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Details for Patent: 8,445,496

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Details for Patent: 8,445,496

Title:Crystalline forms of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile and methods of preparing the same
Abstract: This invention is directed to a crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 2.theta. angles (.degree.) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, and 29.51, and a transition temperature of about 109.degree. C. to about 115.degree. C.
Inventor(s): Tesconi; Marc Sadler (Monroe, NY), Feigelson; Gregg (Chester, NY), Strong; Henry (Somerset, NJ), Wen; Hong (North Potomac, MD)
Assignee: Wyeth LLC (Madison, NY)
Filing Date:Jun 22, 2010
Application Number:12/820,306
Claims:1. An isolated crystalline form of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate, having an x-ray diffraction pattern wherein at least one of the 2.theta. angles (.degree.) of the significant peaks is at about 7.62, 9.89, 10.49, 14.19, 15.24, 16.08, 16.76, 18.46, 21.79, 23.16, 24.88, 26.36, 27.40, 28.28 or 28.76.

2. The isolated crystalline form of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate of claim 1, having an x-ray diffraction pattern wherein 2.theta. angles (.degree.) of significant peaks are at about 7.62, 9.89, 10.49, 14.19, 15.24, 16.08, 16.76, 18.46, 21.79, 23.16, 24.88, 26.36, 27.40, 28.28 and 28.76.

3. A pharmaceutical composition comprising a therapeutically effective amount of a crystalline form of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate which has an x-ray diffraction pattern substantially as shown in FIG. 5, wherein more than 50% by weight of the crystalline form present is said crystalline form, and a pharmaceutically acceptable carrier.

4. The composition of claim 3, further comprising acetic acid.

5. The composition of claim 3, further comprising a detergent.

6. The composition of claim 3, further comprising about 0.5% to about 5.0% by weight of a detergent and about 0.01% to about 0.1% by weight acetic acid.

7. The composition of claim 3, further comprising about 2.0% by weight detergent and about 0.06% by weight acetic acid.

8. The composition of claim 3, wherein the pharmaceutically acceptable carrier is selected from a sugar, a polyol and cellulose, or a combination thereof

9. The composition of claim 8, wherein the pharmaceutically acceptable carrier is a polyol and cellulose.

10. The composition of claim 9, wherein the polyol is selected from mannitol, sorbitol and xylitol.

11. The composition of claim 10, wherein the polyol is mannitol.

12. The composition of claim 11, wherein the crystalline form of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate, the mannitol and the cellulose are individually present in amounts of about 20 to about 50 percent by weight.

13. An isolated crystalline form of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern substantially as shown in FIG. 5.
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