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Claims for Patent: 7,767,678

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Claims for Patent: 7,767,678

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 (Westfield, NJ)
Assignee: Wyeth LLC (Madison, NJ)
Application Number:11/478,216
Patent 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 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.

2. The 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: 9.19, 9.98, 11.48, 14.32, 14.85, 15.64, 19.16, 19.45, 19.71, 20.46, 21.29, 22.33, 22.58, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, 28.42, 29.51, 30.32, 31.40, and 32.39.

3. The 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 2, having the x-ray diffraction pattern substantially as shown in FIG. 1 as Pattern A.

4. 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 a transition temperature to a liquid of about 109.degree. C. to about 115.degree. C.

5. The 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 4, wherein the transition temperature to a liquid is about 112.degree. C.

6. A method of preparing 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate (Form I) comprising the step of treating anhydrous 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile with heated water.

7. A method of preparing 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile monohydrate (Form I) comprising the step of converting polymorphs of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile, which have a x-ray diffraction pattern substantially the same as one of Patterns B, C, and D, as shown in FIG. 1 and as Form VI pattern in FIG. 11, by treatment with water.

8. The method of claim 6, wherein the water is heated to at least about 90.degree. C.

9. The method of claim 8, wherein the water is heated to at least about 95.degree. C.

10. The method of claim 7, wherein the water is at a temperature where no heat source or cold source is applied.

11. The method of claim 10, wherein the water is at room temperature.

12. A pharmaceutical composition comprising a therapeutically effective amount of crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-pipera- zinyl)propoxy]-3-quinolinecarbonitrile and a pharmaceutically acceptable carrier, wherein more than 50% by weight of said therapeutically effective amount consists of a crystalline form having an x-ray diffraction pattern substantially as shown in FIG. 1 as Pattern A and in FIG. 11 as Form I.

13. The composition of claim 12, further comprising acetic acid.

14. The composition of claim 12, further comprising a detergent.

15. The composition of claim 12, 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.

16. The composition of claim 12, further comprising about 2.0% by weight detergent and about 0.06% by weight acetic acid.

17. The composition of claim 12, wherein the pharmaceutically acceptable carrier is selected from a sugar, a polyol and cellulose, or a combination thereof.

18. The composition of claim 17, wherein the pharmaceutically acceptable carrier is a polyol and cellulose.

19. The composition of claim 18, wherein the polyol is selected from mannitol, sorbitol and xylitol.

20. The composition of claim 19, wherein the polyol is mannitol.

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