公开(公告)号：US5238938A

公开(公告)日：1993-08-24

申请号：US857726

申请日：1992-03-26

申请人： Hitoshi Tone ,  Seiji Sato ,  Hideaki Sato ,  Katsumi Tamura ,  Shigeharu Tamada ,  Kazumi Kondo ,  Tomoyuki Kawaguchi ,  Yoshimasa Nakano ,  Yasuyuki Kita ,  Shuji Akai ,  Hiromichi Fujioka ,  Yasumitsu Tamura ,  Katsuhide Matoba ,  Youichi Taniguchi ,  Shinji Nishitani ,  Satoshi Hayakawa ,  Toshinori Kaneyasu ,  Yoshihiko Ito ,  Masahiro Murakami

发明人： Hitoshi Tone ,  Seiji Sato ,  Hideaki Sato ,  Katsumi Tamura ,  Shigeharu Tamada ,  Kazumi Kondo ,  Tomoyuki Kawaguchi ,  Yoshimasa Nakano ,  Yasuyuki Kita ,  Shuji Akai ,  Hiromichi Fujioka ,  Yasumitsu Tamura ,  Katsuhide Matoba ,  Youichi Taniguchi ,  Shinji Nishitani ,  Satoshi Hayakawa ,  Toshinori Kaneyasu ,  Yoshihiko Ito ,  Masahiro Murakami

IPC分类号： C07D403/04 ,  C07D403/06

CPC分类号： C07D403/04 ,  C07D403/06

摘要： The novel indole derivatives and salts thereof represented by the general formula (1) ##STR1## possess, for example, an inhibitory effect against superoxide (O.sub.2.sup.-) released from the macrophage cells of guinea pig by stimulation and an anti-albuminuria activity against Masugi nephritis, and are useful in various clinical fields as an agent for preventing and treating diseases and cases associated with the above superoxide radical, for example, autoimmune diseases (e.g. rheumatism), arteriosclerosis, ischemic disease, ischemic encephalopathia, hepatic insufficiency and renal insufficiency, and also as an agent for preventing and treating nephritis.

摘要翻译： 由通式（1）表示的新的吲哚衍生物及其盐具有例如通过刺激和抗白蛋白尿对豚鼠巨噬细胞释放的对超氧化物（O 2 - ）的抑制作用 针对Masugi肾炎的活性，并且在各种临床领域中用作预防和治疗与上述超氧化物基团相关的疾病和病例的药剂，例如自身免疫性疾病（例如风湿病），动脉硬化，缺血性疾病，缺血性脑病，肝功能不全和 肾功能不全，还可用作预防和治疗肾炎的药剂。

公开(公告)号：US20070249835A1

公开(公告)日：2007-10-25

申请号：US10587509

申请日：2005-11-30

申请人： Shinji Nishitani ,  Norio Fukuda

发明人： Shinji Nishitani ,  Norio Fukuda

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）。

公开(公告)号：US07718805B2

公开(公告)日：2010-05-18

申请号：US10587509

申请日：2005-11-30

申请人： Shinji Nishitani ,  Norio Fukuda

发明人： Shinji Nishitani ,  Norio Fukuda

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）。

公开(公告)号：US4795814A

公开(公告)日：1989-01-03

申请号：US942915

申请日：1986-12-18

申请人： Shinji Nishitani ,  Junichi Minamikawa ,  Masanobu Kano ,  Junichiro Otsubo ,  Yoshiaki Manabe

发明人： Shinji Nishitani ,  Junichi Minamikawa ,  Masanobu Kano ,  Junichiro Otsubo ,  Yoshiaki Manabe

IPC分类号： A61K31/443 ,  A61K31/445 ,  A61K31/451 ,  A61K31/455 ,  A61P3/00 ,  A61P3/08 ,  A61P3/14 ,  A61P7/02 ,  A61P9/12 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C67/00 ,  C07C69/738 ,  C07C229/30 ,  C07C313/00 ,  C07C323/14 ,  C07D211/90 ,  C07D405/12 ,  C07D211/02

CPC分类号： C07D211/90

摘要： Process for preparing dihydropyridine derivatives and salts and esters thereof represented by the general formula ##STR1## from a phenyl derivative and an enamine derivative in which the phenyl derivative is prepared by reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## in the presence of an aromatic amine selected from o-, m-, p- anisidine; m-, p-toluidine; p-chloroaniline; aniline and o-phenetidine.

摘要翻译： 由苯基衍生物和烯胺衍生物制备由通式“IMAGE”表示的二氢吡啶衍生物及其盐和酯的方法，其中苯基衍生物通过使下式化合物与式 在选自邻 - ，间 - ，对 - 茴香胺的芳族胺的存在下， 对 - 甲苯胺; 对氯苯胺; 苯胺和邻苯乙胺。