Title:
SALTS OF COMPOUND, CRYSTALLINE FORMS THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2020/253875
Kind Code:
A1
Abstract:
Disclosed are a fumaric acid salt, a maleic acid salt, an adipic acid salt, a succinic acid salt, a plurality of crystalline forms of a compound 5-fluorine-4-(7'-fluorine-2'-methyl spiro [cyclopentane-1,3'-indol]-5'-yl)-nitrogen-(5-(1-methylpiperidine-4-yl)pyridine-2-yl)pyrimidine-2-amine, a preparation method therefor and an application thereof. It has been proved that the salts or the crystalline forms thereof can replace 5-fluorine-4-(7'-fluorine-2'-methyl spiro [cyclopentane-1,3'-indol]-5'-yl)-nitrogen-(5-(1-methylpiperidine-4-yl)pyridine-2-yl)pyrimidine-2-amine better, overcome the defects thereof such as the solubility, high risk of food effect and stability, and have low hygroscopicity and great application value.
Inventors:
YIN LEI (CN)
YAO ZHENGLIN (CN)
YAO ZHENGLIN (CN)
Application Number:
PCT/CN2020/097482
Publication Date:
December 24, 2020
Filing Date:
June 22, 2020
Export Citation:
Assignee:
GAN & LEE PHARMACEUTICALS (CN)
International Classes:
C07D401/14; A61K31/506; A61P35/00; A61P35/02; C07D471/04
Foreign References:
| CN106810536A | 2017-06-09 | |||
| CN106810536A | 2017-06-09 | |||
| CN106810536A | 2017-06-09 |
Other References:
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YIN, L. ET AL.: "A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 144, 6 December 2017 (2017-12-06), XP055766971, ISSN: 0223-5234, DOI: 20200904170248PX
YIN, L. ET AL.: "A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 144, 6 December 2017 (2017-12-06), XP055766971, ISSN: 0223-5234, DOI: 20200904174508X
MA KE: "Research progress in antitumor effect of a CDK4/6 inhibitor", WORLD NOTES ON ANTIBIOTICS, vol. 34, no. 5, 2013, pages 197 - 202
MALUMBRES MBARBACID M.: "To cycle or not to cycle: a critical decision in cancer [J", NATURE REVIEWS CANCER, vol. 1, no. 3, 2001, pages 222, XP008150580, DOI: 10.1038/35106065
SHAPIRO GI.: "Cyclin-dependent kinase pathways as targets for cancer treatment [J", J CLINICAL ONCOLOGY, vol. 24, no. 11, 2006, pages 1770, XP009148872, DOI: 10.1200/JCO.2005.03.7689
YIN, L. ET AL.: "A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 144, 6 December 2017 (2017-12-06), XP055766971, ISSN: 0223-5234, DOI: 20200904170248PX
YIN, L. ET AL.: "A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 144, 6 December 2017 (2017-12-06), XP055766971, ISSN: 0223-5234, DOI: 20200904174508X
MA KE: "Research progress in antitumor effect of a CDK4/6 inhibitor", WORLD NOTES ON ANTIBIOTICS, vol. 34, no. 5, 2013, pages 197 - 202
MALUMBRES MBARBACID M.: "To cycle or not to cycle: a critical decision in cancer [J", NATURE REVIEWS CANCER, vol. 1, no. 3, 2001, pages 222, XP008150580, DOI: 10.1038/35106065
SHAPIRO GI.: "Cyclin-dependent kinase pathways as targets for cancer treatment [J", J CLINICAL ONCOLOGY, vol. 24, no. 11, 2006, pages 1770, XP009148872, DOI: 10.1200/JCO.2005.03.7689
Attorney, Agent or Firm:
CHINA SCIENCE PATENT & TRADEMARK AGENT LTD. (CN)
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