US 11,993,582 B2
Crystalline forms of a LTA4H inhibitor
Andreas Kordikowski, Binningen (CH); and Yanxiang Wu, Shanghai (CN)
Assigned to Novartis AG, Basel (CH)
Appl. No. 17/264,333
Filed by Novartis AG, Basel (CH)
PCT Filed Jul. 29, 2019, PCT No. PCT/IB2019/056436
§ 371(c)(1), (2) Date Jan. 29, 2021,
PCT Pub. No. WO2020/026108, PCT Pub. Date Feb. 6, 2020.
Claims priority of application No. PCT/CN2018/000278 (WO), filed on Jul. 31, 2018.
Prior Publication US 2021/0300897 A1, Sep. 30, 2021
Int. Cl. C07D 401/12 (2006.01); A61K 31/4439 (2006.01); A61K 45/06 (2006.01)
CPC C07D 401/12 (2013.01) [A61K 31/4439 (2013.01); A61K 45/06 (2013.01); C07B 2200/13 (2013.01)] 16 Claims
 
1. A crystalline form B of the compound (S)-3-amino-4-(5-(4-((5-chloro-3-fluoropyridin-2-yl)oxy)phenyl)-2H-tetrazol-2-yl)butanoic acid in its free form, characterized by one of the following characteristics:
(i) an x-ray powder diffraction pattern comprising representative peaks in terms of 2θ at 22.6±0.2°2θ, 24.1±0.2°2θ and 26.3±0.2°2θ, measured at a temperature of about 25° C. and an x-ray wavelength, λ, of 1.5418 Å;
(ii) an x-ray powder diffraction pattern comprising four or more 2θ values selected from the group consisting of 11.3±0.2°2θ, 12.8 0.2°2θ, 15.2±0.2°2θ, 19.7±0.2°2θ, 20.0±0.2°2θ, 20.3±0.2°2θ, 21.0±0.2°2θ, 22.6±0.2°2θ, 24.1±0.2°2θ, 24.4±0.2°2θ, 25.1±0.2°2θ, 26.3±0.2°2θ, 28.5±0.2°2θ, and 30.0±0.2°2θ, measured at a temperature of about 25° C. and an x-ray wavelength, λ, of 1.5418 Å; and
(iii) an x-ray powder diffraction pattern comprising five or more 2θ values selected from the group consisting of 11.3±0.2°2θ, 12.8 0.2°2θ, 15.2±0.2°2θ, 19.7±0.2°2θ, 20.0±0.2°2θ, 20.3±0.2°2θ, 21.0±0.2°2θ, 22.6±0.2°2θ, 24.1±0.2°2θ, 24.4±0.2°2θ, 25.1±0.2°2θ, 26.3±0.2°2θ, 28.5±0.2°2θ, and 30.0±0.2°2θ, measured at a temperature of about 25° C. and an x-ray wavelength, λ, of 1.5418 Å.