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Crystalline Form of N-(2-(4-(4-fluorobenzylcarbamoyl) -5- hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2-yl)propan-2-yl) -5- methyl-1,3,4-oxadiazole-2- carboxamide

IP.com Disclosure Number: IPCOM000209436D
Publication Date: 2011-Aug-04
Document File: 2 page(s) / 15K

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     Crystalline Form of N-(2-(4-(4-fluorobenzylcarbamoyl) -5- hydroxy-1-methyl-6-oxo-1, 6-dihydropyrimidin-2-yl)propan-2-yl) -5- methyl-1,3,4-oxadiazole-2- carboxamide

    N-(2-(4-(4-fluorobenzylcarbamoyl) -5-hydroxy-1-methyl-6-oxo-1, 6- dihydropyrimidin-2-yl)propan-2-yl) -5-methyl-1,3,4-oxadiazole-2- carboxamide, referred to as Compound I, has the following structure:

O

OH

F

N

   N N

O

  HN O

HN

N

O

    Crystalline form of Compound I was found and described herein. The crystalline form of Compound I is characterized by data selected from: X-ray powder diffraction ("XRPD") peaks at: 9.0, 10.8, 13.8, 14.5, 17.2, 19.7, 20.8, 23.2,


25.0 and 26.4 degrees two-theta ± 0.2 degrees two-theta; an XRPD pattern as depicted in figure 1; and combinations thereof.

Figure 1: XRPD of Crystalline Form of Compound I

10000

Intensity(counts)

6400

3600

1600

400

0

5

10

15

20

25

30

35

2Theta (°)

1


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EXAMPLES PXRD method

The X-ray powder diffraction was performed on a SCINTAG X-Ray powder diffractometer model X'TRA equipped with a solid-state detector. Copper radiation of 1.5418 Å was used to analyze the samples, which were in round aluminum sample holders with zero background. The scanning parameters were: range: 2-40 degrees two-theta; scan mode: continuous scan; step size: 0.05 deg.; and scan rate: 3 deg/min.

Preparation of starting materials

The starting Compound I may be prepared according to U.S. Patent

Application Publication No. US 2006/0122205, Example 1.

Example 1: Preparation o...