Claims for Patent: 9,717,720

Summary for Patent: 9,717,720

Title:	Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
Abstract:	The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2. ##STR00001##
Inventor(s):	Wilson; Jo Ann (San Francisco, CA), Shah; Khalid (South San Francisco, CA)
Assignee:	Exelixis, Inc. (South San Francisco, CA)
Application Number:	13/984,559
Patent Claims:	1. A capsule pharmaceutical composition: TABLE-US-00014 Ingredient .times..times..times..times..times..times..times..times..times. ##EQU00001## Compound IB with 50 ppm or less 10 of 6,7-dimethoxy-quinoline-4-ol (10 percent drug load formulation) Silicified Microcrystalline Cellulose 78.7 Croscarmellose sodium 5 Sodium starch glycolate 5 Fumed Silica 0.3 Stearic acid 1 Total 100 wherein compound IB has the structure: ##STR00034## 2. The capsule pharmaceutical composition of claim 1, wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 25 ppm or less from 0 to 6 months at 25.degree. C. and 60 percent relative humidity. 3. The capsule pharmaceutical composition of claim 1, wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 15 ppm or less from 0 to 6 months at 25.degree. C. and 60 percent relative humidity. 4. The capsule pharmaceutical composition of claim 1, wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 10 ppm or less from 0 to 6 months at 25.degree. C. and 60 percent relative humidity. 5. A capsule pharmaceutical composition: TABLE-US-00015 Ingredient .times..times..times..times..times..times..times..times..times. ##EQU00002## Compound IB with 50 ppm or less 50 of 6,7-dimethoxy-quinoline-4-ol (50 percent drug load formulation) Silicified Microcrystalline Cellulose 37.7 Croscarmellose sodium 5 Sodium starch glycolate 5 Fumed Silica 0.3 Stearic acid 2 Total 100 wherein compound IB has the structure: ##STR00035## 6. The capsule pharmaceutical composition of claim 5, wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 25 ppm or less from 0 to 6 months at 25.degree. C. and 60 percent relative humidity. 7. The capsule pharmaceutical composition of claim 5, wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 15 ppm or less from 0 to 6 months at 25.degree. C. and 60 percent relative humidity. 8. The capsule pharmaceutical composition of claim 5, wherein the formation of 6,7-dimethoxy-quinoline-4-ol in the pharmaceutical composition is minimized to 10 ppm or less from 0 to 6 months at 25.degree. C. and 60 percent relative humidity. 9. The capsule pharmaceutical composition of claim 1 containing 25 mg of Compound IB. 10. The capsule pharmaceutical composition of claim 9 containing: TABLE-US-00016 Ingredient mg/unit dose Silicified Microcrystalline Cellulose 196.75 Croscarmellose sodium 12.5 Sodium starch glycolate 12.5 Fumed Silica 0.75 Stearic acid 2.5. 11. The capsule pharmaceutical composition of claim 5 containing 100 mg of Compound IB. 12. The capsule pharmaceutical composition of claim 11 containing: TABLE-US-00017 Ingredient mg/unit dose Silicified Microcrystalline Cellulose 75.40 Croscarmellose sodium 10.00 Sodium starch glycolate 10.00 Fumed Silica 0.6 Stearic acid 4.0.