Benzisoxazole derivative
The present invention relates to a medicament for treating various nervous system diseases or psychiatric diseases, comprising a compound of formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient, wherein R 1 is hydrogen, etc., R 2 is halogen, etc., R 3 , R 4 , R 5 , and R 6 are hydrogen, etc.
1. A compound of (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide or a pharmaceutically acceptable salt thereof.
2. The compound of claim 1 , which is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 5.7°±0.2 and 17.3°±0.2°.
3. The compound of claim 1 , which is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 8.7°±0.2° and 17.6°±0.2°.
4. The compound of claim 1 , which is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 11.1°±0.2° and 20.3°±0.2°.
5. A pharmaceutical composition, comprising:
the compound of claim 1 or a pharmaceutically acceptable salt thereof.
6. A pharmaceutical composition comprising:
the compound of claim 2 .
7. A pharmaceutical composition comprising:
the compound of claim 3 .
8. A pharmaceutical composition comprising:
the compound of claim 4 .
9. A method for treating at least one of levodopa-induced dyskinesia in Parkinson's disease, essential tremor, chemotherapy-induced peripheral neuropathy, allodynia associated with neuropathic pain, Parkinson's disease, and at least one Parkinson's disease symptom of tremor, muscle stiffness/muscle rigidity, akinesia/bradykinesia, impairment of postural reflex, sleep disorder, and anxiety, comprising:
administering a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof to a subject in need thereof.
10. The method of claim 9 , wherein (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 5.7°±0.2 and 17.3°±0.2°.
11. The method of claim 9 , wherein (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 8.7°±0.2° and 17.6°±0.2°.
12. The method of claim 9 , wherein (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 11.1°±0.2° and 20.3°±0.2°.
13. The method of claim 9 , wherein the disease which is treated is at least one of essential tremor, chemotherapy-induced peripheral neuropathy, Parkinson's disease, and at least one Parkinson's disease symptom of tremor, muscle stiffness/muscle rigidity, akinesia/bradykinesia, and impairment of postural reflex.
14. The method of claim 13 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 5.7°±0.2 and 17.3°±0.2°.
15. The method of claim 13 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 8.7°±0.2° and 17.6°±0.2°.
16. The method of claim 13 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 11.1°±0.2° and 20.3°±0.2°.
17. The method of claim 9 , wherein the disease which is treated is at least one of Parkinson's disease and at least one Parkinson's disease symptom of tremor, muscle stiffness/muscle rigidity, akinesia/bradykinesia, and impairment of postural reflex.
18. The method of claim 17 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 5.7°±0.2 and 17.3°±0.2°.
19. The method of claim 17 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 8.7°±0.2° and 17.6°±0.2°.
20. The method of claim 17 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 11.1°±0.2° and 20.3°±0.2°.
21. The method of claim 9 , wherein tremor as the Parkinson's disease symptom is treated.
22. The method of claim 21 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 5.7°±0.2 and 17.3°±0.2°.
23. The method of claim 21 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 8.7°±0.2° and 17.6°±0.2°.
24. The method of claim 21 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 11.1°±0.2° and 20.3°±0.2°.
25. The method of claim 9 , wherein the disease which is treated is essential tremor.
26. The method of claim 25 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 5.7°±0.2 and 17.3°±0.2°.
27. The method of claim 25 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 8.7°±0.2° and 17.6°±0.2°.
28. The method of claim 25 , wherein the (1R)-1-(1,2-benzoxazol-3-yl)ethane-1-sulfonamide is a crystalline form characterized by a powder x-ray diffraction pattern having diffraction angle (2θ°) peaks of 11.1°±0.2° and 20.3°±0.2°.