Polymorphs with tyrosine kinase activity
AssigneeMerck & Co., Inc.
InventorsMatthew M. Zhao, Mark T. Bilodeau
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Abstract
The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, retinal ischemia, macular edema, inflammatory diseases, and the like in mammals.
Claims36
Polymorph Form 1 of the free base of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide characterized by an X-ray powder diffraction pattern having diffraction angles of:
- 4.42, 8.93, 12.69, 13.39, 13.95, 14.44, 15.44, 15.72, 16.60, 18.31, 19.84, 21.55, 22.86, 23.54, 24.87, 25.92, 27.73, and 28.53.
Polymorph Form 2 of the free base of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide characterized by an X-ray powder diffraction pattern having diffraction angles of:
- 4.29, 8.72, 12.35, 13.16, 14.50, 15.05, 15.83, 16.06, 16.44, 16.84, 18.04, 19.73, 21.15, 22.27, 23.41, 24.65, 25.05, 25.57, 26.25, and 27.11.
The composition of claim 24, wherein the second compound is an estrogen receptor modulator selected from tamoxifen and raloxifene.
The method of claim 31 wherein the GPIIb/IIIa antagonist is tirofiban.
Dependencies are inferred from the claim text.