Claims for Patent: 8,951,504

Summary for Patent: 8,951,504

Title:	(trimethoxyphenylamino) pyrimidinyl formulations
Abstract:	There are provided pharmaceutical compositions comprising greater than 15% w/w of a compound of Formula (I) as defined herein and/or hydrate thereof and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them. ##STR00001##
Inventor(s):	Gururajan; Bindhumadhavan (Moindal, SE), Alhusban; Farhan Abdul Karim (Cheshire, GB), Gabbott; Ian Paul (Cheshire, GB), Sievwright; Dawn (Cheshire, GB), Brook; David Bradley (Cheshire, GB)
Assignee:	Rigel Pharmaceuticals, Inc. (South San Francisco, CA)
Application Number:	14/290,494
Patent Claims:	1. A method of treating a patient for rheumatoid arthritis, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I): ##STR00006## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 2. The method according to claim 1 wherein each X.sup.+ in the compound of Formula (I) represents a sodium cation (Na.sup.+). 3. The method according to claim 1 wherein the compound of Formula (I) is in the form of a hexahydrate. 4. A method of treating a patient for cancer, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I): ##STR00007## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 5. The method according to claim 4 wherein each X.sup.+ in the compound of Formula (I) represents a sodium cation (Na.sup.+). 6. The method according to claim 4 wherein the compound of Formula (I) is in the form of a hexahydrate. 7. A method of treating a patient for systemic lupus erythematosus, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I): ##STR00008## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 8. The method according to claim 7 wherein each X.sup.+ in the compound of Formula (I) represents a sodium cation (Na.sup.+). 9. The method according to claim 7 wherein the compound of Formula (I) is in the form of a hexahydrate. 10. A method of treating a patient for rheumatoid arthritis, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I): ##STR00009## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 11. The method according to claim 10 wherein each X.sup.+ in the compound of Formula (II) represents a sodium cation (Na.sup.+). 12. The method according to claim 10 wherein the compound of Formula (II) is in the form of a hexahydrate. 13. A method of treating a patient for cancer, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I): ##STR00010## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 14. The method according to claim 13 wherein each X.sup.+ in the compound of Formula (II) represents a sodium cation (Na.sup.+). 15. The method according to claim 13 wherein the compound of Formula (II) is in the form of a hexahydrate. 16. A method of treating a patient for systemic lupus erythematosus, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I): ##STR00011## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 17. The method according to claim 16 wherein each X.sup.+ in the compound of Formula (II) represents a sodium cation (Na.sup.+). 18. The method according to claim 16 wherein the compound of Formula (II) is in the form of a hexahydrate. 19. A method of treating a patient for immune thrombocytic purpura, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I): ##STR00012## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 20. The method according to claim 19 wherein each X.sup.+ in the compound of Formula (I) represents a sodium cation (Na.sup.+). 21. The method according to claim 19 wherein the compound of Formula (I) is in the form of a hexahydrate. 22. A method of treating a patient for immune thrombocytic purpura, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I): ##STR00013## and/or a hydrate thereof; wherein each X.sup.+ represents a monovalent cation; and less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and further comprising one or more pharmaceutically acceptable ingredients. 23. The method according to claim 22 wherein each X.sup.+ in the compound of Formula (II) represents a sodium cation (Na.sup.+). 24. The method according to claim 22 wherein the compound of Formula (II) is in the form of a hexahydrate.