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Last Updated: April 23, 2024

Claims for Patent: 9,108,975

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Summary for Patent: 9,108,975

Title:	Crystal of 6,7-unsaturated-7-carbamoyl morphinan derivative and method for producing the same
Abstract:	Stable crystalline forms of a compound represented by the formula (IA): ##STR00001## an acid addition salt, and/or a solvate thereof are provided by the present invention. Said crystalline forms are extremely useful as materials for preparing medicines. Novel processes for preparing 6,7-unsaturated-7-carbamoyl morphinan derivatives are also provided by the present invention.
Inventor(s):	Tamura; Yoshinori (Toyonaka, JP), Noguchi; Kouichi (Amagasaki, JP), Inagaki; Masanao (Toyonaka, JP), Morimoto; Kenji (Toyonaka, JP), Haga; Nobuhiro (Toyonaka, JP), Oda; Shinichi (Iwate-ken, JP), Omura; Sohei (Amagasaki, JP)
Assignee:	Shionogi & Co., LTD. (Osaka, JP)
Application Number:	13/884,770
Patent Claims:	1. A p-toluenesulfonic acid salt of a compound of the formula (IA): ##STR00050## 2. A crystal of a p-toluenesulfonic acid salt of a compound of the formula (IA): ##STR00051## 3. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal has peaks at diffraction angles (2.theta.) of: 7.8.degree..+-.0.2.degree., 10.6.degree.,.+-.0.2.degree., 15.6.degree..+-.0.2, 17.8.degree..+-.0.2.degree. and 21.5.degree..+-.0.2.degree.. 4. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal has peaks at diffraction angles (2.theta.) of: 7.8.degree..+-.0.2.degree., 10.6.degree..+-.0.2.degree., 15.6.degree..+-.0.2.degree., 18.6.degree.,.+-.0.2.degree., 20.4.degree..+-.0,2.degree., 21.9.degree..+-.0.2.degree., 23.6.degree..+-.0.2.degree. and 25.5.degree..+-.0.2.degree.. 5. The crystal of the p-toluenesuifonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal is substantially identical to FIG. 1. 6. The crystal of the p-toluenesuifonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal has peaks at diffraction angles (2.theta.) of: 12.9.degree..+-.0.2.degree., 17.6.degree..+-.0.2.degree., 22.4.degree.,02.degree., 25.4.degree..+-.0,2.degree. and 28.7.degree..+-.0.2.degree.. 7. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal has peaks at diffraction angles (2.theta.) of: 6.6.degree..+-.0.2.degree., 8.9.degree..+-.0.2.degree.11.4.degree..+-.0.2.degree., 12.9.degree..+-.0.2.degree., 14.0.degree..+-.0.2.degree., 15.0.degree..+-.0.2.degree., 17.6.degree..+-.0.2.degree., 18.2.degree..+-.0.2.degree.22.4.degree..+-.0.2.degree.25.4.degree..+-.0.2- .degree. and 28.7.degree...+-.0.2.degree.. 8. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal is substantially identical to FIG. 2. 9. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal has peaks at diffraction angles (2.theta.) of: 8.8.degree..+-.0.2.degree., 17.5.degree..+-.0.2.degree., 21.9.degree..+-.0.2.degree., 23.7.degree..+-.0.2.degree. and 26.1.degree..+-.0.2.degree.. 10. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal has peaks at diffraction angles (2.theta.) of: 7.1.degree..+-.0.2.degree., 8.8.degree..+-.0.2.degree., 17.5.degree..+-.0.2.degree., 19.2.degree..+-.0.2.degree., 19.7.degree..+-.0.2.degree., 21.2.degree..+-.0.2.degree., 21.9.degree..+-.0.2.degree.23.7.degree..+-.0.2.degree., 24.5.degree..+-.0.2.degree. and 26.1.degree..+-.0.2.degree.. 11. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the X-ray powder diffraction spectrum of the crystal is substantially identical to FIG. 3. 12. A pharmaceutical composition comprising the crystal according to claim 2. 13. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the salt is a non-solvate. 14. The crystal of the p-toluenesulfonic acid salt according to claim 2, wherein the salt is a hydrate. 15. The crystal of the p-toluenesulfonic acid salt according to claim 14, wherein the crystal is Form I hydrate. 16. The crystal of the p-toluenesulfonic acid salt according to claim 14, wherein the crystal is Form II hydrate. 17. The p-toluenesulfonic acid salt of claim 1, wherein the salt is a hydrate, 18. The p-toluenesulfonic acid salt of claim 1, wherein the salt is a non-solvate,

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