Loading patent…
AssigneePharmacia Corporation
InventorsKimberley C. Allen, Jerry D. Clark, Thomas P. Fraher, Jason A. Hanko, Kimberly L. Kolbert, Clay R. Little, Michael K. Mao, Patricia S. Miyake, Jodi L. Moe, Partha S. Mudipalli, Tobin C. Schilke, Christine B. Seymour, Ahmad Y. Sheikh, Gopichand Yalamanchili
Estimating the term…
Crystalline forms of the p38 kinase inhibitor N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole are provided. These crystalline forms include (a) a first anhydrous crystalline form possessing improved physical stability relative to other solid-state forms of the compound; (b) a second anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; (c) a third anhydrous crystalline form possessing unique properties relative to other solid-state forms of the compound; and (d) solvated crystalline forms, hydrated crystalline forms, and crystalline salt forms of the compound that are useful, for example, as intermediate solid-state forms in the preparation of other crystalline forms of the compound. Also provided are combinations and pharmaceutical compositions comprising at least one of these crystalline forms, processes for preparing these crystalline forms and for preparing compositions comprising these crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of at least one of these crystalline forms.
Form I crystalline N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole having an X-ray powder diffraction pattern comprising a peak selected from the group consisting of 6.2 ±0.2, 12.3±0.2, 14.9±0.2, 17.1±0.2, and 19.5±0.2 degrees 2θ.
A pharmaceutical composition comprising N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole and one or more pharmaceutically acceptable excipients, wherein a detectable amount of the N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole is present as Form I crystalline N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole.
Form II crystalline N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole having an X-ray powder diffraction pattern comprising a peak selected from the group consisting of 4.7±0.2, 9.6±0.2, 14.5±0.2, 16.2 10.2 and 20.1±0.2 degrees 2θ.
A pharmaceutical composition comprising N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole and one or more pharmaceutically acceptable excipients, wherein a detectable amount of the N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole is present as Form II crystalline N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole.
Form III crystalline N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole having an X-ray powder diffraction pattern comprising a peak selected from the group consisting of 10.5±0.2, 11.7±0.2, 12.4±0.2 and 19.1±0.2 degrees 2θ.
A pharmaceutical composition comprising N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole and one or more pharmaceutically acceptable excipients, wherein a detectable amount of the N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole is present as Form III crystalline N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3 -(4-chlorophenyl)pyrazole.
A solvated crystalline form of N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole.
A hydrated crystalline form of N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole.
A crystalline salt of N-(2-hydroxyacetyl)-5-(4-piperidyl)-4-(4-pyrimidinyl)-3-(4-chlorophenyl)pyrazole selected from the group consisting of:
Dependencies are inferred from the claim text.