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Last Updated: December 28, 2024

Claims for Patent: 8,951,504


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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.

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