Crystalline polymorphs of a CXC-chemokine receptor ligand
View Patent ↗The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
1. A crystalline Form IV of a monohydrate of Compound A of the formula:
that exhibits a powder x-ray diffraction pattern as shown in FIG. 4 .
2. A process for preparing the crystalline Form IV of claim 1 from Compound A
comprising the step of mixing Compound A with acetonitrile as a slurry at room temperature until Form IV crystals precipitate.
3. A process for preparing the crystalline Form IV of claim 1 from Compound A
comprising the steps of:
a) mixing Compound A with a first mixture of n-propanol and water to form a second mixture;
b) agitating said second mixture while heating to about 70 ° C. until substantially all solids are dissolved;
c) cooling said second mixture to about 60 ° C.; and
d) agitating said second mixture until Form IV crystals precipitate.
4. The process of claim 3 wherein the first mixture comprises n-propanol and water in a ratio of about 1.1:1.
5. A capsule comprising a crystalline Form IV of claim 1 , and at least one pharmaceutically acceptable excipient or carrier.