Title:
NOVEL NONCRYSTALLINE BOSENTAN AND METHOD OF PRODUCING THE SAME
Document Type and Number:
Japanese Patent JP2013151431
Kind Code:
A
Abstract:
To solve a problem in which bosentan is N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-pyrimidine-4-yl]-4-tert-butylbenzene sulfonamide, has an endothelin receptor antagonist, and is used as a therapeutic agent of a pulmonary artery hypertension, however, the bosentan is a hardly-soluble drug, thereby the improvement of bioavailability by improving the solubility to water and the convenient industrial improving method are requested.
Bosentan is made noncrystalline bosentan by a solvent method, a fusion method, and a mechano chemical method or the like, thereby the bosentan can be produced more conveniently and in a shorter time than by a conventional production method, and further the solubility can be improved.
Inventors:
HIRAI YOSUKE
OSHIO NAOTAKA
SAKAI HITOSHI
TANAKA NOBUKAZU
SANADA KUNIO
OSHIO NAOTAKA
SAKAI HITOSHI
TANAKA NOBUKAZU
SANADA KUNIO
Application Number:
JP2010151423A
Publication Date:
August 08, 2013
Filing Date:
July 01, 2010
Export Citation:
Assignee:
FUJI CHEM IND CO LTD
International Classes:
C07D239/69; A61K31/506; A61P9/10; A61P9/12; A61P43/00
Domestic Patent References:
| JP2007527924A | 2007-10-04 | |||
| JP2008526780A | 2008-07-24 | |||
| JP2008507567A | 2008-03-13 |
Foreign References:
| WO2009141167A1 | 2009-11-26 | |||
| WO2009047637A1 | 2009-04-16 | |||
| WO2009141167A1 | 2009-11-26 |
Other References:
JPN6010046332; 石津 洋: '噴霧乾燥による難溶性医薬品の非晶化' 分離技術 Ｖｏｌ．３９， Ｎｏ．６, 2009, ｐ．３８８-３９２
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