Crystalline forms of a Bruton's tyrosine kinase inhibitor
AssigneePharmacyclics, Inc.
InventorsNorbert Purro, Mark Smyth, Erick Goldman, David D. Wirth
Life of this patent
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Abstract
Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Claims31
A method of treating cancer in a mammal comprising administering to the mammal a pharmaceutical formulation comprising:
- (a) about 40 mgs to about 200 mgs of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one;
- (b) about 40 wt % to about 50 wt % of a diluent;
- (c) about 3 wt % to about 10 wt % of a disintegrating agent;
- (d) about 2 wt % to about 7 wt % of a surfactant;
- and
- (e) about 0.2 wt % to about 1.0 wt % of a lubricant,
- wherein the cancer is
- (i) a B cell malignancy,
- (ii) lymphoma, leukemia, or a solid tumor, or
- (iii) diffuse large B cell lymphoma, follicular lymphoma, small lymphocytic lymphoma, chronic lymphocytic leukemia, B cell prolymphocytic leukemia, lymphoplasmacytic lymphoma/Waldenström macroglobulinemia, splenic marginal zone lymphoma, plasma cell myeloma, plasmacytoma, extranodal marginal zone B cell lymphoma, nodal marginal zone B cell lymphoma, mantle cell lymphoma, mediastinal (thymic) large B cell lymphoma, intravascular large B cell lymphoma, primary effusion lymphoma, burkitt lymphoma/leukemia, lymphomatoid granulomatosis, or multiple myeloma.
A method of treating cancer in a mammal comprising administering to the mammal a pharmaceutical formulation comprising:
- (a) 140 mgs of 1 ((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one;
- (b) 151.4 mgs of microcrystalline cellulose;
- (c) 23.0 mgs of croscarmellose sodium;
- (d) 14.0 mgs of sodium lauryl sulfate;
- and
- (e) 1.6 mgs of magnesium stearate,
- wherein the cancer is
- (i) a B cell malignancy,
- (ii) lymphoma, leukemia, or a solid tumor, or
- (iii) diffuse large B cell lymphoma, follicular lymphoma, small lymphocytic lymphoma, chronic lymphocytic leukemia, B cell prolymphocytic leukemia, lymphoplasmacytic lymphoma/Waldenström macroglobulinemia, splenic marginal zone lymphoma, plasma cell myeloma, plasmacytoma, extranodal marginal zone B cell lymphoma, nodal marginal zone B cell lymphoma, mantle cell lymphoma, mediastinal (thymic) large B cell lymphoma, intravascular large B cell lymphoma, primary effusion lymphoma, burkitt lymphoma/leukemia, lymphomatoid granulomatosis, or multiple myeloma.
A method of treating cancer in a mammal comprising administering to the mammal a pharmaceutical formulation comprising:
- (a) about 40 wt % to about 50 wt % of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one;
- (b) about 40 wt % to about 50 wt % of microcrystalline cellulose;
- (c) about 3 wt % to about 10 wt % of croscarmellose sodium;
- (d) about 2 wt % to about 7 wt % of sodium lauryl sulfate;
- and
- (e) about 0.2 wt % to about 1.0 wt % of magnesium stearate,
- wherein the cancer is
- (i) a B cell malignancy,
- (ii) lymphoma, leukemia, or a solid tumor, or
- (iii) diffuse large B cell lymphoma, follicular lymphoma, small lymphocytic lymphoma, chronic lymphocytic leukemia, B cell prolymphocytic leukemia, lymphoplasmacytic lymphoma/Waldenström macroglobulinemia, splenic marginal zone lymphoma, plasma cell myeloma, plasmacytoma, extranodal marginal zone B cell lymphoma, nodal marginal zone B cell lymphoma, mantle cell lymphoma, mediastinal (thymic) large B cell lymphoma, intravascular large B cell lymphoma, primary effusion lymphoma, burkitt lymphoma/leukemia, lymphomatoid granulomatosis, or multiple myeloma.
Dependencies are inferred from the claim text.