Patent EA-001881-B1 (EA)
Title: Olanzapine dehydrate d
Inventor: LARSEN SAMUEL D
IPC: A61K31/55
Filed: 1997-09-18
Abstract: 1. Dihydrate D olanzapine polymorph having a typical x-ray powder diffraction pattern as represented by the following interplanar spacings (d) as set forth in Table: Table 1 d 9,4511 7,7098 7,4482 6,9807 6,5252 5,7076 5,5539 5,223 4,9803 4,8908 4,784 4,6947 4,4271 4,3956 4,3492 4,2834 4,1156 3,7837 3,7118 3,5757 3,482 3,3758 3,3274 3,2413 3,1879 3,135 3,0979 3, 016 2,9637 2, 907 2,8256 2,7914 2,7317 2,6732 2. A Dihydrate D polymorph as claimed in Claim 1 further characterized by substantially the following x-ray powder diffraction pattern wherein d represents the interplanar spacing and I/I1, represents the typical relative intensities: D I/I1 9,4511 100,00 7,7098 14,23 7,4482 22,43 6,9807 5,73 6,5252 5,45 5,7076 4,24 5,5539 1,60 5,223 62,98 4,9803 22,21 4,8908 15,03 4,784 27,81 4,6947 5,15 4,4271 13,00 4,3956 16,63 4,3492 34,43 4,2834 51,38 4,1156 18,32 3,7837 5,30 3,7118 1,56 3,5757 0,71 3,482 9,39 3,3758 24,87 3,3274 13,49 3,2413 5,97 3,1879 1,04 3,135 3,18 3,0979 1,43 3,016 1,95 2,9637 0,48 2,907 2,42 2,8256 7,46 2,7914 3,61 2,7317 1,47 2,6732 5,19 2,5863 10,62 3. Dihydrate D of Claim 1 wherein the Dihydrate D comprises less than about 20% of Dehydrate B and less than about 0,5% of accompanying substances. 4. Dihydrate D of Claim 2 wherein the Dihydrate D comprises less than about 20% of Dehydrate B and less than about 0,5% of accompanying substances. 5. Dihydrate D of Claim 3 wherein the Dihydrate D comprises less than about 5% of Dehydrate B. 6. Dihydrate D of Claim 4 wherein the Dihydrate D comprises less than about 5% of Dehydrate B. 7. Dihydrate D of Claim 6 wherein the Dihydrate D comprises less than about 2% of Dehydrate B wherein Dihydrate B has a typical x-ray powder diffraction pattern as represented by the following interplanar spacings (d) as set forth in Table 2: d I/I1 9,9045 100,00 6,9985 0,39 6,763 0,17 6,4079 0,13 6,1548 0,85 6,0611 0,99 5,8933 0,35 5,6987 0,12 5,4395 1,30 5,1983 0,67 5,0843 0,24 4,9478 0,34 4,7941 6,53 4,696 1,26 4,5272 2,65 4,4351 2,18 4,3474 1,85 4,2657 0,49 4,1954 0,69 4,0555 0,42 3,9903 0,89 3,9244 1,52 3,8561 0,99 3,8137 1,44 3,7671 0,92 3,6989 1,78 3,6527 0,60 3,5665 0,34 3,4379 1,41 3,3911 0,27 3,3289 0,20 3,2316 0,31 3,1982 0,19 3,1393 0,35 3,0824 0,18 2,9899 0,26 2,9484 0,38 2,9081 0,29 2,8551 0,37 2,8324 0,49 2,751 0,37 2,7323 0,64 2,6787 0,23 2,6424 0,38 2,5937 0,21 8. Dihydrate D of Claim 1 wherein Dihydrate D is a stable crystalline pharmaceutically elegant polymorph. 9. Dihydrate D of Claim 2 wherein dihydrate D is a stable crystalline pharmaceutically elegant polymorph. 10. A pharmaceutical formulation comprising as an active ingredient a compound of Claim 1 associated with one or more pharmaceutically acceptable carriers, diluents, or excipients therefor. 11. A pharmaceutical formulation comprising as an active ingredient a compound of Claim 2 associated with one or more pharmaceutically acceptable carriers, diluents, or excipients therefor. 12. A formulation of Claim 10 wherein the formulation is an aqueous suspension. 13. A formulation of Claim 10 wherein the formulation is a tablet. 14. A pharmaceutical formulation comprising as an active ingredient a compound of Claim 3 associated with on or more pharmaceutically acceptable carriers, diluents, or excipients therefor. 15. A formulation of Claim 14 wherein the formulation is an aqueous suspension. 16. A method for treating a psychotic condition in a mammal comprising administering an effective amount of a compound of Claim 1. 15. A method for treating a condition selected from the group consisting of anxiety, schizophrenia, schizophreniform disorder, a functional bowel disorder, and psychosis in a mammal comprising administering an effective amount of a compound of Claim 1.