beta 2 adrenergic receptor stimulating and beta 3-adrenergic receptor stimulating effects, is useful in relieving a pain, promoting calculi removal, etc. in urinary lithiasis and shows intense diffraction peaks at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0 DEG in the powder x-ray diffractometry pattern at a diffraction angle (2/ theta 0+/-0.1). It is produced by, for example, hydrolyzing ethyl 2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethy]phenoxy]acetate phosphate by using sodium hydroxide, adding an aqueous solution of phosphoric acid at 40 DEG C or above to give the above compound, adding a solvent mixture comprising methanol with water or methanol and then stirring in a suspended state at from 40 DEG C to the reflux point for 30 minutes to several hours.

    PHENOXYACETIC ACID DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
    7.
    发明公开
    PHENOXYACETIC ACID DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权
    PHENOXYESSIGSÄURE-VERBINDUNGEN UND MEDISINISCHE ZUSAMMENSETZUNGEN，DIEE ENTHALTEN

    公开(公告)号：EP1095932A1

    公开(公告)日：2001-05-02

    申请号：EP99926928.5

    申请日：1999-07-05

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： TANAKA, Nobuyuki ,  TAMAI, Tetsuro ,  MUKAIYAMA, Harunobu ,  HIRABAYASHI, Akihito, Haitsu Kashiwabara A106 ,  MURANAKA, Hideyuki, Rasukasasu Azumino 305 ,  SATO, Masaaki ,  AKAHANAE, Masuo

    IPC分类号： C07C217/60 ,  C07C255/59 ,  C07C235/60 ,  C07C233/43 ,  C07C235/06 ,  A61K31/215 ,  A61K31/195

    CPC分类号： C07C217/60 ,  C07C233/43 ,  C07C235/06 ,  C07C235/60 ,  C07C255/59

    摘要： The present invention provides novel phenoxyacetic acid derivatives represented by the general formula:
    [wherein R 1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, or a mono or di(lower alkyl)amino group; one of R 2 and R 3 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, while the other is a hydrogen atom; R 4 represents a halogen atom, a lower alkyl group, a halo(lower alkyl)group, a hydroxy group, a lower alkoxy group, an aralkoxy group, a cyano group, a nitro group, an amino group, a mono or di(lower alkyl)amino group, a carbamoyl group, a mono or di(lower alkyl)carbamoyl group or a group represented by the general formula:

            -NHCOR 5

    (wherein R 5 represents a hydrogen atom or a lower alkyl group); the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have excellent β 3 -adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of biliary tract.

    摘要翻译： 本发明提供由以下通式表示的新型苯氧基乙酸衍生物：其中R 1表示羟基，低级烷氧基，芳烷氧基，氨基或单或二（低级烷基）氨基 组; R 2和R 3之一是氢原子，卤素原子，低级烷基或低级烷氧基，而另一个是氢原子; R 4表示卤素原子，低级烷基，卤代（低级烷基），羟基，低级烷氧基，芳烷氧基，氰基，硝基，氨基，单或者 二（低级烷基）氨基，氨基甲酰基，一或二（低级烷基）氨基甲酰基或由通式-NHCOR 5表示的基团（其中R 5表示氢原子或低级烷基 组）; 用（R）标记的碳原子表示R构型的碳原子; 标记有（S）的碳原子表示S构型中的碳原子及其药学上可接受的盐，其具有优异的β3肾上腺素能受体刺激作用，并且可用作预防或治疗肥胖，高血糖，由 肠蠕动过多，尿频，尿失禁，抑郁症，胆道结石或胆汁运动障碍引起的疾病。

    CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE
    8.
    发明公开
    CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE 有权
    多元醇多元醇衍生物氨基苯乙烯氧化物

    公开(公告)号：EP1146035A1

    公开(公告)日：2001-10-17

    申请号：EP00900407.8

    申请日：2000-01-17

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： TODA, Michio ,  TAMAI, Tetsuro ,  TANAKA, Nobuyuki ,  KASAI, Kiyoshi ,  SONEHARA, Junichi ,  TSURU, Eiji

    IPC分类号： C07C217/60

    CPC分类号： C07C217/60 ,  C07C213/10

    摘要： Crystal polymorphism of 2-[4-[2-[[1s,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl ethyl]amino]ethyl]phenoxy]acetic acid which has potent β 2 adrenergic receptor stimulating and β 3 -adrenergic receptor stimulating effects, is useful in relieving a pain, promoting calculi removal, etc. in urinary lithiasis and shows intense diffraction peaks at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0° in the powder x-ray diffractometry pattern at a diffraction angle (2/θ0±0.1). It is produced by, for example, hydrolyzing ethyl 2-[4-[2-[[1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethy]phenoxy]acetate phosphate by using sodium hydroxide, adding an aqueous solution of phosphoric acid at 40°C or above to give the above compound, adding a solvent mixture comprising methanol with water or methanol and then stirring in a suspended state at from 40°C to the reflux point for 30 minutes to several hours.

    摘要翻译： 具有强效β2肾上腺素能受体刺激和β3肾上腺素能受体刺激作用的2-Ä4-Ä2-ÄÄs，2RÜ-2-羟基-2-（4-羟基苯基）-1-甲基乙基氨基乙基苯氧基乙酸的晶体多态性可用于 在尿液结石中缓解疼痛，促进结石清除等，并且在衍射角（2 /θ; 0+）下，在粉末x射线衍射图中的10.8,19.1,19.3,19.8,20.6和27.0°处显示出强烈的衍射峰 /-0.1）。 它是通过使用例如氢氧化钠水解2-Ä4-Ä2-ÄÄ1S，2R）-2-羟基-2-（4-羟基苯基）-1-甲基乙基氨基硫代苯氧基乙酸乙酯，加入磷酸水溶液 在40℃以上，得到上述化合物，加入含有甲醇的溶剂混合物与水或甲醇，然后在40℃至回流点的悬浮状态下搅拌30分钟至数小时。

    PHENYLAMINOALKYLCARBOXYLIC ACID DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
    9.
    发明公开
    PHENYLAMINOALKYLCARBOXYLIC ACID DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 有权
    苯并咪唑啉酮衍生物在医学上ZUSAMMENSETZUNGEN，DIEE ENTHALTEN

    公开(公告)号：EP1043308A1

    公开(公告)日：2000-10-11

    申请号：EP98959168.0

    申请日：1998-12-11

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： TAMAI, Tetsuro ,  TANAKA, Nobuyuki ,  MUKAIYAMA, Harunobu ,  HIRABAYASHI, A., Haitsu Kashiwabara A106 ,  MURANAKA, Hideyuki, Rasukasasu Azumino 305 ,  SATO, Masaaki ,  AKAHANE, Masuo

    IPC分类号： C07C229/18 ,  C07C237/06 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215

    CPC分类号： C07D295/185 ,  C07C229/18 ,  C07C237/06

    摘要： The present invention provides novel phenylaminoalkylcarboxylic acid derivatives represented by the general formula:
    wherein R 1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, an alicyclic amino group or a mono or di(lower alkyl)amino group which may have a hydroxy group or a lower alkoxy group as a substituent; R 2 represents a hydroxy group or a lower alkyl group; R 3 represents a hydrogen atom or a halogen atom; R 4 and R 5 are the same or different and each represents a hydrogen atom, a halogen atom or a lower alkyl group; A represents a lower alkylene group; the carbon atom marked with (R) represents a carbon atom in ( R ) configuration; and the carbon atom marked with (S) represents a carbon atom in ( S ) configuration, and pharmaceutically acceptable salts thereof, which have excellent β 3 -adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of the biliary tract.

    摘要翻译： 本发明提供由以下通式表示的新型苯基氨基烷基羧酸衍生物：其中R 1表示羟基，低级烷氧基，芳烷氧基，氨基，脂环族氨基或单或二（ 低级烷基）氨基，其可以具有羟基或低级烷氧基作为取代基; R 2表示羟基或低级烷基; R 3表示氢原子或卤素原子; R 4和R 5相同或不同，各自表示氢原子，卤素原子或低级烷基; A表示低级亚烷基; 用（R）标记的碳原子表示（R）构型的碳原子; 标记有（S）的碳原子表示（S）构型的碳原子及其药学上可接受的盐，其具有优异的β3肾上腺素能受体刺激作用，并且可用作预防或治疗肥胖症，高血糖症， 由肠蠕动，尿频，尿失禁，抑郁症引起的疾病，或胆道结石或胆汁运动障碍引起的疾病。