Process for preparing rebamipide
    1.
    发明授权
    Process for preparing rebamipide 有权
    制备瑞巴派特的方法

    公开(公告)号:US07718805B2

    公开(公告)日:2010-05-18

    申请号:US10587509

    申请日:2005-11-30

    IPC分类号: C07D215/38

    CPC分类号: C07D215/227

    摘要: 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).

    摘要翻译: 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)。

    Process for Preparing Rebamipide
    3.
    发明申请
    Process for Preparing Rebamipide 有权
    制备瑞巴派特的方法

    公开(公告)号:US20070249835A1

    公开(公告)日:2007-10-25

    申请号:US10587509

    申请日:2005-11-30

    IPC分类号: C07D215/02

    CPC分类号: C07D215/227

    摘要: 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).

    摘要翻译: 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)。

    Carbostyril derivatives
    4.
    发明授权
    Carbostyril derivatives 失效
    卡波他汀衍生物

    公开(公告)号:US6143763A

    公开(公告)日:2000-11-07

    申请号:US849664

    申请日:1997-05-29

    CPC分类号: C07D215/227

    摘要: 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.

    摘要翻译: 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。

    Method for manufacturing components for magnetic heads of increased
abrasion resistance
    6.
    发明授权
    Method for manufacturing components for magnetic heads of increased abrasion resistance 失效
    用于制造增加耐磨性的磁头部件的方法

    公开(公告)号:US4336066A

    公开(公告)日:1982-06-22

    申请号:US152782

    申请日:1980-05-23

    摘要: In manufacturing of lamina used for components for magnetic heads such as head cores and shield casings, powder metallurgy is applied to powder material of a permalloy alloy composition in combination with later-staged rolling. Addition of at least one easily oxidizable element is preferably combined with formation of the material powder by means of atomization, more preferably followed by annealing within a reducing atmosphere. Measured formation of oxidized shells on powder particles assists uniform and smooth dispersion of smashed shell flakes into the lamina, thereby greatly raising abrasion resistance of the product without lowering the magnetic properties.

    摘要翻译: 在用于头磁头和屏蔽壳等磁头部件的层板的制造中,粉末冶金被应用于坡莫合金组合物的粉末材料与后期轧制的组合。 添加至少一种容易氧化的元素优选通过雾化与材料粉末的形成相结合,更优选在还原气氛中进行退火。 测量粉末颗粒上的氧化壳的形成有助于将粉碎的壳薄片均匀且平滑地分散到层中,从而大大提高了产品的耐磨性,而不降低磁性能。

    Process for production of carbostyril compound
    7.
    发明授权
    Process for production of carbostyril compound 有权
    喹诺酮类化合物生产工艺

    公开(公告)号:US07718806B2

    公开(公告)日:2010-05-18

    申请号:US11596004

    申请日:2006-04-07

    IPC分类号: C07D215/38

    CPC分类号: C07D215/22

    摘要: The invention provides an improved process for preparing a carbostyril compound (1) or a salt thereof that is useful as a medicament, which makes it possible to prepare it more safely and efficiently.In more detail, the invention provides an improved process for preparing the carbostyril compound (1) by heating the compound (4) with a high boiling solvent in hydrochloric acid under reflux to give the compound (5) safely; and then acylating the compound (5).

    摘要翻译: 本发明提供了一种制备喹诺酮化合物(1)或其盐的改进方法,其可用作药物,这使得可以更安全和有效地制备它。 更详细地说,本发明提供了一种改进的制备喹诺酮化合物(1)的方法,该方法是用高沸点溶剂在盐酸中回流加热化合物(4),以安全地得到化合物(5); 然后酰化化合物(5)。

    Process for Production of Carbostyril Compound
    9.
    发明申请
    Process for Production of Carbostyril Compound 有权
    碳青霉烯化合物生产工艺

    公开(公告)号:US20070299262A1

    公开(公告)日:2007-12-27

    申请号:US11596004

    申请日:2006-04-07

    IPC分类号: C07D215/22

    CPC分类号: C07D215/22

    摘要: The invention provides an improved process for preparing a carbostyril compound (1) or a salt thereof that is useful as a medicament, which makes it possible to prepare it more safely and efficiently. In more detail, the invention provides an improved process for preparing the carbostyril compound (1) by heating the compound (4) with a high boiling solvent in hydrochloric acid under reflux to give the compound (5) safely; and then acylating the compound (5).

    摘要翻译: 本发明提供了一种制备喹诺酮化合物(1)或其盐的改进方法,其可用作药物,这使得可以更安全和有效地制备它。 更详细地说,本发明提供了一种改进的制备喹诺酮化合物(1)的方法,该方法是用高沸点溶剂在盐酸中回流加热化合物(4),以安全地得到化合物(5); 然后酰化化合物(5)。