Claims for Patent: 6,169,084

Summary for Patent: 6,169,084

Title:	2-methyl-thieno-benzodiazepine formulation
Abstract:	The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.
Inventor(s):	Bunnell; Charles Arthur (Lafayette, IN), Ferguson; Thomas Harry (Greenfield, IN), Hendriksen; Barry Arnold (Guildford, GB), Sanchez-Felix; Manuel Vicente (Grayshott, GB), Tupper; David Edward (Reading, GB)
Assignee:	Eli Lilly and Company (Indianapolis, IN)
Application Number:	09/163,769
Patent Claims:	1. A compound which is an olanzapine pamoate salt or a solvates thereof. 2. A compound as claimed in claim 1 wherein the pamoate salt is olanzapine pamoate dimethanolate having a typical x-ray powder diffraction pattern as represented by the following interplanar spacing: TBL d-spacing Intensity 11.17 73 9.37 17 8.73 40 8.29 23 7.77 14 7.22 24 6.84 31 6.66 54 6.42 11 6.40 11 6.17 26 5.87 12 5.56 100 4.84 11 4.66 17 4.57 26 4.48 22 4.35 19 4.28 19 4.12 94 4.03 91 3.89 52 3.62 44 3.54 11 3.29 16 3.13 16. 3. A compound as claimed in claim 1 wherein the pamoate salt is olanzapine pamoate monohydrate having a typical x-ray powder diffraction pattern as represented by the following interplanar spacing: TBL d-spacing Intensity 10.76 98 9.20 62 8.38 85 8.18 24 7.62 20 6.67 18 6.56 18 6.51 20 6.44 20 6.11 26 5.88 22 5.64 15 5.38 100 4.90 11 4.72 12 4.64 17 4.48 18 4.35 23 4.29 31 4.24 32 4.09 71 4.02 84 3.98 73 3.81 23 3.62 14 3.52 30 3.39 11 3.25 12 2.90 15 2.85 13. 4. A compound as claimed in claim 1 wherein the pamoate salt is bis(olanzapine) pamoate acetone solvate having a typical x-ray powder diffraction pattern as represented by the following interplanar spacing: TBL d-spacing Intensity 16.87 32 9.58 35 8.88 80 8.40 16 8.19 35 7.85 16 7.34 29 7.22 25 7.04 30 6.87 18 6.77 11 6.73 11 6.65 21 6.36 12 6.26 26 5.76 31 5.58 79 5.53 100 5.45 61 5.32 42 5.19 39 5.02 55 4.91 69 4.87 51 4.85 57 4.69 44 4.61 68 4.44 23 4.34 14 4.18 17 4.07 36 3.99 28 3.93 65 3.81 23 3.78 24 3.77 20 3.65 23 3.59 28 3.45 13 3.32 19 3.25 26. 5. A compound as claimed in claim 1 wherein the pamoate salt is bis(olanzapine) pamoate monohydrate solvate having a typical x-ray powder diffraction pattern as represented by the following interplanar spacing: TBL d-spacing Intensity 15.77 26 10.44 23 9.64 24 9.31 13 8.27 23 8.17 14 8.13 14 7.84 27 7.81 30 7.41 60 7.12 40 7.00 13 6.96 13 6.55 45 6.18 53 5.87 38 5.80 19 5.59 89 5.25 26 5.00 34 4.96 31 4.88 61 4.85 73 4.71 34 4.52 19 4.33 11 4.19 100 4.12 48 4.05 39 3.97 30 3.89 31 3.80 29 3.72 20 3.70 21 3.58 33 3.45 27 3.04 13 2.84 16. 6. A compound as claimed in claim 1 wherein the pamoate salt is olanzapine pamoate THF solvate having a typical x-ray powder diffraction pattern as represented by the following interplanar spacing: TBL d-spacing Intensity 14.59 100 7.78 16 7.24 56 7.00 19 6.37 12 6.04 11 6.01 11 4.85 19 4.69 42 4.39 25 4.28 19 3.95 13 3.84 20. 7. A method of treating an animal, including a human suffering from or susceptible to psychosis, acute mania or mild anxiety states which comprises administering a pharmaceutically effective amount of a compound of claim 1, 2, 3, 4, 5 or 6.