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Crystalline Form of 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5- (trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide

IP.com Disclosure Number: IPCOM000195326D
Publication Date: 2010-Apr-29
Document File: 2 page(s) / 67K

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     Crystalline Form of 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5- (trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide

   4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3- pyridinyl)-2-pyrimidinyl]amino]-benzamide is known as NLT. NLT has the molecular formula: C28H22F3N7O, a molecular weight of 529.52gr/mol and the following chemical structure:

N

CH3

NH

N

F3C

HN

N

O

N

N

H3C

   NLT is a tyrosine kinase inhibitor used for the treatment of drug resistant chronic myelogenous leukemia (CML), and in particular, for the treatment of chronic phase and accelerated phase Philadelphia chromosome positive chronic myeloid leukemia (CML) in adult patients whose disease has progressed on or who cannot tolerate other therapies that included imatinib. NLT is administrated as a hydrochloride salt.

Crystalline form T5 of NLT HCl was obtained by the process described in example
1. Figure 1 presents the X-ray powder diffraction ("XRPD") of the obtained form.

Figure 1: XRPD of the Crystalline Form of NLT HCl Form T5

2400

2000

1600

1200

800

400

0

6.0 10.0 14.0 18.0 22.0 26.0 30.0 34.0 38.0

   According to figure 1, the crystalline form T5 of NLT HCl is characterized by XRPD peaks at: 7.1, 14.0, 18.4, 20.8, 21.5, 22.5, 24.8, 25.4 and 27.3± 0.2 degrees two-theta.

1

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   The x-ray powder diffraction was performed on an ARL X-ray powder diffractometer model X'TRA-019, with a Peltier detector. Copper Kα1 radiation (λ=1.5418 Å) was used....