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23 条记录 (耗时 0.017 秒)

    Amino alcohol derivatives, medicinal composition containing the same, and use of these
    1.
    发明授权
    Amino alcohol derivatives, medicinal composition containing the same, and use of these 失效
    氨基醇衍生物，含有该组合物的药用组合物及其用途

    公开(公告)号：US07417169B2

    公开(公告)日：2008-08-26

    申请号：US10576753

    申请日：2004-10-05

    申请人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Hideyuki Muranaka ,  Takehiro Ishikawa ,  Tetsuro Tamai ,  Satoshi Akahane

    发明人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Hideyuki Muranaka ,  Takehiro Ishikawa ,  Tetsuro Tamai ,  Satoshi Akahane

    IPC分类号： C07C211/00 ,  C07C311/00 ,  A61K31/18 ,  A61K31/135

    CPC分类号： C07D235/24 ,  C07C233/43 ,  C07C311/21

    摘要： The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is —COR10, -A1-COR10, —O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, —OCH2—, etc, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

    摘要翻译： 本发明提供由通式（I）表示的化合物：其前药或其药学上可接受的盐，其中R 1是氢或低级烷基; R2和R3各自独立地为氢或低级烷基; R 4，R 5和R 6各自独立地是氢，卤素，低级烷基或低级烷氧基; R 7是氢或低级烷基; R 8是氢，卤素，低级烷基，低级烷氧基等; R 9是-COR 10，-A 1 -OR 10，-OA 2， SUP> -COR 10等; Ar是任选取代的苯基或杂芳基; 并且A是表现出有效和选择性的β3肾上腺素受体刺激活性的键-OCH 2 - 2等。 本发明还提供含有所述化合物的药物组合物及其用途。

    Crystal polymorphism of aminoethylphenoxyacetic acid derivative
    6.
    发明授权
    Crystal polymorphism of aminoethylphenoxyacetic acid derivative 失效
    氨基乙基苯氧基乙酸衍生物的晶体多晶型

    公开(公告)号：US06376707B1

    公开(公告)日：2002-04-23

    申请号：US09889857

    申请日：2001-07-23

    申请人： Michio Toda ,  Tetsuro Tamai ,  Nobuyuki Tanaka ,  Kiyoshi Kasai ,  Junichi Sonehara ,  Eiji Tsuru

    发明人： Michio Toda ,  Tetsuro Tamai ,  Nobuyuki Tanaka ,  Kiyoshi Kasai ,  Junichi Sonehara ,  Eiji Tsuru

    IPC分类号： C07C22900

    CPC分类号： C07C217/60 ,  C07C213/10

    摘要： The present invention relates to a crystalline polymorph of 2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methylethyl]amino]ethyl]phenoxy]acetic acid having strong diffraction peaks (diffraction angle: 2&thgr;±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 &bgr;2- and &bgr;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-[[(1S,2R)-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.

    摘要翻译： 本发明涉及2- [4- [2 - [[（1S，2R）-2-羟基-2-（4-羟基 - 苯基）-1-甲基乙基]氨基]乙基]苯氧基]乙酸的结晶多晶型物 在其粉末X射线衍射图中，在10.8,19.1,19.3,19.8,20.6和27.0°处具有强衍射峰（衍射角：2θ±0.1°）的酸，其具有有效的β2-和β3-肾上腺素受体刺激作用，并且是有用的 作为缓解疼痛并促进尿石结石中的结石的去除的药剂等。 例如，结晶多晶型物可以通过水解2- [4- [2 - [[（1S，2R）-2-羟基-2-（4-羟基苯基）-1-甲基乙基] - 氨基]乙基]苯氧基 ]乙酸磷酸盐与氢氧化钠反应，在40℃加入磷酸水溶液，过滤，向所得化合物中加入水和甲醇或甲醇的混合溶剂，并在40℃下将悬浮液在回流温度下搅拌30 几分钟到几个小时。

    Phenylaminoalkylcarboxylic acid derivatives and pharmaceutical compositions comprising the same
    7.
    发明授权
    Phenylaminoalkylcarboxylic acid derivatives and pharmaceutical compositions comprising the same 失效
    苯基氨基烷基羧酸衍生物和包含它们的药物组合物

    公开(公告)号：US06353025B1

    公开(公告)日：2002-03-05

    申请号：US09581851

    申请日：2000-06-19

    申请人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

    发明人： Tetsuro Tamai ,  Nobuyuki Tanaka ,  Harunobu Mukaiyama ,  Akihito Hirabayashi ,  Hideyuki Muranaka ,  Masaaki Sato ,  Masuo Akahane

    IPC分类号： A01N3712

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

    摘要： The present invention provides novel phenylaminoalkyl-carboxylic acid derivatives represented by the general formula: (wherein R1 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; R2 represents a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom or a halogen atom; R4 and R5 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 &bgr;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： 本发明提供由通式（其中R1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））表示的新型苯基氨基烷基 - 羧酸衍生物， 可以具有羟基或低级烷氧基作为取代基的氨基; R2表示氢原子或低级烷基; R3表示氢原子或卤素原子; R4和R5相同或不同，表示 氢原子，卤素原子或低级烷基; A表示低级亚烷基;（R）表示的碳原子表示（R）构型的碳原子，（S）表示的碳原子表示碳原子 （S）构型）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，由肠道超嗜热引起的疾病 遗尿，尿频，尿失禁，抑郁症或由胆汁结石或胆汁运动障碍引起的疾病。

    3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives
    8.
    发明授权
    3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives 有权
    3,4-二取代苯乙醇氨基四氢萘羧酸衍生物

    公开(公告)号：US6136852A

    公开(公告)日：2000-10-24

    申请号：US155345

    申请日：1999-03-08

    申请人： Makio Kitazawa ,  Kosuke Okazaki ,  Tetsuro Tamai ,  Masaru Saito ,  Nobuyuki Tanaka ,  Hiroaki Kobayashi ,  Ken Kikuchi ,  Hideyuki Muranaka

    发明人： Makio Kitazawa ,  Kosuke Okazaki ,  Tetsuro Tamai ,  Masaru Saito ,  Nobuyuki Tanaka ,  Hiroaki Kobayashi ,  Ken Kikuchi ,  Hideyuki Muranaka

    IPC分类号： C07C217/74 ,  C07C229/46 ,  C07C229/50 ,  A61K31/215 ,  A61K31/19 ,  C07C62/06 ,  C07C69/76

    CPC分类号： C07C229/50 ,  C07C217/74 ,  C07C2102/10 ,  Y02P20/55

    摘要： The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.

    摘要翻译： PCT No.PCT / JP97 / 01008 Sec。 371日期1999年3月8日 102（e）1999年3月8日PCT 1997年3月26日PCT公布。 公开号WO97 / 35835 日期：1997年10月2日本发明涉及由以下通式表示的3,4-二取代苯乙醇氨基四氢萘羧酸衍生物：[其中Q表示亚乙烯基或由通式-A-（CH 2）m - 表示的基团 A表示氧原子或亚甲基; m表示1〜6的整数）; R表示氢原子或低级烷基; n为1或2的整数; 标有*的碳原子表示R构型，S构型或其混合物中的碳原子; 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，其具有选择性β2-肾上腺素能受体刺激作用，并且在心脏上缓解负担，例如心动过速，并且可用作 防止威胁堕胎和早产，支气管扩张剂和止痛剂，促进尿石症中的除石。