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Claims for Patent: 5,248,699

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Claims for Patent: 5,248,699

Title: Sertraline polymorph
Abstract:This invention relates to a novel crystalline polymorphic form of sertraline hydrochloride, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4 -tetrahydro-N-methyl-1-naphthalenamine hydrochloride, and to a method for preparing it.
Inventor(s): Sysko; Robert J. (Niantic, CT), Allen; Douglas J. M. (New London, CT)
Assignee: Pfizer Inc. (New York, NY)
Application Number:07/929,326
Patent Claims: 1. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine that exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2 .theta. at approximately 7.1, 12.7, 14.1, 15.3, 15.7, 21.2 23.4 and 26.3.

2. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine that exhibits an infrared absorption spectrum in potassium bromide having characteristic absorption bands expressed in reciprocal centimeters at approximately:

3100-3000 (W)*; 3000-2800(m)*, 2710-2500(m); 2500-2450(m); 1585(m); 1560(m); 1470-1450 (s)*; 1400(s), 1430(m); 1375(m); 1340(m) 1215(m); 1135(s); 1060(m); 1030(m); 1015(m); 955(m); 930(m); 920(m); 825(s); 800(s); 790(s); 760(s); 710(m); 700(s); 670(s); .noteq.*(w) = weak intensity; (m) = medium intensity; (s) = strong intensity.

3. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine according to claim 1 that exhibits an infrared absorption spectrum in potassium bromide having characteristic absorption bands expressed in reciprocal centimeters at approximately:

3100-3000(w)*; 3000-2800(m)*, 2710-2500(m); 2500-2450(m); 1585(m); 1560(m); 1470-1450(s)*; 1400(s), 1430(m); 1375(m); 1340(m) 1215(m); 1135(s); 1060(m); 1030(m); 1015(m); 955(m); 930(m); 920(m); 825(s); 800(s); 790(s); 760(s); 710(m); 700(s); 670(s); .noteq.*(w) = weak intensity; (m) = medium intensity; (s) = strong intensity.

4. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine that exhibits a single crystal X-ray crystallographic analysis with (a) crystal parameters that are approximately equal to the following:

wherein a, b and c and .alpha., .beta. and .gamma. are as previously defined; and (b) atomic positions of all atoms relative to the origin of the unit cell as recited in Tables 3 and 7, and as represented in FIG. 3.

5. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl -1-naphthalenamine according to claim 1 that exhibits a single crystal X-ray crystallographic analysis with (a) crystal parameters that are approximately equal to the following:

wherein a, b and c and .alpha., .beta. and .gamma. are as previously defined; and (b) atomic positions of all atoms relative to the origin of the unit cell as recited in Tables 3 and 7, and as represented in FIG. 3.

6. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine according to claim 2 that exhibits a single crystal X-ray crystallographic analysis with (a) crystal parameters that are approximately equal to the following:

wherein a, b and c and .alpha., .beta. and .gamma. are as previously defined; and (b) atomic positions of all atoms relative to the origin of the unit cell as recited in Tables 3 and 7, and as represented in FIG. 3.

7. A crystalline polymorph of the hydrochloride salt of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine according to claim 3 that exhibits a single crystal X-ray crystallographic analysis with (a) crystal parameters that are approximately equal to the following:

wherein a, b and c and .alpha., .beta. and .gamma. are as previously defined; and (b) atomic positions of all atoms relative to the origin of the unit cell as recited in Tables 3 and 7, and as represented in FIG. 3.

8. A pharmaceutical composition comprising an amount of a polymorph according to claim 1 effective in treating depression, anxiety-related disorders, obesity, chemical dependencies or addictions orpremature ejaculation in a human, and a pharmaceutically acceptable carrier.

9. A pharmaceutical composition comprising an amount of a polymorph according to claim 2 effective in treating depression, anxiety-related disorders, obesity, chemical dependencies or addictions or premature ejaculation in a human, and a pharmaceutically acceptable carrier.

10. A pharmaceutical composition comprising an amount of a polymorph according to claim 4 effective in treating depression, anxiety-related disorders, obesity, chemical dependencies or addictions or premature ejaculation in a human, and a pharmaceutically acceptable carrier.

11. A pharmaceutical composition comprising an amount of a polymorph according to of claim 7 effective in treating depression, anxiety-related disorders, obesity, chemical dependencies or addictions or premature ejaculation in a human, and a pharmaceutically acceptable carrier.

12. A method of treating a condition selected from depression, anxiety-related disorders, obesity, chemical dependencies and addictions and premature ejaculation in a human, comprising administering to said human an amount of a polymorph according to claim 1 effective in treating such condition.

13. A method of treating a condition selected from depression, anxiety-related disorders, obesity, chemical dependencies and addictions and premature ejaculation in a human, comprising administering to said human an amount of a polymorph according to claim 2 effective in treating such condition.

14. A method of treating a condition selected from depression, anxiety-related disorders, obesity, chemical dependencies and addictions and premature ejaculation in a human, comprising administering to said human an amount of a polymorph according to claim 4 effective in treating such condition.

15. A method of treating a condition selected from depression, anxiety-related disorders, obesity, chemical dependencies and addictions and premature ejaculation in a human, comprising administering to said human an amount of a polymorph according to claim 7 effective in treating such condition.
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