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Last Updated: March 29, 2024

Details for Patent: 7,803,805


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Title:Cristalline 3-{(3R,4R)-4 methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}- -3-oxo-propionitrile mono citrate salt
Abstract: This invention relates to novel amorphous and crystallline forms of 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3 -oxo-propionitrile mono citrate salt, useful as inhibitors of protein kinases, and to their methods of preparation.
Inventor(s): Flanagan; Mark E. (Gales Ferry, CT), Li; Zheng J. (Quaker Hill, CT)
Assignee: Pfizer Inc. (Madison, NJ)
Filing Date:Jan 10, 2005
Application Number:11/032,990
Claims:1. A method for treating or preventing organ transplant rejection in a mammal, including a human, comprising administering to said mammal an amount of crystalline 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3-oxo-propionitrile mono citrate salt effective in treating or preventing organ transplant rejection.

2. The method of claim 1 wherein said crystalline 3-{(3R,4R)4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pip- eridin-1-yl}-3-oxo-propionitrile mono citrate salt is characterized by an x-ray powder diffraction pattern having characteristic peaks expressed in degrees two-theta at approximately 5.7, 16.1, 20.2 and 20.5.

3. The method of claim 2 wherein said powder diffraction pattern has characteristic peaks expressed in degree of 2-theta at approximately: TABLE-US-00002 Angle 2-theta 5.7 7.7 8.9 11.0 11.5 13.6 13.9 14.8 15.2 16.1 16.6 17.3 18.7 20.2 20.5 21.1 21.4 22.0 23.0 23.4 24.0 25.0 25.5 26.2 27.0 27.5 28.1 28.7 29.4 30.1 30.3 31.1 32.0 32.8 33.6 34.4 34.8 35.3 35.9 36.5 37.8 38.5 39.2.

4. The method of claim 1 wherein said crystalline 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3-oxo-propionitrile mono citrate salt has an onset melting temperature of between about 199.degree. C. to about 206.degree. C.

5. A method for treating asthma in a mammal comprising administering to said mammal an amount of crystalline 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3-oxo-propionitrile mono citrate salt effective in treating asthma.

6. The method according to claim 5, wherein the crystalline 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3-oxo-propionitrile mono citrate salt is administered in combination with one or more of cyclosporin A, rapamycin, tacrolimus, leflunomide, deoxyspergualin, mycophenolate, azathioprine, daclizumab, muromonab-CD3, antithymocyte globulin, aspirin, acetaminophen, ibuprofen, naproxen, piroxicam, prednisolone or dexamethasone.

7. The method of claim 5 wherein said crystalline 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3-oxo-propionitrile mono citrate salt has an onset melting temperature of between about 199.degree. C. to about 206.degree. C.

8. The method of claim 5 wherein said crystalline 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pi- peridin-1-yl}-3-oxo-propionitrile mono citrate salt is characterized by an x-ray powder diffraction pattern having characteristic peaks expressed in degrees two-theta at approximately 5.7, 16.1, 20.2 and 20.5.

9. The method of claim 8 wherein said powder diffraction pattern has characteristic peaks expressed in degree of 2-theta at approximately: TABLE-US-00003 Angle 2-theta 5.7 7.7 8.9 11.0 11.5 13.6 13.9 14.8 15.2 16.1 16.6 17.3 18.7 20.2 20.5 21.1 21.4 22.0 23.0 23.4 24.0 25.0 25.5 26.2 27.0 27.5 28.1 28.7 29.4 30.1 30.3 31.1 32.0 32.8 33.6 34.4 34.8 35.3 35.9 36.5 37.8 38.5 39.2.

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