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A novel stable and non-solvate crystal form II on Apremilast and processes for the preparation thereof

Times:2015-04-18

 We are planning to transfer the right of patent application on the crystal form II of Apremilast to companies who are interested in. Pls contact with us if you need more information.

We found a novel  crystal form on Apremilast and named it as crystal form II,which is completely different from  crystalline A, B, C, D, E, F and G reported by Celgene. Its DSC spectrum  exhibits a single peak about 150℃and its TG spectrum show a mass loss of less than about  0.5% when heated from about 25 to 150℃.
   
Our study confirmed that the crystal form II is the most thermodynamically stable anhydrous form of apremilast than the crystal form A, B, C, D, E, F and G because the crystal form A-G could  be totally converted to crystal form II in some condition without dissolving. There are almost no difference in solubility between II and B in all kinds of solvents. Recently we performed comparison experiment on rats, and the absorption of those 2 crystallines are very similar, except stronger activity of Crystalline II in female rats. Moreover, the absorption of those 2 crystal are very similar on dog. 
  Now we resubmitted the relate patent application on the Crystal form II of Apremilast in China, the application number is CN201510101009. Next, we will apply for PCT patent ASAP.
Patents on Apremilast:
CN201410335852.6,CN201510101009.6,PCT/CN2015/000566

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