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Title:
CRYSTALLINE FORM OF SOFPIRONIUM BROMIDE AND PREPARATION METHOD THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/235665
Kind Code:
A1
Abstract:
A cocrystal containing the 1'R-diastereomer and the 1'S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1'R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.

Inventors:
MARUBAYASHI KAZUYOSHI (JP)
WATANABE MASAHITO (JP)
BRINKMAN HERBERT R (US)
Application Number:
PCT/JP2020/020210
Publication Date:
November 26, 2020
Filing Date:
May 22, 2020
Export Citation:
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Assignee:
KAKEN PHARMA CO LTD (JP)
BRICKELL BIOTECH INC (US)
International Classes:
C07D207/12; A61K31/4015; A61P17/00; A61P43/00
Domestic Patent References:
WO2018026869A12018-02-08
WO2007059021A12007-05-24
WO2007058971A22007-05-24
Other References:
JI, F. et al., Synthesis and pharmacological effects of new, N-substituted soft anticholinergics based on glycopyrrolate, Journal of Pharmacy and Pharmacology, 2005, 57(11), pp. 1427-1435, DOI : 10.1211/jpp.57.11.0008 page 142, right column 3rd paragraph - page 1430, left column 1st paragraph, 2R-SGE
TOTH-SARUDY, E. et al., Preparation and biological effects of pure stereoisomeric novel soft anticholinergics, Pharmazie, 2006, 61(2), pp. 90-96, ISSN: 0031-7144 page 94, right column 3.1.1.2
See also references of EP 3972955A4
Attorney, Agent or Firm:
SIKS & CO. (JP)
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