IP Library Granted Patent US 8,951,504
Granted Patent B2
US 8,951,504 · App. 14/290,494 · Granted Feb 10, 2015

(trimethoxyphenylamino) pyrimidinyl formulations

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Quick Facts
Patent No.
US 8,951,504
App. No.
14/290,494
Granted
Feb 10, 2015
Kind
B2
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.

Claims (56)

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (I) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (I) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (I) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (II) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (II) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (II) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (I) represents a sodium cation (Na + ).

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):

and/or a hydrate thereof;

wherein each X + 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 + in the compound of Formula (II) represents a sodium cation (Na + ).

24. The method according to claim 22 wherein the compound of Formula (II) is in the form of a hexahydrate.

Assignments (5)
SECURITY INTEREST Recorded May 8, 2026
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FUNDING IV TRUST
Reel/Frame 075576/0880 →
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2014
From: ASTRAZENECA AB
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 033077/0541 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 6, 2014
From: GURURAJAN, BINDHUMADHAVAN; ALHUSBAN, FARHAN ABDUL KARIM; SIMPSON, DAVID BRADLEY BROOK; GABBOTT, IAN PAUL; SIEVWRIGHT, DAWN
To: ASTRAZENECA UK LIMITED
Reel/Frame 033048/0312 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 6, 2014
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 033048/0357 →