会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • Process for preparing rebamipide
    • 制备瑞巴派特的方法
    • US07718805B2
    • 2010-05-18
    • US10587509
    • 2005-11-30
    • Shinji NishitaniNorio Fukuda
    • Shinji NishitaniNorio Fukuda
    • C07D215/38
    • C07D215/227
    • The invention provides an improved process for preparing rebamipide that is useful as a medicament, which makes it possible to prepare rebamipide with high purity and high yield. The invention is an improved process for preparing rebamipide of the formula (1), comprising subjecting a carbostyril amino acid compound of the formula (5) or a salt thereof containing a compound of the formula (11) as an impurity to a reduction treatment in the presence of hydrogen and a catalyst in a basic aqueous solution, thereby selectively reducing the impurity compound (11) to transform into the carbostyril amino acid compound (5); and then acylating the compound (5) in a basic aqueous solution to give rebamipide (1).
    • 本发明提供了一种用于制备可用作药物的瑞巴派特的改进方法,其使得可以以高纯度和高产率制备瑞巴派特。 本发明是制备式(1)的瑞巴派特的改进方法,其包括使式(5)的喹诺酮类氨基酸化合物或其含有式(11)化合物的盐作为杂质进行还原处理 在碱性水溶液中存在氢和催化剂,从而选择性地还原杂质化合物(11)以转化成喹诺酮类氨基酸化合物(5); 然后在碱性水溶液中酰化化合物(5),得到瑞巴派特(1)。
    • 8. 发明申请
    • Process for Preparing Rebamipide
    • 制备瑞巴派特的方法
    • US20070249835A1
    • 2007-10-25
    • US10587509
    • 2005-11-30
    • Shinji NishitaniNorio Fukuda
    • Shinji NishitaniNorio Fukuda
    • C07D215/02
    • C07D215/227
    • The invention provides an improved process for preparing rebamipide that is useful as a medicament, which makes it possible to prepare rebamipide with high purity and high yield. The invention is an improved process for preparing rebamipide of the formula (1), comprising subjecting a carbostyril amino acid compound of the formula (5) or a salt thereof containing a compound of the formula (11) as an impurity to a reduction treatment in the presence of hydrogen and a catalyst in a basic aqueous solution, thereby selectively reducing the impurity compound (11) to transform into the carbostyril amino acid compound (5); and then acylating the compound (5) in a basic aqueous solution to give rebamipide (1).
    • 本发明提供了一种用于制备可用作药物的瑞巴派特的改进方法,其使得可以以高纯度和高产率制备瑞巴派特。 本发明是制备式(1)的瑞巴派特的改进方法,其包括使式(5)的喹诺酮类氨基酸化合物或其含有式(11)化合物的盐作为杂质进行还原处理 在碱性水溶液中存在氢和催化剂,从而选择性地还原杂质化合物(11)以转化成喹诺酮类氨基酸化合物(5); 然后在碱性水溶液中酰化化合物(5),得到瑞巴派特(1)。
    • 9. 发明授权
    • Carbostyril derivatives
    • 卡波他汀衍生物
    • US6143763A
    • 2000-11-07
    • US849664
    • 1997-05-29
    • Yasuo KogaYoshito KiharaMinoru OkadaTakao NishiYoshihiro InoueYukio KimuraHiroyoshi HidakaNorio Fukuda
    • Yasuo KogaYoshito KiharaMinoru OkadaTakao NishiYoshihiro InoueYukio KimuraHiroyoshi HidakaNorio Fukuda
    • C07D215/22C07D215/227A61K31/4704
    • C07D215/227
    • A carbostyril derivative of the formula (1): ##STR1## wherein A is lower alkylene, R is H, halogen or lower alkoxy, R.sup.1 and R.sup.2 are each lower alkyl being optionally substituted by OH, lower alkoxy, phenyl-lower alkoxy or lower alkanoyloxy; cycloalkyl being optionally substituted by OH, hydroxy-lower alkoxy or lower alkanoyloxy; or amino being optionally substituted by lower alkyl or cycloalkyl, R.sup.3 is H, lower alkyl, lower alkenyl or hydroxy-lower alkyl, and the bond between 3- and 4-positions of the carbostyril nucleus is single or double, provided that when R and R.sup.3 are H, R.sup.1 and R.sup.2 should not be either unsubstituted lower alkyl or unsubstituted cycloalkyl, or a salt thereof, which shows antithrombotic activities, intima thickening inhibitory activity, the platelet mass dissociating activity and increasing activity of the blood flow in the brain and the peripheral vessel, and hence, is useful as medicines in the prophylaxis or treatment of various ischemic diseases.
    • PCT No.PCT / JP96 / 02892 Sec。 371日期:1998年5月29日 102(e)日期1998年5月29日PCT提交1996年10月4日PCT公布。 公开号WO97 / 12869 日期:1997年04月10日式(1)的喹诺酮衍生物:其中A为低级亚烷基,R为H,卤素或低级烷氧基,R1和R2各自为低级烷基,任选被OH,低级烷氧基,苯基 - 低级烷氧基 或低级烷酰氧基; 任选被OH,羟基 - 低级烷氧基或低级烷酰氧基取代的环烷基; 或氨基任选被低级烷基或环烷基取代,R 3是H,低级烷基,低级烯基或羟基 - 低级烷基,并且喹诺酮环的3-和4-位之间的键是单或双,条件是当R和 R3是H,R1和R2不应该是未取代的低级烷基或未取代的环烷基或其盐,其显示抗血栓形成活性,内膜增厚抑制活性,血小板质量分解活性和增加脑中血流的活性, 外周血管,因此可用作预防或治疗各种缺血性疾病的药物。