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1. (WO2017004537) (4-((3R,4R)-3-METHOXYTETRAHYDRO-PYRAN-4-YLAMINO)PIPERIDIN-1-YL)(5-METHYL-6-(((2R,6S)-6-(P-TOLYL)TETRAHYDRO-2H-PYRAN-2-YL)METHYLAMINO)PYRIMIDIN-4YL)METHANONE CITRATE
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What is claimed is:

1. Citrate salt of compound I:


having the formula


2. The salt according to claim 1 in crystalline form.

3. The crystalline form according to claim 2 showing a X-ray powder diffraction pattern comprising peaks at the following 2-theta values measured using monochromatic CuKal radiation of λ = 1.54056 A, 40kV, 40mA: 19.1° and 22.4°.

4. The crystalline form according to claim 3, characterized in that the X-ray powder diffraction pattern further comprises a peak at 12.2°.

5. The crystalline form according to any of claims 3 or 4, characterized in that the X-ray powder diffraction pattern further comprises a peak at 13.7°.

6. The crystalline form according to any of claims 3 to 5, characterized in that the X-ray powder diffraction pattern further comprises a peak at 14.6°.

7. The crystalline form according to any of claims 3 to 6, characterized in that the X-ray powder diffraction pattern further comprises a peak at 18.7°.

8. The crystalline form according to any of claims 3 to 7, characterized in that the X-ray powder diffraction pattern further comprises a peak at 24.6°.

9. The crystalline form according to any of claims 3 to 8, characterized in that X-ray powder diffraction pattern further comprises a peak at 26.3°.

10. The crystalline form according to claim 2, exhibiting a X-ray powder diffraction pattern comprising peaks at the following 2-theta values measured using monochromatic CuKal

radiation of λ = 1.54056 A, 40kV, 40mA: 12.2 ± 0.2, 13.7 ± 0.2, 14.6 ± 0.2, 19.1 ± 0.2, and 22.4 ± 0.2.

1 1. The crystalline form according to claim 2, exhibiting a X-ray powder diffraction pattern comprising peaks at the following 2-theta values measured using monochromatic CuKal radiation of λ = 1.54056 A, 40kV, 40mA: 12.2 ± 0.2, 13.7 ± 0.2, 14.6 ± 0.2, 18.7 ± 0.2, 19.1 ± 0.2, 22.4 ± 0.2, 24.6 ± 0.2, and 26.3 ± 0.2.

12. The crystalline form according to any one of claims 3-11 , wherein the relative intensity of the peak at said diffraction angles 2-theta is at least 10%.

13. The crystalline form according to any one of claims 3-11 , wherein the relative intensity of the peak at said diffraction angles 2-theta is at least 15%.

14. The crystalline form according to claim 2, wherein the X-ray powder diffraction pattern is substantially as shown in Figure 2.

15. The crystalline form according to claim 2, characterized by the following X-ray powder diffraction partem expressed in terms of diffraction angle 2Θ, inter-planar distances d, and relative intensity (expressed as a ercentage with respect to the most intense peak):



16. The crystalline form according to any one claims 2-15, wherein the form has a Raman spectrum comprising peaks at any one or all of the following Raman shifts expressed in wavenumbers in cm"1 : 1718, 1242, 731 , 662, 553.

17. The crystalline form according to any one of claims 2-16, wherein the form has a melting point of 212 ± 5°C.

18. The crystalline form according to any one of claims 2-16, wherein the form has a differential scanning calorimetry curve substantially the same as shown in Figure 3.

19. A pharmaceutical composition comprising a salt according to claim 1 together with one or more inert carriers and/or diluents.

20. A pharmaceutical composition comprising a crystalline form according to any one of claims 2-9 together with one or more inert carriers and/or diluents.

21. A pharmaceutical composition comprising a crystalline form according to claim 10 together with one or more inert carriers and/or diluents.

22. A pharmaceutical composition comprising a crystalline form according to any one of claims 11-18 together with one or more inert carriers and/or diluents.

23. The salt according to claim 2 or a crystalline form according to any one of the claims 2-18 for use as a medicament.

24. A method of treating a condition selected from pain, osteroarthritis, diabetic nephropathy, and diabetic polyneuropathy, comprising administering to a patient in need thereof a therapeutically effective amount of a salt of claim 1 or a crystalline form of any one of claims 2-18 to treat the condition.

25. The method of claim 24, wherein the condition is pain.

26. The method of claim 25, wherein the condition is inflammatory pain.

27. The method of claim 24, wherein the condition is chronic pain.

28. The method of claim 24, wherein the condition is pain due to osteoarthritis.

29. The method of claim 24, wherein the condition is neuropathic pain or visceral pain.

30. The method of claim 24, wherein the condition is selected from the group consisting of acute and chronic mild to moderate musculoskeletal pain, low back pain, chronic low back pain, pain related to rheumatoid arthritis, shoulder pain, dental pain, signs and symptoms of osteoarthritis, osteoarthritis of the knee, osteoarthritis of the hip, osteoarthritis of the hand, pain associated with osteoarthritis, cancer pain, diabetic polyneuropathy, visceral pain, acute pain, diabetic nephropathy, and neuropathic pain.

31. The method of claim 24, wherein the condition is pain selected from (a) trigeminal neuralgia and (b) pain due to chemotherapy caused nerve injury.

32. The method of claim 24, wherein the condition is osteoarthritis.

33. The method of any one of claims 24-32, wherein the method comprises administering to the patient a therapeutically effective amount of a salt of claim 1 to treat the condition.

34. A method for preparing compound 1


comprising the following steps:

c) addition of citric acid to a solution of compound I


in an organic solvent

d) isolation of the resulting salt 1 in pure form.

35. The method according to claim 34 characterized in that the organic solvent in step a) is selected from the group consisting of ethyl acetate, isopropanol and a mixture of isopropanol and water.