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Title:
OPTICALLY PURE DIASTEREOMER OF 10-PROPARGYL-10-DEAZA AMINOPTERIN, AND METHOD OF USING THE SAME
Document Type and Number:
Japanese Patent JP2016006111
Kind Code:
A
Abstract:
PROBLEM TO BE SOLVED: To provide a compound that is useful for the treatment of cancer and inflammatory disorder, and a pharmaceutical composition that contains the compound.SOLUTION: Provided is: a compound comprising a substantially pure diastereomer of 10-propargyl-10-deaza aminopterin which is (2S)-2-[[4-[(1S)-1-[(2,4-diamino pteridine-6-yl)methyl]buta-3-ynyl]benzoyl]amino]pentane-dioic acid or (2S)-2-[[4-[(1R)-1-[(2,4-diamino pteridine-6-yl)methyl]buta-3-ynyl]benzoyl]amino]pentane-dioic acid, or a salt thereof; and a pharmaceutical composition containing the compound. The salt preferably is hydrochloride. The pharmaceutical composition preferably is for oral administration or for intravenous administration.

Inventors:
GIJSBERTUS J PRONK
Application Number:
JP2015163581A
Publication Date:
January 14, 2016
Filing Date:
August 21, 2015
Export Citation:
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Assignee:
ALLOS THERAPEUTICS INC
International Classes:
C07D475/08; A61K31/519; A61P19/02; A61P29/00; A61P35/00; A61P35/02
Domestic Patent References:
JP2001505537A2001-04-24
JP2013518879A2013-05-23
Foreign References:
US5374726A1994-12-20
WO2009136572A12009-11-12
Other References:
JPN6014022395; Allos Therapeutics et al: "FOLOTYN (pralatrexate injection)", [online] , 200909, p.1-12, [平成26年5月27日検索]
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JPN6016017073; Clinical pharmacology & Therapeutics Vol.86(2), 2009, p.190-196
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JPN3014000279; 加藤隆一: '光学異性薬物の研究の流れ -その有効性と安全性-' 月刊薬事 VOL. 29, NO. 10, 19871001, PAGES 23-26, 薬業時報社
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JPN3014000281; 岡本一郎 他: '光学活性高分子を用いた光学異性体分離用液体クロマトグラフイーカラムの開発' 日本化学会誌 NO. 2, 19920210, PAGES 133-139
JPN3014000282; 牧野成夫: '液体クロマトグラフイー法によるキラル分離' 分離技術 VOL. 25, NO. 5, 19951005, PAGES 3-8, 分離技術懇話会
JPN3014000283; (社)日本化学会: 化学便覧 応用化学編 第5版, 19950315, PAGES II-567〜II-571, 丸善(株)
Attorney, Agent or Firm:
Shinjiro Ono
Yasushi Kobayashi
Shigeo Takeuchi
Osamu Yamamoto
Akiko Yamaguchi