公开(公告)号：EP0950665A4

公开(公告)日：2004-05-06

申请号：EP97942202

申请日：1997-09-26

申请人： AJINOMOTO KK

发明人： TAKAHARA YOSHIYUKI ,  SATO HARUYA ,  HAYASHI EIKO ,  YATAGAI MASANOBU ,  SUZUKI MANABU ,  TABATA TOMOYUKI ,  EJIMA CHIEKO

IPC分类号： A61K38/00 ,  C07H15/04 ,  C07H15/08 ,  C07K14/00 ,  C07K14/52 ,  C07K14/55 ,  C07K14/56 ,  A61P1/16

CPC分类号： C07H15/08 ,  A61K38/00 ,  C07H15/04 ,  C07K14/00 ,  C07K14/52 ,  C07K14/55 ,  C07K14/56

摘要： Modified physiologically active protein which can be produced by reacting a physiologically active protein having a molecular weight falling within the range of from 1 x 10 to 2 x 10 and carrying at least one Gln residue serving as the substitute of transglutaminase with a branched ligand consisting of an amino acid derivative having a lower binding affinity to the asialoglycoprotein receptor located on hepatic parenchymal cells than that to asialoorsomucoid and carrying an amino group and a galactose (Gal) or N-acetylgalactosamine (GalNAc) group serving as the substrate of transglutaminase in the presence of a transglutaminase originating in a microorganism to thereby form an amide bond between the gamma -carboxyamide group of the glutamate residue in the physiologically active protein and the terminal amino group in the branched ligand; and a process for producing the same.

公开(公告)号：EP1595870A4

公开(公告)日：2009-02-25

申请号：EP04713193

申请日：2004-02-20

申请人： AJINOMOTO KK

发明人： KATAOKA NORIYASU ,  TATARA AKINORI ,  YATAGAI MASANOBU ,  YAMANAKA JUNKO

IPC分类号： C07C233/87 ,  C07D239/96 ,  C07C229/54 ,  C07C275/42

CPC分类号： C07D239/96 ,  C07C233/87

摘要： A process for producing a phenylalanine derivative which has a quinazolinedione ring and is represented by the formula (5), which comprises reacting an acylphenylalanine derivative represented by the formula (1) with a reagent for carbonyl group introduction and an anthranilic acid derivative to form an asymmetric urea intermediate, converting this asymmetric urea intermediate to a quinazolinedione compound in the presence of a base, and N-alkylating the resultant quinazolinedione compound at the amide group of the quinazolinedione ring with an N-alkylating agent. This process is suitable for the industrial production of the phenylalanine derivative containing a quinazolinedione skeleton, which is a compound highly useful as a medicine having integrin α4 inhibitory activity. In the formulae (1) and (5), R1 represents substituted phenyl, etc.; R2 represents alkyl, etc.; R3 represents dialkylamino, etc.; and R4 represents alkyl, etc.

公开(公告)号：EP1219611A4

公开(公告)日：2003-03-19

申请号：EP00956884

申请日：2000-09-01

申请人： AJINOMOTO KK

发明人： SEKIYAMA TAKAAKI ,  MATSUZAWA TOSHIHIRO ,  YAMAMOTO TAKASHI ,  YATAGAI MASANOBU ,  EZAKI JUNKO

IPC分类号： C07D207/16 ,  C07D267/18 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D413/06 ,  C07D207/16 ,  C07D267/18 ,  C07D413/12 ,  C07D413/14

摘要： Industrially advantageous processes for preparing 5-substituted-5,11-dihydrodibenz[b,e][1,4]oxazepine derivatives through intramolecular arylation and reduction from [2-(2-bromobenzyloxy)phenyl]amide derivatives bearing via amide linkage substituents to be introduced at the 5-position. More particularly, a process which comprises subjecting (R)-1-[(4-methoxyphenyl)acetyl]pyrrolidine-2-carboxylic [2-(2-bromobenzyloxy)phenyl]amide to intramolecular arylation to form (R)-[[2-(5,11-dihydrodibenz[b,e][1,4]oxazepine-5-carbonyl)pyrrolidin]-1-yl]-2-(4-methoxyphenyl)ethanone and then reducing the obtained compound.

公开(公告)号：EP1489066A4

公开(公告)日：2006-05-31

申请号：EP03743568

申请日：2003-03-04

申请人： AJINOMOTO KK

发明人： YATAGAI MASANOBU ,  MINOMURA MASAFUMI ,  TSUCHIYA SHIGEKATSU

IPC分类号： C07C51/41 ,  C07C51/43 ,  C07C51/487 ,  C07C61/04 ,  C07B57/00 ,  C07C211/62

CPC分类号： C07C51/43 ,  C07B2200/07 ,  C07C51/412 ,  C07C51/487 ,  C07C2601/02 ,  C07C61/04

摘要： The invention provides a process for production of optically active 2,2-dimethylcyclopropanecarboxylic acid by reacting an optical isomer mixture of 2,2-dimethylcyclo- propanecarboxylic acid with an optically inactive amine to form (precipitate or crystallize) an ammonium salt of optically active 2,2-dimethylcyclopropanecarboxylic acid, e.g., optically active (S)-(+)-2,2-dimethylcyclopropanecarboxylic acid. According to the invention, the production (including optical resolution, separation of optical isomers, and purification of optical isomers) of optically active 2,2-dimethylcyclopropanecarboxylic acid important as an intermediate in the production of agricultural chemicals and drugs can be easily carried out at a low cost. Further, the invention provides intermediates for the above production (e.g., ammonium salts of optically active 2,2-dimethylcyclopropanecarboxylic acid, particularly, ammonium salts of optically active (S)-(+)-2,2-dimethyl- cyclopropanecarboxylic acid) and reagents for optical resolution for the separation of optically active 2,2- dimethylcyclopropanecarboxylic acid (e.g., optically inactive amines).

公开(公告)号：EP0987273A4

公开(公告)日：2001-11-07

申请号：EP98923090

申请日：1998-06-02

申请人： AJINOMOTO KK

发明人： KATAOKA NORIYASU ,  TANAKA KENZO ,  YATAGAI MASANOBU

IPC分类号： C07H17/08

CPC分类号： C07H17/08 ,  Y02P20/55

摘要： An industrializable process for preparing V-28-3M useful as an antifungal by methylating V-28-3 efficiently. The process comprises protecting the amino group of the amino sugar moiety of V-28-3 with a suitable protective group, methylating the carboxyl group of V-28-3 with methyl methanesulfonate or p-toluenesulfonate in the presence of a base, and removing the amino protective group of the resultant methyl ester.

摘要翻译： 用于通过有效地甲基化V-28-3来制备可用作抗真菌剂的V-28-3M的可工业化方法。 该方法包括用合适的保护基保护V-28-3的氨基糖部分的氨基，在碱存在下用甲磺酸甲酯或对甲苯磺酸甲酯将V-28-3的羧基甲基化， 所得甲酯的氨基保护基。