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Title:
CRYSTAL FORM OF DEUTERATED AZD9291, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/214886
Kind Code:
A1
Abstract:
The present invention pertains to the technical field of pharmaceuticals, and specifically discloses a crystal form of a deuterated AZD9291, a method for preparing the crystal form, and a use of the crystal form. An X-ray powder diffraction of the crystal form of the deuterated AZD9291 measured using Cu-Kα rays has diffraction peaks at 7.1 ± 0.2, 8.5 ± 0.2, 9.4 ± 0.2, 10.3 ± 0.2, 15.1 ± 0.2, 16.3 ± 0.2, 18.7 ± 0.2, 22.0 ± 0.2, 25.6 ± 0.2, and 26.0 ± 0.2. The present invention further discloses a use of the crystal form of the deuterated AZD9291 in the preparation of medicaments for the treatment of cancer. The crystal form of the deuterated AZD9291 provided by the present invention has stable physical and chemical properties and good metabolic stability, and blood concentrations in vivo and concentrations in the brain thereof are significantly improved, achieving an improved therapeutic effect.

Inventors:
WU, Yusheng (7 Dongqing Street, Hi-Tech Industries Development ZoneZhengzhou, Henan 0, 450000, CN)
GENG, Yang (7 Dongqing Street, Hi-Tech Industries Development ZoneZhengzhou, Henan 0, 450000, CN)
LIANG, Apeng (7 Dongqing Street, Hi-Tech Industries Development ZoneZhengzhou, Henan 0, 450000, CN)
NIU, Chengshan (7 Dongqing Street, Hi-Tech Industries Development ZoneZhengzhou, Henan 0, 450000, CN)
Application Number:
CN2018/087902
Publication Date:
November 29, 2018
Filing Date:
May 22, 2018
Export Citation:
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Assignee:
DEURACOR THERAPEUTIC, INC. (Room 1403-2, Block A Changxing World Trade Building,No. 1278, Mingzhu Road,Changxing Economic Development Zon, Huzhou Zhejiang 0, 313100, CN)
International Classes:
C07D403/04; A61K31/506; A61P35/00
Domestic Patent References:
WO2013014448A12013-01-31
WO2017219500A12017-12-28
WO2018050052A12018-03-22
Foreign References:
CN104140418A2014-11-12
CN106674202A2017-05-17
CN103702990A2014-04-02
CN106432231A2017-02-22
CN104140418A2014-11-12
CN105237515A2016-01-13
CN102659692A2012-09-12
US8916572B22014-12-23
CN107382879A2017-11-24
Other References:
NEW ENGLAND JOURNAL OF MEDICINE, 2008, pages 1160 - 1174
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2004, pages 1 - 11
SCIENCE, vol. 304, 2004, pages 1497 - 1500
NEW ENGLAND JOURNAL OF MEDICINE, vol. 350, 2004, pages 2129 - 2139
CLIN. CANCER RES., vol. 22, no. 20, 2016, pages 5130 - 5140
Attorney, Agent or Firm:
CHINA WISPRO INTELLECTUAL PROPERTY LLP. (Room A806, Zhongdi BuildingChina University of Geosciences Base,No. 8 Yuexing 3rd Road, High-Tech Industrial Estate, Nanshan Distric, Shenzhen Guangdong 7, 518057, CN)
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