Crystalline forms of a LTA4H inhibitor
AssigneeNovartis AG
InventorsAndreas Kordikowski, Yanxiang Wu
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Abstract
This application relates to various crystalline forms of (S)-3-amino-4-(5-(4-((5-chloro-3-fluoropyridin-2-yl)oxy)phenyl)-2H-tetrazol-2-yl)butanoic acid in its free form, as well as compositions, method of making and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of diseases and disorders which are typically ameliorated by the inhibition of LTA4H. Such diseases and disorders may include inflammatory and autoimmune disorders and pulmonary and respiratory tract inflammation.
Claims16
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;
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- (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.
A crystalline form HB of a hydrate 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 22.1±0.2°2θ, 23.8±0.2°2θ, 24.7±0.2°2θ and 28.7±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 13.4±0.2°, 20.8±0.2°, 22.1±0.2°, 23.5±0.2°, 23.5±0.2°, 23.8±0.2, 24.7±0.2°2θ, 26.1±0.2°2θ, 26.9±0.2°2θ, 28.7±0.2°2θ, 30.4±0.2°2θ, 31.2±0.2°2θ, 33.8±0.2°2θ and 38.7±0.2°2θ, measured at a temperature of about 25° C. and an x-ray wavelength, λ, of 1.5418 Å;
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- (iii) an x-ray powder diffraction pattern comprising five or more 2θ values selected from the group consisting of 13.4±0.2°, 20.8±0.2°, 22.1±0.2°, 23.5±0.2°, 23.5±0.2°, 23.8±0.2, 24.7±0.2°2θ, 26.1±0.2°2θ, 26.9±0.2°2θ, 28.7±0.2°2θ, 30.4±0.2°2θ, 31.2±0.2°2θ, 33.8±0.2°2θ and 38.7±0.2°2θ, measured at a temperature of about 25° C. and an x-ray wavelength, λ, of 1.5418 Å.
Dependencies are inferred from the claim text.