Title:
CRYSTALLINE FORMS OF N- (5- (5- ( (1R, 2S) -2-FLUOROCYCLOPROPYL) -1, 2, 4-OXADIAZOL-3-YL) -2-METHYLPHENYL) IMIDAZO [1, 2-A] PYRIDINE-3-CARBOXAMIDE
Document Type and Number:
WIPO Patent Application WO/2020/228746
Kind Code:
A1
Abstract:
Provided are crystalline forms of N-(5{5-((1R,2S)-2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide fumaric acid, in particular Form A and a N-(5{5-((1R,2S) -2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide fumaric acid co-crystal. Provided are also the processes for preparation of such crystalline forms. Furthermore, Provided is a pharmaceutical composition comprising said N-(5{5-((1R,2S)-2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide fumaric acid Form A, or said N-(5-(5-((1R,2S)-2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide fumaric acid co-crystal, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition can be used as a medicament, in particular for the treatment and/or prophylaxis of a mast-cell associated disease, a respiratory disease, an inflammatory disorder, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), an autoimmune disorder, a metabolic disease, a fibrosis disease.
Inventors:
WANG XIAOYANG (CN)
KORDIKOWSKI ANDREAS (CH)
KORDIKOWSKI ANDREAS (CH)
Application Number:
PCT/CN2020/090060
Publication Date:
November 19, 2020
Filing Date:
May 13, 2020
Export Citation:
Assignee:
NOVARTIS AG (CH)
International Classes:
C07D471/04; A61K31/437; A61P3/00; A61P11/00; A61P17/00; A61P29/00
Domestic Patent References:
| WO2013033070A1 | 2013-03-07 | |||
| WO2013033167A1 | 2013-03-07 | |||
| WO2013033203A1 | 2013-03-07 | |||
| WO2013033116A1 | 2013-03-07 |
Other References:
BABAEI, MARYAM ABBASPOUR ET AL.: "Receptor tyrosine kinase (c-Kit) inhibitors: a potential therapeutic target in cancer cells", DRUG DESIGN, DEVELOPMENT AND THERAPY, vol. 10, 31 December 2016 (2016-12-31), pages 2443 - 2459, XP055484967, DOI: 10.2147/DDDT.S89114
ROSKOSKI ROBERT JR.: "The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders", PHARMACOLOGICAL RESEARCH, vol. 133, 25 April 2018 (2018-04-25), pages 35 - 52, XP055678375, DOI: 10.1016/j.phrs.2018.04.020
See also references of EP 3969453A4
ROSKOSKI ROBERT JR.: "The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders", PHARMACOLOGICAL RESEARCH, vol. 133, 25 April 2018 (2018-04-25), pages 35 - 52, XP055678375, DOI: 10.1016/j.phrs.2018.04.020
See also references of EP 3969453A4
Attorney, Agent or Firm:
SHANGHAI PATENT & TRADEMARK LAW OFFICE, LLC (CN)
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