Title:
TEGAFUR COCRYSTAL
Document Type and Number:
WIPO Patent Application WO/2021/072771
Kind Code:
A1
Abstract:
Provided is a tegafur-1,2-bis(4-pyridyl)ethylene cocrystal. The present invention relates to the technical field of crystal form drug molecules. According to the tegafur cocrystal, Cu-Kα radiation is used, and an X-ray diffraction pattern represented in 2θ has characteristic peaks at 6.26+/−0.2°, 9.30+/−0.2°, 11.89+/−0.2°, 12.60+/−0.2°, 14.79+/−0.2°, 20.28+/−0.2°, 23.98+/−0.2° and 26.43+/−0.2°; the crystallographic measurement parameter is: a triclinic system with a chiral space group of P-1; and cell parameters are: a=5.1391(4) Å, b=9.7392(7) Å, c=13.9658(10) Å, α=96.008(6)°, β=92.368(7)°, γ=103.481(7)°, and unit cell volume V=674.44(9) Å 3. Also provided are a related preparation method and a use. The tegafur-1,2-bis(4-pyridyl)ethylene cocrystal is good in stability and has a high solubility and dissolution rate.
Inventors:
ZHAI LIHAI (CN)
LU YUANSHENG (CN)
MA CHAO (CN)
XIE YINJIE (CN)
LIU YUNNA (CN)
LU YUANSHENG (CN)
MA CHAO (CN)
XIE YINJIE (CN)
LIU YUNNA (CN)
Application Number:
PCT/CN2019/112026
Publication Date:
April 22, 2021
Filing Date:
October 18, 2019
Export Citation:
Assignee:
SHANDONG NEW TIME PHARMACEUTICAL CO LTD (CN)
International Classes:
A61K31/4164; C07D405/04; A61P35/00; C07C231/24; C07C235/46
Foreign References:
| CN104496972A | 2015-04-08 | |||
| CN103159746A | 2013-06-19 |
Other References:
AITIPAMULA SRINIVASULU, CHOW PUI SHAN, TAN REGINALD B. H.: "Crystal Engineering of Tegafur Cocrystals: Structural Analysis and Physicochemical Properties", CRYSTAL GROWTH & DESIGN, ASC WASHINGTON DC, US, vol. 14, no. 12, 3 December 2014 (2014-12-03), US, pages 6557 - 6569, XP055803688, ISSN: 1528-7483, DOI: 10.1021/cg501469r
CYSEWSKI PIOTR: "Transferability of cocrystallization propensities between aromatic and heteroaromatic amides", STRUCTURAL CHEMISTRY, SPRINGER US, NEW YORK, vol. 27, no. 5, 18 April 2016 (2016-04-18), New York, pages 1403 - 1412, XP036047678, ISSN: 1040-0400, DOI: 10.1007/s11224-016-0760-7
CYSEWSKI PIOTR: "Transferability of cocrystallization propensities between aromatic and heteroaromatic amides", STRUCTURAL CHEMISTRY, SPRINGER US, NEW YORK, vol. 27, no. 5, 18 April 2016 (2016-04-18), New York, pages 1403 - 1412, XP036047678, ISSN: 1040-0400, DOI: 10.1007/s11224-016-0760-7
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