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Claims for Patent: 8,470,842

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Claims for Patent: 8,470,842

Title:Hydrochloride salts of 8-[{1-(3,5-Bis-trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza- -spiro[4.5]decan-2-one and preparation process therefor
Abstract: Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
Inventor(s): Hu; Mengwei (Washington, NJ), Paliwal; Sunil (Monroe Township, NJ), Shih; Neng-Yang (Lexington, MA), Guenter; Frank Bruno (Schachen, CH), Mergelsberg; Ingrid (Mahwah, NJ)
Assignee: OPKO Health, Inc. (Miami, FL)
Application Number:12/614,108
Patent Claims: 1. A method of treating or delaying the onset of chemotherapy-induced nausea and/or chemotherapy-induced emesis in a mammal receiving chemotherapy which comprises administering to said mammal a medicament comprising a therapeutically effective amount of a crystalline Form I monohydrate hydrochloride salt form of the compound (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4,5]decan-2-one (Formula I): ##STR00006## wherein the crystalline Form I monohydrate hydrochloride salt form is characterized by an x-ray powder diffraction pattern including at least a strong peak having a diffraction angle (in 2.theta.) of 21.6.+-.0.2 and lattice spacing (in .ANG.) of 4.11.+-.0.04.

2. The method of claim 1 further comprising administering said medicament in combination with a therapeutically effective amount of a chemotherapeutic agent.

3. The method of claim 2 wherein said chemotherapeutic agent is temozolomide.

4. The method of claim 1, wherein one or more additional therapeutic agents are administered in combination with the crystalline Form I monohydrate hydrochloride salt form of the compound (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4,5]decan-2-one.

5. The method of claim 1 further comprising contemporaneous administration of a chemotherapeutic agent.

6. The method of claim 5 wherein the chemotherapeutic agent is temozolomide.

7. The method of claim 1, wherein the crystalline Form I monohydrate hydrochloride salt form of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4,5]decan-2-one is characterized by an x-ray powder diffraction pattern having at least one additional peak selected from TABLE-US-00028 Diffraction angle (2.THETA. .+-. 0.2) RI Lattice Spacing (.ANG. .+-. 0.04) 16.1 Medium 5.49 18.4 Medium 4.83 23.5 Medium 3.78.

8. The method of claim 1, wherein the crystalline Form I monohydrate hydrochloride salt form of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4,5]decan-2-one is characterized by an x-ray powder diffraction pattern having at least two additional peaks selected from TABLE-US-00029 Diffraction angle (2.THETA. .+-. 0.2) RI Lattice Spacing (.ANG. .+-. 0.04) 16.1 Medium 5.49 18.4 Medium 4.83 23.5 Medium 3.78.

9. The method of claim 1, wherein the crystalline Form I monohydrate hydrochloride salt form of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4,5]decan-2-one is characterized by an x-ray powder diffraction pattern which includes the following peaks: TABLE-US-00030 Diffraction angle (2.THETA. .+-. 0.2) RI Lattice Spacing (.ANG. .+-. 0.04) 16.1 Medium 5.49 18.4 Medium 4.83 21.6 Strong 4.11 23.5 Medium 3.78.

10. A method of treating or delaying the onset of nausea and/or emesis in a mammal which comprises administering to said mammal a medicament comprising a therapeutically effective amount of a crystalline Form I monohydrate hydrochloride salt form of the compound (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-ph- enyl-1,7-diazaspiro[4,5]decan-2-one (formula I): ##STR00007## characterized by an x-ray powder diffraction pattern substantially as shown in FIG. 1.

11. The method of claim 4, wherein the one or more additional therapeutic agents are selected from a 5HT.sub.3 inhibitor and a corticosteroid.

12. The method of claim 11, wherein the 5HT.sub.3 inhibitor is selected from ondensetron, granisetron, palonosetron, dolasetron and tropisetron.

13. The method of claim 11, wherein the corticosteroid is dexamethasone.

14. The method of claim 5, wherein the medicament is administered contemporaneously with the chemotherapeutic agent such that the medicament is administered before administration of the chemotherapeutic agent.

15. The method according to claim 5, wherein the medicament is administered contemporaneously with the chemotherapeutic agent such that the medicament is administered during administration of the chemotherapeutic agent.

16. The method according to claim 5, wherein the medicament is administered contemporaneously with the chemotherapeutic agent such that the medicament is administered after administration of the chemotherapeutic agent.
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