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Title:
CRYSTALLINE POLYMORPHIC FORM OF ULIPRISTAL ACETATE
Document Type and Number:
WIPO Patent Application WO/2014/050107
Kind Code:
A1
Abstract:
A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.

Inventors:
IWASHITA SHIGEKI (JP)
HAYASHI HIROYUKI (JP)
MIYAZAKI KOICHI (JP)
Application Number:
PCT/JP2013/005710
Publication Date:
April 03, 2014
Filing Date:
September 26, 2013
Export Citation:
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Assignee:
ASKA PHARM CO LTD (JP)
International Classes:
C07J41/00; A61K31/58; A61P5/36
Domestic Patent References:
WO1996030390A21996-10-03
WO2007144674A12007-12-21
WO1989012448A11989-12-28
WO1996030390A21996-10-03
WO2010119029A12010-10-21
Foreign References:
EP1602662A12005-12-07
JP2953725B21999-09-27
JP2006519255A2006-08-24
JP2006515869A2006-06-08
JP2009539964A2009-11-19
Other References:
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; LUO, JUNZHI ET AL: "Ulipristal acetate with polymorph and preparation method thereof", XP002718838, retrieved from STN Database accession no. 2012:1391254
RAO P N ET AL: "A practical large-scale synthesis of 17alpha-acetoxy-11beta-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-di one (CDB-2914)", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 65, no. 7, 1 July 2000 (2000-07-01), pages 395 - 400, XP004222665, ISSN: 0039-128X, DOI: 10.1016/S0039-128X(00)00100-8
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; LI, JIANBING ET AL: "Ulipristal acetate crystal and its manufacture method", XP002718839, retrieved from STN Database accession no. 2013:137502
"Japanese Pharmacopoeia, (1) Handbook of Pharmaceutical Excipients", 1989, MARUZEN COMPANY, LTD.
"Japanese Pharmaceutical Excipients Dictionary 2007", July 2007, YAKUJI NIPPO LTD.
"Pharmaceutics", 1997, NANKODO, CO., LTD.
"Japanese Pharmaceutical Excipients 2003", August 2003, YAKUJI NIPPO LTD.
Attorney, Agent or Firm:
KUWATA, Mitsuo (6th Floor Minato Umeda Building, 3-17, Nishitemma 6-chome, Kita-ku, Osaka-sh, Osaka 47, JP)
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