Title:
PHARMACEUTICALLY ACCEPTABLE SALT OF EGFR INHIBITOR, CRYSTAL FORM THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/218963
Kind Code:
A1
Abstract:
Provided in the present invention are a pharmaceutically acceptable salt of an epidermal growth factor receptor (EGFR) inhibitor, a crystal form thereof, a preparation method therefor and an application thereof. The structural formula of the EGFR inhibitor is as shown in formula I, and the pharmaceutically acceptable salt is a mesylate, p-toluenesulfonate, phosphate, hydrochloride or citrate salt of the EGFR inhibitor. The pharmaceutically acceptable salt of the EGFR inhibitor of the present invention has a specific crystal form, is more soluble and stable than a corresponding free base, is more suitable for preparing medicine for use in treating cancer (especially non-small cell lung cancer), and satisfies the requirements for bioavailability and efficacy.
Inventors:
ZHOU PING (CN)
WU JIAQUAN (US)
JIN SHENSHUANG (CN)
LI LI (CN)
WU JIAQUAN (US)
JIN SHENSHUANG (CN)
LI LI (CN)
Application Number:
PCT/CN2018/070011
Publication Date:
December 06, 2018
Filing Date:
January 02, 2018
Export Citation:
Assignee:
WUXI SHUANGLIANG BIOTECHNOLOGY CO LTD (CN)
International Classes:
A61P35/00; C07D471/04; C07C59/265; C07C309/04; C07C309/30
Foreign References:
| CN106132957A | 2016-11-16 | |||
| CN103702990A | 2014-04-02 | |||
| CN106132957A | 2016-11-16 |
Other References:
LUO, JIEYING ET AL.: "Passage; Modern Physics and Pharmacy Theory and Practice", MODERN PHYSICS AND PHARMACY THEORY AND PRACTICE,20050430, 30 April 2005 (2005-04-30), pages 293 - 295, XP009515688, ISBN: 978-7-5439-2522-9
JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, 2009, pages 1231 - 1236
"Pharmacopoeia of the People's Republic of China", 2015
"People's Republic of China", 2015
See also references of EP 3502113A4
JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, 2009, pages 1231 - 1236
"Pharmacopoeia of the People's Republic of China", 2015
"People's Republic of China", 2015
See also references of EP 3502113A4
Attorney, Agent or Firm:
LINDA LIU & PARTNERS (CN)
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