Claims for Patent: 10,023,560

Summary for Patent: 10,023,560

Title:	Crystalline salt form of (S)-(2-(6 chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-meth- oxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonist
Abstract:	The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-- yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.
Inventor(s):	Boss; Christoph (Allschwil, CH), Brotschi; Christine (Allschwil, CH), Gude; Markus (Allschwil, CH), Heidmann; Bibia (Allschwil, CH), Sifferlen; Thierry (Allschwil, CH), Von Raumer; Markus (Allschwil, CH), Williams; Jodi T. (Allschwil, CH)
Assignee:	IDORSIA PHARMACEUTICALS LTD (Allschwil, CH)
Application Number:	15/702,281
Patent Claims:	1. A method of treatment of a sleep disorder, an anxiety disorder, or an addiction disorder, a cognitive dysfunction, a mood disorder, or an appetite disorder; comprising administering to a patient an effective amount of the compound (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-- yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride in crystalline form; wherein said crystalline form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2.theta.: 11.0.degree., 24.1.degree. and 24.5.degree., wherein said X-ray powder diffraction diagram is obtained by using combined Cu K.alpha.1 and K.alpha.2 radiation, without K.alpha.2 stripping; and the accuracy of the 2.theta. values is in the range of 2.theta.+/-0.2.degree.. 2. The method of claim 1, wherein said crystalline form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2.theta.: 9.2.degree., 11.0.degree., 13.8.degree., 15.1.degree., 16.3.degree., 16.8.degree., 19.8.degree., 24.1.degree., 24.5.degree., and 27.3.degree., wherein said X-ray powder diffraction diagram is obtained by using combined Cu K.alpha.1 and K.alpha.2 radiation, without K.alpha.2 stripping; and the accuracy of the 2.theta. values is in the range of 2.theta.+/-0.2.degree.. 3. The method of claim 1, wherein said crystalline form essentially shows the X-ray powder diffraction pattern as depicted in FIG. 2. 4. The method of claim 2, wherein the sleep disorder is a dyssomnia, a parasomnia, a sleep disorders associated with a general medical condition, or a substance-induced sleep disorder. 5. The method of claim 4, wherein the anxiety disorder is a post-traumatic stress disorder, an obsessive compulsive disorder, a panic attack, a phobic anxiety, or an avoidance. 6. A method of treatment of a sleep disorder; comprising administering to a patient an effective amount of the compound (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-- yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride in crystalline form; wherein said crystalline form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2.theta.: 11.0.degree., 24.1.degree. and 24.5.degree., wherein said X-ray powder diffraction diagram is obtained by using combined Cu K.alpha.1 and K.alpha.2 radiation, without K.alpha.2 stripping; and the accuracy of the 2.theta. values is in the range of 2.theta.+/-0.2.degree.. 7. The method of claim 6, wherein said crystalline form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2.theta.: 9.2.degree., 11.0.degree., 13.8.degree., 15.1.degree., 16.3.degree., 16.8.degree., 19.8.degree., 24.1.degree., 24.5.degree., and 27.3.degree., wherein said X-ray powder diffraction diagram is obtained by using combined Cu K.alpha.1 and K.alpha.2 radiation, without K.alpha.2 stripping; and the accuracy of the 2.theta. values is in the range of 2.theta.+/-0.2.degree.. 8. The method of claim 7, wherein the sleep disorder is a dyssomnia, a parasomnia, a sleep disorder associated with a general medical condition, or a substance-induced sleep disorder. 9. The method of claim 7, wherein the sleep disorder is an insomnia, a sleep-related dystonia; a restless leg syndrome; a sleep apnea; a jet-lag syndrome; a shift work sleep disorder, a delayed or advanced sleep phase syndrome, or an insomnia related to psychiatric disorders. 10. The method of claim 7, wherein the sleep disorder is an insomnia. 11. A method of treatment of an anxiety disorder; comprising administering to a patient an effective amount of the compound (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-- yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride in crystalline form; wherein said crystalline form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2.theta.: 11.0.degree., 24.1.degree. and 24.5.degree., wherein said X-ray powder diffraction diagram is obtained by using combined Cu K.alpha.1 and K.alpha.2 radiation, without K.alpha.2 stripping; and the accuracy of the 2.theta. values is in the range of 2.theta.+/-0.2.degree.. 12. The method of claim 11, wherein said crystalline form comprises peaks in the X-ray powder diffraction diagram at the following angles of refraction 2.theta.: 9.2.degree., 11.0.degree., 13.8.degree., 15.1.degree., 16.3.degree., 16.8.degree., 19.8.degree., 24.1.degree., 24.5.degree., and 27.3.degree., wherein said X-ray powder diffraction diagram is obtained by using combined Cu K.alpha.1 and K.alpha.2 radiation, without K.alpha.2 stripping; and the accuracy of the 2.theta. values is in the range of 2.theta.+/-0.2.degree.. 13. The method of claim 12, wherein the anxiety disorder is a post-traumatic stress disorder, an obsessive compulsive disorder, a panic attack, a phobic anxiety, or an avoidance.