Aprepitant L-proline composition and cocrystal
A 1:1:1 aprepitant L-proline H 2 O composition and a 1:1:1 aprepitant L-proline H 2 O cocrystal are disclosed as well as pharmaceutical compositions containing a 1:1:1 aprepitant L-proline H 2 O composition or cocrystal and a pharmaceutically acceptable carrier. The 1:1:1 aprepitant L-proline H 2 O composition or cocrystal may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pairs, cancer, a skin disease, itch, a respiratory disease, or an addiction.
1. A 1:1:1 aprepitant L-proline H 2 O cocrystal.
2. A 1:1:1 aprepitant L-proline H 2 O cocrystal characterized by at least one of:
a powder x-ray diffraction pattern having at least three peaks selected from the peaks at 6.4. 9.4, 11.9, 12.9, 14.6, 18.8, and °2θ±0.2°2 θ;
a powder x-ray diffraction pattern substantially similar to FIG. 1 ;
a P 2 1 2 1 2 1 space group at a temperature of about 294 K; or
unit cell dimensions of a =9.1963(4) Å, b =12.8332(9) Å, c =27.4289(19) ⊙, α=90°, β=90°, and γ=90° at a temperature of about 294 K.
3. A pharmaceutical composition comprising a 1:1:1 aprepitant L-proline H 2 O cocrystal of claim 1 and a pharmaceutically acceptable carrier.
4. A method of treating disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch, a respiratory disease, an addiction comprising the step of administering to a patient in need thereof a therapeutically effective amount of a 1:1:1 aprepitant L-proline H 2 O cocrystal of claim 1 .
5. A method of treating disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch, a respiratory disease, an addiction comprising the step of administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition of claim 3 .
6. 1:1:1 aprepitant L-proline hydrate.
7. A pharmaceutical composition comprising 1:1:1 aprepitant L-proline hydrate of claim 6 and a pharmaceutically acceptable carrier.
8. A method of treating disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch, a respiratory disease, an addiction comprising the step of administering to a patient in need thereof a therapeutically effective amount of 1:1:1 aprepitant L-proline hydrate of claim 6 .
9. A method of treating disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch, a respiratory disease, an addiction comprising the step of administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition of claim 7 .
10. A pharmaceutical composition comprising a 1:1:1 aprepitant L-proline H 2 O cocrystal of claim 2 and a pharmaceutically acceptable carrier.
11. A method of treating or preventing disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch, a respiratory disease, an addiction comprising the step of administering to a patient in need thereof a therapeutically effective amount of 1:1:1 aprepitant L-proline H 2 O cocrystal of claim 2 .
12. A method of treating disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch, a respiratory disease, an addiction comprising the step of administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition of claim 10 .